[go: up one dir, main page]

CY1118176T1 - Παραγωγα αζετιδινης και κυκλοβουτανιου ως αναστολεις των jak - Google Patents

Παραγωγα αζετιδινης και κυκλοβουτανιου ως αναστολεις των jak

Info

Publication number
CY1118176T1
CY1118176T1 CY20161101100T CY161101100T CY1118176T1 CY 1118176 T1 CY1118176 T1 CY 1118176T1 CY 20161101100 T CY20161101100 T CY 20161101100T CY 161101100 T CY161101100 T CY 161101100T CY 1118176 T1 CY1118176 T1 CY 1118176T1
Authority
CY
Cyprus
Prior art keywords
humans
animals
vitro
azetidine
matched
Prior art date
Application number
CY20161101100T
Other languages
English (en)
Inventor
James D Rodgers
Stacey Shepard
Yun-Long Li
Jiacheng Zhou
Pingli Liu
David Meloni
Michael Xia
Original Assignee
Incyte Holdings Corporation
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=40591836&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CY1118176(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Holdings Corporation filed Critical Incyte Holdings Corporation
Publication of CY1118176T1 publication Critical patent/CY1118176T1/el

Links

Classifications

    • 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
    • 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B60VEHICLES IN GENERAL
    • B60QARRANGEMENT OF SIGNALLING OR LIGHTING DEVICES, THE MOUNTING OR SUPPORTING THEREOF OR CIRCUITS THEREFOR, FOR VEHICLES IN GENERAL
    • B60Q3/00Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors
    • B60Q3/70Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors characterised by the purpose
    • B60Q3/76Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors characterised by the purpose for spotlighting, e.g. reading lamps
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B60VEHICLES IN GENERAL
    • B60QARRANGEMENT OF SIGNALLING OR LIGHTING DEVICES, THE MOUNTING OR SUPPORTING THEREOF OR CIRCUITS THEREFOR, FOR VEHICLES IN GENERAL
    • B60Q3/00Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors
    • B60Q3/80Circuits; Control arrangements
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S362/00Illumination
    • Y10S362/80Light emitting diode
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S362/00Illumination
    • Y10S362/802Position or condition responsive switch

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Mechanical Engineering (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Η μέθοδος συμπεριλαμβάνει τα στάδια επιτέλεσης in vitro προσδιορισμών που αφορούν το ήπαρ, το έντερο και/ή εκφρασμένα ένζυμα με επιλεγμένες εθνοβοτανικές ενώσεις, σε αμφότερους τους ανθρώπους και ποικίλα ζωικά είδη, προς παραγωγή ενός συνόλου χημικών οντοτήτων, για παράδειγμα μεταβολίτες, προς χρήση στους ανθρώπους και στα ζώα. Κατόπιν επιτελούνται συγκρίσεις μεταξύ των χημικών οντοτήτων από τις in vitro μελέτες σε ανθρώπους και από τις in vitro μελέτες σε ζώα προκειμένου να προσδιοριστεί η πλέον ταιριαστή ένωση. Το ζώο με την πλέον ταιριαστή ένωση κατόπιν χρησιμοποιείται σε in vivo μελέτη. Εάν η ταιριαστή ένωση ανιχνεύεται in vivo σε ζώα και in vitro σε ανθρώπους, η ταιριαστή χημική οντότητα απομονώνεται ή συντίθεται και κατόπιν δοκιμάζεται περαιτέρω προκειμένου να καθοριστεί η καταλληλότητα της ταιριαστής χημικής οντότητας ώστε να αποτελέσει φάρμακο αγωγής.
CY20161101100T 2008-03-11 2016-10-31 Παραγωγα αζετιδινης και κυκλοβουτανιου ως αναστολεις των jak CY1118176T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US3566208P 2008-03-11 2008-03-11
US14498209P 2009-01-15 2009-01-15
PCT/US2009/036635 WO2009114512A1 (en) 2008-03-11 2009-03-10 Azetidine and cyclobutane derivatives as jak inhibitors

Publications (1)

Publication Number Publication Date
CY1118176T1 true CY1118176T1 (el) 2017-06-28

Family

ID=40591836

Family Applications (2)

Application Number Title Priority Date Filing Date
CY20161101100T CY1118176T1 (el) 2008-03-11 2016-10-31 Παραγωγα αζετιδινης και κυκλοβουτανιου ως αναστολεις των jak
CY2017024C CY2017024I2 (el) 2008-03-11 2017-07-10 Παραγωγα αζετιδινης και κυκλοβουτανιου ως αναστολεις των jak

Family Applications After (1)

Application Number Title Priority Date Filing Date
CY2017024C CY2017024I2 (el) 2008-03-11 2017-07-10 Παραγωγα αζετιδινης και κυκλοβουτανιου ως αναστολεις των jak

Country Status (44)

Country Link
US (3) US8158616B2 (el)
EP (1) EP2288610B8 (el)
JP (2) JP5275371B2 (el)
KR (2) KR101240882B1 (el)
CN (2) CN103788098A (el)
AR (1) AR070828A1 (el)
AU (1) AU2009223640B2 (el)
BR (1) BRPI0909040B8 (el)
CA (1) CA2718271C (el)
CL (1) CL2009000576A1 (el)
CO (1) CO6290658A2 (el)
CY (2) CY1118176T1 (el)
DK (1) DK2288610T3 (el)
DO (2) DOP2010000270A (el)
EA (1) EA017218B1 (el)
EC (1) ECSP10010475A (el)
ES (1) ES2602577T3 (el)
HK (1) HK1149005A1 (el)
HN (1) HN2010001761A (el)
HR (1) HRP20161390T1 (el)
HU (2) HUE029767T2 (el)
IL (1) IL208023A (el)
LT (2) LT2288610T (el)
LU (1) LUC00027I2 (el)
MA (1) MA32219B1 (el)
MX (1) MX2010010012A (el)
MY (1) MY165582A (el)
NL (1) NL300886I2 (el)
NO (1) NO2017033I1 (el)
NZ (1) NZ587928A (el)
PA (1) PA8819201A1 (el)
PE (2) PE20091712A1 (el)
PL (1) PL2288610T3 (el)
PT (1) PT2288610T (el)
RS (1) RS55263B1 (el)
SG (1) SG191660A1 (el)
SI (1) SI2288610T1 (el)
SV (1) SV2010003662A (el)
TN (1) TN2010000415A1 (el)
TW (1) TWI444382B (el)
UA (1) UA101493C2 (el)
UY (1) UY31705A1 (el)
WO (1) WO2009114512A1 (el)
ZA (1) ZA201006000B (el)

