[go: up one dir, main page]

EA201891157A1 - Способы и промежуточные соединения при получении ингибитора jak - Google Patents

Способы и промежуточные соединения при получении ингибитора jak

Info

Publication number
EA201891157A1
EA201891157A1 EA201891157A EA201891157A EA201891157A1 EA 201891157 A1 EA201891157 A1 EA 201891157A1 EA 201891157 A EA201891157 A EA 201891157A EA 201891157 A EA201891157 A EA 201891157A EA 201891157 A1 EA201891157 A1 EA 201891157A1
Authority
EA
Eurasian Patent Office
Prior art keywords
methods
intermediate compounds
receiving
jak inhibitor
diseases
Prior art date
Application number
EA201891157A
Other languages
English (en)
Inventor
Пинли Лю
Дэнцзинь Ван
Юнчжун У
Ганьфэн Цао
Майкл Ксиа
Original Assignee
Инсайт Холдингс Корпорейшн
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=50382653&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201891157(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Инсайт Холдингс Корпорейшн filed Critical Инсайт Холдингс Корпорейшн
Publication of EA201891157A1 publication Critical patent/EA201891157A1/ru

Links

Classifications

    • 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
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01JCHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/02Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01JCHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/26Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups B01J31/02 - B01J31/24
    • B01J31/28Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups B01J31/02 - B01J31/24 of the platinum group metals, iron group metals or copper
    • 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
    • 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
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/04Esters of boric acids

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Настоящее изобретение относится к способам и промежуточным соединениям для изготовления {1-{1-[3-фтор-2-(трифторметил)изоникотиноил]пиперидин-4-ил}-3-[4-(7H-пирроло[2,3-d]пиримидин-4-ил)-1Н-пиразол-1-ил]азетидин-3-ил}ацетонитрил, полезными при лечении заболеваний, связанных с активностью киназы Януса (JAK), включая воспалительные заболевания, аутоиммунные заболевания, рак, и других заболеваний.
EA201891157A 2013-03-06 2014-03-05 Способы и промежуточные соединения при получении ингибитора jak EA201891157A1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361773659P 2013-03-06 2013-03-06

Publications (1)

Publication Number Publication Date
EA201891157A1 true EA201891157A1 (ru) 2019-02-28

Family

ID=50382653

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201891157A EA201891157A1 (ru) 2013-03-06 2014-03-05 Способы и промежуточные соединения при получении ингибитора jak
EA201591650A EA030705B1 (ru) 2013-03-06 2014-03-05 Способы и промежуточные соединения при получении ингибитора jak

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA201591650A EA030705B1 (ru) 2013-03-06 2014-03-05 Способы и промежуточные соединения при получении ингибитора jak

Country Status (36)

