AR070828A1 - Derivados de azetidina y ciclobutano como inhibidores de jak - Google Patents

Derivados de azetidina y ciclobutano como inhibidores de jak

Info

Publication number
AR070828A1
AR070828A1 ARP090100869A ARP090100869A AR070828A1 AR 070828 A1 AR070828 A1 AR 070828A1 AR P090100869 A ARP090100869 A AR P090100869A AR P090100869 A ARP090100869 A AR P090100869A AR 070828 A1 AR070828 A1 AR 070828A1
Authority
AR
Argentina
Prior art keywords
alkyl
phenyl
heteroaryl
optionally substituted
azetidine
Prior art date
Application number
ARP090100869A
Other languages
English (en)
Inventor
James D Rodgers
David Meloni
Stacey Shepard
Yun-Long Li
Pingli Liu
Michael Xia
Jiacheng Zhou
Original Assignee
Incyte Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40591836&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR070828(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of AR070828A1 publication Critical patent/AR070828A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B60—VEHICLES IN GENERAL
    • B60Q—ARRANGEMENT OF SIGNALLING OR LIGHTING DEVICES, THE MOUNTING OR SUPPORTING THEREOF OR CIRCUITS THEREFOR, FOR VEHICLES IN GENERAL
    • B60Q3/00—Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors
    • B60Q3/70—Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors characterised by the purpose
    • B60Q3/76—Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors characterised by the purpose for spotlighting, e.g. reading lamps
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B60—VEHICLES IN GENERAL
    • B60Q—ARRANGEMENT OF SIGNALLING OR LIGHTING DEVICES, THE MOUNTING OR SUPPORTING THEREOF OR CIRCUITS THEREFOR, FOR VEHICLES IN GENERAL
    • B60Q3/00—Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors
    • B60Q3/80—Circuits; Control arrangements
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S362/00—Illumination
    • Y10S362/80—Light emitting diode
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S362/00—Illumination
    • Y10S362/802—Position or condition responsive switch

Abstract

La presente se relaciona con derivados de azetidina y ciclobutano, así como sus composiciones, métodos de uso, y procesos para su preparacion, los cuales son inhibidores de JAK utiles en el tratamiento de enfermedades asociadas a JAK incluyendo, por ejemplo, desordenes inflamatorios y autoinmunes, así como cáncer. Reivindicacion 1: Un compuesto de formula 1 o una sal farmacéuticamente aceptable del mismo, caracterizado por que: L es SO2 o CO; R1 es alquilo C1-6, cicloalquilo C3-7, fenilo, heteroarilo de 5 o 6 miembros, indolilo, NR2R3, o OR4, donde dicho alquilo, cicloalquilo, fenilo, o heteroarilo está opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados independientemente de entre F, CN, y alquilo C1-4; R2 y R3 son seleccionados independientemente de entre H, alquilo C1-4, y fenilo; y R4 es alquilo C1-6, fenilo, o bencilo; y por que cuando L es SO2, R1 es diferente de OR4. Reivindicacion 18: Un compuesto de formula 2 una sal farmacéuticamente aceptable del mismo, caracterizado por que: R5 y R6 son seleccionados independientemente de entre H, F, CN, OH, alquilo C1-4, benciloxi, dialquilaminosulfonilo C2-8, y heteroarilo de 5 miembros, donde dicho alquilo es opcionalmente sustituido por 1, 2, o 3 sustituyentes seleccionados de entre F, OH, CN, y alcoxi C1-4, y donde dicho heteroarilo de 5 miembros está opcionalmente sustituido con alquilo C1-4, y por que cuando uno de R5 y R6 es OH, entonces el otro entre R5 y R6 es diferente de CN o F.
