EA200870048A1 - ГЕТЕРОАРИЛ-ЗЕМЕЩЕННЫЕ ПИРРОЛО[2,3-b]ПИРИДИНЫ И ПИРРОЛО[2,3-b]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ - Google Patents

ГЕТЕРОАРИЛ-ЗЕМЕЩЕННЫЕ ПИРРОЛО[2,3-b]ПИРИДИНЫ И ПИРРОЛО[2,3-b]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ

Info

Publication number
EA200870048A1
EA200870048A1 EA200870048A EA200870048A EA200870048A1 EA 200870048 A1 EA200870048 A1 EA 200870048A1 EA 200870048 A EA200870048 A EA 200870048A EA 200870048 A EA200870048 A EA 200870048A EA 200870048 A1 EA200870048 A1 EA 200870048A1
Authority
EA
Eurasian Patent Office
Prior art keywords
pyrrolo
heteroaryl
pyridines
janus
pyrmidines
Prior art date
Application number
EA200870048A
Other languages
English (en)
Other versions
EA019504B1 (ru
Inventor
Джеймс Д. Роджерс
Стейси Шепард
Томас П. Мадускуи
Хайшэн Ван
Нику Фалахатпишех
Мария Рафальски
Аргириос Г. Арванитис
Льюис Сторейс
Рави Кумар Джаллури
Джордан С. Фридман
Кришна Вадди
Original Assignee
Инсайт 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=37903501&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA200870048(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Инсайт Корпорейшн filed Critical Инсайт Корпорейшн
Publication of EA200870048A1 publication Critical patent/EA200870048A1/ru
Publication of EA019504B1 publication Critical patent/EA019504B1/ru

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Настоящее изобретение относится к гетероарилзамещенным пирроло[2,3-b]пиридинам (I) и гетероарилзамещенным пирроло[2,3-b]пиримидинам, которые модулируют активность Янус-киназы и могут использоваться для лечения заболеваний, связанных с активностью Янус-киназы, включая, например, иммунно связанные заболевания, заболевания кожи, миелоидные пролиферативные заболевания, рак и другие заболевания.
EA200870048A 2005-12-13 2006-12-12 ГЕТЕРОАРИЛЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-b]ПИРИДИНЫ И ПИРРОЛО[2,3-b]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ EA019504B1 (ru)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US74990505P 2005-12-13 2005-12-13
US81023106P 2006-06-02 2006-06-02
US85062506P 2006-10-10 2006-10-10
US85687206P 2006-11-03 2006-11-03
US85940406P 2006-11-16 2006-11-16
PCT/US2006/047369 WO2007070514A1 (en) 2005-12-13 2006-12-12 Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors

Publications (2)

Publication Number Publication Date
EA200870048A1 true EA200870048A1 (ru) 2009-02-27
EA019504B1 EA019504B1 (ru) 2014-04-30

Family

ID=37903501

Family Applications (3)

Application Number Title Priority Date Filing Date
EA201691294A EA036785B1 (ru) 2005-12-13 2006-12-12 ГЕТЕРОАРИЛ-ЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ
EA200870048A EA019504B1 (ru) 2005-12-13 2006-12-12 ГЕТЕРОАРИЛЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-b]ПИРИДИНЫ И ПИРРОЛО[2,3-b]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ
EA201200132A EA035795B1 (ru) 2005-12-13 2006-12-12 Гетероарилзамещенные пирроло[2,3-b]пиридины в качестве ингибиторов янус-киназы

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA201691294A EA036785B1 (ru) 2005-12-13 2006-12-12 ГЕТЕРОАРИЛ-ЗАМЕЩЕННЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA201200132A EA035795B1 (ru) 2005-12-13 2006-12-12 Гетероарилзамещенные пирроло[2,3-b]пиридины в качестве ингибиторов янус-киназы

Country Status (36)

Country Link
US (16) US7598257B2 (ru)
EP (10) EP2426129B1 (ru)
JP (4) JP5017278B2 (ru)
KR (4) KR101218214B1 (ru)
CN (4) CN103214484B (ru)
AR (1) AR057995A1 (ru)
AT (1) ATE525374T1 (ru)
AU (1) AU2006326548B2 (ru)
BR (1) BRPI0619817B8 (ru)
CA (1) CA2632466C (ru)
CR (2) CR10065A (ru)
CY (8) CY1112762T1 (ru)
DK (7) DK1966202T3 (ru)
EA (3) EA036785B1 (ru)
EC (2) ECSP088540A (ru)
ES (10) ES2612489T3 (ru)
FR (2) FR13C0007I2 (ru)
HK (5) HK1160115A1 (ru)
HR (7) HRP20110903T1 (ru)
HU (7) HUE030418T2 (ru)
IL (3) IL192019A (ru)
LT (5) LT2426129T (ru)
LU (1) LU92137I2 (ru)
ME (1) ME01312B (ru)
MX (1) MX346183B (ru)
MY (2) MY162590A (ru)
NZ (2) NZ569015A (ru)
PL (7) PL2474545T3 (ru)
PT (7) PT2426129T (ru)
RS (7) RS52101B (ru)
SG (3) SG10202003901UA (ru)
SI (7) SI2474545T1 (ru)
TW (6) TWI664182B (ru)
UA (2) UA98449C2 (ru)
WO (1) WO2007070514A1 (ru)
ZA (1) ZA200805165B (ru)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2563644C2 (ru) * 2010-08-20 2015-09-20 Хатчисон Медифарма Лимитед Пирролопиримидиновые соединения и их применения
RU2701206C2 (ru) * 2014-12-16 2019-09-25 Центаурус Биофарма Ко., Лтд. Пирролопиримидиновое соединение