Country Link
US (3) US8987443B2 (ru)
EP (3) EP3489239B1 (ru)
JP (2) JP6397831B2 (ru)
KR (2) KR102366356B1 (ru)
CN (1) CN105189509B (ru)
AR (2) AR095018A1 (ru)
AU (1) AU2014225938B2 (ru)
BR (2) BR122021015061B1 (ru)
CA (2) CA3091179C (ru)
CL (2) CL2015002468A1 (ru)
CR (2) CR20190518A (ru)
CY (2) CY1121512T1 (ru)
DK (1) DK2964650T3 (ru)
EA (2) EA201891157A1 (ru)
ES (2) ES2900492T3 (ru)
HK (1) HK1218540A1 (ru)
HR (2) HRP20211922T1 (ru)
HU (2) HUE057262T2 (ru)
IL (3) IL240891A0 (ru)
LT (2) LT3489239T (ru)
ME (1) ME03350B (ru)
MX (2) MX2015011667A (ru)
NZ (2) NZ749437A (ru)
PE (2) PE20151902A1 (ru)
PH (1) PH12015501958B1 (ru)
PL (2) PL2964650T3 (ru)
PT (2) PT2964650T (ru)
RS (2) RS62867B1 (ru)
SG (2) SG10201707259PA (ru)
SI (2) SI2964650T1 (ru)
SM (2) SMT202100694T1 (ru)
TR (1) TR201820520T4 (ru)
TW (1) TWI634121B (ru)
UA (2) UA121532C2 (ru)
WO (1) WO2014138168A1 (ru)
ZA (1) ZA201908345B (ru)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2543904T3 (es) 2005-12-13 2015-08-25 Incyte Corporation Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas sustituidas con heteroarilo como inhibidores de quinasas Janus
EP4011883A1 (en) 2007-06-13 2022-06-15 Incyte Holdings Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3-cyclopentylpropanenitrile
SI2432472T1 (sl) 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
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
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
NZ602313A (en) 2010-03-10 2014-08-29 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
MY161078A (en) 2010-05-21 2017-04-14 Incyte Holdings Corp Topical formulation for a jak inhibitor
JP5917545B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Jak阻害剤としてのシクロブチル置換ピロロピリジンおよびピロロピリミジン誘導体
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
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
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
EP2906651B1 (en) 2012-10-09 2021-09-15 Avery Dennison Corporation Adhesives and related methods
TWI646099B (zh) 2012-11-01 2019-01-01 英塞特控股公司 作爲jak抑制劑之三環稠合噻吩衍生物
US10166191B2 (en) 2012-11-15 2019-01-01 Incyte Corporation Sustained-release dosage forms of ruxolitinib
CA2897200C (en) 2013-01-14 2021-07-06 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
TW201932456A (zh) 2013-01-15 2019-08-16 美商英塞特控股公司 適用作pim激酶抑制劑之噻唑甲醯胺及吡啶甲醯胺化合物
UA121532C2 (uk) 2013-03-06 2020-06-10 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки при отриманні інгібітора jak
EP3527263B1 (en) 2013-05-17 2020-10-28 Incyte Corporation Bipyrazole derivatives as jak inhibitors
CN116036089A (zh) 2013-08-07 2023-05-02 因赛特控股公司 Jak1抑制剂的持续释放剂型
CR20160135A (es) 2013-08-23 2016-08-05 Incyte Corp Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de cinasas pim
HUE051625T2 (hu) 2014-04-08 2021-03-29 Incyte Corp B-sejtes rosszindulatú daganatok kezelése JAK és PI3K inhibitorok kombinációjával
CR20160553A (es) 2014-04-30 2017-04-25 Incyte Corp Procesos para preparar un inhibidor de jak1 y nuevas formas de este
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
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
US10106525B2 (en) 2015-01-26 2018-10-23 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
US10857157B2 (en) 2015-01-26 2020-12-08 BioAxone BioSciences, Inc. Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase 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
