HRP20192203T1 - 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori - Google Patents

3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori Download PDF

Info

Publication number
HRP20192203T1
HRP20192203T1 HRP20192203TT HRP20192203T HRP20192203T1 HR P20192203 T1 HRP20192203 T1 HR P20192203T1 HR P20192203T T HRP20192203T T HR P20192203TT HR P20192203 T HRP20192203 T HR P20192203T HR P20192203 T1 HRP20192203 T1 HR P20192203T1
Authority
HR
Croatia
Prior art keywords
pyrrolo
pyrazol
pyrimidin
compound
disease
Prior art date
Application number
HRP20192203TT
Other languages
English (en)
Croatian (hr)
Inventor
Yun-Long Li
James D. Rodgers
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=42246359&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20192203(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 HRP20192203T1 publication Critical patent/HRP20192203T1/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biotechnology (AREA)
  • Child & Adolescent Psychology (AREA)
  • AIDS & HIV (AREA)
HRP20192203TT 2009-05-22 2010-05-21 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori HRP20192203T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18058209P 2009-05-22 2009-05-22
EP10721227.6A EP2432472B1 (en) 2009-05-22 2010-05-21 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
PCT/US2010/035728 WO2010135621A1 (en) 2009-05-22 2010-05-21 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors

Publications (1)

Publication Number Publication Date
HRP20192203T1 true HRP20192203T1 (hr) 2020-03-06

Family

ID=42246359

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20192203TT HRP20192203T1 (hr) 2009-05-22 2010-05-21 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori

Country Status (36)

Country Link
US (3) US8604043B2 (enExample)
EP (2) EP3643312A1 (enExample)
JP (2) JP6172939B2 (enExample)
KR (1) KR20120030447A (enExample)
CN (2) CN102458411A (enExample)
AR (1) AR076920A1 (enExample)
AU (1) AU2010249443B2 (enExample)
BR (1) BRPI1012108B8 (enExample)
CA (1) CA2761954C (enExample)
CL (1) CL2011002955A1 (enExample)
CO (1) CO6470876A2 (enExample)
CR (1) CR20110621A (enExample)
CY (1) CY1122425T1 (enExample)
DK (1) DK2432472T3 (enExample)
EA (1) EA020494B1 (enExample)
EC (1) ECSP11011534A (enExample)
ES (1) ES2761300T3 (enExample)
HR (1) HRP20192203T1 (enExample)
HU (1) HUE046493T2 (enExample)
IL (1) IL216359A (enExample)
LT (1) LT2432472T (enExample)
ME (1) ME03556B (enExample)
MX (1) MX2011012262A (enExample)
MY (1) MY161416A (enExample)
NZ (1) NZ596374A (enExample)
PE (1) PE20120371A1 (enExample)
PL (1) PL2432472T3 (enExample)
PT (1) PT2432472T (enExample)
RS (1) RS59632B1 (enExample)
SG (2) SG176111A1 (enExample)
SI (1) SI2432472T1 (enExample)
SM (1) SMT201900698T1 (enExample)
TW (1) TWI484962B (enExample)
UA (1) UA106078C2 (enExample)
WO (1) WO2010135621A1 (enExample)
ZA (1) ZA201108541B (enExample)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101391900B1 (ko) 2005-12-13 2014-05-02 인사이트 코포레이션 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로［2,3-ｂ］피리딘 및 피롤로［2,3-ｂ］피리미딘
WO2008157208A2 (en) 2007-06-13 2008-12-24 Incyte Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
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.