Families Citing this family (388)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
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.
WO2007031739A1 (en) * 2005-09-16 2007-03-22 Astrazeneca Ab Heterobicyclic compounds as glucokinase activators
CA2621261C (en) 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) * 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
US7528143B2 (en) * 2005-11-01 2009-05-05 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
UA98449C2 (en) 2005-12-13 2012-05-25 Инсайт Корпорейшин Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
KR20080083680A (ko) * 2005-12-23 2008-09-18 스미스클라인 비참 코포레이션 오로라 키나제의 아자인돌 억제제
PL2003132T3 (pl) * 2006-04-03 2014-10-31 Astellas Pharma Inc Pochodne oksadiazolu jako agoniści S1P1
CA2648250A1 (en) * 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
KR20090082507A (ko) 2006-11-20 2009-07-30 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 통증 및 소양증 치료용 방법, 조성물 및 키트
US8513270B2 (en) * 2006-12-22 2013-08-20 Incyte Corporation Substituted heterocycles as Janus kinase inhibitors
CL2008001709A1 (es) * 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
RS53245B2 (sr) 2007-06-13 2022-10-31 Incyte Holdings Corp Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila
WO2009003998A2 (en) * 2007-07-02 2009-01-08 Boehringer Ingelheim International Gmbh Antiproliferative compounds based on 5-membered heterocycles
WO2009032338A1 (en) * 2007-09-09 2009-03-12 University Of Florida Research Foundation Apratoxin therapeutic agents: mechanism and methods of treatment
WO2009049028A1 (en) * 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
CA2703125C (en) * 2007-10-25 2012-08-28 David J. Guerin Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of 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
CN101981036B (zh) * 2008-02-06 2013-09-04 诺瓦提斯公司 吡咯并[2,3-d]嘧啶及其作为酪氨酸激酶抑制剂的用途
US20110105436A1 (en) * 2008-03-10 2011-05-05 Auckland Uniservices Limited Heteroaryl compounds, compositions, and methods of use in cancer treatment
JP5275371B2 (ja) * 2008-03-11 2013-08-28 インサイト・コーポレイション Jak阻害剤としてのアゼチジン誘導体およびシクロブタン誘導体
AU2009274454A1 (en) * 2008-04-21 2010-01-28 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
WO2009132202A2 (en) * 2008-04-24 2009-10-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
AR071717A1 (es) 2008-05-13 2010-07-07 Array Biopharma Inc Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer.
AU2009260389A1 (en) * 2008-06-18 2009-12-23 Merck Sharp & Dohme Corp. Inhibitors of Janus kinases
PE20110063A1 (es) * 2008-06-20 2011-02-16 Genentech Inc DERIVADOS DE [1, 2, 4]TRIAZOLO[1, 5-a]PIRIDINA COMO INHIBIDORES DE JAK
MX2010014005A (es) * 2008-06-20 2011-02-15 Genentech Inc Compuestos de triazolopiridina inhibidores de jak y los metodos.
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
WO2010085597A1 (en) * 2009-01-23 2010-07-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
BRPI1012159B1 (pt) * 2009-05-22 2022-01-25 Incyte Holdings Corporation Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos
LT2432472T (lt) * 2009-05-22 2020-02-10 Incyte Holdings Corporation 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai
SI2440558T1 (sl) 2009-06-08 2015-10-30 Takeda Pharmaceutical Company Limited Spojine dihidropirolonaftiridinona kot inhibitorji JAK
SI2448938T1 (sl) 2009-06-29 2014-08-29 Incyte Corporation Experimental Station Pirimidinoni kot zaviralci pi3k
CA3027255C (en) 2009-07-10 2022-06-21 The General Hospital Corporation Permanently charged sodium and calcium channel blockers as anti-inflammatory agents
TWI466885B (zh) 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
EP2485589A4 (en) 2009-09-04 2013-02-06 Biogen Idec Inc HETEROARYARY INHIBITORS OF BTK
KR101481872B1 (ko) 2009-09-10 2015-01-12 에프. 호프만-라 로슈 아게 Jak의 억제제
AU2010302584B2 (en) 2009-10-02 2015-09-10 Avexxin As Anti inflammatory 2-oxothiazoles and 2 -oxooxazoles
JP5946768B2 (ja) * 2009-10-09 2016-07-06 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation 3−(4−(7H−ピロロ[2,3−d]ピリミジン−4−イル)−1H−ピラゾール−1−イル)−3−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体
US8389728B2 (en) * 2009-11-06 2013-03-05 The Arizona Board Of Regents Pollen tube stimulants from Arabidopsis pistils
CA2790070C (en) * 2010-02-18 2018-03-06 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
WO2011109217A2 (en) * 2010-03-02 2011-09-09 Immunodiagnostics, Inc. Methods of treating or preventing rna polymerase dependent viral disorders by administration of jak2 kinase inhibitors
AU2015205858B2 (en) * 2010-03-10 2017-04-13 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
AU2011224484A1 (en) 2010-03-10 2012-09-27 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
AU2011240808B2 (en) 2010-04-14 2015-01-22 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of JAK kinases
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
US9133123B2 (en) 2010-04-23 2015-09-15 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
CN103002875B (zh) 2010-05-21 2016-05-04 因塞特控股公司 Jak抑制剂的局部用制剂
WO2012040527A2 (en) * 2010-09-24 2012-03-29 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
EP2632903A4 (en) * 2010-10-28 2014-11-26 Viamet Pharmaceuticals Inc METALLOENZYMHEMMERVERBINDUNGEN
WO2012060847A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
EA036970B1 (ru) * 2010-11-19 2021-01-21 Инсайт Холдингс Корпорейшн Применение {1-{1-[3-фтор-2-(трифтометил)изоникотиноил] пиперидин-4-ил}-3-[4-(7h-пирроло[2,3-d]пиримидин-4-ил)-1н-пиразол-1-ил]азетидин-3-ил}ацетонитрила для лечения заболеваний, связанных с активностью jak1
PE20140146A1 (es) * 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
EP2651930B1 (en) * 2010-12-16 2015-10-28 Boehringer Ingelheim International GmbH Biarylamide inhibitors of leukotriene production
ES2764848T3 (es) 2010-12-20 2020-06-04 Incyte Holdings Corp N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K
CA2824970C (en) 2011-02-11 2016-05-03 Batmark Limited Inhaler component
CN103732226B (zh) * 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
CA2826651A1 (en) * 2011-02-24 2012-08-30 Cephalon, Inc. Substituted aromatic sulfur compounds and methods of their use
AU2012232658B2 (en) 2011-03-22 2016-06-09 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
US8759380B2 (en) 2011-04-22 2014-06-24 Cytokinetics, Inc. Certain heterocycles, compositions thereof, and methods for their use
CN103502249A (zh) * 2011-05-17 2014-01-08 普林斯匹亚生物制药公司 作为酪氨酸激酶抑制剂的氮杂吲哚衍生物
AU2012271814A1 (en) 2011-06-14 2013-12-12 Novartis Ag Combination of panobinostat and ruxolitinib in the treatment of cancer such as a myeloproliferative neoplasm
AR086983A1 (es) 2011-06-20 2014-02-05 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
AU2012282229B2 (en) 2011-07-08 2015-05-07 Novartis Ag Novel pyrrolo pyrimidine derivatives
EP2741747A1 (en) 2011-08-10 2014-06-18 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
HUE030869T2 (en) 2011-09-02 2017-06-28 Incyte Holdings Corp Heterocyclic amines as inhibitors of PI3K
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AU2012312303B2 (en) * 2011-09-22 2016-09-15 Merck Sharp & Dohme Corp. Cyanomethylpyrazole carboxamides as janus kinase inhibitors
WO2013055645A1 (en) * 2011-10-12 2013-04-18 Array Biopharma Inc. 5,7-substituted-imidazo[1,2-c]pyrimidines
CA3131037A1 (en) 2011-11-30 2013-06-06 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
US10821111B2 (en) 2011-11-30 2020-11-03 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
US8993756B2 (en) * 2011-12-06 2015-03-31 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
AU2013274030B2 (en) * 2012-06-15 2016-07-07 Sun Pharmaceutical Industries, Inc. Deuterated derivatives of ruxolitinib
US20150197525A1 (en) 2012-06-15 2015-07-16 Concert Pharmaceuticals, Inc. Deuterated derivatives of ruxolitinib
CA2880896C (en) 2012-06-26 2021-11-16 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
EA201590272A1 (ru) 2012-07-27 2015-05-29 Рациофарм Гмбх Пероральные дозированные формы для модифицированного высвобождения, содержащие руксолитиниб
CN104507923B (zh) 2012-08-02 2018-02-09 内尔维阿诺医学科学有限公司 作为激酶抑制剂的取代的吡咯类活性剂
US9593115B2 (en) 2012-09-21 2017-03-14 Advinus Therapeutics Ltd. Substituted fused tricyclic compounds, compositions, and medicinal applications thereof
CA2881070A1 (en) * 2012-10-26 2014-05-01 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
MY191357A (en) * 2012-11-15 2022-06-19 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
US9310374B2 (en) 2012-11-16 2016-04-12 Redwood Bioscience, Inc. Hydrazinyl-indole compounds and methods for producing a conjugate
US10130632B2 (en) 2012-11-27 2018-11-20 Beth Israel Deaconess Medical Center, Inc. Methods for treating renal disease
AU2013355220B2 (en) * 2012-12-06 2018-08-02 Baruch S. Blumberg Institute Functionalized benzamide derivatives as antiviral agents against HBV infection