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Pim激酶抑制劑之鹽
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
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
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
CN107759623B (zh) * 2016-08-23 2020-08-14 苏州旺山旺水生物医药有限公司 Jak抑制剂的中间体及其制备方法
CN106496195B (zh) * 2016-10-18 2019-03-08 杭州科巢生物科技有限公司 巴瑞替尼及其中间体的合成方法
US11198680B2 (en) 2016-12-21 2021-12-14 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
JP7117306B2 (ja) * 2016-12-21 2022-08-12 バイオアクソン バイオサイエンシーズ インコーポレイテッド Rhoキナーゼ阻害剤BA‐1049(R)及びその活性代謝物
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
WO2019014322A1 (en) 2017-07-11 2019-01-17 BioAxone BioSciences, Inc. KINASE INHIBITORS FOR THE TREATMENT OF DISEASES
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
CR20200379A (es) 2018-01-30 2021-03-05 Incyte Corp Procesos e intermedio para elaborar un inhibidor de jak campo técnico
PE20212186A1 (es) 2018-02-16 2021-11-11 Incyte Corp Inhibidores de la via de jak1 para el tratamiento de trastornos relacionados con citoquinas
AU2019245420B2 (en) 2018-03-30 2024-10-10 Incyte Corporation Treatment of hidradenitis suppurativa using JAK inhibitors
JP7565798B2 (ja) 2018-03-30 2024-10-11 インサイト・コーポレイション 炎症性皮膚疾患のバイオマーカー
JP7378420B2 (ja) 2018-04-13 2023-11-13 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
EP3801533A1 (en) 2018-06-01 2021-04-14 Incyte Corporation Dosing regimen for the treatment of pi3k related disorders
TWI808250B (zh) * 2018-09-04 2023-07-11 美商施萬生物製藥研發 Ip有限責任公司 用於製備jak抑制劑之方法及其中間體
MX2021004946A (es) 2018-10-31 2021-07-15 Incyte Corp Terapia combinada para tratamiento de enfermedades hematológicas.
EP3897627A1 (en) 2018-12-19 2021-10-27 Incyte Corporation Jak1 pathway inhibitors for the treatment of gastrointestinal disease
CA3132371A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Jak1 pathway inhibitors for the treatment of chronic lung allograft dysfunction
TW202102222A (zh) 2019-03-19 2021-01-16 美商英塞特公司 白斑病之生物標記物
CN112225739B (zh) * 2019-07-15 2024-04-26 宜昌东阳光制药有限公司 一种氮杂环丁烷化合物的制备方法
WO2021072098A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021072116A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
CN110627714A (zh) * 2019-10-16 2019-12-31 安庆博曼生物技术有限公司 3-氟-2-三氟甲基异烟酸的合成方法
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)
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
CN111320634A (zh) * 2020-04-14 2020-06-23 浙江工业大学 一种乙酰氧取代的吡咯并[2,3-d]嘧啶衍生物的制备方法
BR112022024632A2 (pt) 2020-06-02 2023-02-28 Incyte Corp Processos para preparar um inibidor de jak1
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
IL300557A (en) 2020-08-18 2023-04-01 Incyte Corp Process and intermediates for preparing a JAK1 inhibitor
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
JP2023552424A (ja) 2020-12-04 2023-12-15 インサイト・コーポレイション 皮膚疾患の治療のためのビタミンd類似体を有するjak阻害剤
TW202237089A (zh) 2020-12-08 2022-10-01 美商英塞特公司 用於治療白斑病之jak1途徑抑制劑
CN112625030A (zh) * 2020-12-25 2021-04-09 杭州澳赛诺生物科技有限公司 一种一锅法合成n-保护3-溴代吡唑的合成方法
US11918581B2 (en) 2021-01-11 2024-03-05 Incyte Corporation Combination therapy comprising JAK pathway inhibitor and rock inhibitor
JP2024526762A (ja) 2021-07-12 2024-07-19 インサイト・コーポレイション Jak阻害剤を調製するためのプロセス及び中間体
IL318652A (en) 2022-08-05 2025-03-01 Incyte Corp Treatment of urticaria with JAK inhibitors