CN101910152B (zh) * 2007-11-16 2014-08-06 因塞特公司 作为janus激酶抑制剂的4-吡唑基-n-芳基嘧啶-2-胺和4-吡唑基-n-杂芳基嘧啶-2-胺
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
TW201100429A (en) 2009-05-22 2011-01-01 Incyte Corp 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
DK2432472T3 (da) 2009-05-22 2019-11-18 Incyte Holdings Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer
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
PH12015502575A1 (en) 2010-03-10 2017-04-24 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EP3087972A1 (en) 2010-05-21 2016-11-02 Incyte Holdings Corporation Topical formulation for a jak inhibitor
CA2818545C (en) 2010-11-19 2019-04-16 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
PL2675451T3 (pl) 2011-02-18 2016-05-31 Novartis Pharma Ag Terapia skojarzona z inhibitorem mTOR/JAK
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/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
ES2633793T3 (es) * 2011-09-22 2017-09-25 Merck Sharp & Dohme Corp. Pirazol carboxamidas como inhibidores de quinasa Janus
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
CA2888816A1 (en) 2012-11-01 2014-05-08 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
EP3949953A1 (en) 2012-11-15 2022-02-09 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
WO2014118388A1 (en) 2013-02-04 2014-08-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
BR112015021458B1 (pt) 2013-03-06 2022-06-07 Incyte Holdings Corporation "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases
UA117830C2 (uk) 2013-05-17 2018-10-10 Інсайт Корпорейшн Похідні біпіразолу як інгібітори jak
WO2015021153A1 (en) 2013-08-07 2015-02-12 Incyte Corporation Sustained release dosage forms for a jak1 inhibitor
TW201529074A (zh) 2013-08-20 2015-08-01 Incyte Corp 在ｃ-反應蛋白含量較高之實體腫瘤患者中的存活益處
NZ763326A (en) 2014-04-08 2023-04-28 Incyte Holdings Corp Treatment of b-cell malignancies by a combination jak and pi3k inhibitor
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
SI3179992T1 (sl) 2014-08-11 2022-09-30 Acerta Pharma B.V. Terapevtske kombinacije zaviralca BTK, zaviralca PD-1 in/ali zaviralca PD-L1
TW201618773A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑、及／或ｃｄｋ４／６抑制劑的治療組合物
TW201618772A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑及／或ｂｃｌ－２抑制劑之治療組合物
JP2020502224A (ja) * 2016-12-21 2020-01-23 日本たばこ産業株式会社 ヤヌスキナーゼ阻害剤の結晶形
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
EP3610264A1 (en) 2017-04-13 2020-02-19 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma
BR112020008850A2 (pt) 2017-11-03 2020-10-20 Aclaris Therapeutics, Inc. composto, composição farmacêutica e método para tratar uma doença mediada por jak1 e jak3
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
DK3746429T3 (da) 2018-01-30 2022-05-02 Incyte Corp Fremgangsmåder til fremstilling af (1-(3-fluor-2-(trifluormethyl)isonicotinyl)piperidin-4-on)
BR122023022189A2 (pt) 2018-02-16 2024-02-20 Incyte Corporation Usos de inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas
CN112423759A (zh) 2018-03-30 2021-02-26 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
EP3775284A1 (en) 2018-03-30 2021-02-17 Incyte Corporation Biomarkers for inflammatory skin disease
MX2020010815A (es) 2018-04-13 2020-12-11 Incyte Corp Biomarcadores para enfermedad de injerto contra hospedero.
PE20211208A1 (es) 2018-06-01 2021-07-05 Incyte Corp Regimen de dosificacion para el tratamiento de trastornos relacionados con pi3k
KR102545594B1 (ko) 2018-07-31 2023-06-21 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제
CN119080779A (zh) 2018-08-10 2024-12-06 阿克拉瑞斯治疗股份有限公司 吡咯并嘧啶itk抑制剂
EA202191170A1 (ru) 2018-10-31 2021-07-27 Инсайт Корпорейшн Комбинированная терапия для лечения гематологических заболеваний
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
JP2022515197A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220088699A (ko) 2019-09-27 2022-06-28 디스크 메디슨, 인크. 골수섬유증 및 관련 상태의 치료 방법
CN110538183B (zh) * 2019-10-09 2021-05-04 吉林大学 一种预防和治疗小儿湿疹的组合物及其制备方法
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
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
CN115038443A (zh) 2019-11-22 2022-09-09 因西特公司 包含alk2抑制剂和jak2抑制剂的组合疗法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
IL298118B1 (en) 2020-06-02 2025-10-01 Incyte Corp Processes for preparing JAK1 inhibitor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CA3189561A1 (en) * 2020-07-17 2022-01-20 Pfizer Inc. Stable pharmaceutical topical formulation containing immunosuppressant for treating dermatological conditions
MX2023002035A (es) 2020-08-18 2023-06-12 Incyte Corp Proceso e intermediarios para preparar un inhibidor de cinasa janus 1 (jak1).