Families Citing this family (289)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105814A1 (en) * 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
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
WO2008079965A1 (en) 2006-12-22 2008-07-03 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
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.
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
CN102083830B (zh) * 2008-03-24 2014-11-12 梅迪维新技术公司 吡啶并[3,4-b]吲哚和应用方法
KR20110033223A (ko) * 2008-06-20 2011-03-30 제넨테크, 인크. 트리아졸로피리딘 jak 억제제 화합물 및 방법
BRPI0909945A2 (pt) * 2008-06-20 2015-07-28 Genentech Inc "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinase em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase"
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
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
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
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
AU2015205858B2 (en) * 2010-03-10 2017-04-13 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
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
SI2574168T1 (sl) 2010-05-21 2016-07-29 Incyte Holdings Corporation Topična formulacija zaviralca jak
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
EA036970B1 (ru) * 2010-11-19 2021-01-21 Инсайт Холдингс Корпорейшн Применение {1-{1-[3-фтор-2-(трифтометил)изоникотиноил] пиперидин-4-ил}-3-[4-(7h-пирроло[2,3-d]пиримидин-4-ил)-1н-пиразол-1-ил]азетидин-3-ил}ацетонитрила для лечения заболеваний, связанных с активностью jak1
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
SG190957A1 (en) * 2010-12-01 2013-07-31 Nissan Chemical Ind Ltd Pyrazole compounds having therapeutic effect on multiple myeloma
EP2675451B9 (en) 2011-02-18 2017-07-26 Novartis Pharma AG mTOR/JAK INHIBITOR COMBINATION THERAPY
EP2675459A4 (en) 2011-02-18 2014-08-06 Medivation Technologies Inc COMPOUNDS AND METHODS FOR TREATING DIABETES
JP5938422B2 (ja) * 2011-03-08 2016-06-22 ジーイー・ヘルスケア・リミテッド Pet前駆体の製造
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
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
CN107898790B (zh) 2011-11-30 2024-06-21 埃默里大学 用于治疗或预防逆转录病毒和其它病毒感染的抗病毒jak抑制剂
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
SG10201805807PA (en) 2012-06-26 2018-08-30 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
RU2666538C2 (ru) * 2012-08-02 2018-09-11 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Замещенные пирролы, активные в качестве ингибиторов киназ
MX361499B (es) 2012-08-17 2018-12-06 Concert Pharmaceuticals Inc Baricitinib deuterado.
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
CN103965114B (zh) * 2013-01-28 2016-01-06 苏州泽璟生物制药有限公司 氘代的苯基氨基嘧啶化合物以及包含该化合物的药物组合物
KR102366356B1 (ko) 2013-03-06 2022-02-23 인사이트 홀딩스 코포레이션 Jak 저해제를 제조하기 위한 방법 및 중간생성물
WO2014146249A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
WO2014168986A1 (en) 2013-04-08 2014-10-16 Brown Dennis M Therapeutic benefit of suboptimally administered chemical compounds
EA036448B1 (ru) * 2013-05-17 2020-11-11 Инсайт Корпорейшн Производные бипиразола в качестве ингибиторов jak
CN105764501A (zh) 2013-07-26 2016-07-13 现代化制药公司 改善比生群治疗效益的组合物
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
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
SG10201806846RA (en) 2014-02-13 2018-09-27 Incyte Corp Cyclopropylamines as lsd1 inhibitors
PH12020552066A1 (en) 2014-02-13 2022-05-11 Incyte Corp Cyclopropylamines as lsd1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
PL3110409T3 (pl) 2014-02-28 2018-12-31 Incyte Corporation Inhibitory jak1 do leczenia zespołów mielodysplastycznych
US9340540B2 (en) 2014-02-28 2016-05-17 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
EP3134412A1 (en) 2014-03-28 2017-03-01 Sun Pharmaceutical Industries Limited Amorphous form of baricitinib
BR112016025427A2 (pt) 2014-04-30 2017-08-15 Incyte Corp processos de preparação de um inibidor de jak1 e formas do mesmo
EP3136857A4 (en) 2014-05-01 2017-09-20 Sun Pharmaceutical Industries Limited Crystalline form of baricitinib
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
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
ES2921875T3 (es) 2014-08-11 2022-09-01 Acerta Pharma Bv Combinaciones terapéuticas de un inhibidor BTK, un inhibidor PD-1 y/o un inhibidor PD-L1
WO2016024232A1 (en) 2014-08-11 2016-02-18 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor
SI3179991T1 (sl) 2014-08-11 2022-04-29 Acerta Pharma B.V. Terapevtske kombinacije zaviralca BTK in zaviralca BCL-2
AU2015303835B2 (en) 2014-08-12 2020-04-09 Monash University Lymph directing prodrugs
TWI679205B (zh) 2014-09-02 2019-12-11 日商日本新藥股份有限公司 吡唑并噻唑化合物及醫藥