ARP090100869A 2008-03-11 2009-03-11 Derivados de azetidina y ciclobutano como inhibidores de jak AR070828A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3566208P 2008-03-11 2008-03-11
US14498209P 2009-01-15 2009-01-15

Publications (1)

Publication Number Publication Date
AR070828A1 true AR070828A1 (es) 2010-05-05

Family

ID=40591836

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090100869A AR070828A1 (es) 2008-03-11 2009-03-11 Derivados de azetidina y ciclobutano como inhibidores de jak

Country Status (44)

Country Link
US (3) US8158616B2 (es)
EP (1) EP2288610B8 (es)
JP (2) JP5275371B2 (es)
KR (2) KR20120108042A (es)
CN (2) CN102026999B (es)
AR (1) AR070828A1 (es)
AU (1) AU2009223640B2 (es)
BR (1) BRPI0909040B8 (es)
CA (1) CA2718271C (es)
CL (1) CL2009000576A1 (es)
CO (1) CO6290658A2 (es)
CY (2) CY1118176T1 (es)
DK (1) DK2288610T3 (es)
DO (2) DOP2010000270A (es)
EA (1) EA017218B1 (es)
EC (1) ECSP10010475A (es)
ES (1) ES2602577T3 (es)
HK (1) HK1149005A1 (es)
HN (1) HN2010001761A (es)
HR (1) HRP20161390T1 (es)
HU (2) HUE029767T2 (es)
IL (1) IL208023A (es)
LT (2) LT2288610T (es)
LU (1) LUC00027I2 (es)
MA (1) MA32219B1 (es)
MX (1) MX2010010012A (es)
MY (1) MY165582A (es)
NL (1) NL300886I2 (es)
NO (1) NO2017033I1 (es)
NZ (1) NZ587928A (es)
PA (1) PA8819201A1 (es)
PE (2) PE20140099A1 (es)
PL (1) PL2288610T3 (es)
PT (1) PT2288610T (es)
RS (1) RS55263B1 (es)
SG (1) SG191660A1 (es)
SI (1) SI2288610T1 (es)
SV (1) SV2010003662A (es)
TN (1) TN2010000415A1 (es)
TW (1) TWI444382B (es)
UA (1) UA101493C2 (es)
UY (1) UY31705A1 (es)
WO (1) WO2009114512A1 (es)
ZA (1) ZA201006000B (es)

Families Citing this family (270)

* 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
WO2007070514A1 (en) * 2005-12-13 2007-06-21 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
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.
RS58449B1 (sr) 2007-06-13 2019-04-30 Incyte Holdings Corp Upotreba soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h- pirazol-1-il)-3-ciklopentilpropionitrila
AU2008321046B2 (en) * 2007-11-16 2013-10-24 Incyte Holdings Corporation 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
TWI443098B (zh) 2008-03-24 2014-07-01 Medivation Technologies Inc 吡啶并〔３，４－ｂ〕吲哚及使用方法
KR20110031475A (ko) * 2008-06-20 2011-03-28 제넨테크, 인크. 트리아졸로피리딘 ｊａｋ 억제제 화합물 및 방법
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.
JOP20190231A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
AU2010249380B2 (en) 2009-05-22 2015-08-20 Incyte Holdings Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as Janus kinase inhibitors
EP3643312A1 (en) 2009-05-22 2020-04-29 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak 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
KR20180126619A (ko) * 2009-10-09 2018-11-27 인사이트 홀딩스 코포레이션 3-（4-（7Ｈ-피롤로〔2,3-ｄ〕피리미딘-4-일）-1Ｈ-피라졸-1-일）-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체
BR112012020693B1 (pt) * 2010-02-18 2020-05-12 Incyte Holdings Corporation Derivados de ciclobutano e metilciclobutano como inibidores de janus quinase e composição que os compreende
AU2015205858B2 (en) * 2010-03-10 2017-04-13 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
CN102985417B (zh) * 2010-03-10 2015-01-28 因塞特公司 作为jak1抑制剂的哌啶-4-基氮杂环丁烷衍生物
UA109131C2 (ru) 2010-04-14 2015-07-27 Еррей Біофарма Інк. 5,7-ЗАМЕЩЕННЫЕ ИМИДАЗО[1,2-c]ПИРИМИДИНЫ КАК ИНГИБИТОРЫ JAK-КИНАЗ
EA035981B1 (ru) 2010-05-21 2020-09-09 Инсайт Холдингс Корпорейшн Композиция ингибитора jak для местного применения
TW201249845A (en) 2010-11-19 2012-12-16 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
EA036970B1 (ru) * 2010-11-19 2021-01-21 Инсайт Холдингс Корпорейшн Применение {1-{1-[3-фтор-2-(трифтометил)изоникотиноил] пиперидин-4-ил}-3-[4-(7h-пирроло[2,3-d]пиримидин-4-ил)-1н-пиразол-1-ил]азетидин-3-ил}ацетонитрила для лечения заболеваний, связанных с активностью jak1
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
KR20130121857A (ko) * 2010-12-01 2013-11-06 닛산 가가쿠 고교 가부시키 가이샤 다발성 골수종의 치료 효과를 갖는 피라졸 화합물
JP2014505738A (ja) 2011-02-18 2014-03-06 メディベイション テクノロジーズ， インコーポレイテッド 高血圧を処置するための化合物および方法
EP2675451B9 (en) 2011-02-18 2017-07-26 Novartis Pharma AG mTOR/JAK INHIBITOR COMBINATION THERAPY
MX341089B (es) * 2011-03-08 2016-08-08 Ge Healthcare Ltd Preparacion de un derivado de acido 1-amaino-3-hidroxi-ciclobutan- 1-carboxilico.