AU2021329303A1 (en) 2020-08-18 2023-04-06 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
WO2022125670A1 (en) 2020-12-08 2022-06-16 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
TW202302104A (zh) * 2021-02-18 2023-01-16 美商阿克拉里斯醫療股份有限公司 Jak 1/3抑制劑的局部配方及其用於治療異位性皮膚炎和其他皮膚狀況之用法
DK4333840T3 (da) 2021-05-03 2025-11-24 Incyte Corp Jak1-vejinhibitorer til behandling af prurigo nodularis
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
CN113813228B (zh) * 2021-10-11 2023-04-18 北京鑫开元医药科技有限公司 一种具有jak激酶抑制活性的注射液及其制备方法和用途
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

Family Cites Families (280)

* 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
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
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
ATE139232T1 (de) 1989-10-11 1996-06-15 Teijin Ltd Bizyklische pyrimidinderivate, verfahren zu deren herstellung und diese enthaltende pharmazeutische zusammensetzung
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
DK0836605T3 (da) 1995-07-06 2002-05-13 Novartis Ag Pyrrolopyrimidiner og fremgangsmåder til deres fremstilling
US5630943A (en) * 1995-11-30 1997-05-20 Merck Patent Gesellschaft Mit Beschrankter Haftung Discontinuous countercurrent chromatographic process and apparatus
GB9604361D0 (en) 1996-02-29 1996-05-01 Pharmacia Spa 4-Substituted pyrrolopyrimidine compounds as tyrosine kinase inhibitors
CA2250232A1 (en) 1996-04-03 1997-10-09 Allen I. Oliff A method of treating cancer
WO1997038664A2 (en) 1996-04-18 1997-10-23 Merck & Co., Inc. A method of treating cancer
US5795909A (en) 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
JP2000508335A (ja) 1996-05-30 2000-07-04 メルク エンド カンパニー インコーポレーテッド 癌の治療方法
US6624138B1 (en) 2001-09-27 2003-09-23 Gp Medical Drug-loaded biological material chemically treated with genipin
JP2001524079A (ja) 1997-04-07 2001-11-27 メルク エンド カンパニー インコーポレーテッド ガンの治療方法
US6060038A (en) * 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
US6063284A (en) 1997-05-15 2000-05-16 Em Industries, Inc. Single column closed-loop recycling with periodic intra-profile injection
CA2295620A1 (en) * 1997-08-11 1999-02-18 Boehringer Ingelheim Pharmaceuticals, Inc. 5,6-heteroaryl-dipyrido¬2,3-b:3',2'-f|azepines and their use in the prevention or treatment of hiv infection
US6075056A (en) 1997-10-03 2000-06-13 Penederm, Inc. Antifungal/steroid topical compositions
IL139811A0 (en) 1998-06-04 2002-02-10 Abbott Lab Cell adhesion-inhibiting antinflammatory compounds
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
RS50087B (sr) 1998-06-19 2009-01-22 Pfizer Products Inc., Pirolo (2,3-d) pirimidin jedinjenja
EP1107964B8 (en) 1998-08-11 2010-04-07 Novartis AG Isoquinoline derivatives with angiogenesis inhibiting activity
JP2000119271A (ja) 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd １ｈ―イミダゾピリジン誘導体
TR200100708T2 (tr) 1998-09-10 2001-07-23 Nycomed Danmark A/S İlaç maddelerine mahsus çabuk salımlı farmasötik bileşimler.
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
JP2002538121A (ja) 1999-03-03 2002-11-12 メルク エンド カムパニー インコーポレーテッド プレニルタンパク質トランスフェラーゼの阻害剤
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US6217895B1 (en) * 1999-03-22 2001-04-17 Control Delivery Systems Method for treating and/or preventing retinal diseases with sustained release corticosteroids
US6239113B1 (en) * 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
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
CZ303875B6 (cs) 1999-12-10 2013-06-05 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidinová sloucenina a farmaceutická kompozice s jejím obsahem
IL150388A0 (en) * 1999-12-24 2002-12-01 Aventis Pharma Ltd Azaindoles
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
ES2206363T3 (es) 2000-04-07 2004-05-16 Laboratoire Medidom S.A. Formulaciones oftalmicas a base de ciclosporina, de acido hialuronico y de polisorbato.