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
KR102268357B1 (ko) 2013-01-29 2021-06-23 아벡신 에이에스 항염증성 및 항종양성 2-옥소티아졸 및 2-옥소티오펜 화합물
JP6274199B2 (ja) * 2013-02-12 2018-02-07 コニカミノルタ株式会社 有機エレクトロルミネッセンス素子及び照明装置
UA120162C2 (uk) 2013-03-06 2019-10-25 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки при отриманні інгібітора jak
US20140343034A1 (en) 2013-04-25 2014-11-20 Japan Tobacco Inc. Skin barrier function improving agent
TWI719401B (zh) 2013-05-17 2021-02-21 美商英塞特公司 作為jak抑制劑之聯吡唑衍生物
PT3030227T (pt) * 2013-08-07 2020-06-25 Incyte Corp Formas de dosagem de libertação prolongada para um inibidor de jak1
CN105555313A (zh) 2013-08-20 2016-05-04 因赛特公司 在c-反应蛋白水平较高的实体肿瘤患者中的存活益处
EP3757130A1 (en) 2013-09-26 2020-12-30 Costim Pharmaceuticals Inc. Methods for treating hematologic cancers
WO2015054283A1 (en) * 2013-10-08 2015-04-16 Calcimedica, Inc. Compounds that modulate intracellular calcium
US9440977B2 (en) * 2013-10-15 2016-09-13 Bohan Jin Compositions, uses and methods for their preparation
EP3074043A1 (en) 2013-11-27 2016-10-05 Novartis AG Combination therapy comprising an inhibitor of jak, cdk and pim
JP6192839B2 (ja) 2013-12-05 2017-09-06 ファイザー・インク ピロロ[2,3−d]ピリミジニル、ピロロ[2,3−b]ピラジニル、およびピロロ[2,3−d]ピリジニルアクリルアミド
JP6367545B2 (ja) * 2013-12-17 2018-08-01 コンサート ファーマシューティカルズ インコーポレイテッド ルキソリチニブの重水素化誘導体
KR102261733B1 (ko) * 2013-12-18 2021-06-04 콘서트 파마슈티컬즈, 인크. 룩소리티닙의 중수소화된 유도체
CN104725380B (zh) * 2013-12-18 2019-06-28 康塞特医药品有限公司 卢索替尼的氘代衍生物
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
WO2015131080A1 (en) 2014-02-28 2015-09-03 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
EA201691745A1 (ru) 2014-02-28 2016-12-30 Инсайт Корпорейшн Ингибиторы jak1 для лечения миелодиспластических синдромов
CU24481B1 (es) 2014-03-14 2020-03-04 Immutep Sas Moléculas de anticuerpo que se unen a lag-3
PL3129021T3 (pl) 2014-04-08 2021-05-31 Incyte Corporation Leczenie nowotworów złośliwych z komórek b za pomocą skojarzenia inhibitora jak i pi3k
WO2015168246A1 (en) 2014-04-30 2015-11-05 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
RU2564891C1 (ru) * 2014-05-27 2015-10-10 Александр Александрович Кролевец Способ получения нанокапсул цитокининов
EP4233870A3 (en) * 2014-05-28 2024-01-24 Onco Tracker, Inc. Anti-cancer effects of jak2 inhibitors in combination with thalidomide derivatives and glucocorticoids
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
CN105218548A (zh) * 2014-06-09 2016-01-06 上海海和药物研究开发有限公司 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
NZ629796A (en) * 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
JP2017520603A (ja) * 2014-07-14 2017-07-27 シグナル ファーマシューティカルズ,エルエルシー 置換ピロロピリミジン化合物を使用するがんの治療方法及びその組成物
GB201413695D0 (en) 2014-08-01 2014-09-17 Avexxin As Compound
WO2016024232A1 (en) 2014-08-11 2016-02-18 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor
TW201618775A (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、pd-1抑制劑及/或pd-l1抑制劑之治療組合物
HRP20211813T1 (hr) 2014-08-11 2022-03-04 Acerta Pharma B.V. Terapeutske kombinacije inhibitora btk i inhibitora bcl-2
CN117164657A (zh) 2014-08-12 2023-12-05 莫纳什大学 定向淋巴的前药
ES2874537T3 (es) * 2014-08-21 2021-11-05 Ratiopharm Gmbh Sal oxalato de ruxolitinib
JP6681905B2 (ja) 2014-09-13 2020-04-15 ノバルティス アーゲー Alk阻害剤の併用療法
CN105524067A (zh) * 2014-09-28 2016-04-27 江苏柯菲平医药股份有限公司 4-取代吡咯并[2,3-d]嘧啶化合物及其用途
AU2015327868A1 (en) 2014-10-03 2017-04-20 Novartis Ag Combination therapies
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
CR20170143A (es) 2014-10-14 2017-06-19 Dana Farber Cancer Inst Inc Moléculas de anticuerpo que se unen a pd-l1 y usos de las mismas
WO2016063294A2 (en) * 2014-10-20 2016-04-28 Msn Laboratories Private Limited Process for the preparation of (r)-3-(4-(7h-pyrrolo[2,3-d], pyrimidin-4-yl)-1 h-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and its polymorphs thereof
GB2535427A (en) 2014-11-07 2016-08-24 Nicoventures Holdings Ltd Solution
CZ2014773A3 (cs) 2014-11-10 2016-05-18 Zentiva, K.S. Soli (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu
TWI748941B (zh) 2015-02-27 2021-12-11 美商英塞特公司 Pi3k抑制劑之鹽及製備方法
TWI788655B (zh) 2015-02-27 2023-01-01 美商林伯士拉克許米公司 酪胺酸蛋白質激酶2(tyk2)抑制劑及其用途
TN2017000375A1 (en) 2015-03-10 2019-01-16 Aduro Biotech Inc Compositions and methods for activating "stimulator of interferon gene" -dependent signalling
KR101859170B1 (ko) * 2015-04-17 2018-05-17 광주과학기술원 트리아졸 화합물 및 이의 용도
ES2734048T3 (es) * 2015-04-29 2019-12-04 Wuxi Fortune Pharmaceutical Co Ltd Inhibidores de Janus cinasas (JAK)
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
CZ2015496A3 (cs) 2015-07-14 2017-01-25 Zentiva, K.S. Krystalické formy solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a jejich příprava
WO2017011720A1 (en) * 2015-07-16 2017-01-19 Signal Pharmaceuticals, Llc Solod forms 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d] oxazol-6-yl)17h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
WO2017019896A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to pd-1
PT3317301T (pt) 2015-07-29 2021-07-09 Novartis Ag Terapias de associação compreendendo moléculas de anticorpo contra lag-3
US20180207273A1 (en) 2015-07-29 2018-07-26 Novartis Ag Combination therapies comprising antibody molecules to tim-3
JP6833811B2 (ja) 2015-08-03 2021-02-24 プレジデント アンド フェローズ オブ ハーバード カレッジ 荷電イオンチャネル遮断薬及び使用方法
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
JP6802263B2 (ja) 2015-09-02 2020-12-16 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用
WO2017041139A1 (en) 2015-09-08 2017-03-16 Monash University Lymph directing prodrugs
WO2017044720A1 (en) 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
CA3234750A1 (en) 2015-10-23 2017-04-27 Navitor Pharmaceuticals, Inc. Modulators of sestrin-gator2 interaction and uses thereof
SG11201803520PA (en) 2015-11-03 2018-05-30 Janssen Biotech Inc Antibodies specifically binding pd-1 and their uses
MA43169B1 (fr) 2015-11-06 2022-05-31 Incyte Corp Composés héterocycliques en tant qu' inhibiteurs pi3k-gamma
AU2016354009B2 (en) 2015-11-09 2021-05-20 R.P. Scherer Technologies, Llc Anti-CD22 antibody-maytansine conjugates and methods of use thereof
RU2601410C1 (ru) * 2015-11-13 2016-11-10 ЗАО "Р-Фарм" {3-[(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)АЗОЛИЛ]АЗЕТИДИН-3-ИЛ}АЦЕТОНИТРИЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС КИНАЗ
US11370792B2 (en) 2015-12-14 2022-06-28 Raze Therapeutics, Inc. Caffeine inhibitors of MTHFD2 and uses thereof
CN108368115B (zh) * 2015-12-15 2020-01-03 正大天晴药业集团股份有限公司 吡咯并嘧啶化合物的盐
AU2016369537B2 (en) 2015-12-17 2024-03-14 Novartis Ag Antibody molecules to PD-1 and uses thereof
AU2016369623A1 (en) 2015-12-17 2018-06-28 Novartis Ag Combination of c-Met inhibitor with antibody molecule to PD-1 and uses thereof
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
JP6921087B2 (ja) * 2015-12-31 2021-08-18 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. ルキソリチニブの合成プロセス
EP4079320A1 (en) 2016-01-12 2022-10-26 Inc. Oncotracker Improved methods for monitoring immune status of a subject
CZ201629A3 (cs) 2016-01-22 2017-08-02 Zentiva, K.S. Krystalické modifikace solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a způsoby jejich přípravy
WO2017129116A1 (zh) * 2016-01-26 2017-08-03 杭州华东医药集团新药研究院有限公司 吡咯嘧啶五元氮杂环衍生物及其应用
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
ES2965264T3 (es) 2016-03-09 2024-04-11 Raze Therapeutics Inc Inhibidores de la 3-fosfoglicerato deshidrogenasa y sus usos
EP4234552A3 (en) 2016-03-09 2023-10-18 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
GB201604318D0 (en) 2016-03-14 2016-04-27 Avexxin As Combination therapy
RS65129B1 (sr) 2016-03-28 2024-02-29 Incyte Corp Jedinjenja pirolotriazina kao inhibitori tam
WO2017177230A1 (en) 2016-04-08 2017-10-12 X4 Pharmaceuticals, Inc. Methods for treating cancer
KR20190003711A (ko) 2016-05-04 2019-01-09 콘서트 파마슈티컬즈, 인크. 중수소화된 jak 저해제를 이용한 탈모 장애의 치료
CN107759600A (zh) * 2016-06-16 2018-03-06 正大天晴药业集团股份有限公司 作为jak抑制剂的吡咯并嘧啶化合物的结晶
CN107513067A (zh) * 2016-06-16 2017-12-26 北京赛林泰医药技术有限公司 含有取代环戊基的吡咯并嘧啶化合物
CN107513069A (zh) * 2016-06-16 2017-12-26 正大天晴药业集团股份有限公司 手性吡咯并嘧啶化合物的制备方法
JP6994767B2 (ja) 2016-06-21 2022-01-14 エックス4 ファーマシューティカルズ, インコーポレイテッド Cxcr4阻害剤およびその使用
ES2870920T3 (es) 2016-06-21 2021-10-28 X4 Pharmaceuticals Inc Inhibidores de CXCR4 y usos de los mismos
WO2017223229A1 (en) 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
JP2019519579A (ja) 2016-06-30 2019-07-11 デウン ファーマシューティカル カンパニー リミテッド キナーゼ阻害剤としてのピラゾロピリミジン誘導体
WO2018009466A1 (en) 2016-07-05 2018-01-11 Aduro Biotech, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
CN109790158B (zh) * 2016-07-26 2022-06-24 苏州隆博泰药业有限公司 作为jak抑制剂杂环化合物,该化合物的盐类及其治疗用途
US11020398B2 (en) 2016-08-24 2021-06-01 Arqule, Inc. Amino-pyrrolopyrimidinone compounds and methods of use thereof
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