CN105524067A (zh) * 2014-09-28 2016-04-27 江苏柯菲平医药股份有限公司 4-取代吡咯并[2,3-d]嘧啶化合物及其用途
EP3227298A4 (en) * 2014-12-05 2018-05-23 Sun Pharmaceutical Industries Ltd Process for the preparation of baricitinib and an intermediate thereof
CN105777754B (zh) 2014-12-16 2019-07-26 北京赛林泰医药技术有限公司 吡咯并嘧啶化合物
US10526350B2 (en) 2015-02-02 2020-01-07 Sun Pharmaceutical Industries Limited Process for the preparation of baricitinib and an intermediate thereof
EP3253760A4 (en) * 2015-02-02 2018-06-20 Sun Pharmaceutical Industries Limited Process for the preparation of baricitinib and an intermediate thereof
EP3262049B1 (en) 2015-02-27 2022-07-20 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CN105924444B (zh) * 2015-03-11 2019-06-18 苏州晶云药物科技股份有限公司 Jak抑制剂的晶型及其制备方法
EP3269719B1 (en) * 2015-03-11 2020-05-13 Crystal Pharmatech Co. Ltd. Crystal form of jak inhibitor and preparation method thereof
PH12017501817B1 (en) 2015-04-03 2023-06-16 Incyte Holdings Corp Heterocyclic compounds as lsd1 inhibitors
AR104918A1 (es) * 2015-06-19 2017-08-23 Lilly Co Eli Procesos e intermediarios para la preparación de {1-(etilsulfonil)-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrilo
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
TWI765860B (zh) 2015-08-12 2022-06-01 美商英塞特公司 Lsd1抑制劑之鹽
TWI707852B (zh) 2015-09-02 2020-10-21 美商林伯士拉克許米公司 Tyk2 抑制劑及其用途
WO2017041139A1 (en) 2015-09-08 2017-03-16 Monash University Lymph directing prodrugs
WO2017044720A1 (en) 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
CN106554363B (zh) * 2015-09-28 2019-03-05 正大天晴药业集团股份有限公司 一种Baricitinib中间体的制备方法
AU2016342027B2 (en) 2015-10-23 2021-05-13 Navitor Pharmaceuticals, Inc. Modulators of Sestrin-GATOR2 interaction and uses thereof
RU2601410C1 (ru) * 2015-11-13 2016-11-10 ЗАО "Р-Фарм" {3-[(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)АЗОЛИЛ]АЗЕТИДИН-3-ИЛ}АЦЕТОНИТРИЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС КИНАЗ
RU2603959C1 (ru) * 2015-11-13 2016-12-10 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") ДИХЛОРАЦЕТАТ {3-[4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-ПИРАЗОЛ-1-ИЛ]-1-ЭТИЛСУЛЬФОНИЛ-АЗЕТИДИН-3-ИЛ}-АЦЕТОНИТРИЛА В КАЧЕСТВЕ ИНГИБИТОРА ЯНУС КИНАЗ
CN105294699B (zh) * 2015-12-04 2019-06-11 上海勋和医药科技有限公司 巴瑞替尼的制备方法
EP3360878B9 (en) * 2015-12-11 2021-05-05 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Azetidine derivative, preparation method therefor, and use thereof
WO2017106352A1 (en) 2015-12-14 2017-06-22 Raze Therapeutics, Inc. Caffeine inhibitors of mthfd2 and uses thereof
HU230805B1 (hu) * 2015-12-23 2018-06-28 Egis Gyógyszergyár Zrt Eljárás és köztitermék baricitinib előállítására
HU230931B1 (hu) * 2016-01-21 2019-04-29 Egis Gyógyszergyár Zrt. Baricitinib sók
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
CN105566332B (zh) * 2016-01-29 2018-01-16 上海宣创生物科技有限公司 巴瑞克替尼三氟乙酸盐a晶型和b晶型及其制备方法
CN105601635B (zh) * 2016-02-01 2017-12-12 上海宣创生物科技有限公司 巴瑞克替尼磷酸盐的a晶型、h晶型和i晶型及其制备方法
CN105541891B (zh) * 2016-02-04 2017-11-28 东南大学 巴瑞替尼的中间体及其制备方法及由该中间体制备巴瑞替尼的方法
TWI712604B (zh) 2016-03-01 2020-12-11 日商日本新藥股份有限公司 具jak抑制作用之化合物之結晶
ES2949357T3 (es) 2016-03-09 2023-09-28 Raze Therapeutics Inc Inhibidores de 3-fosfoglicerato deshidrogenasa y usos de los mismos
EP3884939B1 (en) 2016-03-09 2023-10-25 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
CN107200742A (zh) * 2016-03-18 2017-09-26 罗欣生物科技(上海)有限公司 一种巴瑞克替尼磷酸盐晶体及其制备方法
CN107226814A (zh) * 2016-03-23 2017-10-03 罗欣生物科技(上海)有限公司 一种巴瑞克替尼中间体的制备方法
US11337969B2 (en) 2016-04-08 2022-05-24 X4 Pharmaceuticals, Inc. Methods for treating cancer
CN109414410B (zh) 2016-04-22 2022-08-12 因赛特公司 Lsd1抑制剂的制剂
CN107334738B (zh) * 2016-04-28 2021-02-09 天津科伦药物研究有限公司 一种含巴瑞克替尼的药物组合物及其制备方法和用途
JP7054529B2 (ja) 2016-06-21 2022-04-14 エックス4 ファーマシューティカルズ, インコーポレイテッド Cxcr4阻害剤およびその使用
US10988465B2 (en) 2016-06-21 2021-04-27 X4 Pharmaceuticals, Inc. CXCR4 inhibitors and uses thereof
EP3472129A4 (en) 2016-06-21 2019-12-04 X4 Pharmaceuticals, Inc. CXCR4 INHIBITORS AND USES THEREOF
WO2018019222A1 (zh) * 2016-07-26 2018-02-01 张文燕 作为jak抑制剂杂环化合物,该化合物的盐类及其治疗用途
CN106496233B (zh) * 2016-09-26 2018-05-15 东南大学 吡咯并嘧啶类化合物、其制备方法及其用途
TWI763722B (zh) 2016-10-14 2022-05-11 美商林伯士拉克許米公司 Tyk2抑制劑及其用途
JP7082120B2 (ja) 2016-10-21 2022-06-07 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用
EP3538091A4 (en) 2016-11-08 2020-06-10 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF
CZ2016705A3 (cs) 2016-11-11 2018-05-23 Zentiva, K.S. Krystalické formy 2- [1-ethylsulfonyl-3- [4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) pyrazol-1-yl] azetidin-3-yl] acetonitrilových solí a jejich příprava
CN110177544A (zh) 2016-11-29 2019-08-27 普尔泰克健康有限公司 用于递送治疗剂的外泌体