Family Cites Families (285)

* 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
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
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
US4921947A (en) 1986-03-31 1990-05-01 Eli Lilly And Company Process for preparing macrolide 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
US5378700A (en) 1989-10-11 1995-01-03 Teijin Limited Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient
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
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
CN1105113C (zh) 1995-07-05 2003-04-09 纳幕尔杜邦公司 杀真菌嘧啶酮
CN1100778C (zh) 1995-07-06 2003-02-05 诺瓦蒂斯有限公司 吡咯并嘧啶及其制备方法
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
JP2000504023A (ja) 1996-04-03 2000-04-04 メルク エンド カンパニー インコーポレーテッド 癌治療方法
CA2251955A1 (en) 1996-04-18 1997-10-23 Nancy E. Kohl A method of treating cancer
US5795909A (en) 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
EP0934270A1 (en) 1996-05-30 1999-08-11 Merck & Co., Inc. A method of treating cancer
US6624138B1 (en) 2001-09-27 2003-09-23 Gp Medical Drug-loaded biological material chemically treated with genipin
EP0973396A4 (en) 1997-04-07 2001-02-07 Merck & Co Inc METHOD FOR TREATING CANCER
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
US5908841A (en) 1997-08-11 1999-06-01 Boehringer Ingelheim Pharmaceuticals, Inc. 5,11-dihydro-6H-dipyrido 3,2-b:2',3'-e!azepine-6-ones and their use in the prevention of treatment of HIV infection
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
SK18542000A3 (sk) 1998-06-04 2001-12-03 Abbott Laboratories Protizápalové zlúčeniny inhibujúce bunkovú adhéziu
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
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
ES2342240T3 (es) 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
JP2000119271A (ja) 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd 1h―イミダゾピリジン誘導体
US6713089B1 (en) 1998-09-10 2004-03-30 Nycomed Danmark A/S Quick release pharmaceutical compositions of drug substances
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
US6375839B1 (en) 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
WO2000051614A1 (en) 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferases
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
WO2000063168A1 (en) 1999-04-16 2000-10-26 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
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
DK1382339T3 (da) 1999-12-10 2008-01-28 Pfizer Prod Inc Kompositioner indeholdende pyrrolo 2,3-d pyrimidinderivater
KR100910488B1 (ko) 1999-12-24 2009-08-04 아벤티스 파마 리미티드 아자인돌
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
PT1142566E (pt) 2000-04-07 2004-02-27 Medidom Lab Formulacao oftalmica topica na forma de uma solucao aquosa e uso de uma ciclosporina em associacao com acido hialuronico ou um de seus sais e com polisorbato 80
WO2001081345A1 (fr) 2000-04-20 2001-11-01 Mitsubishi Pharma Corporation Composes d'amides aromatiques
AU5566701A (en) 2000-04-25 2001-11-07 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
EP1294752A2 (en) 2000-06-16 2003-03-26 Curis, Inc. Angiogenesis-modulating compositions and uses
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
CN100548375C (zh) 2000-06-23 2009-10-14 田边三菱制药株式会社 抗肿瘤作用增效剂
CA2412560C (en) 2000-06-26 2008-12-30 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine compounds as immunosuppressive agents
KR100786927B1 (ko) 2000-06-28 2007-12-17 스미스클라인비이참피이엘시이 습식 분쇄방법
AU2001278790A1 (en) 2000-08-22 2002-03-04 Hokuriku Seiyaku Co. Ltd 1h-imidazopyridine derivatives
MXPA03005001A (es) 2000-12-05 2003-09-05 Vertex Pharma Inhibidores de n- terminal c-jun cinasas (jnk) y otras proteinas cinasas.
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
JP2004528295A (ja) 2001-01-30 2004-09-16 サイトピア ピーティワイ リミテッド キナーゼ阻害方法
AU2002308748A1 (en) 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as 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
JP4286134B2 (ja) 2001-08-01 2009-06-24 メルク エンド カムパニー インコーポレーテッド ベンズイミダゾ[4,5−f]イソキノリノン誘導体
EA007983B1 (ru) 2001-09-19 2007-02-27 Авентис Фарма С.А. Индолизины в качестве ингибиторов киназных белков
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
CA2462657C (en) 2001-10-30 2011-04-26 Novartis Ag Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
JP2003155285A (ja) 2001-11-19 2003-05-27 Toray Ind Inc 環状含窒素誘導体
KR20040058340A (ko) 2001-11-30 2004-07-03 데이진 가부시키가이샤 5-(3-시아노페닐)-3-포르밀벤조산 화합물의 제조 방법
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
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
EP1506189A1 (en) 2002-04-26 2005-02-16 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
AU2003234439A1 (en) 2002-05-07 2003-11-11 Control Delivery Systems, Inc. Processes for forming a drug delivery device
ATE377004T1 (de) 2002-05-23 2007-11-15 Cytopia Pty Ltd Proteinkinaseinhibitoren