IT201600092051A1 (it) * 2016-09-13 2018-03-13 Alessandro Antonelli Composto medicale per il trattamento di tumori della tiroide
CN109952303B (zh) 2016-10-14 2022-10-21 林伯士拉克许米公司 Tyk2抑制剂及其用途
WO2018075937A1 (en) 2016-10-21 2018-04-26 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
EP3538091A4 (en) 2016-11-08 2020-06-10 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF
AU2017368050A1 (en) 2016-11-29 2019-06-20 Puretech Lyt, Inc. Exosomes for delivery of therapeutic agents
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
RU2644155C1 (ru) * 2016-12-12 2018-02-08 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") 2-(3-(4-(7H-пирроло[2,3-d]пиримидин-4-ил)-1H-пиразол-1-ил)-1-(этилсульфонил)азетидин-3-ил)ацетонитрила геминафтилдисульфонат в качестве ингибитора Янус киназ
JP2020502238A (ja) 2016-12-23 2020-01-23 バイスクルアールディー・リミテッド 新規連結構造を有するペプチド誘導体
EP3565638B8 (en) 2017-01-06 2024-04-10 BicycleRD Limited Bicycle conjugate for treating cancer
EA039344B1 (ru) * 2017-01-19 2022-01-17 Сучжоу Лонгбайотек Фармасьютикалз Ко., Лтд. Гетероциклическое соединение в качестве ингибитора jak и его соли и терапевтическое применение
TWI783978B (zh) 2017-03-08 2022-11-21 美商林伯士拉克許米公司 Tyk2抑制劑、其用途及生產方法
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
US11339144B2 (en) 2017-04-10 2022-05-24 Navitor Pharmaceuticals, Inc. Heteroaryl Rheb inhibitors and uses thereof
JOP20180036A1 (ar) 2017-04-18 2019-01-30 Vifor Int Ag أملاح لمثبطات فروبورتين جديدة
CN116370448A (zh) 2017-04-26 2023-07-04 纳维托制药有限公司 Sestrin-gator2相互作用的调节剂及其用途
US10857196B2 (en) 2017-04-27 2020-12-08 Bicycletx Limited Bicyclic peptide ligands and uses thereof
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
NZ759764A (en) 2017-05-23 2022-07-01 Theravance Biopharma R&D Ip Llc Glucuronide prodrugs of janus kinase inhibitors
US11635435B2 (en) 2017-06-13 2023-04-25 Oncotracker, Inc. Diagnostic, prognostic, and monitoring methods for solid tumor cancers
WO2018237173A1 (en) 2017-06-22 2018-12-27 Novartis Ag ANTIBODY MOLECULES DIRECTED AGAINST CD73 AND CORRESPONDING USES
SG11201912473PA (en) 2017-06-22 2020-01-30 Novartis Ag Antibody molecules to cd73 and uses thereof
JP7301757B2 (ja) 2017-06-26 2023-07-03 バイスクルアールディー・リミテッド 検出可能部分を持つ二環式ペプチドリガンドおよびその使用
CN107298680A (zh) * 2017-07-12 2017-10-27 海门华祥医药科技有限公司 一种4‑氯‑7‑氮杂吲哚的生产工艺
PT3658557T (pt) 2017-07-28 2024-09-11 Nimbus Lakshmi Inc Inibidores de tyk2 e usos dos mesmos
JP2020529427A (ja) 2017-08-04 2020-10-08 バイスクルテクス・リミテッド Cd137に対して特異的な二環式ペプチドリガンド
US20200283482A1 (en) 2017-08-14 2020-09-10 Bicyclerd Limited Bicyclic peptide ligand prr-a conjugates and uses thereof
EP3668887A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
AU2018324037A1 (en) 2017-08-29 2020-04-16 Monash University Lymphatic system-directing lipid prodrugs
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
JP7366031B2 (ja) 2017-09-22 2023-10-20 カイメラ セラピューティクス, インコーポレイテッド タンパク質分解剤およびそれらの使用
EP3988552A1 (en) 2017-09-27 2022-04-27 Incyte Corporation Salts of pyrrolotriazine derivatives useful as tam inhibitors
CN109651424B (zh) * 2017-10-11 2021-01-22 新发药业有限公司 一种7-保护基-4-(1-氢-吡唑-4-基)吡咯[2,3-d]嘧啶的合成方法
CN111566095B (zh) 2017-11-03 2024-09-27 阿克拉瑞斯治疗股份有限公司 被取代的吡咯并吡啶jak抑制剂及其制造方法和使用方法
US10800775B2 (en) 2017-11-03 2020-10-13 Aclaris Therapeutics, Inc. Pyrazolyl pyrrolo[2,3-b]pyrmidine-5-carboxylate analogs and methods of making the same
KR102034538B1 (ko) 2017-11-28 2019-10-21 주식회사한국파마 Jak 저해제 화합물, 및 이의 제조방법
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID MEDICINAL PRODUCTS AND THEIR USES
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc IRAK joints and used in them
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
AU2019212969A1 (en) 2018-01-29 2020-08-13 Merck Patent Gmbh GCN2 inhibitors and uses thereof
CN111918651B (zh) 2018-01-29 2024-01-30 默克专利股份有限公司 Gcn2抑制剂及其用途
KR20200129099A (ko) 2018-01-30 2020-11-17 인사이트 코포레이션 (1-(3-플루오로-2-(트리플루오로메틸)이소니코티닐)피페리딘-4-온)의 제조 방법
IL276725B2 (en) 2018-02-16 2024-09-01 Incyte Corp JAK1 pathway inhibitors for the treatment of cytokine-related disorders
KR102526964B1 (ko) 2018-02-26 2023-04-28 길리애드 사이언시즈, 인코포레이티드 Hbv 복제 억제제로서의 치환된 피롤리진 화합물
AU2019229258B2 (en) 2018-02-27 2023-09-14 Artax Biopharma Inc. Chromene derivatives as inhibitors of TCR-Nck interaction
RU2020132460A (ru) 2018-03-08 2022-04-08 Новартис Аг Применение антитела к p-селектину
CN110357887B (zh) * 2018-03-26 2022-09-16 武汉誉祥医药科技有限公司 取代的7H-吡咯并[2,3-d]嘧啶衍生物及其制备方法和用途
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
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
SG11202010092XA (en) 2018-04-13 2020-11-27 Incyte Corp Biomarkers for graft-versus-host disease
CN112236428A (zh) 2018-04-24 2021-01-15 默克专利股份有限公司 抗增殖化合物及其用途
CN112218865B (zh) 2018-04-24 2024-03-12 沃泰克斯药物股份有限公司 喋啶酮化合物及其用途
AR126019A1 (es) 2018-05-30 2023-09-06 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
US20210214459A1 (en) 2018-05-31 2021-07-15 Novartis Ag Antibody molecules to cd73 and uses thereof
US12065441B2 (en) 2018-06-06 2024-08-20 Gengle Therapeutics, Inc. Pyrazolopyrimidine derivative, use thereof and pharmaceutical composition
IL279329B1 (en) 2018-06-15 2024-09-01 Navitor Pharm Inc Rapamycin analogs and their uses
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
US11180531B2 (en) 2018-06-22 2021-11-23 Bicycletx Limited Bicyclic peptide ligands specific for Nectin-4
AU2019293618A1 (en) 2018-06-29 2021-02-18 Incyte Corporation Formulations of an AXL/MER inhibitor
JP6830460B2 (ja) * 2018-07-05 2021-02-17 コンサート ファーマシューティカルズ インコーポレイテッド ルキソリチニブの重水素化誘導体
EP3817748A4 (en) 2018-07-06 2022-08-24 Kymera Therapeutics, Inc. TRICYCLIC CRBN LIGANDS AND USES THEREOF
KR102653681B1 (ko) 2018-07-31 2024-04-03 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제
AU2019317625A1 (en) 2018-08-10 2021-02-18 Aclaris Therapeutics, Inc. Pyrrolopyrimidine ITK inhibitors
WO2020039401A1 (en) 2018-08-24 2020-02-27 Novartis Ag Treatment comprising il-1βeta binding antibodies and combinations thereof
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
EP3846793B1 (en) 2018-09-07 2024-01-24 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
EP3866789A4 (en) 2018-10-15 2022-07-06 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
CN112955459A (zh) 2018-10-23 2021-06-11 拜斯科技术开发有限公司 双环肽配体和其用途
US11345654B2 (en) 2018-10-24 2022-05-31 Navitor Pharmaceuticals, Inc. Polymorphic compounds and uses thereof
JP7431845B2 (ja) 2018-10-31 2024-02-15 インサイト・コーポレイション 血液疾患の治療のための併用療法
MX2021006154A (es) 2018-11-30 2021-08-24 Kymera Therapeutics Inc Degradadores de cinasas asociadas al receptor de interleucina 1 (irak) y usos de los mismos.
US11053241B2 (en) 2018-11-30 2021-07-06 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
CN109394768B (zh) * 2018-12-10 2019-08-23 牡丹江医学院 一种治疗湿疹的药物及其制备方法
CN111320633B (zh) * 2018-12-14 2022-09-27 中国医药研究开发中心有限公司 吡咯/咪唑并六元杂芳环类化合物及其制备方法和医药用途
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
JP2022518505A (ja) 2019-01-23 2022-03-15 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
CN111620873B (zh) * 2019-02-28 2021-12-28 沈阳药科大学 一类含哌啶的吡咯并[2,3-d]嘧啶衍生物及其制备和用途
MA55201A (fr) 2019-03-05 2022-01-12 Incyte Corp Inhibiteurs de la voie jak1 pour le traitement d'un dysfonctionnement chronique de l'allogreffe pulmonaire
US10968179B2 (en) 2019-03-11 2021-04-06 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
MA55320A (fr) 2019-03-11 2022-01-19 Nocion Therapeutics Inc Bloqueurs de canaux ioniques substitués par un ester et méthodes d'utilisation
US10780083B1 (en) 2019-03-11 2020-09-22 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
EP3937945A4 (en) 2019-03-11 2023-01-04 Nocion Therapeutics, Inc. CHARGED ION CHANNEL BLOCKERS AND METHODS OF USE
US10786485B1 (en) 2019-03-11 2020-09-29 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
JP2022526301A (ja) 2019-03-19 2022-05-24 インサイト・コーポレイション 尋常性白斑のバイオマーカー
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
AU2020253990A1 (en) 2019-04-02 2021-10-28 Bicycletx Limited Bicycle toxin conjugates and uses thereof
US11485750B1 (en) 2019-04-05 2022-11-01 Kymera Therapeutics, Inc. STAT degraders and uses thereof
AU2020262100B2 (en) 2019-04-24 2023-03-16 Elanco Us Inc. A 7H-pyrrolo[2,3-d]pyrimidine JAK-inhibitor
EP3962897A4 (en) 2019-05-02 2022-12-14 Aclaris Therapeutics, Inc. SUBSTITUTED PYRROLOPYRIDINES AS JAK INHIBITORS
CN110028509B (zh) * 2019-05-27 2020-10-09 上海勋和医药科技有限公司 作为选择性jak2抑制剂的吡咯并嘧啶类化合物、其合成方法及用途
KR102286372B1 (ko) 2019-05-27 2021-08-05 주식회사한국파마 Jak 저해제 화합물, 및 이를 포함하는 의약 조성물
JP2022534425A (ja) 2019-05-31 2022-07-29 イケナ オンコロジー, インコーポレイテッド Tead阻害剤およびその使用
TW202112377A (zh) * 2019-06-10 2021-04-01 美商英塞特公司 藉由jak抑制劑局部治療白斑症
WO2020261219A1 (en) 2019-06-27 2020-12-30 Crispr Therapeutics Ag Use of chimeric antigen receptor t cells and nk cell inhibitors for treating cancer
