[go: up one dir, main page]

MX336932B - Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1). - Google Patents

Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).

Info

Publication number
MX336932B
MX336932B MX2012010344A MX2012010344A MX336932B MX 336932 B MX336932 B MX 336932B MX 2012010344 A MX2012010344 A MX 2012010344A MX 2012010344 A MX2012010344 A MX 2012010344A MX 336932 B MX336932 B MX 336932B
Authority
MX
Mexico
Prior art keywords
piperidin
azetidine derivatives
jak1
jak1 inhibitors
activity
Prior art date
Application number
MX2012010344A
Other languages
English (en)
Other versions
MX2012010344A (es
Inventor
Chu-Biao Xue
Hui-Yin Li
James D Rodgers
Haisheng Wang
Wenqing Yao
Anlai Wang
Taisheng Huang
Stacey Shepard
Lixin Shao
Ling Kong
Hai Fen Ye
Qun Li
Original Assignee
Incyte Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44065466&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MX336932(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of MX2012010344A publication Critical patent/MX2012010344A/es
Publication of MX336932B publication Critical patent/MX336932B/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Physics & Mathematics (AREA)
  • Condensed Matter Physics & Semiconductors (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención proporciona derivados de piperidin-4-ilazetidina, como también sus composiciones y métodos de uso, que modulan la actividad de Janus cinasa 1 (JAK1) y son útiles en el tratamiento de las enfermedades relacionadas con la actividad de JAK1 que incluye, por ejemplo, trastornos inflamatorios, trastornos autoinmunes, cáncer, y otras enfermedades.
MX2012010344A 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1). MX336932B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31258810P 2010-03-10 2010-03-10
US41560210P 2010-11-19 2010-11-19
PCT/US2011/027665 WO2011112662A1 (en) 2010-03-10 2011-03-09 Piperidin-4-yl azetidine derivatives as jak1 inhibitors

Publications (2)

Publication Number Publication Date
MX2012010344A MX2012010344A (es) 2012-11-16
MX336932B true MX336932B (es) 2016-02-08

Family

ID=44065466

Family Applications (5)

Application Number Title Priority Date Filing Date
MX2018002077A MX364636B (es) 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
MX2017006392A MX354212B (es) 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
MX2012010344A MX336932B (es) 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
MX2016001708A MX347851B (es) 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
MX2019005232A MX2019005232A (es) 2010-03-10 2012-09-06 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).

Family Applications Before (2)

Application Number Title Priority Date Filing Date
MX2018002077A MX364636B (es) 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
MX2017006392A MX354212B (es) 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).

Family Applications After (2)

Application Number Title Priority Date Filing Date
MX2016001708A MX347851B (es) 2010-03-10 2011-03-09 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
MX2019005232A MX2019005232A (es) 2010-03-10 2012-09-06 Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).

Country Status (38)

Country Link
US (6) US8765734B2 (es)
EP (6) EP2545045B1 (es)
JP (7) JP5858484B2 (es)
KR (7) KR101911697B1 (es)
CN (1) CN102985417B (es)
AR (1) AR081315A1 (es)
AU (1) AU2011224484A1 (es)
BR (1) BR112012022513A2 (es)
CA (1) CA2792508C (es)
CL (1) CL2012002501A1 (es)
CO (1) CO6602158A2 (es)
CR (1) CR20120510A (es)
CY (2) CY1120154T1 (es)
DK (3) DK2545045T3 (es)
EA (1) EA030376B1 (es)
EC (1) ECSP12012218A (es)
ES (5) ES2662588T3 (es)
HK (2) HK1177741A1 (es)
HR (3) HRP20160326T1 (es)
HU (3) HUE049914T2 (es)
IL (1) IL221823A (es)
LT (2) LT3050882T (es)
ME (2) ME02386B (es)
MX (5) MX364636B (es)
MY (2) MY175156A (es)
NO (1) NO3050882T3 (es)
NZ (1) NZ602313A (es)
PE (1) PE20130038A1 (es)
PH (2) PH12012501768A1 (es)
PL (3) PL3354652T3 (es)
PT (2) PT3050882T (es)
RS (3) RS57219B1 (es)
SG (1) SG183551A1 (es)
SI (3) SI3050882T1 (es)
SM (3) SMT201800137T1 (es)
TW (6) TWI694826B (es)
WO (1) WO2011112662A1 (es)
ZA (1) ZA201207420B (es)