WO2001081345A1 (en) 2000-04-20 2001-11-01 Mitsubishi Pharma Corporation Aromatic amide compounds
US7498304B2 (en) * 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
EP1294752A2 (en) 2000-06-16 2003-03-26 Curis, Inc. Angiogenesis-modulating compositions and uses
US6335342B1 (en) 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
ATE465756T1 (de) * 2000-06-23 2010-05-15 Mitsubishi Tanabe Pharma Corp Antitumoreffekt-verstärker
EA006153B1 (ru) 2000-06-26 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ
EP1294358B1 (en) 2000-06-28 2004-08-18 Smithkline Beecham Plc Wet milling process
AU2001278790A1 (en) 2000-08-22 2002-03-04 Hokuriku Seiyaku Co. Ltd 1h-imidazopyridine derivatives
ES2307667T3 (es) 2000-12-05 2008-12-01 Vertex Pharmaceuticals Incorporated Inhibidires de quinasas terminales c-jun(jnk) y otras proteinas quinasas.
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
WO2002055496A1 (en) 2001-01-15 2002-07-18 Glaxo Group Limited Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
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
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
CA2455181C (en) 2001-08-01 2010-04-06 Merck & Co., Inc. Benzimidazo[4,5-f]isoquinolinone derivatives
WO2003024967A2 (en) 2001-09-19 2003-03-27 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
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
EP1441737B1 (en) 2001-10-30 2006-08-09 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
US6949668B2 (en) * 2001-11-30 2005-09-27 Teijin Limited Process for producing 5-(3-cyanophenyl)-3-formylbenzoic acid compound
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
US6995144B2 (en) * 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
WO2003091246A1 (en) * 2002-04-26 2003-11-06 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
EP1503757B1 (en) 2002-05-02 2007-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
MXPA04011004A (es) * 2002-05-07 2005-01-25 Control Delivery Sys Inc Procesos para formar un dispositivo de administracion de farmaco.
US7122550B2 (en) 2002-05-23 2006-10-17 Cytopia Pty Ltd Protein kinase inhibitors
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
WO2004007472A1 (ja) * 2002-07-10 2004-01-22 Ono Pharmaceutical Co., Ltd. Ｃｃｒ４アンタゴニストおよびその医薬用途
CA2497977A1 (en) 2002-09-20 2004-04-01 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
US7259161B2 (en) 2002-11-04 2007-08-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
US20040099204A1 (en) 2002-11-25 2004-05-27 Nestor John J. Sheet, page, line, position marker
CA2507392A1 (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
TWI335819B (en) * 2002-12-24 2011-01-11 Alcon Inc Use of oculosurface selective glucocorticoid in the treatment of dry eye
US7135493B2 (en) * 2003-01-13 2006-11-14 Astellas Pharma Inc. HDAC inhibitor
US7167750B2 (en) 2003-02-03 2007-01-23 Enteromedics, Inc. Obesity treatment with electrically induced vagal down regulation
US7407962B2 (en) 2003-02-07 2008-08-05 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors or protein kinases
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
JP2006522124A (ja) 2003-04-03 2006-09-28 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 プロテインキナーゼのインヒビターとして有用な組成物
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
FR2857454B1 (fr) 2003-07-08 2006-08-11 Aventis Pasteur Dosage des acides techoiques des bacteries gram+
AU2004259755A1 (en) 2003-07-22 2005-02-03 Janssen Pharmaceutica, N.V. Quinolinone derivatives as inhibitors of c-fms kinase
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
JP5010917B2 (ja) 2003-08-29 2012-08-29 エグゼリクシス， インコーポレイテッド ｃ−Ｋｉｔ調節因子および使用方法
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
SI1679074T1 (sl) * 2003-10-24 2011-04-29 Santen Pharmaceutical Co Ltd Terapevtsko sredstvo za keratokonjuktivno motnjo
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
WO2005051393A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
MXPA06007002A (es) 2003-12-17 2006-08-31 Pfizer Prod Inc Compuestos de pirrolo[2,3-d]pirimidina para tratar rechazo de transplantes.