TW202110485A (zh) 2019-07-30 2021-03-16 英商拜西可泰克斯有限公司 異質雙環肽複合物
CN110305140B (zh) 2019-07-30 2020-08-04 上海勋和医药科技有限公司 二氢吡咯并嘧啶类选择性jak2抑制剂
US20220235043A1 (en) * 2019-07-31 2022-07-28 Aclaris Therapeutics, Inc. Substituted sulfonamide pyrrolopyridines as jak inhibitors
WO2021022076A1 (en) * 2019-08-01 2021-02-04 St. Jude Children's Research Hospital Molecules and methods related to treatment of uncontrolled cellular proliferation
AU2020345962A1 (en) 2019-09-11 2022-03-31 Vincere Biosciences, Inc. USP30 inhibitors and uses thereof
BR112022004451A2 (pt) 2019-09-13 2022-06-21 Nimbus Saturn Inc Antagonistas de hpk1 e usos dos mesmos
JP2022548627A (ja) 2019-09-16 2022-11-21 ノバルティス アーゲー 骨髄線維症の治療のための、高親和性のリガンドを遮断するヒト化抗t細胞免疫グロブリンドメイン及びムチンドメイン3(tim-3)igg4抗体の使用
CN114450008A (zh) 2019-09-16 2022-05-06 诺华股份有限公司 Mdm2抑制剂用于治疗骨髓纤维化的用途
EP4031578A1 (en) 2019-09-18 2022-07-27 Novartis AG Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies
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
US20210123931A1 (en) 2019-10-10 2021-04-29 Incyte Corporation Biomarkers for graft-versus-host disease
CA3157499A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
WO2021076124A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Use of jak1 inhibitors for the treatment of cutaneous lupus erythematosus and lichen planus (lp)
WO2021087432A1 (en) 2019-11-01 2021-05-06 Navitor Pharmaceuticals, Inc. Methods of treatment using an mtorc1 modulator
US10933055B1 (en) 2019-11-06 2021-03-02 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
WO2021091585A1 (en) 2019-11-06 2021-05-14 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021102258A1 (en) 2019-11-22 2021-05-27 Incyte Corporation Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
US11819476B2 (en) 2019-12-05 2023-11-21 Janssen Pharmaceutica Nv Rapamycin analogs and uses thereof
US11591332B2 (en) 2019-12-17 2023-02-28 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
KR20220145325A (ko) 2019-12-17 2022-10-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
CN115297931A (zh) 2019-12-23 2022-11-04 凯麦拉医疗公司 Smarca降解剂和其用途
JP2023509452A (ja) 2020-01-03 2023-03-08 バーグ エルエルシー がんを処置するためのube2kモジュレータとしての多環式アミド
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
KR20220149534A (ko) 2020-02-05 2022-11-08 퓨어테크 엘와이티, 아이엔씨. 신경스테로이드의 지질 전구약물
CN111728975A (zh) * 2020-02-25 2020-10-02 广东省检迅检测科技有限公司 用于减少运动损伤和促进运动损伤修复的组合物
WO2021178488A1 (en) 2020-03-03 2021-09-10 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
AU2021236130A1 (en) 2020-03-11 2022-09-22 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
JP2023518423A (ja) 2020-03-19 2023-05-01 カイメラ セラピューティクス, インコーポレイテッド Mdm2分解剤およびそれらの使用
US11324750B2 (en) 2020-04-09 2022-05-10 Children's Hospital Medical Center Compositions and methods for the treatment of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection
WO2021206766A1 (en) 2020-04-09 2021-10-14 Children's Hospital Medical Center Sars-cov-2 infection biomarkers and uses thereof
EP3892280A3 (en) 2020-04-09 2022-01-12 Children's Hospital Medical Center Sars-cov-2 infection biomarkers and uses thereof
US20230218644A1 (en) 2020-04-16 2023-07-13 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
WO2021236139A1 (en) 2020-05-21 2021-11-25 Concert Pharmaceuticals, Inc. Novel deuterated jak inhibitor and uses thereof
US11685731B2 (en) 2020-06-02 2023-06-27 Incyte Corporation Processes of preparing a JAK1 inhibitor
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4161528A1 (en) 2020-06-03 2023-04-12 Incyte Corporation Combination of ruxolitinib with incb057643 for treatment of myeloproliferative neoplasms
CN116057045A (zh) 2020-06-05 2023-05-02 金耐特生物制药公司 成纤维细胞生长因子受体激酶抑制剂
WO2021260657A1 (en) 2020-06-26 2021-12-30 Crispr Therapeutics Ag Allogeneic cell therapy of b cell malignancies using genetically engineered t cells targeting cd19
EP3944859A1 (en) 2020-07-30 2022-02-02 Assistance Publique Hôpitaux de Paris Method for treating immune toxicities induced by immune checkpoint inhibitors
US11751108B2 (en) * 2020-08-05 2023-09-05 Qualcomm Incorporated Execution of reduced signaling handover
CA3194469A1 (en) * 2020-08-12 2022-02-17 Concert Pharmaceuticals, Inc. Process for preparing enantiomerically enriched jak inhibitors
WO2022038158A1 (en) 2020-08-17 2022-02-24 Bicycletx Limited Bicycle conjugates specific for nectin-4 and uses thereof
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
TW202212341A (zh) 2020-08-18 2022-04-01 美商英塞特公司 製備jak1抑制劑之方法及中間體
EP4213800A1 (en) 2020-09-16 2023-07-26 Incyte Corporation Topical treatment of vitiligo
CA3190461A1 (en) * 2020-09-16 2022-03-24 Young Jun Park Pyrimido pyrimidinone compound and pharmaceutical composition comprising the same
CA3197645A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Topical ruxolitinib for treating lichen planus
EP4225316A1 (en) 2020-10-08 2023-08-16 Novartis AG Use of an erk inhibitor for the treatment of myelofibrosis
US20240000777A1 (en) 2020-10-08 2024-01-04 Novartis Ag Use of an erk inhibitor for the treatment of myelofibrosis
CN114437079A (zh) * 2020-10-30 2022-05-06 杭州邦顺制药有限公司 吡咯嘧啶五元氮杂环化合物的晶型
KR102551758B1 (ko) 2020-11-30 2023-07-05 주식회사한국파마 신규한 jak 특이 저해제 화합물, 및 이의 제조방법
CA3200814A1 (en) 2020-12-02 2022-06-09 Alfredo C. Castro Tead inhibitors and uses thereof
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
KR20230128472A (ko) 2020-12-04 2023-09-05 인사이트 코포레이션 피부 질환의 치료를 위한 비타민 d 유사체를 함유하는jak 억제제
EP4259131A1 (en) 2020-12-08 2023-10-18 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
AU2021401834A1 (en) 2020-12-18 2023-07-06 Boehringer Ingelheim Animal Health USA Inc. Boron containing pyrazole compounds, compositions comprising them, methods and uses thereof
US11918581B2 (en) 2021-01-11 2024-03-05 Incyte Corporation Combination therapy comprising JAK pathway inhibitor and rock inhibitor
WO2022165530A1 (en) * 2021-02-01 2022-08-04 Janssen Biotech, Inc. Small molecule inhibitors of salt inducible kinases
EP4288427A1 (en) 2021-02-02 2023-12-13 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
US20230091528A1 (en) 2021-02-02 2023-03-23 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
TW202245774A (zh) * 2021-02-05 2022-12-01 大陸商上海齊魯製藥研究中心有限公司 嘧啶或吡啶並雜環類腺苷受體抑制劑及其製備方法和用途
CN116867494A (zh) 2021-02-15 2023-10-10 凯麦拉医疗公司 Irak4降解剂和其用途
EP4297750A1 (en) 2021-02-25 2024-01-03 Impact Biomedicines, Inc. Use of a bet inhibitor alone or in combination with fedratinib or ruxolitinib for treating a hematological malignancy such as myelofibrosis
WO2022187856A1 (en) 2021-03-05 2022-09-09 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
JP2024513011A (ja) 2021-03-29 2024-03-21 ニンバス サターン, インコーポレイテッド Hpk1アンタゴニスト及びその使用
AU2022258968A1 (en) 2021-04-16 2023-10-19 Ikena Oncology, Inc. Mek inhibitors and uses thereof
TW202309030A (zh) 2021-05-07 2023-03-01 美商凱麥拉醫療公司 Cdk2降解劑及其用途
WO2023288197A1 (en) 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
TW202315621A (zh) 2021-08-25 2023-04-16 美商皮克醫療公司 Eif4e抑制劑及其用途
JP2024532276A (ja) 2021-08-25 2024-09-05 ピク セラピューティクス, インコーポレイテッド eIF4E阻害剤及びその使用
CA3231996A1 (en) * 2021-09-18 2023-03-23 Satya Srinivas HANUMARA An improved process for the preparation of ruxolitinib phosphate
AU2022378463A1 (en) 2021-10-25 2024-05-09 Kymera Therapeutics, Inc. Tyk2 degraders and uses thereof
WO2023102559A1 (en) 2021-12-03 2023-06-08 Incyte Corporation Topical formulations of ruxolitinib with an organic amine ph adjusting agent for treatment of skin diseases
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CN114044777B (zh) * 2022-01-10 2022-04-19 南京佰麦生物技术有限公司 一种磷酸芦可替尼的制备方法
AU2023214044A1 (en) 2022-01-31 2024-08-08 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CN114456181A (zh) * 2022-02-21 2022-05-10 浙江乐普药业股份有限公司 一种芦可替尼的制备方法
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
TW202415650A (zh) 2022-08-02 2024-04-16 英商利米那生物科技有限公司 芳基-三唑基及相關gpr84拮抗劑及其用途
TW202416950A (zh) 2022-08-02 2024-05-01 英商利米那生物科技有限公司 雜芳基甲醯胺及相關gpr84拮抗劑及其用途
WO2024028365A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Substituted pyridone gpr84 antagonists and uses thereof
WO2024028193A1 (en) 2022-08-03 2024-02-08 Medichem, S.A. Stable oral pharmaceutical formulation containing ruxolitinib hemifumarate
US20240166654A1 (en) * 2022-11-11 2024-05-23 Zhejiang Ausun Pharmaceutical Co., Ltd. Ruxolitinib crystal and pharmaceutical composition thereof
US20240208961A1 (en) 2022-11-22 2024-06-27 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
WO2024184926A1 (en) * 2023-03-08 2024-09-12 Aarti Pharmalabs Limited Process for preparation of chiral ruxolitinib and salts thereof
WO2024187416A1 (en) * 2023-03-15 2024-09-19 Zhejiang Qizheng Pharmaceutical Co., Ltd. Pharmaceutical composition comprising ruxolitinib
WO2024187415A1 (en) * 2023-03-15 2024-09-19 Zhejiang Qizheng Pharmaceutical Co., Ltd. Pharmaceutical composition comprising ruxolitinib