Families Citing this family (127)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT2426129T (lt) * 2005-12-13 2017-02-10 Incyte Holdings Corporation Heteroarilu pakeisti pirolo[2,3-b]piridinai ir pirolo[2,3-b]pirimidinai kaip janus kinazės inhibitoriai
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
RS54878B1 (sr) 2007-06-13 2016-10-31 Incyte Holdings Corp Kristalne soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropionitril
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
JOP20190231A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
WO2010135650A1 (en) 2009-05-22 2010-11-25 Incyte Corporation N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
UA106078C2 (uk) 2009-05-22 2014-07-25 Інсайт Корпорейшн 3-[4-(7H-ПІРОЛО[2,3-d]ПІРИМІДИН-4-ІЛ)-1H-ПІРАЗОЛ-1-ІЛ]ОКТАН- АБО ГЕПТАННІТРИЛ ЯК JAK-ІНГІБІТОРИ
MY162507A (en) 2009-06-29 2017-06-15 Incyte Holdings Corp Pyrimidinones as pi3k inhibitors
WO2011028685A1 (en) * 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
MX364636B (es) * 2010-03-10 2019-05-03 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
SI2574168T1 (sl) 2010-05-21 2016-07-29 Incyte Holdings Corporation Topična formulacija zaviralca jak
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
US9096600B2 (en) 2010-12-20 2015-08-04 Incyte Corporation N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
EP2675451B9 (en) 2011-02-18 2017-07-26 Novartis Pharma AG mTOR/JAK INHIBITOR COMBINATION THERAPY
AU2012273164B2 (en) 2011-06-20 2015-05-28 Incyte Holdings Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
JP2014521725A (ja) 2011-08-10 2014-08-28 ノバルティス・ファルマ・アクチェンゲゼルシャフト JAKPI3K/mTOR併用療法
TW201313721A (zh) * 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
RS55737B1 (sr) 2011-09-02 2017-07-31 Incyte Holdings Corp Heterociklilamini kao inhibitori pi3k
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
JP6014149B2 (ja) * 2011-09-22 2016-10-25 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. ヤヌスキナーゼ阻害剤としての非環式シアノエチルピラゾール
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
AR091079A1 (es) * 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
DK2903968T3 (en) 2012-10-02 2017-01-30 Gilead Sciences Inc INHIBITORS OF HISTON DEMETHYLASES
AR093308A1 (es) 2012-11-01 2015-05-27 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de jak
JP2015537030A (ja) 2012-11-15 2015-12-24 インサイト・コーポレイションIncyte Corporation ルキソリチニブの徐放性投薬形態
ES2649156T3 (es) 2013-01-14 2018-01-10 Incyte Holdings Corporation Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim
SMT202000244T1 (it) 2013-01-15 2020-07-08 Incyte Holdings Corp Composti di tiazolocarbossammide e piridincarbossammide utili come inibitori di chinasi pim
MD20150085A2 (ro) 2013-02-27 2016-02-29 Epitherapeutics Aps Inhibitori ai histon-demetilazelor
KR102366356B1 (ko) 2013-03-06 2022-02-23 인사이트 홀딩스 코포레이션 Jak 저해제를 제조하기 위한 방법 및 중간생성물
DK2970101T3 (en) 2013-03-14 2018-08-20 Alkermes Pharma Ireland Ltd PRO-DRUGS OF FUMARATES AND THEIR USE IN TREATING DIFFERENT DISEASES
US8669281B1 (en) 2013-03-14 2014-03-11 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
WO2014146249A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
CA2901766A1 (en) 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors
CN105121444B (zh) 2013-03-19 2018-02-16 默沙东公司 作为janus激酶抑制剂的非环形的氰基乙基吡唑并吡啶酮
WO2014146246A1 (en) 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors
US20160045498A1 (en) * 2013-04-04 2016-02-18 The Walter And Eliza Hall Institute Of Medical Research Methods of treating diseases characterized by excessive wnt signalling
EA036448B1 (ru) 2013-05-17 2020-11-11 Инсайт Корпорейшн Производные бипиразола в качестве ингибиторов jak
EP3721873A1 (en) * 2013-08-07 2020-10-14 Incyte Corporation Sustained release dosage forms for a jak1 inhibitor
EA201690421A1 (ru) * 2013-08-20 2016-06-30 Инсайт Корпорейшн Положительный эффект в форме увеличения продолжительности жизни у больных с солидными опухолями с повышенными уровнями c-реактивного белка
CA2921959A1 (en) 2013-08-23 2015-02-26 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
JP6367545B2 (ja) * 2013-12-17 2018-08-01 コンサート ファーマシューティカルズ インコーポレイテッド ルキソリチニブの重水素化誘導体
NZ723269A (en) 2014-02-24 2017-04-28 Alkermes Pharma Ireland Ltd Sulfonamide and sulfinamide prodrugs of fumarates and their use in treating various diseases
PL3110409T3 (pl) * 2014-02-28 2018-12-31 Incyte Corporation Inhibitory jak1 do leczenia zespołów mielodysplastycznych
CN111494386A (zh) 2014-04-08 2020-08-07 因赛特公司 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤
BR112016025427A2 (pt) 2014-04-30 2017-08-15 Incyte Corp processos de preparação de um inibidor de jak1 e formas do mesmo
WO2015184305A1 (en) * 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
AU2015306662A1 (en) * 2014-08-27 2017-03-09 Gilead Sciences, Inc. Compounds and methods for inhibiting histone demethylases
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
MD3831833T2 (ro) 2015-02-27 2023-04-30 Incyte Holdings Corp Procedee pentru prepararea unui inhibitor PI3K
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
US9840503B2 (en) 2015-05-11 2017-12-12 Incyte Corporation Heterocyclic compounds and uses thereof
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
WO2017013270A1 (en) 2015-07-23 2017-01-26 Universite De Strasbourg Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Pim激酶抑制劑之鹽
TW201718546A (zh) 2015-10-02 2017-06-01 英塞特公司 適用作pim激酶抑制劑之雜環化合物
US11780848B2 (en) 2015-10-16 2023-10-10 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof
RU2018117889A (ru) 2015-10-16 2019-11-20 Эббви Инк. СПОСОБЫ ПОЛУЧЕНИЯ (3S,4R)-3-ЭТИЛ-4-(3H-ИМИДАЗО[1,2-a]ПИРРОЛО[2,3-e]-ПИРАЗИН-8-ИЛ)-N-(2,2,2-ТРИФТОРЭТИЛ)ПИРРОЛИДИН-1-КАРБОКСАМИДА И ЕГО ТВЕРДОФАЗНЫХ ФОРМ
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
HRP20220599T1 (hr) 2015-11-06 2022-06-24 Incyte Corporation Heterociklički spojevi kao inhibitori pi3k-gama