WO2012177606A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
US9358229B2 (en) 2011-08-10 2016-06-07 Novartis Pharma Ag JAK PI3K/mTOR combination therapy
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
CA2849357A1 (en) * 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Acyclic cyanoethylpyrazoles as janus kinase inhibitors
EP3750544A3 (en) 2011-11-30 2021-03-24 Emory University Jak inhibitors for use in the prevention or treatment of viral infection
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
KR102427777B1 (ko) 2012-06-26 2022-08-01 델 마 파마슈티컬스 디안하이드로갈락티톨, 디아세틸디안하이드로갈락티톨, 디브로모둘시톨, 또는 그의 유사체 또는 유도체를 이용하여 유전학적 다형성이 있는 환자에 있어서 티로신-키나아제-억제제 내성 악성종양, ahi1 조절곤란 또는 돌연변이를 치료하는 방법
ES2726833T3 (es) * 2012-08-02 2019-10-09 Nerviano Medical Sciences Srl Pirroles sustituidos activos como inhibidores de cinasas
CA2880083A1 (en) 2012-08-17 2014-02-20 Concert Pharmaceuticals, Inc. Deuterated baricitinib
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
CN113384545A (zh) 2012-11-15 2021-09-14 因赛特公司 鲁索利替尼的缓释剂型
CN103965114B (zh) * 2013-01-28 2016-01-06 苏州泽璟生物制药有限公司 氘代的苯基氨基嘧啶化合物以及包含该化合物的药物组合物
SI3489239T1 (sl) * 2013-03-06 2022-04-29 Incyte Holdings Corporation Postopki in intermediati za pripravo zaviralca JAK
WO2014146249A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
WO2014168986A1 (en) 2013-04-08 2014-10-16 Brown Dennis M Therapeutic benefit of suboptimally administered chemical compounds
ES2845210T3 (es) 2013-05-17 2021-07-26 Incyte Corp Derivados de bipirazol como inhibidores de JAK
WO2015013579A1 (en) 2013-07-26 2015-01-29 Update Pharma Inc. Compositions to improve the therapeutic benefit of bisantrene
EA201690357A1 (ru) * 2013-08-07 2016-07-29 Инсайт Корпорейшн Лекарственные формы с замедленным высвобождением для ингибитора jak1
EP3035966A1 (en) 2013-08-20 2016-06-29 Incyte Corporation Survival benefit in patients with solid tumors with elevated c-reactive protein levels
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US9670210B2 (en) 2014-02-13 2017-06-06 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
US9493442B2 (en) 2014-02-13 2016-11-15 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
ME03580B (me) 2014-02-13 2020-07-20 Incyte Corp Ciklopropilamini kao lsd1 inhibitori
WO2015131031A1 (en) 2014-02-28 2015-09-03 Incyte Corporation Jak1 inhibitors for the treatment of myelodysplastic syndromes
JP6526065B2 (ja) 2014-02-28 2019-06-05 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
WO2015145286A1 (en) * 2014-03-28 2015-10-01 Sun Pharmaceutical Industries Limited Amorphous form of baricitinib
MX2016014192A (es) 2014-04-30 2017-05-01 Incyte Corp Procesos para preparar un inhibidor de cinasas de janus 1 (jak1) y nuevas formas de este.