EP3327020A1 (en) 2016-11-29 2018-05-30 Sandoz Ag Citrate salts of a janus kinase (jak) inhibitor
WO2018106636A1 (en) 2016-12-05 2018-06-14 Raze Therapeutics, Inc. Shmt inhibitors and uses thereof
RU2644155C1 (ru) * 2016-12-12 2018-02-08 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") 2-(3-(4-(7H-пирроло[2,3-d]пиримидин-4-ил)-1H-пиразол-1-ил)-1-(этилсульфонил)азетидин-3-ил)ацетонитрила геминафтилдисульфонат в качестве ингибитора Янус киназ
CZ2016816A3 (cs) 2016-12-21 2018-07-04 Zentiva, K.S. Krystalické formy 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrilu s kyselinou fosforečnou a způsob jejich přípravy
CN110603261A (zh) 2016-12-23 2019-12-20 拜斯科阿迪有限公司 具有新型键结构的肽衍生物
EP3565638B8 (en) 2017-01-06 2024-04-10 BicycleRD Limited Bicycle conjugate for treating cancer
EA039344B1 (ru) * 2017-01-19 2022-01-17 Сучжоу Лонгбайотек Фармасьютикалз Ко., Лтд. Гетероциклическое соединение в качестве ингибитора jak и его соли и терапевтическое применение
US11524961B2 (en) 2017-01-23 2022-12-13 Shanghai Longwood Biopharmaceuticals Co., Ltd. JAK kinase inhibitor and preparation method and use thereof
AU2018230737B2 (en) 2017-03-08 2022-09-22 Takeda Pharmaceutical Company Limited Tyk2 inhibitors, uses, and methods for production thereof
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
CN106946917B (zh) * 2017-03-20 2019-06-11 杭州科巢生物科技有限公司 一种jak抑制剂巴瑞替尼及其中间体的新合成方法
CN107176955B (zh) * 2017-03-24 2019-04-09 南京优科制药有限公司 一种巴瑞替尼的制备方法
WO2018191146A1 (en) 2017-04-10 2018-10-18 Navitor Pharmaceuticals, Inc. Heteroaryl rheb inhibitors and uses thereof
US10912750B2 (en) 2017-04-26 2021-02-09 Navitor Pharmaceuticals, Inc. Modulators of Sestrin-GATOR2 interaction and uses thereof
WO2018197893A1 (en) 2017-04-27 2018-11-01 Bicycletx Limited Bicyclic peptide ligands and uses thereof
AU2018273866B2 (en) 2017-05-23 2021-09-30 Theravance Biopharma R&D Ip, Llc Glucuronide prodrugs of Janus kinase inhibitors
DK3636647T3 (da) * 2017-06-07 2023-02-06 Sichuan Kelun Biotech Biopharmaceutical Co Ltd Fastform af azetidinderivat og fremstillingsfremgangsmåde derfor samt anvendelse deraf
CN110799512A (zh) * 2017-06-22 2020-02-14 苏州科睿思制药有限公司 巴瑞克替尼的晶型及其制备方法
EP3645549A1 (en) 2017-06-26 2020-05-06 BicycleRD Limited Bicyclic peptide ligands with detectable moieties and uses thereof
WO2019003249A1 (en) 2017-06-28 2019-01-03 Mylan Laboratories Limited POLYMORPHIC FORMS OF BARICITINIB
BR112020001714A2 (pt) 2017-07-28 2020-07-21 Nimbus Lakshmi, Inc. inibidores de tyk2 e usos dos mesmos
CN118772242A (zh) 2017-08-04 2024-10-15 拜斯科技术开发有限公司 Cd137特异性的双环肽配体
EP3668887A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
WO2019034868A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF
EP3675838A4 (en) 2017-08-29 2021-04-21 PureTech LYT, Inc. Lymphatic system-directing lipid prodrugs
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
EP3684366A4 (en) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES OF THE LATEST
IL273432B (en) 2017-09-22 2022-09-01 Kymera Therapeutics Inc Protein degraders and uses thereof
CN109651424B (zh) * 2017-10-11 2021-01-22 新发药业有限公司 一种7-保护基-4-(1-氢-吡唑-4-基)吡咯[2,3-d]嘧啶的合成方法
LT3697789T (lt) 2017-10-18 2021-12-10 Incyte Corporation Kondensuoti imidazolo dariniai, pakeisti tretinėmis hidroksigrupėmis, kaip pi3k-gama inhibitoriai
SG11202002947TA (en) * 2017-11-03 2020-04-29 Aclaris Therapeutics Inc Substituted pyrrolopyrimidine jak inhibitors and methods of making and using the same
CN113149993A (zh) * 2017-12-01 2021-07-23 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
CN108129482A (zh) * 2017-12-13 2018-06-08 江苏中邦制药有限公司 一种巴瑞替尼的制备方法
WO2019126378A1 (en) 2017-12-19 2019-06-27 Ariya Therapeutics, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
EP3502114A1 (en) 2017-12-20 2019-06-26 Sandoz AG Co-crystal of an orally available janus kinase inhibitor
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
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
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
IL312674A (en) 2018-01-29 2024-07-01 Merck Patent Gmbh GCN2 inhibitors and uses thereof
CN118005640A (zh) 2018-01-29 2024-05-10 默克专利股份有限公司 Gcn2抑制剂及其用途
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
EP3759086A1 (en) 2018-02-27 2021-01-06 Artax Biopharma Inc. Chromene derivatives as inhibitors of tcr-nck interaction
CN110357887B (zh) * 2018-03-26 2022-09-16 武汉誉祥医药科技有限公司 取代的7H-吡咯并[2,3-d]嘧啶衍生物及其制备方法和用途
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
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
MX2020010815A (es) 2018-04-13 2020-12-11 Incyte Corp Biomarcadores para enfermedad de injerto contra hospedero.
SMT202200308T1 (it) 2018-04-24 2022-09-14 Vertex Pharma Composti antiproliferazione e loro usi