ATE406356T1 (de) 2003-12-19 2008-09-15 Schering Corp Thiadiazole als cxc- und cc- chemokinrezeptorliganden
DK1696920T3 (en) 2003-12-19 2015-01-19 Plexxikon Inc RELATIONS AND PROCEDURES FOR THE DEVELOPMENT OF LAW MODULATORS
HRP20100675T1 (hr) 2003-12-23 2011-01-31 Astex Therapeutics Limited Derivati pirazola kao modulatori protein kinaze
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 METHOD FOR THE TREATMENT OF SYNUCLEINOPATHIES
WO2005095400A1 (en) 2004-03-30 2005-10-13 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of jak and other protein kinases
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
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
WO2005105814A1 (en) * 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
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
RU2401265C2 (ru) 2004-06-10 2010-10-10 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназы
WO2006001463A1 (ja) * 2004-06-23 2006-01-05 Ono Pharmaceutical Co., Ltd. Ｓ１ｐ受容体結合能を有する化合物およびその用途
WO2006004984A1 (en) 2004-06-30 2006-01-12 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
CN101006186A (zh) 2004-08-23 2007-07-25 财团法人牧岩生命工学研究所 用于检测sars冠状病毒的引物和探针，包括该引物和/或探针的试剂盒及其检测方法
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
CN101899049A (zh) * 2004-10-13 2010-12-01 霍夫曼-拉罗奇有限公司 二取代吡唑并苯并二氮杂*类
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
US7528138B2 (en) * 2004-11-04 2009-05-05 Vertex Pharmaceuticals Incorporated Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
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
US20060128803A1 (en) * 2004-12-14 2006-06-15 Alcon, Inc. Method of treating dry eye disorders using 13(S)-HODE and its analogs
WO2006067445A2 (en) 2004-12-22 2006-06-29 Astrazeneca Ab Csf-1r 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.
EP1844037A1 (en) 2005-01-20 2007-10-17 Pfizer Limited Chemical compounds
JP5227032B2 (ja) * 2005-02-03 2013-07-03 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 プロテインキナーゼの阻害剤として有用なピロロピリミジン
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
BRPI0608513A2 (pt) 2005-03-15 2010-01-05 Irm Llc compostos e composições como inibidores da proteìna quinase
AU2006232105A1 (en) 2005-04-05 2006-10-12 Pharmacopeia, Inc. Purine and imidazopyridine derivatives for immunosuppression
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
RU2435769C2 (ru) 2005-05-20 2011-12-10 Вертекс Фармасьютикалз Инкорпорейтед Пирролопиридины, полезные в качестве ингибиторов протеинкиназы
RU2485106C2 (ru) 2005-06-08 2013-06-20 Райджел Фамэсьютикэлз, Инк. Соединения, проявляющие активность в отношении jak-киназы (варианты), способ лечения заболеваний, опосредованных jak-киназой, способ ингибирования активности jak-киназы (варианты), фармацевтическая композиция на основе указанных соединений
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
WO2007002433A1 (en) 2005-06-22 2007-01-04 Plexxikon, Inc. Pyrrolo [2, 3-b] pyridine derivatives as protein kinase inhibitors
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
US20070149506A1 (en) 2005-09-22 2007-06-28 Arvanitis Argyrios G Azepine inhibitors of Janus kinases
NZ567133A (en) 2005-09-30 2011-07-29 Vertex Pharma Deazapurines useful as inhibitors of janus kinases
WO2007044894A2 (en) 2005-10-11 2007-04-19 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
WO2007049041A1 (en) 2005-10-28 2007-05-03 Astrazeneca Ab 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
MY167260A (en) * 2005-11-01 2018-08-14 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
KR101391900B1 (ko) * 2005-12-13 2014-05-02 인사이트 코포레이션 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로［2,3-ｂ］피리딘 및 피롤로［2,3-ｂ］피리미딘
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
WO2007076423A2 (en) 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
SI1962830T1 (sl) * 2005-12-23 2013-07-31 Glaxosmithkline Llc Azaindolni inhibitorji kinaz Aurora
NZ601687A (en) 2006-01-17 2014-03-28 Vertex Pharma Azaindoles useful as inhibitors of janus kinases
EP1979353A2 (en) * 2006-01-19 2008-10-15 OSI Pharmaceuticals, Inc. Fused heterobicyclic kinase inhibitors
JP2009525350A (ja) * 2006-02-01 2009-07-09 スミスクライン ビーチャム コーポレーション Ｒａｆキナーゼ阻害薬として有用なピロロ［２，３，ｂ］ピリジン誘導体
US7745477B2 (en) 2006-02-07 2010-06-29 Hoffman-La Roche Inc. Heteroaryl and benzyl amide compounds
US8003642B2 (en) * 2006-03-10 2011-08-23 Ono Pharmaceutical Co., Ltd. Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient
AU2007236707C1 (en) * 2006-04-03 2012-05-24 Astellas Pharma Inc. Hetero compound
US8741912B2 (en) 2006-04-05 2014-06-03 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of Janus kinases
US20090124636A1 (en) 2006-04-12 2009-05-14 Pfizer Inc. Chemical compounds
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
US20080051427A1 (en) 2006-05-18 2008-02-28 Fritz Schuckler Pharmaceutical Compositions 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
CA2658764A1 (en) * 2006-07-20 2008-01-24 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
WO2008013622A2 (en) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
US8492378B2 (en) * 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
US8318723B2 (en) * 2006-08-16 2012-11-27 Boehringer Ingelheim International Gmbh Pyrazine compounds, their use and methods of preparation
AU2007293653B2 (en) 2006-09-08 2011-02-17 Novartis Ag N-biaryl (hetero) arylsulphonamide derivatives useful in the treatment of diseases mediated by lymphocytes interactions
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
US7915268B2 (en) * 2006-10-04 2011-03-29 Wyeth Llc 8-substituted 2-(benzimidazolyl)purine derivatives for immunosuppression
AR063142A1 (es) 2006-10-04 2008-12-30 Pharmacopeia Inc Derivados de 2-(bencimidazolil) purina y purinonas 6-sustituidas utiles como inmunosupresores,y composiciones farmaceuticas que los contienen.