WO2015166434A1 (en) * 2014-05-01 2015-11-05 Sun Pharmaceutical Industries Limited Crystalline form of baricitinib
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
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
TW201618773A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑、及／或ｃｄｋ４／６抑制劑的治療組合物
PL3179991T3 (pl) 2014-08-11 2022-02-14 Acerta Pharma B.V. Kombinacje terapeutyczne inhibitora btk i inhibitora bcl-2
DK3179992T3 (da) 2014-08-11 2022-07-11 Acerta Pharma Bv Terapeutisk kombination af en btk-inhibitor, en pd-1-inhibitor og/eller en pd-l1-inhibitor
AU2015303835B2 (en) 2014-08-12 2020-04-09 Monash University Lymph directing prodrugs
TWI679205B (zh) 2014-09-02 2019-12-11 日商日本新藥股份有限公司 吡唑并噻唑化合物及醫藥
CN105524067A (zh) * 2014-09-28 2016-04-27 江苏柯菲平医药股份有限公司 4-取代吡咯并[2,3-d]嘧啶化合物及其用途
EP3227298A4 (en) * 2014-12-05 2018-05-23 Sun Pharmaceutical Industries Ltd Process for the preparation of baricitinib and an intermediate thereof
CN105777754B (zh) * 2014-12-16 2019-07-26 北京赛林泰医药技术有限公司 吡咯并嘧啶化合物
EP3253760A4 (en) * 2015-02-02 2018-06-20 Sun Pharmaceutical Industries Limited Process for the preparation of baricitinib and an intermediate thereof
US10526350B2 (en) 2015-02-02 2020-01-07 Sun Pharmaceutical Industries Limited Process for the preparation of baricitinib and an intermediate thereof
ES2930585T3 (es) 2015-02-27 2022-12-19 Nimbus Lakshmi Inc Inhibidores de TYK2 y usos de los mismos
CN105924444B (zh) * 2015-03-11 2019-06-18 苏州晶云药物科技股份有限公司 Jak抑制剂的晶型及其制备方法
US10377757B2 (en) 2015-03-11 2019-08-13 Crystal Pharmatech Co., Ltd. Crystal form of JAK inhibitor and preparation method thereof
US9944647B2 (en) 2015-04-03 2018-04-17 Incyte Corporation Heterocyclic compounds as LSD1 inhibitors
AR104918A1 (es) * 2015-06-19 2017-08-23 Lilly Co Eli Procesos e intermediarios para la preparación de {1-(etilsulfonil)-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrilo
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
US10329255B2 (en) 2015-08-12 2019-06-25 Incyte Corporation Salts of an LSD1 inhibitor
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
US11738087B2 (en) 2015-09-08 2023-08-29 Monash University Lymph directing prodrugs
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
CN106554363B (zh) * 2015-09-28 2019-03-05 正大天晴药业集团股份有限公司 一种Baricitinib中间体的制备方法
PT3364958T (pt) 2015-10-23 2023-04-10 Navitor Pharm Inc Moduladores de interação sestrina-gator2 e utilizações dos mesmos
RU2603959C1 (ru) * 2015-11-13 2016-12-10 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") ДИХЛОРАЦЕТАТ {3-[4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-ПИРАЗОЛ-1-ИЛ]-1-ЭТИЛСУЛЬФОНИЛ-АЗЕТИДИН-3-ИЛ}-АЦЕТОНИТРИЛА В КАЧЕСТВЕ ИНГИБИТОРА ЯНУС КИНАЗ
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
CN105294699B (zh) * 2015-12-04 2019-06-11 上海勋和医药科技有限公司 巴瑞替尼的制备方法
DK3360878T3 (da) 2015-12-11 2020-11-09 Sichuan Kelun Biotech Biopharmaceutica Co Ltd Azetidinderivat, fremstillingsfremgangsmåde derfor og anvendelse deraf