US11059826B2 (en) 2018-04-24 2021-07-13 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
CN108752254B (zh) * 2018-05-22 2021-11-02 道合(潍坊)医药技术有限公司 2-[1-(乙基磺酰基)-3-氮杂环丁亚基]乙腈的制备方法
CN112804994A (zh) * 2018-05-25 2021-05-14 卡托斯医疗公司 治疗骨髓增殖性肿瘤的方法
CN110446713B (zh) * 2018-06-06 2022-05-24 杭州澳津生物医药技术有限公司 一种吡唑嘧啶衍生物及其用途和药物组合物
KR20210021534A (ko) 2018-06-15 2021-02-26 나비토르 파마슈티칼스 인코포레이티드 라파마이신 유사체 및 이의 용도
US11180531B2 (en) 2018-06-22 2021-11-23 Bicycletx Limited Bicyclic peptide ligands specific for Nectin-4
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
MA53561A (fr) 2018-09-05 2022-05-11 Incyte Corp Formes cristallines d'un inhibiteur de phosphoinositide 3-kinase (pi3k)
JP2022500499A (ja) 2018-09-07 2022-01-04 ピク セラピューティクス, インコーポレイテッド Eif4e阻害剤およびその使用
CN109215136B (zh) 2018-09-07 2020-03-20 百度在线网络技术(北京)有限公司 一种真实数据增强方法、装置以及终端
CN109146898B (zh) 2018-09-07 2020-07-24 百度在线网络技术(北京)有限公司 一种仿真数据量增强方法、装置以及终端
WO2020072870A1 (en) 2018-10-05 2020-04-09 Johnson Matthey Public Limited Company Co-crystal forms of baricitinib
CN113271940A (zh) 2018-10-15 2021-08-17 林伯士拉克许米公司 Tyk2抑制剂和其用途
TW202033198A (zh) 2018-10-17 2020-09-16 美商美國禮來大藥廠 以巴瑞克替尼(baricitinib)治療原發性膽汁性膽管炎及原發性硬化性膽管炎
JP2022512779A (ja) 2018-10-23 2022-02-07 バイスクルテクス・リミテッド 二環式ペプチドリガンドおよびその使用
JP2022505849A (ja) 2018-10-24 2022-01-14 ナビター ファーマシューティカルズ, インコーポレイテッド 多形化合物およびその使用
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
JP7623943B2 (ja) 2018-11-30 2025-01-29 カイメラ セラピューティクス, インコーポレイテッド Irak分解剤およびそれらの使用
WO2020112937A1 (en) 2018-11-30 2020-06-04 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CN111320633B (zh) * 2018-12-14 2022-09-27 中国医药研究开发中心有限公司 吡咯/咪唑并六元杂芳环类化合物及其制备方法和医药用途
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
WO2020154474A1 (en) 2019-01-23 2020-07-30 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
AU2019426113B2 (en) * 2019-01-30 2022-06-16 Felicamed Biotechnology Co., Ltd. JAK inhibitor and preparation method therefor
WO2020163431A1 (en) 2019-02-05 2020-08-13 Teva Pharmaceuticals International Gmbh Crystalline solid forms of baricitinib
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
WO2020173364A1 (zh) * 2019-02-27 2020-09-03 四川科伦博泰生物医药股份有限公司 以氮杂环丁烷衍生物为活性成分的口服药物组合物、其制备方法及用途
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
WO2020188015A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
WO2020201753A1 (en) 2019-04-02 2020-10-08 Bicycletx Limited Bicycle toxin conjugates and uses thereof
AU2020253633A1 (en) 2019-04-05 2021-11-04 Kymera Therapeutics, Inc. STAT degraders and uses thereof
EP3725305A1 (en) 2019-04-17 2020-10-21 Zentiva K.S. Pharmaceutical composition containing baricitinib hydrobromide
KR20210141634A (ko) * 2019-04-24 2021-11-23 엘랑코 유에스 인코포레이티드 7h-피롤로[2,3-d]피리미딘 jak-억제제
CN110028509B (zh) * 2019-05-27 2020-10-09 上海勋和医药科技有限公司 作为选择性jak2抑制剂的吡咯并嘧啶类化合物、其合成方法及用途
BR112021024224A2 (pt) 2019-05-31 2022-04-26 Ikena Oncology Inc Inibidores de tead e usos dos mesmos
CN110256441A (zh) * 2019-06-24 2019-09-20 江苏君若医药有限公司 一种巴瑞克替尼的制备方法
TWI862640B (zh) 2019-07-30 2024-11-21 英商拜西可泰克斯有限公司 異質雙環肽複合物
EP3771715A1 (en) 2019-08-02 2021-02-03 Zaklady Farmaceutyczne "Polpharma" S.A. Crystalline forms of baricitinib
EP3771716A1 (en) 2019-08-02 2021-02-03 Zaklady Farmaceutyczne "Polpharma" S.A. Low hygroscopic amorphous form of baricitinib
WO2021050992A1 (en) 2019-09-11 2021-03-18 Vincere Biosciences, Inc. Usp30 inhibitors and uses thereof
PH12022550605A1 (en) 2019-09-13 2023-09-25 Nimbus Saturn Inc Hpk1 antagonists and uses thereof
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
CN110683978A (zh) * 2019-10-30 2020-01-14 西安医学院 一种3-腈基亚甲基氮杂环丁烷-1-碳酸叔丁酯的制备方法
EP4051259A4 (en) 2019-11-01 2023-11-22 Navitor Pharmaceuticals, Inc. Methods of treatment using an mtorc1 modulator
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
KR20220107213A (ko) 2019-11-22 2022-08-02 인사이트 코포레이션 Alk2 억제제 및 jak2 억제제를 포함하는 병용 요법
CN115209897A (zh) 2019-12-05 2022-10-18 安纳库利亚治疗公司 雷帕霉素类似物及其用途
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
KR20220145325A (ko) 2019-12-17 2022-10-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
AU2020405549A1 (en) 2019-12-19 2022-08-11 Liminal Biosciences Limited Cycloalkyl-containing carboxylic acids and uses thereof
CN115297931A (zh) 2019-12-23 2022-11-04 凯麦拉医疗公司 Smarca降解剂和其用途
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CA3166908A1 (en) 2020-02-05 2021-08-12 Daniel Kenneth BONNER Lipid prodrugs of neurosteroids
MX2022010944A (es) 2020-03-03 2022-11-09 Pic Therapeutics Inc Inhibidores del factor de iniciacion de traduccion eucariotica 4e (eif4e) y sus usos.
JP2023518423A (ja) 2020-03-19 2023-05-01 カイメラ セラピューティクス, インコーポレイテッド Mdm2分解剤およびそれらの使用