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
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
GEP20125658B (en) 2006-11-22 2012-10-10 Incyte Corp Imidazotriazines and imidazo pyrimidines as kinase inhibitors
WO2008067119A2 (en) 2006-11-27 2008-06-05 Smithkline Beecham Corporation Novel compounds
AU2007334436A1 (en) 2006-12-15 2008-06-26 Abbott Laboratories Novel oxadiazole compounds
AU2007338792B2 (en) 2006-12-20 2012-05-31 Amgen Inc. Substituted heterocycles and methods of use
MX2009006543A (es) * 2006-12-20 2009-06-26 Amgen Inc Compuestos heterociclicos y su uso en el tratamiento de la inflamacion, angiogenesis y cancer.
AU2007338210B2 (en) 2006-12-22 2013-01-31 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Gel useful for the delivery of ophthalmic drugs
EP2121692B1 (en) * 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
WO2008082840A1 (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
WO2008082839A2 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
EA019951B1 (ru) 2007-03-01 2014-07-30 Новартис Аг Ингибиторы киназы pim и способы их применения
UA101611C2 (ru) 2007-04-03 2013-04-25 Аррей Байофарма Инк. СОЕДИНЕНИЯ ИМИДАЗО[1,2-а]ПИРИДИНА КАК ИНГИБИТОРЫ ТИРОЗИНКИНАЗЫ РЕЦЕПТОРОВ
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
WO2008145681A2 (en) 2007-05-31 2008-12-04 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
WO2008157208A2 (en) 2007-06-13 2008-12-24 Incyte Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
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.
EP2175858B1 (en) 2007-07-11 2014-09-10 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
WO2009064486A2 (en) 2007-11-15 2009-05-22 Musc Foundation For Research Development Inhibitors of pim protein kinases, compositions, and methods for treating cancer
CN101910152B (zh) 2007-11-16 2014-08-06 因塞特公司 作为janus激酶抑制剂的4-吡唑基-n-芳基嘧啶-2-胺和4-吡唑基-n-杂芳基嘧啶-2-胺
GB0723815D0 (en) 2007-12-05 2008-01-16 Glaxo Group Ltd Compounds
TR201815961T4 (tr) * 2008-01-18 2018-11-21 Inst Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Yeni sitostatik 7-deazapürin nükleozidleri.
MY158994A (en) 2008-02-04 2016-11-30 Mercury Therapeutics Inc Ampk modulators
AR070531A1 (es) 2008-03-03 2010-04-14 Novartis Ag Inhibidores de cinasa pim y metodos para su uso
MX2010010012A (es) 2008-03-11 2010-10-20 Incyte Corp Derivados de azetidina y ciclobutano como inhibidores de jak.
CN102015686B (zh) 2008-03-21 2014-07-02 诺华股份有限公司 杂环化合物及其用途
US8344144B2 (en) 2008-06-18 2013-01-01 Merck Sharp & Dohme Corp. Inhibitors of Janus kinases
KR20160130519A (ko) 2008-06-26 2016-11-11 안테리오스, 인코퍼레이티드 경피 운반
UY31952A (es) 2008-07-02 2010-01-29 Astrazeneca Ab 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim
FR2933409B1 (fr) 2008-07-03 2010-08-27 Centre Nat Rech Scient NOUVEAUX PYRROLO °2,3-a! CARBAZOLES ET LEUR UTILISATION COMME INHIBITEURS DES KINASES PIM
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
PT2384326E (pt) 2008-08-20 2014-06-09 Zoetis Llc Compostos de pirrolo[2,3-d]pirimidina
MX2011002367A (es) 2008-09-02 2011-04-04 Novartis Ag Inhibidores de cinasa biciclicos.