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
CN1630668A (zh) 2002-06-26 2005-06-22 出光兴产株式会社 氢化共聚物及其制备方法以及包含氢化共聚物的热熔粘合剂组合物
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
AU2003252478A1 (en) 2002-07-10 2004-02-02 Ono Pharmaceutical Co., Ltd. Ccr4 antagonist and medicinal use thereof
EP1542768A1 (en) 2002-09-20 2005-06-22 Alcon, Inc. Use of cytokine synthesis inhibitors for the treatment of dry eye disorders
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
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
US20040099204A1 (en) 2002-11-25 2004-05-27 Nestor John J. Sheet, page, line, position marker
WO2004047843A1 (en) 2002-11-26 2004-06-10 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
WO2004072063A1 (en) 2003-02-07 2004-08-26 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
CA2522595A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301373D0 (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
US8362017B2 (en) 2003-08-29 2013-01-29 Exelixis, Inc. C-kit modulators and methods of use
EP1678147B1 (en) 2003-09-15 2012-08-08 Lead Discovery Center GmbH Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
CA2543452C (en) 2003-10-24 2012-03-13 Santen Pharmaceutical Co., Ltd. Therapeutic agent for keratoconjunctival disorder
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
EP1689407A1 (en) 2003-11-25 2006-08-16 Pfizer Products Inc. Method of treatment of atherosclerosis
RU2006120956A (ru) 2003-12-17 2008-01-27 Пфайзер Продактс Инк. (Us) Пирроло{2, 3-d}пиримидиновые соединения для лечения отторжения трансплантата
MXPA06007076A (es) 2003-12-19 2006-08-31 Pharmacopeia Drug Discovery Tiadiazoles como ligandos del receptor cxc y cc-quimiocina.
DK1696920T3 (en) 2003-12-19 2015-01-19 Plexxikon Inc RELATIONS AND PROCEDURES FOR THE DEVELOPMENT OF LAW MODULATORS
CA2548374C (en) 2003-12-23 2014-05-27 Astex Therapeutics Limited 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
EP1744751A4 (en) 2004-03-18 2010-03-10 Brigham & Womens Hospital TREATMENT OF SYNUCLEINOPATHIES
MXPA06011327A (es) 2004-03-30 2006-12-15 Vertex Pharma Azaindoles utiles como inhibidores de jak y otras proteinas cinasas.
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス, インコーポレイテッド キナーゼ調節因子および使用方法
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
EP1755680A1 (en) 2004-05-03 2007-02-28 Novartis AG Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor
US20060074102A1 (en) 2004-05-14 2006-04-06 Kevin Cusack Kinase inhibitors as therapeutic agents
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
JP4688876B2 (ja) 2004-06-10 2011-05-25 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
EP1760071A4 (en) 2004-06-23 2008-03-05 Ono Pharmaceutical Co COMPOUND WITH S1P RECEPTOR BINDING ABILITY AND USE THEREOF
AU2005260689B2 (en) 2004-06-30 2012-05-10 Vertex Pharmaceuticals 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
KR100858262B1 (ko) 2004-10-13 2008-09-11 에프. 호프만-라 로슈 아게 Cdk2 및 혈관신생에 대한 저해제로서 유용하고, 유방암,대장암, 폐암 및 전립선암의 치료용으로 유용한이중치환된 피라졸로벤조디아제핀
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
KR20070090172A (ko) 2004-11-04 2007-09-05 버텍스 파마슈티칼스 인코포레이티드 단백질 키나아제의 억제제로서 유용한피라졸로[1,5-a]피리미딘
KR20070085433A (ko) 2004-11-24 2007-08-27 노파르티스 아게 Jak 저해제들과 bcr-abl, flt-3, fak 또는raf 키나제 저해제들 중 하나 이상의 조합물
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
WO2006065916A1 (en) 2004-12-14 2006-06-22 Alcon, Inc. Method of treating dry eye disorders using 13(s)-hode and its analogs
TW200635899A (en) 2004-12-22 2006-10-16 Astrazeneca Ab Chemical compounds
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.
US20090124635A1 (en) 2005-01-20 2009-05-14 Pfizer Inc. Chemical compounds
MX2007009429A (es) 2005-02-03 2008-03-18 Vertex Pharma Pirrolopirimidinas utiles como inhibidores de proteinas cinasas.
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
RU2383545C2 (ru) 2005-03-15 2010-03-10 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназы
BRPI0610514A2 (pt) 2005-04-05 2016-11-16 Pharmacopeia Inc composto, composição farmacêutica, e, método de tratamento de um distúrbio
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
CA2609126A1 (en) 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
ES2651349T3 (es) 2005-06-08 2018-01-25 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta JAK
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
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
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
WO2007038215A1 (en) 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic inhibitors of janus kinases
ES2401192T3 (es) 2005-09-30 2013-04-17 Vertex Pharmceuticals Incorporated Deazapurinas útiles como inhibidores de janus cinasas
US20070128633A1 (en) 2005-10-11 2007-06-07 Chembridge Research Laboratories, Inc. Cell-free protein expression systems and methods of use thereof