US20230218644A1 (en) 2020-04-16 2023-07-13 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
CN111362853A (zh) * 2020-04-27 2020-07-03 安徽大学 一种3-氧杂氮杂环丁烷-1-羧酸叔丁酯的制备方法
CN113582901A (zh) * 2020-05-01 2021-11-02 浙江瑞博制药有限公司 一种氧化反应氧化醇制备醛或酮的方法
TW202210471A (zh) 2020-06-02 2022-03-16 美商英塞特公司 製備jak1抑制劑之方法
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4161521A4 (en) 2020-06-03 2024-07-10 Kymera Therapeutics, Inc. DEUTERED IRAQ DEGRADERS AND USES THEREOF
CN111704617B (zh) * 2020-06-15 2022-08-23 嘉兴特科罗生物科技有限公司 一种小分子化合物
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
MX2023000056A (es) 2020-07-02 2023-04-12 Incyte Corp Compuestos tricíclicos de urea como inhibidores de la variante v617f de la cinasa de janus 2 (jak2 v617f).
CN111999400B (zh) * 2020-07-15 2022-07-01 安徽联创生物医药股份有限公司 一种用hplc分离测定巴瑞替尼原料药杂质的方法
CN111875534B (zh) * 2020-08-10 2022-06-17 烟台大学 1,8-二甲酰基咔唑的安全高效制备方法
CN111848491B (zh) * 2020-08-10 2022-06-17 烟台大学 1-甲酰基咔唑的制备方法
JP2023538906A (ja) 2020-08-17 2023-09-12 バイシクルティーエクス・リミテッド ネクチン-4に特異的な二環コンジュゲート及びその使用
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
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
US20230404925A1 (en) 2020-10-23 2023-12-21 Elanco Us Inc. Jak inhibitors having a specific particle size distribution
CN114437079B (zh) * 2020-10-30 2024-11-01 杭州邦顺制药有限公司 吡咯嘧啶五元氮杂环化合物的晶型
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
EP4255895A1 (en) 2020-12-02 2023-10-11 Ikena Oncology, Inc. Tead inhibitors and uses thereof
MX2023006542A (es) 2020-12-08 2023-08-25 Incyte Corp Inhibidores de la vía cinasa jano 1 (jak1) para el tratamiento del vitiligo.
EP4263559A1 (en) 2020-12-18 2023-10-25 Boehringer Ingelheim Animal Health USA Inc. Boron containing pyrazole compounds, compositions comprising them, methods and uses thereof
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
CN116867758A (zh) 2020-12-30 2023-10-10 凯麦拉医疗公司 Irak降解剂和其用途
EP4288430A1 (en) 2021-02-02 2023-12-13 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
CN117098757A (zh) 2021-02-02 2023-11-21 里米诺生物科学有限公司 Gpr84拮抗剂和其用途
CN114907354B (zh) * 2021-02-07 2024-04-09 南京知和医药科技有限公司 一种磺酰胺类多环化合物及其制备方法与用途
US12171768B2 (en) 2021-02-15 2024-12-24 Kymera Therapeutics, Inc. IRAK4 degraders and uses thereof
WO2022174269A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
AR125273A1 (es) 2021-02-25 2023-07-05 Incyte Corp Lactamas espirocíclicas como inhibidores de jak2 v617f
CN118459504A (zh) * 2021-02-26 2024-08-09 南京知和医药科技有限公司 一种巴瑞替尼衍生物及其制备方法与用途
US11926625B2 (en) 2021-03-05 2024-03-12 Nimbus Saturn, Inc. HPK1 antagonists and uses thereof
JP2024513011A (ja) 2021-03-29 2024-03-21 ニンバス サターン, インコーポレイテッド Hpk1アンタゴニスト及びその使用
WO2022221866A1 (en) 2021-04-16 2022-10-20 Ikena Oncology, Inc. Mek inhibitors and uses thereof
BR112023023223A2 (pt) 2021-05-07 2024-01-30 Kymera Therapeutics Inc Degradadores de cdk2 e usos dos mesmos
WO2023288197A1 (en) 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
EP4376844A1 (en) 2021-07-30 2024-06-05 Eli Lilly and Company Treatment of hand eczema with baricitinib
CN118019739A (zh) 2021-08-25 2024-05-10 皮克医疗公司 Eif4e抑制剂及其用途
TW202315621A (zh) 2021-08-25 2023-04-16 美商皮克醫療公司 Eif4e抑制劑及其用途
CN118302168A (zh) 2021-10-29 2024-07-05 凯麦拉医疗公司 Irak4降解剂和其制备
CN114373808B (zh) * 2021-11-26 2023-11-10 江苏科来材料科技有限公司 一种高效晶硅电池
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
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
JP2025504059A (ja) 2022-01-31 2025-02-06 カイメラ セラピューティクス, インコーポレイテッド Irakデグレーダー及びその使用
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
EP4493558A1 (en) 2022-03-17 2025-01-22 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
WO2023194842A1 (en) 2022-04-05 2023-10-12 Unichem Laboratories Limited Substituted tricyclic compounds and their use in rheumatoid arthritis
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
AU2023276599A1 (en) 2022-05-25 2024-12-05 Ikena Oncology, Inc. Mek inhibitors and uses thereof
CN117384163A (zh) * 2022-07-05 2024-01-12 盛世泰科生物医药技术(苏州)股份有限公司 一种含偕二氟基的化合物及其制备方法和用途
TW202415650A (zh) 2022-08-02 2024-04-16 英商利米那生物科技有限公司 芳基-三唑基及相關gpr84拮抗劑及其用途
TW202416972A (zh) 2022-08-02 2024-05-01 英商利米那生物科技有限公司 經取代之吡啶酮gpr84拮抗劑及其用途
WO2024028363A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Heteroaryl carboxamide and related gpr84 antagonists and uses thereof
CN115181103B (zh) * 2022-08-16 2023-11-07 上海博悦生物科技有限公司 一种巴瑞替尼的制备方法
TW202430148A (zh) 2022-11-22 2024-08-01 美商皮克醫療公司 eIF4E抑制劑及其用途
CN118255769A (zh) * 2022-12-28 2024-06-28 格格巫(珠海)生物科技有限公司 一种立体异构体的制备方法及中间体
WO2024193496A1 (zh) * 2023-03-17 2024-09-26 北京普祺医药科技股份有限公司 吡咯并嘧啶化合物或其可药用盐的制备方法
CN116444529B (zh) * 2023-06-16 2023-12-05 药康众拓(江苏)医药科技有限公司 一种氘代氮杂环丁烷类jak抑制剂及其用途