EP3360878B9 (en) * 2015-12-11 2021-05-05 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Azetidine derivative, preparation method therefor, and use thereof
TW201734003A (zh) 2016-01-05 2017-10-01 英塞特公司 作為PI3K-γ抑制劑之吡啶及嘧啶化合物
WO2017129116A1 (zh) * 2016-01-26 2017-08-03 杭州华东医药集团新药研究院有限公司 吡咯嘧啶五元氮杂环衍生物及其应用
US20190086392A1 (en) 2016-03-21 2019-03-21 Inserm (Institut National De La Sante Et De La Recherch Medicale) Methods for diagnosis and treatment of solar lentigo
HRP20231614T1 (hr) 2016-03-28 2024-03-15 Incyte Corporation Spojevi pirolotriazina kao tam inhibitori
US10138248B2 (en) 2016-06-24 2018-11-27 Incyte Corporation Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
US11397145B2 (en) * 2016-08-24 2022-07-26 The University Of Melbourne Diagnostic methods and device
GB201617871D0 (en) * 2016-10-21 2016-12-07 Sareum Limited Pharmaceutical compounds
US20180153922A1 (en) 2016-12-06 2018-06-07 New York Society For The Ruptured And Crippled Maintaining The Hospital For Special Surgery Inhibition of expansion and function of pathogenic age-associated b cells and use for the prevention and treatment of autoimmune disease
EP4219470A1 (en) 2017-01-17 2023-08-02 Astrazeneca AB Jak1 selective inhibitors
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
CN109422753B (zh) * 2017-09-03 2021-12-31 上海美志医药科技有限公司 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物
GEP20227429B (en) 2017-09-27 2022-10-25 Incyte Corp Salts of pyrrolotriazine derivatives useful as tam inhibitors
LT3697789T (lt) 2017-10-18 2021-12-10 Incyte Corporation Kondensuoti imidazolo dariniai, pakeisti tretinėmis hidroksigrupėmis, kaip pi3k-gama inhibitoriai
CN109867676B (zh) * 2017-12-01 2020-10-30 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
EP3743418B1 (en) 2018-01-26 2024-07-31 RAPT Therapeutics, Inc. Chemokine receptor modulators and uses thereof
AR114810A1 (es) * 2018-01-30 2020-10-21 Incyte Corp Procesos e intermedios para elaborar un inhibidor de jak
IL276725B2 (en) * 2018-02-16 2024-09-01 Incyte Corp Jak1 pathway inhibitors for the treatment of cytokine-related disorders
AU2019229885A1 (en) 2018-03-08 2020-09-10 Anna Rita Franco MIGLIACCIO Use of an anti-P-selectin antibody
CN113768934A (zh) * 2018-03-30 2021-12-10 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
MX2020010815A (es) 2018-04-13 2020-12-11 Incyte Corp Biomarcadores para enfermedad de injerto contra hospedero.
SG11202011680YA (en) 2018-06-01 2020-12-30 Incyte Corp Dosing regimen for the treatment of pi3k related disorders
SG11202013163TA (en) 2018-06-29 2021-01-28 Incyte Corp Formulations of an axl/mer inhibitor
WO2020039401A1 (en) 2018-08-24 2020-02-27 Novartis Ag Treatment comprising il-1βeta binding antibodies and combinations thereof
MA53561A (fr) 2018-09-05 2022-05-11 Incyte Corp Formes cristallines d'un inhibiteur de phosphoinositide 3-kinase (pi3k)
JP7431845B2 (ja) 2018-10-31 2024-02-15 インサイト・コーポレイション 血液疾患の治療のための併用療法
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
KR101992148B1 (ko) 2018-11-30 2019-06-25 한승훈 안전벨트의 꼬임방지장치
US11596632B2 (en) * 2018-12-19 2023-03-07 Incyte Corporation JAK1 pathway inhibitors for the treatment of gastrointestinal disease
JP2022524997A (ja) 2019-03-05 2022-05-11 インサイト・コーポレイション 慢性肺同種移植片機能不全の治療のためのjak1経路阻害剤
JP7248256B2 (ja) 2019-03-14 2023-03-29 上海華匯拓医薬科技有限公司 Jakキナーゼ阻害剤及びその調製方法、並びにその医薬分野での使用
JP2022526301A (ja) 2019-03-19 2022-05-24 インサイト・コーポレイション 尋常性白斑のバイオマーカー
WO2020256739A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2021091535A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Treating myeloproliferative disorders with cpi-0610 and a jak inhibitor
WO2020257644A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
AU2020351324B2 (en) 2019-09-16 2023-08-03 Novartis Ag Use of an MDM2 inhibitor for the treatment of myelofibrosis
CN114423786A (zh) 2019-09-16 2022-04-29 诺华股份有限公司 高亲和力的、配体阻断性、人源化的抗T细胞免疫球蛋白结构域和粘蛋白结构域3(TIM-3)IgG4抗体用于治疗骨髓纤维化的用途
JP2022551649A (ja) 2019-10-10 2022-12-12 インサイト・コーポレイション 移植片対宿主病のバイオマーカー
WO2021072098A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
WO2021076124A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Use of jak1 inhibitors for the treatment of cutaneous lupus erythematosus and lichen planus (lp)
KR20220107213A (ko) 2019-11-22 2022-08-02 인사이트 코포레이션 Alk2 억제제 및 jak2 억제제를 포함하는 병용 요법
KR20230017165A (ko) 2020-03-06 2023-02-03 인사이트 코포레이션 Axl/mer 및 pd-1/pd-l1 억제제를 포함하는 병행 요법
TW202210471A (zh) 2020-06-02 2022-03-16 美商英塞特公司 製備jak1抑制劑之方法
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4200300A1 (en) 2020-08-18 2023-06-28 Incyte Corporation Process and intermediates for preparing a jak inhibitor
US11897889B2 (en) 2020-08-18 2024-02-13 Incyte Corporation Process and intermediates for preparing a JAK1 inhibitor
WO2022074600A1 (en) 2020-10-08 2022-04-14 Novartis Ag Use of an erk inhibitor for the treatment of myelofibrosis
MX2023006638A (es) 2020-12-04 2023-08-22 Incyte Corp Inhibidor de la cinasa janus (jak) con un análogo de la vitamina d para el tratamiento de enfermedades de la piel.
MX2023006542A (es) 2020-12-08 2023-08-25 Incyte Corp Inhibidores de la vía cinasa jano 1 (jak1) para el tratamiento del vitiligo.
JP2024503021A (ja) 2021-01-11 2024-01-24 インサイト・コーポレイション Jak経路阻害剤及びrock阻害剤を含む併用療法
TWI820622B (zh) 2021-03-04 2023-11-01 美商美國禮來大藥廠 Fgfr3抑制劑化合物
JP2024516302A (ja) 2021-05-03 2024-04-12 インサイト・コーポレイション 結節性痒疹を治療するためのjak1経路阻害薬
WO2023288197A1 (en) 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
CN114149437A (zh) * 2021-12-24 2022-03-08 安徽大学 一种吡咯并嘧啶五元氮杂环衍生物及其制备方法和用途
AU2023320077A1 (en) 2022-08-05 2025-02-13 Incyte Corporation Treatment of urticaria using jak inhibitors
WO2024192350A1 (en) 2023-03-16 2024-09-19 Incyte Corporation Jak1 pathway inhibitors for the treatment of asthma
WO2024222835A1 (en) * 2023-04-27 2024-10-31 Sironax Ltd. Sarm1 modulators, preparations, and uses thereof