US8759338B2 (en) 2008-09-02 2014-06-24 Novartis Ag Heterocyclic kinase inhibitors
BRPI0918268B1 (pt) 2008-09-02 2021-08-03 Novartis Ag Derivados de picolinamida, seu uso, e composição farmacêutica
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
DK2432472T3 (da) 2009-05-22 2019-11-18 Incyte Holdings Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer
TW201100429A (en) 2009-05-22 2011-01-01 Incyte Corp 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
US9346809B2 (en) 2009-07-08 2016-05-24 Leo Pharma A/S Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors
WO2011066371A2 (en) 2009-11-24 2011-06-03 Alder Biopharmaceuticals, Inc. Antibodies to il-6 and use thereof
EP2470534A4 (en) 2009-08-24 2013-02-27 Merck Sharp & Dohme JAK INHIBITION FOR BLOCKING TOXICITY ASSOCIATED WITH RNA INTERFERENCE
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
EP2475659B1 (en) 2009-09-08 2015-10-28 F.Hoffmann-La Roche Ag 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
EP2305660A1 (en) 2009-09-25 2011-04-06 Almirall, S.A. New thiadiazole derivatives
ES2435491T3 (es) 2009-10-09 2013-12-19 Incyte Corporation Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
AU2010309882B2 (en) 2009-10-20 2016-01-28 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as JAK inhibitors
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
KR20140015162A (ko) 2010-01-12 2014-02-06 에프. 호프만-라 로슈 아게 트라이사이클릭 헤테로사이클릭 화합물, 조성물 및 이의 사용 방법
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
JP5858434B2 (ja) * 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
PH12015502575A1 (en) * 2010-03-10 2017-04-24 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
NZ603446A (en) 2010-04-14 2014-05-30 Array Biopharma Inc 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
EP2390252A1 (en) 2010-05-19 2011-11-30 Almirall, S.A. New pyrazole derivatives
EP3087972A1 (en) 2010-05-21 2016-11-02 Incyte Holdings Corporation Topical formulation for a jak inhibitor
US8637529B2 (en) * 2010-06-11 2014-01-28 AbbYie Inc. Pyrazolo[3,4-d]pyrimidine compounds
US9351943B2 (en) 2010-07-01 2016-05-31 Matthew T. McLeay Anti-fibroblastic fluorochemical emulsion therapies
EP2621489A1 (en) 2010-09-30 2013-08-07 Portola Pharmaceuticals, Inc. Combinations of 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide and fludarabine
CN103415515B (zh) * 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
CA2818545C (en) * 2010-11-19 2019-04-16 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
US20140073643A1 (en) 2010-12-03 2014-03-13 Ym Biosciences Australia Pty Ltd Treatment of jak2-mediated conditions
PL2675451T3 (pl) * 2011-02-18 2016-05-31 Novartis Pharma Ag Terapia skojarzona z inhibitorem mTOR/JAK
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
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
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/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
CA2888816A1 (en) 2012-11-01 2014-05-08 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
EP3949953A1 (en) 2012-11-15 2022-02-09 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
BR112015021458B1 (pt) 2013-03-06 2022-06-07 Incyte Holdings Corporation "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases
UA117830C2 (uk) 2013-05-17 2018-10-10 Інсайт Корпорейшн Похідні біпіразолу як інгібітори jak
WO2015021153A1 (en) 2013-08-07 2015-02-12 Incyte Corporation Sustained release dosage forms for a jak1 inhibitor