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US4548990A (en) 1983-08-15 1985-10-22 Ciba-Geigy Corporation Crosslinked, porous polymers for controlled drug delivery
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
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
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.
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
AU3565999A (en) 1999-04-16 2000-11-02 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
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
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
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
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
HU230798B1 (hu) 2001-10-30 2018-06-28 Novartis Ag Staurosporin-származékok mint az FLT3 receptor tirozin-kináz aktivitás inhibitorai
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
US20040019066A1 (en) * 2002-05-06 2004-01-29 Institut Pasteur Methionine salvage pathway in bacillus
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
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
GB0215676D0 (en) 2002-07-05 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
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
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
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
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
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
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
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
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
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
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
EP1760071A4 (en) 2004-06-23 2008-03-05 Ono Pharmaceutical Co COMPOUND WITH S1P RECEPTOR BINDING ABILITY AND USE THEREOF
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
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
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
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
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.
ES2320487T3 (es) 2005-02-03 2009-05-22 Vertex Pharmaceuticals, Inc. Pirrolopirimidinas utiles como inhibidores de proteina quinasas.
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
EP2354140A1 (en) 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
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
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
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
UA95940C2 (uk) 2006-01-17 2011-09-26 Вертекс Фармасьютикалс Інкорпорейтед Азаіндоли як інгібітори кіназ януса
AU2007235487A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
TW200805992A (en) * 2006-07-04 2008-01-16 Benq Corp Method and apparatus for barring short message
WO2008079965A1 (en) 2006-12-22 2008-07-03 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
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