KR101315574B1 (ko) 2005-10-14 2013-10-08 스미또모 가가꾸 가부시끼가이샤 히드라지드 화합물 및 이의 살충 용도
EP2388259A1 (en) 2005-10-28 2011-11-23 AstraZeneca AB 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
DK1951684T3 (en) 2005-11-01 2016-10-24 Targegen Inc BIARYLMETAPYRIMIDIN kinase inhibitors
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
ES2543904T3 (es) 2005-12-13 2015-08-25 Incyte Corporation Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas sustituidas con heteroarilo como inhibidores de quinasas Janus
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
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
ES2408318T3 (es) 2005-12-23 2013-06-20 Glaxosmithkline Llc Inhibidores de azaindol de las cinasas Aurora
TW201412738A (zh) 2006-01-17 2014-04-01 Vertex Pharma 適合作為傑納斯激酶(janus kinase)抑制劑之氮雜吲哚
EP1979353A2 (en) 2006-01-19 2008-10-15 OSI Pharmaceuticals, Inc. Fused heterobicyclic kinase inhibitors
EP1981887A2 (en) 2006-02-01 2008-10-22 SmithKline Beecham Corporation 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
RU2008140144A (ru) 2006-03-10 2010-04-20 Оно Фармасьютикал Ко., Лтд. (Jp) Азотосодержащее гетероциклическое производное и фармацевтическое средство, включающее такое производное в качестве активного ингредиента
MX356221B (es) 2006-04-03 2018-05-18 Astellas Pharma Inc Heterocompuesto.
SG170828A1 (en) 2006-04-05 2011-05-30 Vertex Pharmaceuticals Inc Us Deazapurines useful as inhibitors of janus kinases
WO2007116313A2 (en) 2006-04-12 2007-10-18 Pfizer Limited Pyrrolidine derivatives as modulators of chemokine ccr5 receptors
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
EP2040704A2 (en) 2006-05-18 2009-04-01 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
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
WO2008016123A1 (fr) 2006-08-03 2008-02-07 Takeda Pharmaceutical Company Limited INHIBITEUR DE LA GSK-3β
EP2061762B1 (en) 2006-08-16 2011-07-27 Boehringer Ingelheim International GmbH Pyrazine compounds, their use and methods of preparation
BRPI0716598A2 (pt) 2006-09-08 2013-12-10 Novartis Ag Derivados de (hetero) arilsulfonamida de n-biarila úteis no tratamento de doenças medidas por interações de linfócitos
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
WO2008043031A1 (en) 2006-10-04 2008-04-10 Pharmacopeia, Inc. 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
WO2008043019A1 (en) 2006-10-04 2008-04-10 Pharmacopeia, Inc 8-substituted 2-(benzimidazolyl) purine derivatives for immunosuppression
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
CA2667487C (en) 2006-11-06 2017-04-04 Supergen, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
US20080119496A1 (en) 2006-11-16 2008-05-22 Pharmacopeia Drug Discovery, Inc. 7-Substituted Purine Derivatives for Immunosuppression
RS52677B (en) 2006-11-22 2013-06-28 Incyte Corporation IMIDAZOTRIAZINI I IMIDAZOPIRIMIDINI KAO INHIBITORI KINAZE
WO2008067119A2 (en) 2006-11-27 2008-06-05 Smithkline Beecham Corporation Novel compounds
RU2009127095A (ru) 2006-12-15 2011-01-20 Эбботт Лэборетриз (Us) Новые оксадиазольные соединения
AU2007338792B2 (en) 2006-12-20 2012-05-31 Amgen Inc. Substituted heterocycles and methods of use
AU2007338793B2 (en) 2006-12-20 2012-05-03 Amgen Inc. Heterocyclic compounds and their use in treating inflammation, angiogenesis and cancer
EP2094236A1 (en) 2006-12-22 2009-09-02 SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A. Gel useful for the delivery of ophthalmic drugs
CA2673038C (en) 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
WO2008082840A1 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
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
WO2008106692A1 (en) 2007-03-01 2008-09-04 Novartis Vaccines And Diagnostics, Inc. Pim kinase inhibitors and methods of their use
CA2682981C (en) 2007-04-03 2015-11-17 Array Biopharma Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
EP2155689B1 (en) 2007-05-31 2015-07-08 Boehringer Ingelheim International GmbH Ccr2 receptor antagonists and uses thereof
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
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.
EP4011883A1 (en) 2007-06-13 2022-06-15 Incyte Holdings Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3-cyclopentylpropanenitrile
AU2008273804B2 (en) 2007-07-11 2014-07-10 Pfizer Inc. Pharmaceutical compositions and methods of treating dry eye disorders
KR20100038119A (ko) 2007-08-01 2010-04-12 화이자 인코포레이티드 피라졸 화합물 및 raf 억제제로서 이의 용도
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
MY152948A (en) * 2007-11-16 2014-12-15 Incyte Corp 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
SI3133080T1 (sl) 2008-01-18 2018-12-31 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Novi citostatski 7-deazapurin nukleozidi
CN101959404B (zh) 2008-02-04 2015-12-02 墨丘瑞医疗有限公司 单磷酸腺苷活化蛋白激酶调节剂