Family Cites Families (309)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2985589A (en) 1957-05-22 1961-05-23 Universal Oil Prod Co Continuous sorption process employing fixed bed of sorbent and moving inlets and outlets
US3632836A (en) 1968-10-25 1972-01-04 Dow Chemical Co Solid curable polyepoxides modified with hydrolyzed liquid polyepoxides
US3832460A (en) 1971-03-19 1974-08-27 C Kosti Anesthetic-vasoconstrictor-antihistamine composition for the treatment of hypertrophied oral tissue
US4140755A (en) 1976-02-13 1979-02-20 Hoffmann-La Roche Inc. Sustained release tablet formulations
DE3036390A1 (de) 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
DE3220113A1 (de) 1982-05-28 1983-12-01 Basf Ag, 6700 Ludwigshafen Difluormethoxiphenylthiophosphorsaeureester
US4402832A (en) 1982-08-12 1983-09-06 Uop Inc. High efficiency continuous separation process
US4404335A (en) 1982-08-16 1983-09-13 The Dow Chemical Company Hydrolyzing epoxy resins in absence of solvent and in presence of oxalic acid and a phosphonium compound
US4548990A (en) 1983-08-15 1985-10-22 Ciba-Geigy Corporation Crosslinked, porous polymers for controlled drug delivery
US4498991A (en) 1984-06-18 1985-02-12 Uop Inc. Serial flow continuous separation process
NL8403224A (nl) 1984-10-24 1986-05-16 Oce Andeno Bv Dioxafosforinanen, de bereiding ervan en de toepassing voor het splitsen van optisch actieve verbindingen.
CA1306260C (en) 1985-10-18 1992-08-11 Shionogi & Co., Ltd. Condensed imidazopyridine derivatives
JPH0710876Y2 (ja) 1989-08-31 1995-03-15 石垣機工株式会社 スクリュープレスにおける脱水筒の洗浄装置
CA2067221C (en) 1989-10-11 1997-04-15 Yasuji Sakuma Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient
US5403593A (en) 1991-03-04 1995-04-04 Sandoz Ltd. Melt granulated compositions for preparing sustained release dosage forms
IT1258781B (it) 1992-01-16 1996-02-29 Zambon Spa Composizione farmaceutica oftalmica contenente n-acetilcisteina e polivinilalcol
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
FR2695126B1 (fr) 1992-08-27 1994-11-10 Sanofi Elf Dérivés d'acide thiényl ou pyrrolyl carboxyliques, leur préparation et médicaments les contenant.
AU671491B2 (en) 1992-12-18 1996-08-29 F. Hoffmann-La Roche Ag N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines
JPH0710876A (ja) 1993-06-24 1995-01-13 Teijin Ltd 4位に環状アミノ基を有するピロロ[2,3―d]ピリミジン
USH1439H (en) 1993-10-18 1995-05-02 The Dow Chemical Company Method to increase the level of α-glycol in liquid epoxy resin
EP0727217A3 (en) 1995-02-10 1997-01-15 Suntory Ltd Pharmaceutical and cosmetic compositions containing God-type ellagitannin as an active ingredient
US5856326A (en) 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
KR19990028709A (ko) 1995-07-05 1999-04-15 미리암 디. 메코너헤이 살진균 피리미디논
DK0836605T3 (da) 1995-07-06 2002-05-13 Novartis Ag Pyrrolopyrimidiner og fremgangsmåder til deres fremstilling
US5630943A (en) 1995-11-30 1997-05-20 Merck Patent Gesellschaft Mit Beschrankter Haftung Discontinuous countercurrent chromatographic process and apparatus
GB9604361D0 (en) 1996-02-29 1996-05-01 Pharmacia Spa 4-Substituted pyrrolopyrimidine compounds as tyrosine kinase inhibitors
AU727939B2 (en) 1996-04-03 2001-01-04 Merck & Co., Inc. A method of treating cancer
JP2000513711A (ja) 1996-04-18 2000-10-17 メルク エンド カンパニー インコーポレーテッド 癌の治療法
US5795909A (en) 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
JP2000508335A (ja) 1996-05-30 2000-07-04 メルク エンド カンパニー インコーポレーテッド 癌の治療方法
US6624138B1 (en) 2001-09-27 2003-09-23 Gp Medical Drug-loaded biological material chemically treated with genipin
JP2001524079A (ja) 1997-04-07 2001-11-27 メルク エンド カンパニー インコーポレーテッド ガンの治療方法
US6063284A (en) 1997-05-15 2000-05-16 Em Industries, Inc. Single column closed-loop recycling with periodic intra-profile injection
US6060038A (en) 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
JP2001513502A (ja) 1997-08-11 2001-09-04 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 5,6−ヘテロアリールジピリド[2,3−b:3’,2’−f]アゼピン類及びHIV感染の予防及び治療におけるそれらの使用
US7153845B2 (en) 1998-08-25 2006-12-26 Columbia Laboratories, Inc. Bioadhesive progressive hydration tablets
US6075056A (en) 1997-10-03 2000-06-13 Penederm, Inc. Antifungal/steroid topical compositions
US6025366A (en) 1998-04-02 2000-02-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
BR9910864A (pt) 1998-06-04 2002-02-05 Abbott Lab Compostos anti-inflamatórios para inibição de aderência celular
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
EP1087970B1 (en) 1998-06-19 2004-04-28 Pfizer Products Inc. PYRROLO 2,3-d]PYRIMIDINE COMPOUNDS
BR9912938B1 (pt) 1998-08-11 2011-06-28 derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos.
JP2000119271A (ja) 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd 1h―イミダゾピリジン誘導体
AU5504599A (en) 1998-09-10 2000-04-03 Nycomed Danmark A/S Quick release pharmaceutical compositions of drug substances
US6375839B1 (en) 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
US6413419B1 (en) 1998-10-29 2002-07-02 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic
FR2785196B1 (fr) 1998-10-29 2000-12-15 Inst Francais Du Petrole Procede et dispositif de separation avec des zones chromatographiques a longueur variable
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
JP2002538121A (ja) 1999-03-03 2002-11-12 メルク エンド カムパニー インコーポレーテッド プレニルタンパク質トランスフェラーゼの阻害剤
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US6217895B1 (en) 1999-03-22 2001-04-17 Control Delivery Systems Method for treating and/or preventing retinal diseases with sustained release corticosteroids
US6239113B1 (en) 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
AU3565999A (en) 1999-04-16 2000-11-02 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
US6915718B2 (en) * 1999-09-02 2005-07-12 United Parts Fhs Automobil Systeme Gmbh Selector handle in a motor vehicle
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
DE60013464T2 (de) * 1999-10-13 2005-09-15 Banyu Pharmaceutical Co., Ltd. Substituierte imidazolin-derivate
US7235258B1 (en) 1999-10-19 2007-06-26 Nps Pharmaceuticals, Inc. Sustained-release formulations for treating CNS-mediated disorders
ATE380031T1 (de) 1999-12-10 2007-12-15 Pfizer Prod Inc Pyrrolo 2,3-d pyrimidinderivate enthaltende zusammensetzungen
NZ519121A (en) 1999-12-24 2004-05-28 Aventis Pharma Ltd Azaindoles useful as Syk kinase inhibitors
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
ATE250924T1 (de) 2000-04-07 2003-10-15 Medidom Lab Cyklosporin, hyaluronsäure und polysorbate enthaltenes augenarzneimittel
AU4878601A (en) 2000-04-20 2001-11-07 Mitsubishi Corporation Aromatic amide compounds
SI2223922T1 (sl) 2000-04-25 2016-04-29 Icos Corporation Inhibitorji humane fosfatidil-inositol 3-kinazne delta izoforme
JP4954426B2 (ja) 2000-06-16 2012-06-13 キュリス,インコーポレイテッド 血管形成調節組成物及び利用
US7498304B2 (en) 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
US6335342B1 (en) 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
ATE465756T1 (de) 2000-06-23 2010-05-15 Mitsubishi Tanabe Pharma Corp Antitumoreffekt-verstärker
ES2257410T3 (es) 2000-06-26 2006-08-01 Pfizer Products Inc. Compuestos de pirrolo(2,3-d)pirimidina como agentes inmunosupresores.
NZ522783A (en) 2000-06-28 2004-07-30 Smithkline Beecham P Wet milling process for pharmaceuticals with agitator or chamber having nylon with internal lubricant