Also Published As

Publication number Publication date
JP5275371B2 (ja) 2013-08-28
EP2288610B1 (en) 2016-08-31
LTC2288610I2 (lt) 2019-02-25
US20130225556A1 (en) 2013-08-29
BRPI0909040B8 (pt) 2021-05-25
CN102026999B (zh) 2014-03-05
PE20091712A1 (es) 2009-11-21
PL2288610T3 (pl) 2017-12-29
KR101240882B1 (ko) 2013-03-11
ES2602577T3 (es) 2017-02-21
HK1149005A1 (zh) 2011-09-23
HN2010001761A (es) 2013-09-02
MA32219B1 (fr) 2011-04-01
JP2013155179A (ja) 2013-08-15
JP2011514909A (ja) 2011-05-12
US20120077798A1 (en) 2012-03-29
MY165582A (en) 2018-04-05
CL2009000576A1 (es) 2009-06-19
BRPI0909040A8 (pt) 2017-12-12
US8420629B2 (en) 2013-04-16
LUC00027I1 (el) 2017-07-12
NO2017033I2 (no) 2017-07-11
EA201071057A1 (ru) 2011-02-28
PA8819201A1 (es) 2010-07-27
TW200942545A (en) 2009-10-16
NL300886I2 (nl) 2017-10-24
AU2009223640A1 (en) 2009-09-17
CO6290658A2 (es) 2011-06-20
DOP2010000270A (es) 2010-10-15
LT2288610T (lt) 2016-12-12
MX2010010012A (es) 2010-10-20
HUS1700031I1 (hu) 2017-09-28
KR20120108042A (ko) 2012-10-04
LUC00027I2 (el) 2017-09-25
CY2017024I1 (el) 2017-11-14
BRPI0909040A2 (el) 2017-09-19
BRPI0909040B1 (pt) 2019-10-22
NZ587928A (en) 2012-08-31
HRP20161390T1 (hr) 2016-12-02
EP2288610B8 (en) 2016-10-12
US20090233903A1 (en) 2009-09-17
RS55263B1 (sr) 2017-02-28
US8158616B2 (en) 2012-04-17
CA2718271C (en) 2014-05-06
CA2718271A1 (en) 2009-09-17
ECSP10010475A (es) 2010-10-30
PT2288610T (pt) 2016-10-17
KR20100121657A (ko) 2010-11-18
ZA201006000B (en) 2012-01-25
CN102026999A (zh) 2011-04-20
TN2010000415A1 (en) 2011-12-29
HUE029767T2 (en) 2017-04-28
SI2288610T1 (sl) 2016-11-30
NO2017033I1 (no) 2017-07-11
SG191660A1 (en) 2013-07-31
WO2009114512A1 (en) 2009-09-17
AU2009223640B2 (en) 2013-07-04
AR070828A1 (es) 2010-05-05
CY2017024I2 (el) 2017-11-14
LTPA2017023I1 (lt) 2017-08-10
EP2288610A1 (en) 2011-03-02
CN103788098A (zh) 2014-05-14
DK2288610T3 (en) 2016-11-28
TWI444382B (zh) 2014-07-11
SV2010003662A (es) 2011-03-17
IL208023A (en) 2015-08-31
UY31705A1 (es) 2009-08-03
UA101493C2 (ru) 2013-04-10
EA017218B1 (ru) 2012-10-30
IL208023A0 (en) 2010-12-30
PE20140099A1 (es) 2014-02-06
DOP2013000036A (es) 2013-03-15

Similar Documents

Publication Publication Date Title
CY1118176T1 (el) Παραγωγα αζετιδινης και κυκλοβουτανιου ως αναστολεις των jak
CY1124426T1 (el) Φαρμακευτικες συνθεσεις οι οποιες περιεχουν νιτρωδες νατριο
EA200801565A1 (ru) Производные пиримидиниларилмочевины в качестве ингибиторов фактора роста фибробластов ( fgf-фактора )
CY1118611T1 (el) Συνδυασμοι που περιεχουν παραγωγα της 6-βενζυλο-φαινυλο-2-θειοτετραϋδροπυραν-3,4,5-τριολης ως αναστολεις των συμμεταφορεων 1 και 2 νατριου-γλυκοζης για να χρησιμοποιηθουν σε διαβητικους ασθενεις
CY1117319T1 (el) Τρικυκλικα παραγωγα αμινης ως αναστολεις πρωτεϊνικης τυροσινης κινασης
CY1112369T1 (el) 2-μεθυλο-2-[4-(3-μεθυλο-2-οξο-8-κινολιν-3-υλο-2,3-διϋδρο-ιμιδαζο[4,5-c]κινολινυλο)-φαινυλο]προπιονιτριλιο ως αναστολεας λιπιδικης κινασης
EA200970149A1 (ru) Производные n-(аминогетероарил)-1h-индол-2-карбоксамидов, их получение и их применение в терапии
CY1116700T1 (el) Παρασκευη συνθετικου χολικου οξεος
CY1114617T1 (el) Αμινοτετραϋδροπυρανια ως αναστολεις διπεπτιδυλο πεπτιδασης-iv για την αγωγη ή προληψη διαβητη
UY30498A1 (es) Nueva clase de compuestos de benzimidazolilo, sus sales, composiciones farmacéuticas conteniéndolos y aplicaciones
NO20070293L (no) Aryl-substituerte piperazinderivater
EA201170772A1 (ru) Органические соединения
EA200800321A1 (ru) Ингибиторы гистондеацетилазы
EA200801560A1 (ru) Бифенилкарбоксамиды
ATE514755T1 (de) Fluoreszenzfarbstoffe zur verwendung bei der glukoseerfassung
EA200801291A1 (ru) Карбониламинопирролопиразолы в качестве эффективных ингибиторов киназ
ECSP088376A (es) Derivados de triazolopiridina en calidad de inhibidores de lipasas y fosfolipasas
CY1111789T1 (el) Ετεροκυκλικες ενωσεις
CY1114397T1 (el) Φαρμακευτικες συνθεσεις οι οποιες περιλαμβανουν βακτηρια τα οποια μειωνουν οξαλικα
CY1111706T1 (el) Παραγωγα αρυλο- και ετεροαρυλο-πιπεριδινοκαρβοξυλικων αλατων, η παρασκευη τους και η εφαρμογη τους ως αναστολεις του ενζυμου faah
EA200970605A1 (ru) Ингибиторы mapk/erk-киназ
EA200802213A1 (ru) Способы лечения заболеваний крови
UA106875C2 (uk) Тіадіазолілоксифеніламідини та їх застосування як фунгіцидів
EA201270535A1 (ru) Пуриновые производные, применимые в качестве ингибиторов hsp90
CY1113651T1 (el) Αντιφλεγμονωδη σκευασματα