TW201529074A (zh) 2013-08-20 2015-08-01 Incyte Corp 在ｃ-反應蛋白含量較高之實體腫瘤患者中的存活益處
SI3110409T1 (sl) 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
NZ763326A (en) 2014-04-08 2023-04-28 Incyte Holdings Corp Treatment of b-cell malignancies by a combination jak and pi3k inhibitor
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
PE20120371A1 (es) 2012-05-17
PT2432472T (pt) 2019-12-09
CN106967070A (zh) 2017-07-21
BRPI1012108B8 (pt) 2021-05-25
CN102458411A (zh) 2012-05-16
EP2432472A1 (en) 2012-03-28
AU2010249443B2 (en) 2015-08-13
TWI484962B (zh) 2015-05-21
IL216359A0 (en) 2012-01-31
EA020494B1 (ru) 2014-11-28
DK2432472T3 (da) 2019-11-18
CA2761954A1 (en) 2010-11-25
US20160067253A1 (en) 2016-03-10
AU2010249443A1 (en) 2011-12-01
EP2432472B1 (en) 2019-10-02
US9623029B2 (en) 2017-04-18
CA2761954C (en) 2018-07-31
CL2011002955A1 (es) 2012-03-30
EP3643312A1 (en) 2020-04-29
ZA201108541B (en) 2018-11-28
UA106078C2 (uk) 2014-07-25
US20100298355A1 (en) 2010-11-25
TW201106951A (en) 2011-03-01
EA201101666A1 (ru) 2012-05-30
SG176111A1 (en) 2011-12-29
MY161416A (en) 2017-04-14
CO6470876A2 (es) 2012-06-29
KR20120030447A (ko) 2012-03-28
LT2432472T (lt) 2020-02-10
JP2012527481A (ja) 2012-11-08
JP2016040271A (ja) 2016-03-24
NZ596374A (en) 2014-01-31
RS59632B1 (sr) 2020-01-31
US9216984B2 (en) 2015-12-22
MX2011012262A (es) 2012-01-25
US20140073657A1 (en) 2014-03-13
HUE046493T2 (hu) 2020-03-30
AR076920A1 (es) 2011-07-20
SG10201402492TA (en) 2014-08-28
US8604043B2 (en) 2013-12-10
SI2432472T1 (sl) 2019-11-29
IL216359A (en) 2016-09-29
ECSP11011534A (es) 2012-01-31
PL2432472T3 (pl) 2020-03-31
JP6302442B2 (ja) 2018-03-28
BRPI1012108B1 (pt) 2020-08-25
WO2010135621A1 (en) 2010-11-25
CR20110621A (es) 2012-02-09
BRPI1012108A2 (pt) 2016-03-29
SMT201900698T1 (it) 2020-01-14
JP6172939B2 (ja) 2017-08-02
ME03556B (me) 2020-07-20
CY1122425T1 (el) 2021-01-27
ES2761300T3 (es) 2020-05-19

Similar Documents

Publication Publication Date Title
HRP20192203T1 (hr) 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori
JP2016040271A5 (enExample)
HRP20140541T4 (hr) Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila
US10562904B2 (en) Synthesis process of ruxolitinib
JP6458023B2 (ja) 繊維芽細胞成長因子受容体の阻害剤
JP6851454B2 (ja) キラルジペプチジルペプチダーゼ−ｉｖ阻害剤の製造方法
JP2013502396A5 (enExample)
RU2012132278A (ru) Трициклические гетероциклические соединения, содержащие их композиции и способы их применения
CA2588398A1 (en) Potassium salt of an hiv integrase inhibitor
JP2014520146A5 (enExample)
TW200406210A (en) Processes for preparing substituted pyrimidines
JP2011148817A5 (enExample)
US20100256149A1 (en) Novel arylamino n-heteraryl compounds as mek inhibitors
HRP20150584T1 (hr) Soli i polimorfi tetraciklinskog spoja
CA3031021A1 (en) Isoquinolinone compounds and use thereof in preparation of antiviral drugs
AU2013244859B2 (en) New alpha2 adrenoceptor agonists
CN102367253B (zh) 一种制备他达拉非晶型a的方法
WO2014102830A1 (en) A process for preparation of ticagrelor and intermediates thereof
RU2016139286A (ru) Способ получения лекарственных средств
JP2014510746A5 (enExample)
RU2014145481A (ru) Циклопропанкарбоксилатные эфиры пуриновых аналогов
JP6332818B2 (ja) チカグレロルの中間体およびその製造法、およびチカグレロルの製造法
RU2013137753A (ru) Твердые формы ингибитора гиразы (r)-1-этил-3-[5-[2-(1-гидрокси-1-метилэтил)пиримидин-5-ил]-7-(тетрагидрофуран-2-ил)-1н-бензимидазол-2-ил]мочевины
WO2012024625A3 (en) Novel synthesis of nucleoside 5 ' -triphosphates and their derivatives
JP2013531058A5 (enExample)