WO2017106352A1 (en) 2015-12-14 2017-06-22 Raze Therapeutics, Inc. Caffeine inhibitors of mthfd2 and uses thereof
HU230805B1 (hu) * 2015-12-23 2018-06-28 Egis Gyógyszergyár Zrt Eljárás és köztitermék baricitinib előállítására
HU230931B1 (hu) * 2016-01-21 2019-04-29 Egis Gyógyszergyár Zrt. Baricitinib sók
US10822339B2 (en) 2016-01-26 2020-11-03 Hangzhou Huadong Medicine Group Biopharmaceutical Co. Ltd Pyrrolopyrimidine five-membered azacyclic derivative and application thereof
CN107573348B (zh) * 2016-01-29 2019-09-03 上海宣创生物科技有限公司 巴瑞克替尼三氟乙酸盐b晶型及其制备方法
CN105601635B (zh) * 2016-02-01 2017-12-12 上海宣创生物科技有限公司 巴瑞克替尼磷酸盐的a晶型、h晶型和i晶型及其制备方法
CN105541891B (zh) * 2016-02-04 2017-11-28 东南大学 巴瑞替尼的中间体及其制备方法及由该中间体制备巴瑞替尼的方法
TWI712604B (zh) 2016-03-01 2020-12-11 日商日本新藥股份有限公司 具jak抑制作用之化合物之結晶
EP3426244B1 (en) 2016-03-09 2023-06-07 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
RS62271B1 (sr) 2016-03-09 2021-09-30 Raze Therapeutics Inc Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba
CN107200742A (zh) * 2016-03-18 2017-09-26 罗欣生物科技（上海）有限公司 一种巴瑞克替尼磷酸盐晶体及其制备方法
CN107226814A (zh) * 2016-03-23 2017-10-03 罗欣生物科技（上海）有限公司 一种巴瑞克替尼中间体的制备方法
CA3019394A1 (en) 2016-04-08 2017-10-12 X4 Pharmaceuticals, Inc. Methods for treating cancer
MA44725A (fr) 2016-04-22 2019-02-27 Incyte Corp Formulations d'un inhibiteur de lsd1
CN107334738B (zh) * 2016-04-28 2021-02-09 天津科伦药物研究有限公司 一种含巴瑞克替尼的药物组合物及其制备方法和用途
EP3808748A1 (en) 2016-06-21 2021-04-21 X4 Pharmaceuticals, Inc. Substituted piperidines as cxcr4-inhibitors
CN109641838A (zh) 2016-06-21 2019-04-16 X4 制药有限公司 Cxcr4抑制剂及其用途
WO2017223229A1 (en) 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
JP6978098B2 (ja) * 2016-07-26 2021-12-08 スーヂョウ ロングバイオテック ファーマシューティカルズ カンパニー リミテッドSuzhou Longbiotech Pharmaceuticals Co., Ltd. 選択的ｊａｋ阻害剤としての化合物、該化合物の塩類および治療への使用
CN106496233B (zh) * 2016-09-26 2018-05-15 东南大学 吡咯并嘧啶类化合物、其制备方法及其用途
CA3039202A1 (en) 2016-10-14 2018-04-19 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
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
CZ2016705A3 (cs) 2016-11-11 2018-05-23 Zentiva, K.S. Krystalické formy 2- [1-ethylsulfonyl-3- [4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) pyrazol-1-yl] azetidin-3-yl] acetonitrilových solí a jejich příprava
AU2017368050A1 (en) 2016-11-29 2019-06-20 Puretech Lyt, Inc. Exosomes for delivery of therapeutic agents
EP3327020A1 (en) 2016-11-29 2018-05-30 Sandoz Ag Citrate salts of a janus kinase (jak) inhibitor
WO2018106636A1 (en) 2016-12-05 2018-06-14 Raze Therapeutics, Inc. Shmt inhibitors and uses thereof
RU2644155C1 (ru) * 2016-12-12 2018-02-08 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") 2-(3-(4-(7H-пирроло[2,3-d]пиримидин-4-ил)-1H-пиразол-1-ил)-1-(этилсульфонил)азетидин-3-ил)ацетонитрила геминафтилдисульфонат в качестве ингибитора Янус киназ
CZ2016816A3 (cs) 2016-12-21 2018-07-04 Zentiva, K.S. Krystalické formy 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrilu s kyselinou fosforečnou a způsob jejich přípravy