UY31679A1 (es) 2008-03-03 2009-09-30 Inhibidores de cinasa pim y metodos para su uso
TWI444382B (zh) * 2008-03-11 2014-07-11 Incyte Corp 作為jak抑制劑之氮雜環丁烷及環丁烷衍生物
JP5384611B2 (ja) 2008-03-21 2014-01-08 ノバルティス アーゲー 新規ヘテロ環式化合物およびそれらの使用
CA2727928A1 (en) 2008-06-18 2009-12-23 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
EP2310000B1 (en) 2008-06-26 2019-09-18 Anterios, Inc. Dermal delivery
TWI461423B (zh) 2008-07-02 2014-11-21 Astrazeneca Ab 用於治療Pim激酶相關病狀及疾病之噻唑啶二酮化合物
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
US8557809B2 (en) 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
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
PL2384326T3 (pl) 2008-08-20 2014-09-30 Zoetis Services Llc Związki pirolo[2,3-d]pirymidyonowe
BRPI0918846A2 (pt) 2008-09-02 2019-09-24 Novartis Ag inibidores de cinase heterocíclica
CN104311480A (zh) 2008-09-02 2015-01-28 诺华股份有限公司 作为激酶抑制剂的吡啶甲酰胺衍生物
KR20110058866A (ko) 2008-09-02 2011-06-01 노파르티스 아게 비시클릭 키나제 억제제
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.
JOP20190230A1 (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
SI2432472T1 (sl) 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
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
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
WO2011066371A2 (en) 2009-11-24 2011-06-03 Alder Biopharmaceuticals, Inc. Antibodies to il-6 and use thereof
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
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CN102625807B (zh) 2009-09-08 2016-03-09 霍夫曼-拉罗奇有限公司 4-取代的吡啶-3-基-甲酰胺化合物和使用方法
EP2305660A1 (en) 2009-09-25 2011-04-06 Almirall, S.A. New thiadiazole derivatives
WO2011044481A1 (en) 2009-10-09 2011-04-14 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
CN102666545B (zh) 2009-10-20 2016-04-06 塞尔卓姆有限公司 作为jak抑制剂的杂环吡唑并嘧啶类似物
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
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
EP2523957A1 (en) 2010-01-12 2012-11-21 F. Hoffmann-La Roche AG Tricyclic heterocyclic compounds, compositions and methods of use thereof
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
US20110207754A1 (en) 2010-02-18 2011-08-25 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
NZ602313A (en) * 2010-03-10 2014-08-29 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
MX2012011941A (es) 2010-04-14 2013-08-27 Array Biopharma Inc Imidazo [1, 2-c] pirimidinas 5, 7-substituidas como inhibidores de jak cinasas.
EP2390252A1 (en) 2010-05-19 2011-11-30 Almirall, S.A. New pyrazole derivatives
MY161078A (en) 2010-05-21 2017-04-14 Incyte Holdings Corp Topical formulation for a jak inhibitor
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
JP5833392B2 (ja) * 2010-09-17 2015-12-16 公益財団法人相模中央化学研究所 (トリフルオロビニル)ベンゼン類およびその製造方法
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
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
JP5917545B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Jak阻害剤としてのシクロブチル置換ピロロピリジンおよびピロロピリミジン誘導体
EP2646029A4 (en) 2010-12-03 2014-06-18 Ym Biosciences Australia Pty TREATMENT OF JAK2-MEDIATED DISEASES
PT2675451E (pt) 2011-02-18 2015-10-16 Incyte Corp Terapia de combinação com inibidores mtor/jak
CN103797010B (zh) * 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
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
WO2013007765A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
US9358229B2 (en) 2011-08-10 2016-06-07 Novartis Pharma Ag JAK PI3K/mTOR combination therapy
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
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
US10155987B2 (en) 2012-06-12 2018-12-18 Dana-Farber Cancer Institute, Inc. Methods of predicting resistance to JAK inhibitor therapy
EP2890691B1 (en) 2012-08-31 2018-04-25 Principia Biopharma Inc. Benzimidazole derivatives as itk inhibitors
TWI646099B (zh) 2012-11-01 2019-01-01 英塞特控股公司 作爲jak抑制劑之三環稠合噻吩衍生物
US10166191B2 (en) 2012-11-15 2019-01-01 Incyte Corporation Sustained-release dosage forms of ruxolitinib
UA121532C2 (uk) 2013-03-06 2020-06-10 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки при отриманні інгібітора jak
EP3527263B1 (en) 2013-05-17 2020-10-28 Incyte Corporation Bipyrazole derivatives as jak inhibitors
CN116036089A (zh) 2013-08-07 2023-05-02 因赛特控股公司 Jak1抑制剂的持续释放剂型
WO2015026818A1 (en) 2013-08-20 2015-02-26 Incyte Corporation Survival benefit in patients with solid tumors with elevated c-reactive protein levels
WO2015131031A1 (en) 2014-02-28 2015-09-03 Incyte Corporation Jak1 inhibitors for the treatment of myelodysplastic syndromes
HUE051625T2 (hu) 2014-04-08 2021-03-29 Incyte Corp B-sejtes rosszindulatú daganatok kezelése JAK és PI3K inhibitorok kombinációjával
CR20160553A (es) 2014-04-30 2017-04-25 Incyte Corp Procesos para preparar un inhibidor de jak1 y nuevas formas de este
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