Family Cites Families (311)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2985589A (en) 1957-05-22 1961-05-23 Universal Oil Prod Co Continuous sorption process employing fixed bed of sorbent and moving inlets and outlets
US3632836A (en) 1968-10-25 1972-01-04 Dow Chemical Co Solid curable polyepoxides modified with hydrolyzed liquid polyepoxides
US3832460A (en) * 1971-03-19 1974-08-27 C Kosti Anesthetic-vasoconstrictor-antihistamine composition for the treatment of hypertrophied oral tissue
US4140755A (en) * 1976-02-13 1979-02-20 Hoffmann-La Roche Inc. Sustained release tablet formulations
DE3036390A1 (de) 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
DE3220113A1 (de) 1982-05-28 1983-12-01 Basf Ag, 6700 Ludwigshafen Difluormethoxiphenylthiophosphorsaeureester
US4402832A (en) 1982-08-12 1983-09-06 Uop Inc. High efficiency continuous separation process
US4404335A (en) 1982-08-16 1983-09-13 The Dow Chemical Company Hydrolyzing epoxy resins in absence of solvent and in presence of oxalic acid and a phosphonium compound
US4548990A (en) 1983-08-15 1985-10-22 Ciba-Geigy Corporation Crosslinked, porous polymers for controlled drug delivery
US4498991A (en) 1984-06-18 1985-02-12 Uop Inc. Serial flow continuous separation process
NL8403224A (nl) * 1984-10-24 1986-05-16 Oce Andeno Bv Dioxafosforinanen, de bereiding ervan en de toepassing voor het splitsen van optisch actieve verbindingen.
CA1306260C (en) 1985-10-18 1992-08-11 Shionogi & Co., Ltd. Condensed imidazopyridine derivatives
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
US5403593A (en) 1991-03-04 1995-04-04 Sandoz Ltd. Melt granulated compositions for preparing sustained release dosage forms
IT1258781B (it) 1992-01-16 1996-02-29 Zambon Spa Composizione farmaceutica oftalmica contenente n-acetilcisteina e polivinilalcol
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
FR2695126B1 (fr) 1992-08-27 1994-11-10 Sanofi Elf Dérivés d'acide thiényl ou pyrrolyl carboxyliques, leur préparation et médicaments les contenant.
AU671491B2 (en) 1992-12-18 1996-08-29 F. Hoffmann-La Roche Ag N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines
JPH0710876A (ja) * 1993-06-24 1995-01-13 Teijin Ltd 4位に環状アミノ基を有するピロロ[2,3―d]ピリミジン
USH1439H (en) 1993-10-18 1995-05-02 The Dow Chemical Company Method to increase the level of α-glycol in liquid epoxy resin
EP0727217A3 (en) 1995-02-10 1997-01-15 Suntory Ltd Pharmaceutical and cosmetic compositions containing God-type ellagitannin as an active ingredient
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
US5856326A (en) 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
MX9800136A (es) 1995-07-05 1998-03-29 Du Pont Pirimidinonas fungicidas.
CA2224435C (en) 1995-07-06 2008-08-05 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
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
AU2802297A (en) 1996-04-18 1997-11-07 Merck & Co., Inc. 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
WO1998044797A1 (en) 1997-04-07 1998-10-15 Merck & Co., Inc. A method of treating cancer
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
JP2001513502A (ja) 1997-08-11 2001-09-04 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 5,6−ヘテロアリールジピリド[2,3−b:3’,2’−f]アゼピン類及びHIV感染の予防及び治療におけるそれらの使用
US7153845B2 (en) 1998-08-25 2006-12-26 Columbia Laboratories, Inc. Bioadhesive progressive hydration tablets
US6075056A (en) 1997-10-03 2000-06-13 Penederm, Inc. Antifungal/steroid topical compositions
SE9800729L (sv) 1998-03-06 1999-09-07 Scotia Lipidteknik Ab Ny topikal formulering I
US6025366A (en) 1998-04-02 2000-02-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
BR9910864A (pt) 1998-06-04 2002-02-05 Abbott Lab Compostos anti-inflamatórios para inibição de aderência celular
JP4666762B2 (ja) 1998-06-19 2011-04-06 ファイザー・プロダクツ・インク ピロロ[2.3−d]ピリミジン化合物
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
BR9912938B1 (pt) 1998-08-11 2011-06-28 derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos.
JP2000119271A (ja) 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd 1h―イミダゾピリジン誘導体
JP5026635B2 (ja) * 1998-09-10 2012-09-12 ニュコメデ ダンマルク アンパーツセルスカブ 医薬物質の迅速放出医薬組成物
US6375839B1 (en) 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
FR2785196B1 (fr) 1998-10-29 2000-12-15 Inst Francais Du Petrole Procede et dispositif de separation avec des zones chromatographiques a longueur variable
US6413419B1 (en) 1998-10-29 2002-07-02 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
EP1165084A4 (en) 1999-03-03 2002-05-15 Merck & Co Inc PRENYL PROTEIN TRANSFERASES INHIBITORS
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
ATE275141T1 (de) 1999-10-13 2004-09-15 Banyu Pharma Co Ltd Substituierte imidazolin-derivate
US7235258B1 (en) 1999-10-19 2007-06-26 Nps Pharmaceuticals, Inc. Sustained-release formulations for treating CNS-mediated disorders
KR100477818B1 (ko) * 1999-12-10 2005-03-22 화이자 프로덕츠 인코포레이티드 피롤로[2,3-d] 피리미딘 화합물
OA12514A (en) * 1999-12-24 2006-05-29 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.
AU4878601A (en) 2000-04-20 2001-11-07 Mitsubishi Corporation Aromatic amide compounds
SI2223922T1 (sl) * 2000-04-25 2016-04-29 Icos Corporation Inhibitorji humane fosfatidil-inositol 3-kinazne delta izoforme
JP4954426B2 (ja) 2000-06-16 2012-06-13 キュリス,インコーポレイテッド 血管形成調節組成物及び利用
US7498304B2 (en) 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
AU2001274598A1 (en) * 2000-06-23 2002-01-02 Mitsubishi Pharma Corporation Antitumor effect potentiators
PT1294724E (pt) * 2000-06-26 2006-07-31 Pfizer Prod Inc Compostos pirrolo (2,3-d ) pirimidina como agentes imunosupressivos
CZ303572B6 (cs) 2000-06-28 2012-12-12 Smithkline Beecham P. L. C. Jemne rozmelnený prostredek a zpusob jeho prípravy
AU2001278790A1 (en) 2000-08-22 2002-03-04 Hokuriku Seiyaku Co. Ltd 1h-imidazopyridine derivatives
AU2002228783A1 (en) 2000-12-05 2002-06-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
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
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
CA2446864C (en) 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
WO2003011285A1 (en) 2001-08-01 2003-02-13 Merck & Co., Inc. BENZIMIDAZO[4,5-f]ISOQUINOLINONE DERIVATIVES
CN100391958C (zh) 2001-09-19 2008-06-04 安万特医药股份有限公司 化合物
US6429231B1 (en) 2001-09-24 2002-08-06 Bradley Pharmaceuticals, Inc. Compositions containing antimicrobials and urea for the treatment of dermatological disorders and methods for their use
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
WO2003048111A1 (en) 2001-11-30 2003-06-12 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
EP1503739A4 (en) 2002-04-15 2006-06-21 Adams Respiratory Therapeutics REGULAR RELEASE OF COMBINED MEDICINAL PRODUCTS FROM GUAIFENESIN
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
US7304061B2 (en) 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
US7125888B2 (en) 2002-05-02 2006-10-24 Merck & Co., Inc. Tyrosine kinase inhibitors
CA2484632C (en) 2002-05-07 2012-12-11 Control Delivery Systems, Inc. Processes for forming a drug delivery device
CA2486183C (en) 2002-05-23 2012-01-10 Cytopia Pty Ltd. Protein kinase inhibitors
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
WO2004003026A1 (ja) * 2002-06-26 2004-01-08 Idemitsu Kosan Co., Ltd. 共重合体水素添加物、その製造方法及びそれを用いたホットメルト接着剤組成物
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
US20060004010A1 (en) * 2002-07-10 2006-01-05 Hiromu Habashita Ccr4 antagonist and medical use thereof
AU2003278727A1 (en) 2002-09-20 2004-04-08 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
US8034831B2 (en) 2002-11-06 2011-10-11 Celgene Corporation Methods for the treatment and management of myeloproliferative diseases using 4-(amino)-2-(2,6-Dioxo(3-piperidyl)-isoindoline-1,3-dione in combination with other therapies
CL2003002353A1 (es) 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
US20040099204A1 (en) 2002-11-25 2004-05-27 Nestor John J. Sheet, page, line, position marker
JP2006509000A (ja) 2002-11-26 2006-03-16 ファイザー・プロダクツ・インク 移植片拒絶反応の処置の方法
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
TW200418806A (en) 2003-01-13 2004-10-01 Fujisawa Pharmaceutical Co HDAC inhibitor
US7167750B2 (en) * 2003-02-03 2007-01-23 Enteromedics, Inc. Obesity treatment with electrically induced vagal down regulation
CA2515132C (en) * 2003-02-07 2012-01-03 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrroles 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
WO2005020921A2 (en) 2003-08-29 2005-03-10 Exelixis, Inc. C-kit modulators and methods of use
US8084457B2 (en) 2003-09-15 2011-12-27 Lead Discovery Center Gmbh Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
CA2543452C (en) 2003-10-24 2012-03-13 Santen Pharmaceutical Co., Ltd. Therapeutic agent for keratoconjunctival disorder
US7387793B2 (en) 2003-11-14 2008-06-17 Eurand, Inc. Modified release dosage forms of skeletal muscle relaxants
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
WO2005051393A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
EP1734967A2 (en) 2003-12-17 2006-12-27 Pfizer Products Incorporated Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
EP1696920B8 (en) 2003-12-19 2015-05-06 Plexxikon Inc. Compounds and methods for development of ret modulators
MXPA06007076A (es) 2003-12-19 2006-08-31 Pharmacopeia Drug Discovery Tiadiazoles como ligandos del receptor cxc y cc-quimiocina.
EP2228369A1 (en) 2003-12-23 2010-09-15 Astex Therapeutics Ltd. Pyrazole derivatives as protein kinase modulators
WO2005069865A2 (en) * 2004-01-13 2005-08-04 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
EP2332940B1 (en) 2004-03-30 2012-10-31 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
CA2563699C (en) 2004-04-23 2014-03-25 Exelixis, Inc. Kinase modulators and method of use
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
JP2007536310A (ja) 2004-05-03 2007-12-13 ノバルティス アクチエンゲゼルシャフト S1p受容体アゴニストおよびjak3キナーゼ阻害剤を含む、組合せ剤
JP2007537296A (ja) 2004-05-14 2007-12-20 アボット・ラボラトリーズ 治療薬としてのキナーゼ阻害薬
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
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
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
GB0421525D0 (en) 2004-09-28 2004-10-27 Novartis Ag Inhibitors of protein kineses
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
ES2308551T3 (es) 2004-10-13 2008-12-01 F. Hoffmann-La Roche Ag Pirazolobenzodiazepinas disustituidas utiles como inhibidores para cdk2 y angiogenesis, y para el tratamiento de cancer de mama, colon, pulmon y prostata.
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
CA2586375A1 (en) 2004-11-04 2006-05-18 Juan-Miguel Jimenez Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
US20090156602A1 (en) 2004-11-24 2009-06-18 Nigel Graham Cooke Organic Compounds
US7517870B2 (en) 2004-12-03 2009-04-14 Fondazione Telethon Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization
US20060128803A1 (en) 2004-12-14 2006-06-15 Alcon, Inc. Method of treating dry eye disorders using 13(S)-HODE and its analogs
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
WO2006067445A2 (en) 2004-12-22 2006-06-29 Astrazeneca Ab Csf-1r kinase inhibitors
JP2008528477A (ja) 2005-01-20 2008-07-31 ファイザー・リミテッド 化合物
MX2007009429A (es) * 2005-02-03 2008-03-18 Vertex Pharma Pirrolopirimidinas utiles como inhibidores de proteinas cinasas.
US7683171B2 (en) 2005-02-04 2010-03-23 Bristol-Myers Squibb Company 1H-imidazo[4,5-d]thieno[3,2-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
MX2007011316A (es) 2005-03-15 2007-11-12 Irm Llc Compuestos y composiciones como inhibidores de cinasa de proteina.
WO2006108103A1 (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
EP2354140A1 (en) * 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