US11730819B2 (en) 2016-12-23 2023-08-22 Bicycletx Limited Peptide derivatives having novel linkage structures
WO2018127699A1 (en) 2017-01-06 2018-07-12 Bicyclerd Limited Compounds for treating cancer
EA039352B1 (ru) * 2017-01-19 2022-01-17 Сучжоу Лонгбайотек Фармасьютикалз Ко., Лтд. Соединение в качестве селективного ингибитора jak и его соли и терапевтическое применение
CA3055233C (en) * 2017-01-23 2022-08-09 Shanghai Longwood Biopharmaceuticals Co., Ltd. Jak kinase inhibitor and preparation method and use thereof
EP4338802A2 (en) 2017-03-08 2024-03-20 Takeda Pharmaceutical Company Limited Tyk2 inhibitors, uses, and methods for production thereof
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
CN106946917B (zh) * 2017-03-20 2019-06-11 杭州科巢生物科技有限公司 一种jak抑制剂巴瑞替尼及其中间体的新合成方法
CN107176955B (zh) * 2017-03-24 2019-04-09 南京优科制药有限公司 一种巴瑞替尼的制备方法
WO2018191146A1 (en) 2017-04-10 2018-10-18 Navitor Pharmaceuticals, Inc. Heteroaryl rheb inhibitors and uses thereof
CN110809467B (zh) 2017-04-26 2023-03-10 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
BR112019024509A2 (pt) 2017-05-23 2020-06-23 Theravance Biopharma R&D Ip, Llc Glicuronídeo de pró-fármacos dos inibidores da janus quinase
CN110494435B (zh) * 2017-06-07 2022-02-15 四川科伦博泰生物医药股份有限公司 氮杂环丁烷衍生物的固体形式及其制备方法和用途
US11124517B2 (en) * 2017-06-22 2021-09-21 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of Baricitinib and preparation method thereof
US10899798B2 (en) 2017-06-26 2021-01-26 Bicyclerd Limited Bicyclic peptide ligands with detectable moieties and uses thereof
WO2019003249A1 (en) 2017-06-28 2019-01-03 Mylan Laboratories Limited POLYMORPHIC FORMS OF BARICITINIB
CN111194317A (zh) 2017-07-28 2020-05-22 林伯士拉克许米公司 Tyk2抑制剂与其用途
WO2019034866A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited BICYCLIC PEPTIDE LIGANDS CONJUGATES AND USES THEREOF
WO2019034868A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
AU2018324037A1 (en) 2017-08-29 2020-04-16 Monash University Lymphatic system-directing lipid prodrugs
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
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
CN109651424B (zh) * 2017-10-11 2021-01-22 新发药业有限公司 一种7-保护基-4-(1-氢-吡唑-4-基)吡咯[2,3-d]嘧啶的合成方法
US10738057B2 (en) 2017-10-18 2020-08-11 Incyte Corporation Tertiary alcohols as PI3K-γ inhibitors
JP2021502400A (ja) * 2017-11-03 2021-01-28 アクラリス セラピューティクス，インコーポレイテッド 置換ピロロピリミジンｊａｋ阻害剤ならびにこれを作製および使用する方法
CN113149993A (zh) * 2017-12-01 2021-07-23 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
CN108129482A (zh) * 2017-12-13 2018-06-08 江苏中邦制药有限公司 一种巴瑞替尼的制备方法
WO2019126378A1 (en) 2017-12-19 2019-06-27 Ariya Therapeutics, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
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
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
EP3502114A1 (en) 2017-12-20 2019-06-26 Sandoz AG Co-crystal of an orally available janus kinase inhibitor
BR112020012997A2 (pt) 2017-12-26 2020-12-01 Kymera Therapeutics, Inc. degradadores de irak e usos dos mesmos