WO2002016370A1 (fr) 2000-08-22 2002-02-28 Hokuriku Seiyaku Co., Ltd. Derives de 1h-imidazopyridine
ATE407132T1 (de) 2000-12-05 2008-09-15 Vertex Pharma Inhibitoren von c-jun n-terminalen kinasen (jnk) und anderen proteinkinasen
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
EP1351936A1 (en) 2001-01-15 2003-10-15 Glaxo Group Limited Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
CA2446864C (en) 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
CA2455181C (en) 2001-08-01 2010-04-06 Merck & Co., Inc. Benzimidazo[4,5-f]isoquinolinone derivatives
CN100391958C (zh) 2001-09-19 2008-06-04 安万特医药股份有限公司 化合物
US6429231B1 (en) 2001-09-24 2002-08-06 Bradley Pharmaceuticals, Inc. Compositions containing antimicrobials and urea for the treatment of dermatological disorders and methods for their use
HU230798B1 (hu) 2001-10-30 2018-06-28 Novartis Ag Staurosporin-származékok mint az FLT3 receptor tirozin-kináz aktivitás inhibitorai
JP2003155285A (ja) 2001-11-19 2003-05-27 Toray Ind Inc 環状含窒素誘導体
AU2002224131A1 (en) 2001-11-30 2003-06-17 Teijin Limited Process for producing 5-(3-cyanophenyl)-3-formylbenzoic acid compound
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
CA2481739C (en) 2002-04-15 2012-10-02 Adams Laboratories, Inc. Sustained release of guaifenesin combination drugs
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
AU2003237121A1 (en) 2002-04-26 2003-11-10 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
WO2003092595A2 (en) 2002-05-02 2003-11-13 Merck & Co., Inc Tyrosine kinase inhibitors
JP2005532313A (ja) 2002-05-07 2005-10-27 コントロール・デリバリー・システムズ・インコーポレイテッド 薬物送達装置の形成方法
GB2392154B (en) 2002-05-23 2005-01-19 Cytopia Pty Ltd Protein Kinase Inhibitors
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
EP1535934A4 (en) 2002-06-26 2005-11-02 Idemitsu Kosan Co HYDROGENATED COPOLYMER, METHOD FOR THE PRODUCTION THEREOF AND THIS CONTAINING HOTMELT ADHESIVE COMPOSITION
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
JPWO2004007472A1 (ja) 2002-07-10 2005-11-17 小野薬品工業株式会社 Ccr4アンタゴニストおよびその医薬用途
JP2006502183A (ja) 2002-09-20 2006-01-19 アルコン,インコーポレイテッド ドライアイ障害の処置のためのサイトカイン合成インヒビターの使用
US20040204404A1 (en) 2002-09-30 2004-10-14 Robert Zelle Human N-type calcium channel blockers
JP4688498B2 (ja) 2002-11-04 2011-05-25 バーテックス ファーマシューティカルズ インコーポレイテッド Jakインヒビターとしてのヘテロアリール−ピリミジン誘導体
US8034831B2 (en) 2002-11-06 2011-10-11 Celgene Corporation Methods for the treatment and management of myeloproliferative diseases using 4-(amino)-2-(2,6-Dioxo(3-piperidyl)-isoindoline-1,3-dione in combination with other therapies
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
US20040099204A1 (en) 2002-11-25 2004-05-27 Nestor John J. Sheet, page, line, position marker
AU2003276591A1 (en) 2002-11-26 2004-06-18 Pfizer Products Inc. Method of treatment of transplant rejection
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
UY28126A1 (es) 2002-12-24 2004-06-30 Alcon Inc Uso de glucocorticoides selectivos para la superficie ocular en el tratamiento de la sequedad ocular
US7135493B2 (en) 2003-01-13 2006-11-14 Astellas Pharma Inc. HDAC inhibitor
US7167750B2 (en) 2003-02-03 2007-01-23 Enteromedics, Inc. Obesity treatment with electrically induced vagal down regulation
US7407962B2 (en) 2003-02-07 2008-08-05 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors or protein kinases
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
AU2004230841A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
FR2857454B1 (fr) 2003-07-08 2006-08-11 Aventis Pasteur Dosage des acides techoiques des bacteries gram+
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
WO2005020921A2 (en) 2003-08-29 2005-03-10 Exelixis, Inc. C-kit modulators and methods of use
WO2005026129A1 (en) 2003-09-15 2005-03-24 Gpc Biotech Ag Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
ATE490771T1 (de) 2003-10-24 2010-12-15 Santen Pharmaceutical Co Ltd Therapeutisches mittel für keratokonjunktive erkrankungen
US7387793B2 (en) 2003-11-14 2008-06-17 Eurand, Inc. Modified release dosage forms of skeletal muscle relaxants
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
MXPA06005882A (es) 2003-11-25 2006-06-27 Pfizer Prod Inc Metodo de tratamiento de la aterosclerosis.
KR20060096153A (ko) 2003-12-17 2006-09-07 화이자 프로덕츠 인코포레이티드 이식 거부 치료용 피롤로[2,3-d]피리미딘 화합물
DE602004016211D1 (en) 2003-12-19 2008-10-09 Schering Corp Thiadiazole als cxc- und cc-chemokinrezeptorliganden
CN1925855B (zh) 2003-12-19 2010-06-16 普莱希科公司 开发Ret调节剂的化合物和方法
EP2228369A1 (en) 2003-12-23 2010-09-15 Astex Therapeutics Ltd. Pyrazole derivatives as protein kinase modulators
US20050187389A1 (en) 2004-01-13 2005-08-25 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
US20050277629A1 (en) 2004-03-18 2005-12-15 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies (Lansbury)
EP2786995A1 (en) 2004-03-30 2014-10-08 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
EP1750727A2 (en) 2004-04-23 2007-02-14 Exelixis, Inc. Kinase modulators and methods of use
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
US20090163523A1 (en) 2004-05-03 2009-06-25 Philip Lake Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor
MXPA06013250A (es) 2004-05-14 2007-02-28 Abbott Lab Inhibidores de quinasa como agentes terapeuticos.
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
AR049511A1 (es) 2004-06-10 2006-08-09 Irm Llc Compuestos y composiciones como inhibidores de quinasa de proteina
EP1760071A4 (en) 2004-06-23 2008-03-05 Ono Pharmaceutical Co COMPOUND WITH S1P RECEPTOR BINDING ABILITY AND USE THEREOF
EP2325184A1 (en) 2004-06-30 2011-05-25 Vertex Pharmceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
US7138423B2 (en) 2004-07-20 2006-11-21 Bristol-Myers Squibb Company Arylpyrrolidine derivatives as NK-1 /SSRI antagonists
FR2873691B1 (fr) 2004-07-29 2006-10-06 Sanofi Synthelabo Derives d'amino-piperidine, leur preparation et leur application en therapeutique
WO2006013114A1 (en) 2004-08-06 2006-02-09 Develogen Aktiengesellschaft Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome
WO2006022459A1 (en) 2004-08-23 2006-03-02 Mogam Biotechnology Institute Primer and probe for detection of sars coronavirus, kit comprising the primer and/or the probe, and detection method thereof
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
RU2394826C2 (ru) 2004-10-13 2010-07-20 Ф.Хоффманн-Ля Рош Аг Дизамещенные пиразолобензодиазепины, используемые в качестве ингибиторов cdk2 и ангиогенеза, а также для лечения злокачественных новообразований молочной железы, толстого кишечника, легкого и предстательной железы
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
CA2586375A1 (en) 2004-11-04 2006-05-18 Juan-Miguel Jimenez Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
AU2005309019A1 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors
US7517870B2 (en) 2004-12-03 2009-04-14 Fondazione Telethon Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization
US20060128803A1 (en) 2004-12-14 2006-06-15 Alcon, Inc. Method of treating dry eye disorders using 13(S)-HODE and its analogs
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
AR053992A1 (es) 2004-12-22 2007-05-30 Astrazeneca Ab Compuestos quimicos con actividad anticancerosa, un procedimiento para su preparacion, su uso en la preparacion de medicamentos y composicion farmaceutica.
WO2006077499A1 (en) 2005-01-20 2006-07-27 Pfizer Limited Chemical compounds