NZ565255A (en) 2005-06-22 2010-04-30 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
CA2621261C (en) * 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
SG151327A1 (en) 2005-09-30 2009-04-30 Vertex Pharmaceuticals Incopor 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
DK1937664T3 (da) 2005-10-14 2011-07-18 Sumitomo Chemical Co Hydrazidforbindelse og pesticid anvendelse af den samme
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
US7528143B2 (en) 2005-11-01 2009-05-05 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
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
UA98449C2 (en) 2005-12-13 2012-05-25 Инсайт Корпорейшин 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
KR20080083680A (ko) 2005-12-23 2008-09-18 스미스클라인 비참 코포레이션 오로라 키나제의 아자인돌 억제제
JP4643455B2 (ja) 2006-01-12 2011-03-02 株式会社ユニバーサルエンターテインメント 遊技システム
RU2453548C2 (ru) 2006-01-17 2012-06-20 Вертекс Фармасьютикалз Инкорпорейтед Азаиндолы, полезные в качестве ингибиторов янус-киназ
US20070208053A1 (en) 2006-01-19 2007-09-06 Arnold Lee D 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
US20070202172A1 (en) 2006-02-24 2007-08-30 Tomer Gold Metoprolol succinate E.R. tablets and methods for their preparation
BRPI0708731A2 (pt) 2006-03-10 2011-06-07 Ono Pharmaceutical Co derivado heterocìclico nitrogenado, e agente farmacêutico compreendendo o derivado como ingrediente ativo
PL2003132T3 (pl) 2006-04-03 2014-10-31 Astellas Pharma Inc Pochodne oksadiazolu jako agoniści S1P1
CA2648250A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
EP2059515A2 (en) 2006-04-12 2009-05-20 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
CA2652751A1 (en) 2006-05-18 2007-11-29 Bayer Healthcare Ag 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
TWI398252B (zh) 2006-05-26 2013-06-11 Novartis Ag 吡咯并嘧啶化合物及其用途
NZ573174A (en) 2006-06-01 2012-01-12 Msd Consumer Care Inc Sustained release pharmaceutical dosage form containing phenylephrine
EP2044061A2 (en) 2006-07-20 2009-04-08 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
WO2008022164A2 (en) 2006-08-16 2008-02-21 Boehringer Ingelheim International Gmbh Pyrazine compounds, their use and methods of preparation
AR062677A1 (es) 2006-09-08 2008-11-26 Novartis Ag Derivados de biaril-sulfonamida, procesos de produccion y composiciones farmaceuticas que los comprenden
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
CL2007002866A1 (es) 2006-10-04 2008-07-04 Pharmacopeia Inc Compuestos derivados de 6-sustituidos-2-(bencimidazolil) purina y purinona; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto en el tratamiento de enfermedades autoinmunes, enfermedad inflamatoria, enfermedad mediada por m
AR063141A1 (es) 2006-10-04 2008-12-30 Pharmacopeia Inc Derivados de 2- ( benzimidazolil ) purina 8- sustituida para inmunosupresion
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
SG176461A1 (en) 2006-11-06 2011-12-29 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
AU2007323725B2 (en) 2006-11-22 2014-02-20 Incyte Holdings Corporation Imidazotriazines and imidazopyrimidines as kinase inhibitors
WO2008067119A2 (en) 2006-11-27 2008-06-05 Smithkline Beecham Corporation Novel compounds
NZ577111A (en) 2006-12-15 2012-05-25 Abbott Lab Novel oxadiazole compounds
AU2007338793B2 (en) 2006-12-20 2012-05-03 Amgen Inc. Heterocyclic compounds and their use in treating inflammation, angiogenesis and cancer
AU2007338792B2 (en) 2006-12-20 2012-05-31 Amgen Inc. Substituted heterocycles and methods of use
BRPI0720434A2 (pt) 2006-12-22 2014-01-07 Sigma Tau Ind Farmaceuti Gel útil para liberação de fármacos oftálmicos
US8513270B2 (en) * 2006-12-22 2013-08-20 Incyte Corporation Substituted heterocycles as Janus kinase inhibitors
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
WO2008082840A1 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008106692A1 (en) 2007-03-01 2008-09-04 Novartis Vaccines And Diagnostics, Inc. Pim kinase inhibitors and methods of their use
UA101611C2 (ru) 2007-04-03 2013-04-25 Аррей Байофарма Инк. СОЕДИНЕНИЯ ИМИДАЗО[1,2-а]ПИРИДИНА КАК ИНГИБИТОРЫ ТИРОЗИНКИНАЗЫ РЕЦЕПТОРОВ
US8188178B2 (en) 2007-05-07 2012-05-29 3M Innovative Properties Company Cold shrinkable article including an epichlorohydrin composition
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
JP5603770B2 (ja) 2007-05-31 2014-10-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr2受容体拮抗薬およびその使用
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
RS53245B2 (sr) 2007-06-13 2022-10-31 Incyte Holdings Corp Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila
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.
CN101743009A (zh) 2007-07-11 2010-06-16 辉瑞大药厂 治疗干眼病的药物组合物和方法
CA2695114A1 (en) 2007-08-01 2009-02-05 Pfizer Inc. Pyrazole compounds and their use as raf inhibitors
WO2009049028A1 (en) 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
CA2743756A1 (en) 2007-11-15 2009-05-22 Musc Foundation For Research Development Inhibitors of pim protein kinases, compositions, and methods for treating 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
PL3133080T3 (pl) 2008-01-18 2018-12-31 Inst Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Nowe cytostatyczne nukleozydy 7-deazapurynowe
KR20100115789A (ko) 2008-02-04 2010-10-28 머큐리 테라퓨틱스, 인코포레이티드 Ampk 조절자
UY31679A1 (es) 2008-03-03 2009-09-30 Inhibidores de cinasa pim y metodos para su uso
JP5275371B2 (ja) 2008-03-11 2013-08-28 インサイト・コーポレイション Jak阻害剤としてのアゼチジン誘導体およびシクロブタン誘導体
KR101408517B1 (ko) 2008-03-21 2014-06-17 노파르티스 아게 신규한 헤테로시클릭 화합물 및 그의 용도
AU2009260389A1 (en) 2008-06-18 2009-12-23 Merck Sharp & Dohme Corp. Inhibitors of Janus kinases
BRPI0914630A2 (pt) 2008-06-26 2019-09-24 Anterios Inc liberação dérmica
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
TWI496779B (zh) 2008-08-19 2015-08-21 Array Biopharma Inc 作為pim激酶抑制劑之三唑吡啶化合物
US8557809B2 (en) 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
BRPI0917459B1 (pt) 2008-08-20 2017-09-12 Zoetis Services Llc N-methyl-1- [trans-4- [methyl (7h-pyrrol [2,3-d] pyridol [2,3-d] pyrimidine compounds, use of these in therapy and crystalline a form of n-methyl- pyrimidin-4-yl) amino] cyclohexyl} methanosulphonamide
EP2344474B1 (en) 2008-09-02 2015-09-23 Novartis AG Picolinamide derivatives as kinase inhibitors
MX2011002362A (es) 2008-09-02 2011-04-04 Novartis Ag Inhibidores heterociclicos de cinasa pim.
EP2342190A1 (en) 2008-09-02 2011-07-13 Novartis AG Bicyclic kinase inhibitors
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
WO2010043052A1 (en) 2008-10-17 2010-04-22 Merck Frosst Canada Ltd. Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
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
LT2432472T (lt) 2009-05-22 2020-02-10 Incyte Holdings Corporation 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai
BRPI1012159B1 (pt) 2009-05-22 2022-01-25 Incyte Holdings Corporation Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos
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
EP2470534A4 (en) 2009-08-24 2013-02-27 Merck Sharp & Dohme INHIBITION OF JAK BLOCKES TOXICITIES ASSOCIATED WITH INTERFERENCE RNA
TW201111385A (en) 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
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
JP5946768B2 (ja) 2009-10-09 2016-07-06 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation 3−(4−(7H−ピロロ[2,3−d]ピリミジン−4−イル)−1H−ピラゾール−1−イル)−3−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体
BR112012009327A2 (pt) 2009-10-20 2017-06-06 Cellzome Ltd análogos de heterociclil pirazolopirimidina como inibidores de jak
US20110113416A1 (en) 2009-11-09 2011-05-12 Bank Of America Corporation Network-Enhanced Control Of Software Updates Received Via Removable Computer-Readable Medium
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
WO2011066374A2 (en) 2009-11-24 2011-06-03 Alder Biopharmaceuticals, Inc. Antagonists of il-6 to prevent or treat cachexia, weakness, fatigue, and/or fever
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
ES2461967T3 (es) 2009-12-18 2014-05-21 Pfizer Inc. Compuestos de pirrolo[2,3-d]pirimidina
TW201129565A (en) 2010-01-12 2011-09-01 Hoffmann La Roche Tricyclic heterocyclic compounds, compositions and methods of use thereof
AU2011213198B2 (en) 2010-02-05 2014-04-24 Zoetis Llc Pyrrolo [ 2,3-d] pyrimidine urea compounds as JAK inhibitors
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
CA2790070C (en) 2010-02-18 2018-03-06 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
AU2011224484A1 (en) 2010-03-10 2012-09-27 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
AU2011240808B2 (en) 2010-04-14 2015-01-22 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
CN103002875B (zh) 2010-05-21 2016-05-04 因塞特控股公司 Jak抑制剂的局部用制剂
WO2011156698A2 (en) 2010-06-11 2011-12-15 Abbott Laboratories NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
US9351943B2 (en) 2010-07-01 2016-05-31 Matthew T. McLeay Anti-fibroblastic fluorochemical emulsion therapies
US20130252917A1 (en) 2010-09-30 2013-09-26 Portola Pharmaceuticals, Inc. Combination therapy of 4-(3-(2h-1,2,3-triazo-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide and fludarabine
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
CN103370068A (zh) 2010-12-03 2013-10-23 Ym生物科学澳大利亚私人有限公司 Jak-2 介导的病症的治疗
CN103732226B (zh) 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
CN102247368B (zh) 2011-05-19 2013-05-29 安徽永生堂药业有限责任公司 一种复方阿伐斯汀缓释片及其制备方法
CN102218042A (zh) 2011-05-26 2011-10-19 青岛黄海制药有限责任公司 富马酸喹硫平组合物的缓释片剂及其制备方法
AR086983A1 (es) 2011-06-20 2014-02-05 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
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
EP2741747A1 (en) 2011-08-10 2014-06-18 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
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
US10155987B2 (en) 2012-06-12 2018-12-18 Dana-Farber Cancer Institute, Inc. Methods of predicting resistance to JAK inhibitor therapy
AU2013274030B2 (en) 2012-06-15 2016-07-07 Sun Pharmaceutical Industries, Inc. Deuterated derivatives of ruxolitinib
EA201590272A1 (ru) 2012-07-27 2015-05-29 Рациофарм Гмбх Пероральные дозированные формы для модифицированного высвобождения, содержащие руксолитиниб
CN102772384A (zh) 2012-08-07 2012-11-14 四川百利药业有限责任公司 一种盐酸米诺环素缓释片及其制备方法
JP2015526520A (ja) 2012-08-31 2015-09-10 プリンシピア バイオファーマ インコーポレイテッド Itk阻害剤としてのベンズイミダゾール誘導体
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
MY191357A (en) 2012-11-15 2022-06-19 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
UA120162C2 (uk) 2013-03-06 2019-10-25 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки при отриманні інгібітора jak
TWI719401B (zh) 2013-05-17 2021-02-21 美商英塞特公司 作為jak抑制劑之聯吡唑衍生物
PT3030227T (pt) 2013-08-07 2020-06-25 Incyte Corp Formas de dosagem de libertação prolongada para um inibidor de jak1
CN105555313A (zh) 2013-08-20 2016-05-04 因赛特公司 在c-反应蛋白水平较高的实体肿瘤患者中的存活益处
EA201691745A1 (ru) 2014-02-28 2016-12-30 Инсайт Корпорейшн Ингибиторы jak1 для лечения миелодиспластических синдромов
PL3129021T3 (pl) 2014-04-08 2021-05-31 Incyte Corporation Leczenie nowotworów złośliwych z komórek b za pomocą skojarzenia inhibitora jak i pi3k
WO2015168246A1 (en) 2014-04-30 2015-11-05 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
EP4233870A3 (en) 2014-05-28 2024-01-24 Onco Tracker, Inc. Anti-cancer effects of jak2 inhibitors in combination with thalidomide derivatives and glucocorticoids
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
US10766900B2 (en) 2017-12-29 2020-09-08 Formosa Laboratories, Inc. Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof
WO2020163653A1 (en) 2019-02-06 2020-08-13 Concert Pharmaceuticals, Inc. Process for preparing enantiomerically enriched jak inhibitors