Also Published As

Publication number Publication date
AR095018A1 (es) 2015-09-16
SG10201707259PA (en) 2017-10-30
CA3091179C (en) 2023-01-17
SMT202100694T1 (it) 2022-03-21
CL2015002468A1 (es) 2016-02-05
JP2019023190A (ja) 2019-02-14
JP2016512196A (ja) 2016-04-25
WO2014138168A1 (en) 2014-09-12
UA120162C2 (uk) 2019-10-25
PH12015501958A1 (en) 2016-01-18
NZ749437A (en) 2020-07-31
TW201506026A (zh) 2015-02-16
PE20200298A1 (es) 2020-02-06
ES2900492T3 (es) 2022-03-17
CA3091179A1 (en) 2014-09-12
EP3985008A1 (en) 2022-04-20
US8987443B2 (en) 2015-03-24
AU2014225938B2 (en) 2018-07-19
AR118162A2 (es) 2021-09-22
CY1125072T1 (el) 2023-03-24
KR102236232B1 (ko) 2021-04-05
IL259723B (en) 2019-08-29
SMT201900081T1 (it) 2019-05-10
EP3489239B1 (en) 2021-09-15
TWI634121B (zh) 2018-09-01
DK2964650T3 (en) 2019-02-11
SI2964650T1 (sl) 2019-05-31
CR20150471A (es) 2016-01-04
CA2903418A1 (en) 2014-09-12
US9714233B2 (en) 2017-07-25
EA201591650A1 (ru) 2016-01-29
US20140256941A1 (en) 2014-09-11
PL3489239T3 (pl) 2022-03-07
HK1218540A1 (zh) 2017-02-24
US20150183805A1 (en) 2015-07-02
MX2020003446A (es) 2021-07-29
IL268452A (en) 2019-09-26
CL2018001791A1 (es) 2018-08-31
HUE057262T2 (hu) 2022-04-28
ME03350B (me) 2019-10-20
KR20150140287A (ko) 2015-12-15
BR112015021458B1 (pt) 2022-06-07
PT2964650T (pt) 2019-02-26
EP2964650A1 (en) 2016-01-13
MX2015011667A (es) 2015-12-16
BR112015021458A2 (pt) 2017-07-18
AU2014225938A1 (en) 2015-09-24
RS62867B1 (sr) 2022-02-28
PE20151902A1 (es) 2015-12-26
IL240891A0 (en) 2015-10-29
ZA201908345B (en) 2022-03-30
ES2707355T3 (es) 2019-04-03
PT3489239T (pt) 2021-12-17
EP2964650B1 (en) 2018-12-05
TR201820520T4 (tr) 2019-01-21
HRP20190233T1 (hr) 2019-05-03
LT2964650T (lt) 2019-04-25
RS58547B1 (sr) 2019-05-31
CA2903418C (en) 2021-03-23
HUE042466T2 (hu) 2019-06-28
CN105189509B (zh) 2017-12-19
JP6640297B2 (ja) 2020-02-05
LT3489239T (lt) 2022-03-10
US20160347734A1 (en) 2016-12-01
CY1121512T1 (el) 2020-05-29
JP6397831B2 (ja) 2018-09-26
KR20210038705A (ko) 2021-04-07
SI3489239T1 (sl) 2022-04-29
EA030705B1 (ru) 2018-09-28
PH12015501958B1 (en) 2016-01-18
UA121532C2 (uk) 2020-06-10
KR102366356B1 (ko) 2022-02-23
CR20190518A (es) 2020-01-10
US9221845B2 (en) 2015-12-29
IL259723A (en) 2018-07-31
BR112015021458A8 (pt) 2021-09-08
NZ711976A (en) 2019-01-25
HRP20211922T1 (hr) 2022-03-04
EP3489239A1 (en) 2019-05-29
BR122021015061B1 (pt) 2022-10-18
CN105189509A (zh) 2015-12-23
SG11201506758RA (en) 2015-09-29
PL2964650T3 (pl) 2019-06-28

Similar Documents

Publication Publication Date Title
CY1125072T1 (el) Μεθοδοι και ενδιαμεσες ενωσεις για την παρασκευη αναστολεα jak
EA201490575A1 (ru) Способы и промежуточные соединения для получения ингибиторов jak
EA201690357A1 (ru) Лекарственные формы с замедленным высвобождением для ингибитора jak1
CL2020001983A1 (es) Procesos para la preparación de (1 - (3-fluoro-2-(trifluorometilo)isonicotinoil)piperidina - 4 - ona)
CY1122425T1 (el) 3-[4-(7η-πυρρολο[2,3-d]πυριμιδιν-4-υλο)-1η-πυραζολ-1-υλ]οκτανο-ή επτανονιτριλιο ως αναστολεις jak
MY196185A (en) Salts of a Pim Kinase Inhibitor
MY191906A (en) Processes and intermediates for making a jak inhibitor
NZ779712A (en) Salts of a pim kinase inhibitor