ES2320487T3 (es) 2005-02-03 2009-05-22 Vertex Pharmaceuticals, Inc. Pirrolopirimidinas utiles como inhibidores de proteina quinasas.
WO2007044050A2 (en) 2005-02-04 2007-04-19 Bristol-Myers Squibb Company 1h-imidazo[4,5-d]thieno[3,2-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
KR20070119690A (ko) 2005-03-15 2007-12-20 아이알엠 엘엘씨 단백질 키나제 억제제로서의 화합물 및 조성물
AU2006232105A1 (en) 2005-04-05 2006-10-12 Pharmacopeia, Inc. Purine and imidazopyridine derivatives for immunosuppression
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
EP2354140A1 (en) 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
EP1904457B1 (en) 2005-06-08 2017-09-06 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
CN102603581B (zh) 2005-06-22 2015-06-24 普莱希科公司 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
EP2251341A1 (en) 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
FR2889662B1 (fr) 2005-08-11 2011-01-14 Galderma Res & Dev Emulsion de type huile-dans-eau pour application topique en dermatologie
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
US20070149506A1 (en) 2005-09-22 2007-06-28 Arvanitis Argyrios G Azepine inhibitors of Janus kinases
EP2532667A1 (en) 2005-09-30 2012-12-12 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
US20070128633A1 (en) 2005-10-11 2007-06-07 Chembridge Research Laboratories, Inc. Cell-free protein expression systems and methods of use thereof
US7867949B2 (en) 2005-10-14 2011-01-11 Sumitomo Chemical Company, Limited Hydrazide compound and pesticidal use of the same
US20080287475A1 (en) 2005-10-28 2008-11-20 Astrazeneca Ab 4-(3-Aminopyrazole) Pyrimidine Derivatives for Use as Tyrosine Kinase Inhibitors in the Treatment of Cancer
JP5191391B2 (ja) 2005-11-01 2013-05-08 ターゲジェン インコーポレーティッド キナーゼのビ−アリールメタ−ピリミジン阻害剤
DK2275103T3 (da) 2005-11-21 2014-07-07 Novartis Ag mTor-inhibitorer ved behandling af endokrine tumorer
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
LT2426129T (lt) 2005-12-13 2017-02-10 Incyte Holdings Corporation Heteroarilu pakeisti pirolo[2,3-b]piridinai ir pirolo[2,3-b]pirimidinai kaip janus kinazės inhibitoriai
US20130137681A1 (en) 2005-12-13 2013-05-30 Incyte Corporation HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS
JP2009521504A (ja) 2005-12-22 2009-06-04 スミスクライン・ビーチャム・コーポレイション Akt活性阻害剤
EP1962830B1 (en) 2005-12-23 2013-03-27 GlaxoSmithKline LLC Azaindole inhibitors of aurora kinases
JP4643455B2 (ja) 2006-01-12 2011-03-02 株式会社ユニバーサルエンターテインメント 遊技システム
UA95940C2 (uk) 2006-01-17 2011-09-26 Вертекс Фармасьютикалс Інкорпорейтед Азаіндоли як інгібітори кіназ януса
EP1979353A2 (en) 2006-01-19 2008-10-15 OSI Pharmaceuticals, Inc. Fused heterobicyclic kinase inhibitors
US20090018156A1 (en) 2006-02-01 2009-01-15 Jun Tang Pyrrolo [2,3,B] Pyridine Derivatives Useful As RAF Kinase Inhibitors
US7745477B2 (en) 2006-02-07 2010-06-29 Hoffman-La Roche Inc. Heteroaryl and benzyl amide compounds
KR20080099334A (ko) 2006-02-24 2008-11-12 테바 파마슈티컬 인더스트리즈 리미티드 메토프로롤 숙시네이트 서방정 및 이의 제조 방법
AU2007225836A1 (en) 2006-03-10 2007-09-20 Ono Pharmaceutical Co., Ltd. Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient
TWI382984B (zh) 2006-04-03 2013-01-21 Astellas Pharma Inc 雜環化合物
AU2007235487A1 (en) * 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
US20090124636A1 (en) 2006-04-12 2009-05-14 Pfizer Inc. Chemical compounds
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
WO2007135461A2 (en) 2006-05-18 2007-11-29 Bayer Healthcare Ag Pharmaceutical compositions comprising implitapide and methods of using same
US7691811B2 (en) 2006-05-25 2010-04-06 Bodor Nicholas S Transporter-enhanced corticosteroid activity and methods and compositions for treating dry eye
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
NZ573174A (en) 2006-06-01 2012-01-12 Msd Consumer Care Inc Sustained release pharmaceutical dosage form containing phenylephrine
CN101790527A (zh) 2006-07-20 2010-07-28 凯利普西斯公司 Rho激酶的苯并噻吩抑制剂
WO2008013622A2 (en) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
ATE517868T1 (de) 2006-08-16 2011-08-15 Boehringer Ingelheim Int Pyrazinverbindungen, ihre verwendung und herstellungsverfahren
PE20080769A1 (es) 2006-09-08 2008-08-14 Novartis Ag Derivados de biaril-sulfonamida
WO2008035376A2 (en) 2006-09-19 2008-03-27 Council Of Scientific & Industrial Research A novel bio-erodible insert for ophthalmic applications and a process for the preparation thereof
WO2008043019A1 (en) 2006-10-04 2008-04-10 Pharmacopeia, Inc 8-substituted 2-(benzimidazolyl) purine derivatives for immunosuppression
AR063142A1 (es) 2006-10-04 2008-12-30 Pharmacopeia Inc Derivados de 2-(bencimidazolil) purina y purinonas 6-sustituidas utiles como inmunosupresores,y composiciones farmaceuticas que los contienen.
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
JP5357763B2 (ja) 2006-11-06 2013-12-04 トレロ ファーマシューティカルズ, インコーポレイテッド イミダゾ[1,2−b]ピリダジン誘導体およびピラゾロ[1,5−a]ピリダジン誘導体およびプロテインキナーゼインヒビターとしてのこれらの使用
US20080119496A1 (en) 2006-11-16 2008-05-22 Pharmacopeia Drug Discovery, Inc. 7-Substituted Purine Derivatives for Immunosuppression
SI3034075T1 (sl) 2006-11-22 2018-12-31 Incyte Holdings Corporation Imidazotriazini in imidazopirimidini kot inhibitorji kinaze
WO2008067119A2 (en) 2006-11-27 2008-06-05 Smithkline Beecham Corporation Novel compounds
SG177221A1 (en) 2006-12-15 2012-01-30 Abbott Lab Novel oxadiazole compounds
US7687522B2 (en) 2006-12-20 2010-03-30 Amgen Inc. Substituted pyridines and pyrimidines and their use in treatment of cancer
JP5528812B2 (ja) 2006-12-20 2014-06-25 アムジエン・インコーポレーテツド 複素環式化合物ならびに炎症、血管形成および癌の治療におけるこれらの使用
WO2008079965A1 (en) 2006-12-22 2008-07-03 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
JP5315252B2 (ja) 2006-12-22 2013-10-16 シグマ−タウ・インドゥストリエ・ファルマチェウチケ・リウニテ・ソシエタ・ペル・アチオニ 眼科用薬物の輸送に有用なゲル
WO2008082839A2 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
WO2008082840A1 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008106692A1 (en) 2007-03-01 2008-09-04 Novartis Vaccines And Diagnostics, Inc. Pim kinase inhibitors and methods of their use
NZ580327A (en) 2007-04-03 2012-02-24 Array Biopharma Inc IMIDAZO[1,2-a]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS
US8188178B2 (en) 2007-05-07 2012-05-29 3M Innovative Properties Company Cold shrinkable article including an epichlorohydrin composition
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
WO2008145681A2 (en) 2007-05-31 2008-12-04 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
RS54878B1 (sr) 2007-06-13 2016-10-31 Incyte Holdings Corp Kristalne soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropionitril
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
KR20120115413A (ko) 2007-07-11 2012-10-17 화이자 인코포레이티드 안구 건조증 치료용 약학 조성물 및 방법
BRPI0815042A2 (pt) 2007-08-01 2015-02-10 Pfizer Compostos de pirazol
WO2009049028A1 (en) 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
US20110263664A1 (en) 2007-11-15 2011-10-27 Musc Foundation For Research Development Inhibitors of PIM-1 Protein Kinases, Compositions and Methods for Treating Prostate Cancer
US8309718B2 (en) 2007-11-16 2012-11-13 Incyte Corporation 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
GB0723815D0 (en) 2007-12-05 2008-01-16 Glaxo Group Ltd Compounds
WO2009089804A1 (en) 2008-01-18 2009-07-23 Institute Of Organic Chemistry And Biochemistry As Cr, V.V.I. Novel cytostatic 7-deazapurine nucleosides