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2563644C2 (ru) * 2010-08-20 2015-09-20 Хатчисон Медифарма Лимитед Пирролопиримидиновые соединения и их применения
RU2701206C2 (ru) * 2014-12-16 2019-09-25 Центаурус Биофарма Ко., Лтд. Пирролопиримидиновое соединение

Also Published As

Publication number Publication date
PL1966202T3 (pl) 2012-02-29
CY2017015I1 (el) 2017-09-13
US9662335B2 (en) 2017-05-30
FR13C0007I2 (fr) 2014-03-07
EP2348023A1 (en) 2011-07-27
CA2632466C (en) 2013-09-24
EP2348023B1 (en) 2015-05-06
ME01312B (me) 2013-12-20
CR20130506A (es) 2013-10-30
EA036785B1 (ru) 2020-12-21
HRP20170200T1 (hr) 2017-04-07
SI1966202T1 (sl) 2012-01-31
CN103214483A (zh) 2013-07-24
EP2343299B1 (en) 2015-11-04
DK2455382T3 (da) 2017-01-02
CN103214484B (zh) 2016-07-06
SI2455382T1 (sl) 2017-03-31
IL231992A (en) 2016-11-30
EP3838903B1 (en) 2023-11-22
FR13C0007I1 (fr) 2013-01-03
EP2343299B9 (en) 2017-03-08
HRP20160112T1 (hr) 2016-02-26
EP3184526A1 (en) 2017-06-28
EA201691294A2 (ru) 2018-11-30
JP2011252024A (ja) 2011-12-15
RS58113B1 (sr) 2019-02-28
US8933086B2 (en) 2015-01-13
KR20080079677A (ko) 2008-09-01
EP2455382A1 (en) 2012-05-23
SI3184526T1 (sl) 2019-03-29
US8415362B2 (en) 2013-04-09
MY159449A (en) 2017-01-13
HRP20170090T1 (hr) 2017-03-24
US8530485B2 (en) 2013-09-10
HRP20170162T1 (hr) 2017-03-24
DK3184526T3 (en) 2019-01-14
LT3184526T (lt) 2019-02-25
EP2343298A1 (en) 2011-07-13
EP3466953B1 (en) 2021-02-03
FR17C1013I1 (fr) 2017-06-02
HUE028588T2 (hu) 2016-12-28
HUE030418T2 (en) 2017-05-29
PT3184526T (pt) 2018-12-19
SI2348023T1 (sl) 2015-10-30
TW201240663A (en) 2012-10-16
HK1160115A1 (zh) 2012-08-10
LT2474545T (lt) 2017-02-27
RS55632B1 (sr) 2017-06-30
TW201522344A (zh) 2015-06-16
CN103214484A (zh) 2013-07-24
CY1116574T1 (el) 2018-03-07
LT2426129T (lt) 2017-02-10
KR101391900B1 (ko) 2014-05-02
WO2007070514A1 (en) 2007-06-21
US20090181959A1 (en) 2009-07-16
PL3184526T3 (pl) 2019-04-30
CY2013006I1 (el) 2015-10-07
US9079912B2 (en) 2015-07-14
HRP20150837T1 (hr) 2015-09-11
DK1966202T3 (da) 2012-01-16
EA201200132A8 (ru) 2018-10-31
DK2426129T3 (en) 2017-01-16
EP2426129B1 (en) 2016-11-02
BRPI0619817A2 (pt) 2011-11-22
TW201704235A (zh) 2017-02-01
TWI664182B (zh) 2019-07-01
US20070135461A1 (en) 2007-06-14
PT2474545T (pt) 2017-02-14
RS54683B1 (en) 2016-08-31
US20100022522A1 (en) 2010-01-28
JP2014051531A (ja) 2014-03-20
US11331320B2 (en) 2022-05-17
US20160346286A1 (en) 2016-12-01
US20110223210A1 (en) 2011-09-15
EP3184526B1 (en) 2018-10-03
EP2426129A1 (en) 2012-03-07
PT1966202E (pt) 2012-01-03
UA116187C2 (uk) 2018-02-26
CY1118724T1 (el) 2017-07-12
KR101218214B1 (ko) 2013-01-04
AR057995A1 (es) 2008-01-09
KR20120120462A (ko) 2012-11-01
US10398699B2 (en) 2019-09-03
KR20120120463A (ko) 2012-11-01
IL248938A0 (en) 2017-01-31
MX346183B (es) 2017-03-10
TW201434835A (zh) 2014-09-16
NZ569015A (en) 2011-06-30
ATE525374T1 (de) 2011-10-15
TWI630207B (zh) 2018-07-21
JP5876026B2 (ja) 2016-03-02
CY2013006I2 (el) 2015-10-07
HUS1700017I1 (hu) 2017-05-29
CR10065A (es) 2008-07-10
ES2612489T3 (es) 2017-05-17
ES2543904T9 (es) 2017-05-29
US11744832B2 (en) 2023-09-05
CY1118506T1 (el) 2017-07-12
LU92137I2 (fr) 2014-01-18
AU2006326548B2 (en) 2012-04-05
US20150238492A1 (en) 2015-08-27
KR101324737B1 (ko) 2013-11-05
BRPI0619817A8 (pt) 2018-01-23
TW200728275A (en) 2007-08-01
US20200338077A1 (en) 2020-10-29
HUE025173T2 (hu) 2016-01-28
KR20110137406A (ko) 2011-12-22
DK2474545T3 (en) 2017-01-23
RS55634B1 (sr) 2017-06-30
JP2015193641A (ja) 2015-11-05
BRPI0619817B8 (pt) 2021-05-25
EP2474545A1 (en) 2012-07-11
ECSP12008540A (es) 2012-04-30
JP2009519340A (ja) 2009-05-14
EP2474545B1 (en) 2016-11-09
US20180338978A1 (en) 2018-11-29
CA2632466A1 (en) 2007-06-21
US20170071947A1 (en) 2017-03-16
LT2455382T (lt) 2017-02-10
US20110224157A1 (en) 2011-09-15
JP5710430B2 (ja) 2015-04-30
CN103254190A (zh) 2013-08-21
RS55576B1 (sr) 2017-05-31
US9206187B2 (en) 2015-12-08
US9974790B2 (en) 2018-05-22
US8541425B2 (en) 2013-09-24
ES2612196T3 (es) 2017-05-12
HRP20110903T1 (hr) 2012-01-31
ES2561507T3 (es) 2016-02-26
LTPA2017012I1 (lt) 2017-05-10
US20140018374A1 (en) 2014-01-16
US8946245B2 (en) 2015-02-03
CY1118607T1 (el) 2017-07-12
DK2348023T3 (da) 2015-06-22
US10639310B2 (en) 2020-05-05
HRP20181912T1 (hr) 2019-03-22
PT2343299E (pt) 2016-02-26
ES2970354T3 (es) 2024-05-28
PL2343299T3 (pl) 2016-09-30
ES2611588T3 (es) 2017-05-09
SI2474545T1 (sl) 2017-03-31
US9814722B2 (en) 2017-11-14
SG179430A1 (en) 2012-04-27
US20140005210A1 (en) 2014-01-02
PL2455382T3 (pl) 2017-04-28
RS52101B (en) 2012-06-30
CN103214483B (zh) 2014-12-17
ES2543903T3 (es) 2015-08-25
HUE041382T2 (hu) 2019-05-28
HK1171023A1 (zh) 2013-03-15
NZ778831A (en) 2022-12-23
US20220395506A1 (en) 2022-12-15
PT2426129T (pt) 2017-02-10
IL231992A0 (en) 2014-05-28
HK1124840A1 (en) 2009-07-24
BRPI0619817B1 (pt) 2020-03-17
TWI553008B (zh) 2016-10-11
US7598257B2 (en) 2009-10-06
LU92137I9 (ru) 2019-01-04
EP1966202B1 (en) 2011-09-21
US20160272648A1 (en) 2016-09-22
CY2017015I2 (el) 2017-09-13
EA201200132A1 (ru) 2017-01-30
DK2343299T3 (en) 2016-01-18
CY1112762T1 (el) 2015-10-07
EP3466953A1 (en) 2019-04-10
HUE032337T2 (en) 2017-09-28
JP6138865B2 (ja) 2017-05-31
TWI410407B (zh) 2013-10-01
ECSP088540A (es) 2008-07-30
HRP20150837T2 (hr) 2017-04-07
ES2543904T3 (es) 2015-08-25
EP3838903A1 (en) 2021-06-23
SG10202003901UA (en) 2020-05-28
EP2343298B9 (en) 2020-05-06
PT2455382T (pt) 2017-01-31
EP1966202A1 (en) 2008-09-10
DK2348023T5 (da) 2017-05-15
PL2426129T3 (pl) 2017-04-28
ZA200805165B (en) 2012-05-30
HK1160111A1 (en) 2012-08-10
HK1160137A1 (en) 2012-08-10
US20140243360A1 (en) 2014-08-28
CN103254190B (zh) 2016-12-07
IL192019A (en) 2014-04-30
PL2474545T3 (pl) 2017-04-28
JP5017278B2 (ja) 2012-09-05
TWI468162B (zh) 2015-01-11
EP2343298B1 (en) 2015-05-06
RS54181B9 (sr) 2020-01-31
EA035795B1 (ru) 2020-08-11
SG10201506912RA (en) 2015-10-29
PL2348023T3 (pl) 2015-11-30
ES2373688T3 (es) 2012-02-07
ES2700433T3 (es) 2019-02-15
FR17C1013I2 (fr) 2018-05-04
SI2343299T1 (sl) 2016-06-30
EP2343299A1 (en) 2011-07-13
EP2455382B1 (en) 2016-10-26
IL192019A0 (en) 2008-12-29
EP2348023B9 (en) 2017-03-08
MY162590A (en) 2017-06-30
AU2006326548A1 (en) 2007-06-21
UA98449C2 (en) 2012-05-25
SI2426129T1 (sl) 2017-02-28
HUE030235T2 (en) 2017-04-28
RS54181B1 (en) 2015-12-31
CN101448826A (zh) 2009-06-03
EA019504B1 (ru) 2014-04-30
CY1121202T1 (el) 2020-05-29
TW201831490A (zh) 2018-09-01
KR101216055B1 (ko) 2012-12-27
PT2348023E (pt) 2015-09-15
US20190125750A1 (en) 2019-05-02
ES2867505T3 (es) 2021-10-20

Similar Documents

Publication Publication Date Title
EA200870048A1 (ru) ГЕТЕРОАРИЛ-ЗЕМЕЩЕННЫЕ ПИРРОЛО[2,3-b]ПИРИДИНЫ И ПИРРОЛО[2,3-b]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ
UA104849C2 (ru) 4-пиразолил-n-арилпиримидин-2-амины и 4-пиразолил-n-гетероарилпиримидин-2-амины как ингибиторы киназ janus
UA95244C2 (ru) Соединения и способ модулирования активности киназ, и показания для их применения
TW200634010A (en) Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-4-yl-amines as janus kinase inhibitors
MX2009012623A (es) Moduladores de cinasa heterociclicos.
MX2009006688A (es) Compuestos y metodos para modulacion de cinasas, e indicaciones para ello.
MX2009006162A (es) Compuestos y metodos para modulacion de cinasas, e indicaciones para ello.
EA201070013A1 (ru) СОЛИ ИНГИБИТОРА ЯНУС-КИНАЗЫ (R)-3-(4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1H-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
TN2009000142A1 (en) Bicyclic triazoles as protein kinase modulators
TW200801008A (en) Protein kinase inhibitors
UA98297C2 (en) Triazolopyridazines as tyrosine kinase modulators
EA200970402A1 (ru) Триазолопиридазиновые модуляторы протеинкиназ
EA200970738A1 (ru) Ингибиторы активности akt
ATE517901T1 (de) Pyrazolopyrimidine als hemmer der proteinkinase b (akt)
BRPI0510177A (pt) heterociclos monocìclicos como inibidores de cinase
BRPI0511111A (pt) compostos de pirrol como inibidores de cinase de proteìna de erk, sua sìntese e seus intermediários
EA201171454A1 (ru) N-(ГЕТЕРО)АРИЛПИРРОЛИДИНОВЫЕ ПРОИЗВОДНЫЕ ПИРАЗОЛ-4-ИЛПИРРОЛО[2,3-d]ПИРИМИДИНОВ И ПИРРОЛ-3-ИЛПИРРОЛО[2,3-d]ПИРИМИДИНОВ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ
MX2009012079A (es) Compuestos heterociclicos condensados como inhibidores de proteina cinasas.
DE50308230D1 (de) Pyrazoloisoquinolinenderivaten zur inhibierung von nfkappab-induzierende kinase
EA202091617A1 (ru) Гетероарил-замещенные пирроло[2,3-b]пиридины и пирроло[2,3-b]пиримидины в качестве ингибиторов янус-киназы
TW200602023A (en) Monocyclic heterocycles as kinase inhibitors
TW200801020A (en) Improved methods for preparing benzofused heteroaryl amide derivatives of thienopyridines

Legal Events

Date Code Title Description
ND4A Extension of term of a eurasian patent
ND4A Extension of term of a eurasian patent
PC4A Registration of transfer of a eurasian patent by assignment
ND4A Extension of term of a eurasian patent