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
US11485743B2 (en) 2018-01-12 2022-11-01 Kymera Therapeutics, Inc. Protein degraders and uses thereof
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
SG11202006701TA (en) 2018-01-29 2020-08-28 Merck Patent Gmbh Gcn2 inhibitors and uses thereof
CA3089769A1 (en) 2018-01-29 2019-08-01 Merck Patent Gmbh Gcn2 inhibitors and uses thereof
SI3746429T1 (sl) 2018-01-30 2023-01-31 Incyte Corporation Postopki za pripravo (1-(3-fluoro-2-(trifluorometil)izonikotinil) piperidin-4-ona)
WO2019161098A1 (en) 2018-02-16 2019-08-22 Incyte Corporation Jak1 pathway inhibitors for the treatment of cytokine-related disorders
CN112189009B (zh) 2018-02-27 2023-09-29 阿塔克斯生物制药有限公司 作为tcr-nck相互作用的抑制剂的色烯衍生物
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
JP2021519772A (ja) 2018-03-30 2021-08-12 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ 炎症性皮膚疾患のバイオマーカー
WO2019191684A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Treatment of hidradenitis suppurativa using jak inhibitors
US11372003B2 (en) 2018-04-13 2022-06-28 Incyte Corporation Biomarkers for graft-versus-host disease
HUE058746T2 (hu) 2018-04-24 2022-09-28 Merck Patent Gmbh Antiproliferációs vegyületek és felhasználásuk
WO2019209757A1 (en) 2018-04-24 2019-10-31 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
CN108752254B (zh) * 2018-05-22 2021-11-02 道合(潍坊)医药技术有限公司 2-[1-(乙基磺酰基)-3-氮杂环丁亚基]乙腈的制备方法
CN112804994A (zh) * 2018-05-25 2021-05-14 卡托斯医疗公司 治疗骨髓增殖性肿瘤的方法
JP7083203B2 (ja) * 2018-06-06 2022-06-10 ジェングル セラピューティクス，インコーポレイテッド ピラゾロピリミジン誘導体、その用途並びに医薬組成物
US10980784B2 (en) 2018-06-15 2021-04-20 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
US11180531B2 (en) 2018-06-22 2021-11-23 Bicycletx Limited Bicyclic peptide ligands specific for Nectin-4
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
WO2020010177A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Tricyclic crbn ligands and uses thereof
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
WO2020051169A1 (en) 2018-09-05 2020-03-12 Incyte Corporation Crystalline forms of a phosphoinositide 3-kinase (pi3k) inhibitor
CN109215136B (zh) 2018-09-07 2020-03-20 百度在线网络技术（北京）有限公司 一种真实数据增强方法、装置以及终端
CN109146898B (zh) 2018-09-07 2020-07-24 百度在线网络技术（北京）有限公司 一种仿真数据量增强方法、装置以及终端
EP3846793B1 (en) 2018-09-07 2024-01-24 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
WO2020072870A1 (en) 2018-10-05 2020-04-09 Johnson Matthey Public Limited Company Co-crystal forms of baricitinib
CA3115088A1 (en) 2018-10-15 2020-04-23 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
TW202033198A (zh) 2018-10-17 2020-09-16 美商美國禮來大藥廠 以巴瑞克替尼(baricitinib)治療原發性膽汁性膽管炎及原發性硬化性膽管炎
JP2022512779A (ja) 2018-10-23 2022-02-07 バイスクルテクス・リミテッド 二環式ペプチドリガンドおよびその使用
US11345654B2 (en) 2018-10-24 2022-05-31 Navitor Pharmaceuticals, Inc. Polymorphic compounds and uses thereof
MX2021004946A (es) 2018-10-31 2021-07-15 Incyte Corp Terapia combinada para tratamiento de enfermedades hematológicas.