MX2010008376A (es) 2008-02-04 2011-02-22 Mercury Therapeutics Inc Moduladores ampk.
AR070531A1 (es) 2008-03-03 2010-04-14 Novartis Ag Inhibidores de cinasa pim y metodos para su uso
JP5275371B2 (ja) 2008-03-11 2013-08-28 インサイト・コーポレイション Jak阻害剤としてのアゼチジン誘導体およびシクロブタン誘導体
WO2009115572A2 (en) 2008-03-21 2009-09-24 Novartis Ag Novel heterocyclic compounds and uses therof
AU2009260389A1 (en) 2008-06-18 2009-12-23 Merck Sharp & Dohme Corp. Inhibitors of Janus kinases
CA2726836C (en) 2008-06-26 2019-06-18 Anterios, Inc. Use of nanoemulsions in the manufacture of a medicament for treating skin disorders
UY31952A (es) 2008-07-02 2010-01-29 Astrazeneca Ab 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim
FR2933409B1 (fr) 2008-07-03 2010-08-27 Centre Nat Rech Scient NOUVEAUX PYRROLO °2,3-a! CARBAZOLES ET LEUR UTILISATION COMME INHIBITEURS DES KINASES PIM
TWI496779B (zh) 2008-08-19 2015-08-21 Array Biopharma Inc 作為pim激酶抑制劑之三唑吡啶化合物
US8557809B2 (en) 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
CN102131812B (zh) 2008-08-20 2014-04-09 硕腾有限责任公司 吡咯并[2,3-d]嘧啶化合物
US8759338B2 (en) 2008-09-02 2014-06-24 Novartis Ag Heterocyclic kinase inhibitors
MX2011002367A (es) 2008-09-02 2011-04-04 Novartis Ag Inhibidores de cinasa biciclicos.
CA2734415C (en) 2008-09-02 2016-07-26 Novartis Ag Picolinamide derivatives as kinase inhibitors
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
WO2010043052A1 (en) 2008-10-17 2010-04-22 Merck Frosst Canada Ltd. Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
JOP20190231A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
EP2210890A1 (en) 2009-01-19 2010-07-28 Almirall, S.A. Oxadiazole derivatives as S1P1 receptor agonists
US8263601B2 (en) 2009-02-27 2012-09-11 Concert Pharmaceuticals, Inc. Deuterium substituted xanthine derivatives
WO2010135650A1 (en) 2009-05-22 2010-11-25 Incyte Corporation N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
UA106078C2 (uk) 2009-05-22 2014-07-25 Інсайт Корпорейшн 3-[4-(7H-ПІРОЛО[2,3-d]ПІРИМІДИН-4-ІЛ)-1H-ПІРАЗОЛ-1-ІЛ]ОКТАН- АБО ГЕПТАННІТРИЛ ЯК JAK-ІНГІБІТОРИ
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077465A1 (es) 2009-07-08 2011-08-31 Leo Pharma As Derivados de pirrolopirimidina como inhibidores de receptores jak y protein tirosin quinasas y uso farmaceutico de los mismos
US20120157500A1 (en) 2009-08-24 2012-06-21 Weikang Tao Jak inhibition blocks rna interference associated toxicities
TW201111385A (en) 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
WO2011028685A1 (en) 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EP2475659B1 (en) 2009-09-08 2015-10-28 F.Hoffmann-La Roche Ag 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
EP2305660A1 (en) 2009-09-25 2011-04-06 Almirall, S.A. New thiadiazole derivatives
KR101805936B1 (ko) 2009-10-09 2017-12-07 인사이트 홀딩스 코포레이션 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체
JP5744887B2 (ja) 2009-10-20 2015-07-08 セルゾーム リミティッド Jak阻害剤としてのヘテロシクリルピラゾロピリミジン類似体
US8671402B2 (en) 2009-11-09 2014-03-11 Bank Of America Corporation Network-enhanced control of software updates received via removable computer-readable medium
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
JP5934652B2 (ja) 2009-11-24 2016-06-15 アルダーバイオ ホールディングス エルエルシー Il−6に対する抗体およびその使用
WO2011069141A2 (en) 2009-12-04 2011-06-09 Board Of Regents, The University Of Texas System Interferon therapies in combination with blockade of stat3 activation
JP5739446B2 (ja) 2009-12-18 2015-06-24 ファイザー・インク ピロロ[2,3−d]ピリミジン化合物
JP2013517220A (ja) 2010-01-12 2013-05-16 エフ.ホフマン−ラ ロシュ アーゲー 三環式複素環式化合物、その組成物、及び使用の方法
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
JP5858434B2 (ja) 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Janusキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
MX364636B (es) * 2010-03-10 2019-05-03 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
NZ603446A (en) 2010-04-14 2014-05-30 Array Biopharma Inc 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
EP2390252A1 (en) 2010-05-19 2011-11-30 Almirall, S.A. New pyrazole derivatives
SI2574168T1 (sl) 2010-05-21 2016-07-29 Incyte Holdings Corporation Topična formulacija zaviralca jak
WO2011156698A2 (en) 2010-06-11 2011-12-15 Abbott Laboratories NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
US9351943B2 (en) 2010-07-01 2016-05-31 Matthew T. McLeay Anti-fibroblastic fluorochemical emulsion therapies
US20130252917A1 (en) 2010-09-30 2013-09-26 Portola Pharmaceuticals, Inc. Combination therapy of 4-(3-(2h-1,2,3-triazo-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide and fludarabine
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
AU2011335882B2 (en) 2010-12-03 2016-03-10 Ym Biosciences Australia Pty Ltd Treatment of JAK2-mediated conditions
EP2675451B9 (en) 2011-02-18 2017-07-26 Novartis Pharma AG mTOR/JAK INHIBITOR COMBINATION THERAPY
CN102247368B (zh) 2011-05-19 2013-05-29 安徽永生堂药业有限责任公司 一种复方阿伐斯汀缓释片及其制备方法
CN102218042A (zh) 2011-05-26 2011-10-19 青岛黄海制药有限责任公司 富马酸喹硫平组合物的缓释片剂及其制备方法
AU2012273164B2 (en) 2011-06-20 2015-05-28 Incyte Holdings Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
WO2013007765A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
WO2013007768A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors
JP2014521725A (ja) 2011-08-10 2014-08-28 ノバルティス・ファルマ・アクチェンゲゼルシャフト JAKPI3K/mTOR併用療法
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
US10155987B2 (en) 2012-06-12 2018-12-18 Dana-Farber Cancer Institute, Inc. Methods of predicting resistance to JAK inhibitor therapy
ES2867048T3 (es) 2012-06-15 2021-10-20 Concert Pharmaceuticals Inc Derivados deuterados de ruxolitinib
WO2014016396A1 (en) 2012-07-27 2014-01-30 Ratiopharm Gmbh Oral dosage forms for modified release comprising ruxolitinib
CN102772384A (zh) 2012-08-07 2012-11-14 四川百利药业有限责任公司 一种盐酸米诺环素缓释片及其制备方法
WO2014036016A1 (en) 2012-08-31 2014-03-06 Principia Biopharma Inc. Benzimidazole derivatives as itk inhibitors
AR093308A1 (es) 2012-11-01 2015-05-27 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de jak
JP2015537030A (ja) 2012-11-15 2015-12-24 インサイト・コーポレイションIncyte Corporation ルキソリチニブの徐放性投薬形態
KR102366356B1 (ko) 2013-03-06 2022-02-23 인사이트 홀딩스 코포레이션 Jak 저해제를 제조하기 위한 방법 및 중간생성물
EA036448B1 (ru) 2013-05-17 2020-11-11 Инсайт Корпорейшн Производные бипиразола в качестве ингибиторов jak
EP3721873A1 (en) 2013-08-07 2020-10-14 Incyte Corporation Sustained release dosage forms for a jak1 inhibitor
EA201690421A1 (ru) 2013-08-20 2016-06-30 Инсайт Корпорейшн Положительный эффект в форме увеличения продолжительности жизни у больных с солидными опухолями с повышенными уровнями c-реактивного белка
PL3110409T3 (pl) 2014-02-28 2018-12-31 Incyte Corporation Inhibitory jak1 do leczenia zespołów mielodysplastycznych
CN111494386A (zh) 2014-04-08 2020-08-07 因赛特公司 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤
BR112016025427A2 (pt) 2014-04-30 2017-08-15 Incyte Corp processos de preparação de um inibidor de jak1 e formas do mesmo
ES2946179T3 (es) 2014-05-28 2023-07-13 Onco Tracker Inc Efectos antineoplásicos de inhibidores de JAK2 en combinación con derivados de talidomida y glucocorticoides
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
US10766900B2 (en) 2017-12-29 2020-09-08 Formosa Laboratories, Inc. Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof
CA3129096A1 (en) 2019-02-06 2020-08-13 Concert Pharmaceuticals, Inc. Process for preparing enantiomerically enriched jak inhibitors

Also Published As

Publication number Publication date
RS54823B1 (sr) 2016-10-31
NZ602313A (en) 2014-08-29
BR112012022513A2 (pt) 2016-08-30
US8765734B2 (en) 2014-07-01
PL3050882T3 (pl) 2018-08-31
HUE028723T2 (en) 2016-12-28
KR20200124776A (ko) 2020-11-03
ES2982015T3 (es) 2024-10-14
JP2020114868A (ja) 2020-07-30
TW202304922A (zh) 2023-02-01
RS57219B1 (sr) 2018-07-31
TWI694826B (zh) 2020-06-01
HUE049914T2 (hu) 2020-11-30
JP2017149779A (ja) 2017-08-31
TW201638088A (zh) 2016-11-01
SG183551A1 (en) 2012-10-30
PH12012501768A1 (en) 2012-11-12
SI3050882T1 (en) 2018-06-29
HRP20201086T1 (hr) 2020-10-30
EP3354652B1 (en) 2020-05-06
IL221823A (en) 2016-10-31
HUE037077T2 (hu) 2018-08-28
US20110224190A1 (en) 2011-09-15
KR20210095229A (ko) 2021-07-30
ES2908412T3 (es) 2022-04-29
SI3354652T1 (sl) 2020-08-31
HRP20160326T1 (hr) 2016-05-20
ZA201207420B (en) 2014-03-26
JP2025019114A (ja) 2025-02-06
EP3715347B1 (en) 2021-12-22
MX2012010344A (es) 2012-11-16
CR20120510A (es) 2013-01-11
US9464088B2 (en) 2016-10-11
KR20200033996A (ko) 2020-03-30
CN102985417B (zh) 2015-01-28
US9999619B2 (en) 2018-06-19
JP6318291B2 (ja) 2018-04-25
DK2545045T3 (en) 2016-01-25
KR101857680B1 (ko) 2018-05-14
EP4036088A1 (en) 2022-08-03
EP4400172A3 (en) 2024-11-06
US11285140B2 (en) 2022-03-29
MX2019005232A (es) 2019-08-05
KR20220015492A (ko) 2022-02-08
EP3050882B1 (en) 2018-01-31
CA2792508A1 (en) 2011-09-15
KR20130038834A (ko) 2013-04-18
JP2018118992A (ja) 2018-08-02
CA2792508C (en) 2018-01-16
TWI592413B (zh) 2017-07-21
JP2016094443A (ja) 2016-05-26
WO2011112662A1 (en) 2011-09-15
ME02386B (me) 2016-09-20
AU2011224484A1 (en) 2012-09-27
JP2023099660A (ja) 2023-07-13
MX347851B (es) 2017-05-16
HK1258929A1 (zh) 2019-11-22
US10695337B2 (en) 2020-06-30
CO6602158A2 (es) 2013-01-18
EA201290894A1 (ru) 2013-04-30
US20170246157A1 (en) 2017-08-31
PT3354652T (pt) 2020-07-20
PH12015502575A1 (en) 2017-04-24
NO3050882T3 (es) 2018-06-30
DK3050882T3 (en) 2018-03-19
ES2569539T3 (es) 2016-05-11
MY175156A (en) 2020-06-11
SMT201600085B (it) 2016-07-01
SMT201800137T1 (it) 2018-07-17
EP4400172A2 (en) 2024-07-17
MX364636B (es) 2019-05-03
TW201734014A (zh) 2017-10-01
ES2796377T3 (es) 2020-11-26
JP5858484B2 (ja) 2016-02-10
KR101911697B1 (ko) 2018-10-25
PT3050882T (pt) 2018-04-16
PL2545045T3 (pl) 2016-08-31
RS60680B1 (sr) 2020-09-30
US20200397774A1 (en) 2020-12-24
EA030376B1 (ru) 2018-07-31
EP3050882A1 (en) 2016-08-03
KR102354472B1 (ko) 2022-01-21
LT3050882T (lt) 2018-06-11
ECSP12012218A (es) 2012-11-30
CY1120154T1 (el) 2018-12-12
TWI766281B (zh) 2022-06-01
PE20130038A1 (es) 2013-01-28
LT3354652T (lt) 2020-09-25
EP3715347A1 (en) 2020-09-30
KR102172742B1 (ko) 2020-11-02
CN102985417A (zh) 2013-03-20
JP6158282B2 (ja) 2017-07-05
TW201906613A (zh) 2019-02-16
TWI850648B (zh) 2024-08-01
TW202102223A (zh) 2021-01-16
PH12015502575B1 (en) 2017-04-24
CY1123175T1 (el) 2021-10-29
DK3354652T3 (da) 2020-05-18
US20180353499A1 (en) 2018-12-13
ME03002B (me) 2018-10-20
TWI531572B (zh) 2016-05-01
KR20180054890A (ko) 2018-05-24
EP2545045A1 (en) 2013-01-16
US20230043959A1 (en) 2023-02-09
ES2662588T3 (es) 2018-04-09
SMT202000373T1 (it) 2020-09-10
KR20180117206A (ko) 2018-10-26
SI2545045T1 (sl) 2016-05-31
EP4036088B1 (en) 2024-04-03
PL3354652T3 (pl) 2020-11-16
MX354212B (es) 2018-02-19
MY192255A (en) 2022-08-11
EP2545045B1 (en) 2016-01-06
TW201206923A (en) 2012-02-16
JP7592784B2 (ja) 2024-12-02
AR081315A1 (es) 2012-08-08
HRP20180552T1 (hr) 2018-06-15
JP2013522214A (ja) 2013-06-13
EP3354652A1 (en) 2018-08-01
US20140275031A1 (en) 2014-09-18
CL2012002501A1 (es) 2012-12-14
HK1177741A1 (zh) 2013-08-30
TWI643857B (zh) 2018-12-11
KR102283091B1 (ko) 2021-07-30

Similar Documents

Publication Publication Date Title
PH12015502575B1 (en) Piperidin-4-yl azetidine derivatives as jak1 inhibitors
AU2018236800B2 (en) DNA-PK inhibitors
PH12018502125A1 (en) Bipyrazole derivatives as jak inhibitors
CA2871471C (en) Dna-pk inhibitors
PH12013502612A1 (en) Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
MY156727A (en) N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
PH12015500963A1 (en) Tricyclic fused thiophene derivatives as jak inhibitors
UA101493C2 (ru) Производные азетидина и циклобутана как ингибиторы jak
SG178986A1 (en) 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
PH12013502369A1 (en) Diazacarbazoles and methods of use
MX2011013032A (es) Inhibidores de fosfatidilinositol 3-cinasa.
MX2011008645A (es) Inhibidores de tetrahidrotiazolopiridina de fosfatidilinositol 3 cinasa.
MY198316A (en) Piperidin-4-YL Azetidine Derivatives as JAK1 Inhibitors
UA110108C2 (xx) Азетидинові похідні піперидин-4-ілу як інгібітори jak1
CY1117435T1 (el) Παραγωγα πιπεριδιν-4-υλ αζετιδινης ως αναστολεις jak1
EA201890558A1 (ru) Азетидиновые производные пиперидин-4-ила как ингибиторы jak1
UA110978C2 (uk) Азетидинілфенілові, піридилові або піразинілкарбоксамідні похідні як інгібітори jak

Legal Events

Date Code Title Description
FG Grant or registration