US11053241B2 (en) 2018-11-30 2021-07-06 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
WO2020113233A1 (en) 2018-11-30 2020-06-04 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CN111320633B (zh) * 2018-12-14 2022-09-27 中国医药研究开发中心有限公司 吡咯/咪唑并六元杂芳环类化合物及其制备方法和医药用途
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
JPWO2020130125A1 (ja) 2018-12-21 2021-11-04 第一三共株式会社 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ
CA3126034A1 (en) 2019-01-23 2020-07-30 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
US20220106319A1 (en) * 2019-01-30 2022-04-07 Gargamel (Zhuhai) Biotech Ltd. Jak inhibitor and preparation method therefor
WO2020163431A1 (en) 2019-02-05 2020-08-13 Teva Pharmaceuticals International Gmbh Crystalline solid forms of baricitinib
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
WO2020173364A1 (zh) * 2019-02-27 2020-09-03 四川科伦博泰生物医药股份有限公司 以氮杂环丁烷衍生物为活性成分的口服药物组合物、其制备方法及用途
WO2020182159A1 (zh) 2019-03-14 2020-09-17 上海华汇拓医药科技有限公司 Jak激酶抑制剂及其制备方法和在医药领域的应用
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
EP3946462A1 (en) 2019-04-02 2022-02-09 BicycleTX Limited Bicycle toxin conjugates and uses thereof
SG11202110829YA (en) 2019-04-05 2021-10-28 Kymera Therapeutics Inc Stat degraders and uses thereof
EP3725305A1 (en) 2019-04-17 2020-10-21 Zentiva K.S. Pharmaceutical composition containing baricitinib hydrobromide
AU2020262100B2 (en) * 2019-04-24 2023-03-16 Elanco Us Inc. A 7H-pyrrolo[2,3-d]pyrimidine JAK-inhibitor
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
CA3141826A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CN110256441A (zh) * 2019-06-24 2019-09-20 江苏君若医药有限公司 一种巴瑞克替尼的制备方法
EP3771715A1 (en) 2019-08-02 2021-02-03 Zaklady Farmaceutyczne "Polpharma" S.A. Crystalline forms of baricitinib
EP3771716A1 (en) 2019-08-02 2021-02-03 Zaklady Farmaceutyczne "Polpharma" S.A. Low hygroscopic amorphous form of baricitinib
WO2021050992A1 (en) 2019-09-11 2021-03-18 Vincere Biosciences, Inc. Usp30 inhibitors and uses thereof
WO2021050964A1 (en) 2019-09-13 2021-03-18 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
CN110683978A (zh) * 2019-10-30 2020-01-14 西安医学院 一种3-腈基亚甲基氮杂环丁烷-1-碳酸叔丁酯的制备方法
BR112022008287A2 (pt) 2019-11-01 2022-07-26 Navitor Pharm Inc Métodos de tratamento usando um modulador de mtorc1
AU2020378630A1 (en) 2019-11-08 2022-05-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
EP4061367A1 (en) 2019-11-22 2022-09-28 Incyte Corporation Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
CA3163680A1 (en) 2019-12-05 2021-06-10 David John O'neill Rapamycin analogs and uses thereof
JP2023509366A (ja) 2019-12-17 2023-03-08 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ分解剤およびそれらの使用
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
JP2023506398A (ja) 2019-12-19 2023-02-16 リミナル・バイオサイエンシーズ・リミテッド シクロアルキル含有カルボン酸及びそれらの使用
JP2023509394A (ja) 2019-12-23 2023-03-08 カイメラ セラピューティクス， インコーポレイテッド Ｓｍａｒｃａ分解剤およびそれらの使用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
AR121506A1 (es) 2020-03-03 2022-06-08 Pic Therapeutics Inc Inhibidores del eif4e y sus usos
IL296451A (en) 2020-03-19 2022-11-01 Kymera Therapeutics Inc mdm2 joints and their uses
WO2021209563A1 (en) 2020-04-16 2021-10-21 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
CN111362853A (zh) * 2020-04-27 2020-07-03 安徽大学 一种3-氧杂氮杂环丁烷-1-羧酸叔丁酯的制备方法
TW202210471A (zh) 2020-06-02 2022-03-16 美商英塞特公司 製備ｊａｋ１抑制劑之方法
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
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
CN111704617B (zh) * 2020-06-15 2022-08-23 嘉兴特科罗生物科技有限公司 一种小分子化合物
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
CR20230057A (es) 2020-07-02 2023-08-15 Incyte Corp Compuestos tríciclicos de urea como inhibidores de jak2 v617f
CN111999400B (zh) * 2020-07-15 2022-07-01 安徽联创生物医药股份有限公司 一种用hplc分离测定巴瑞替尼原料药杂质的方法
CN111848491B (zh) * 2020-08-10 2022-06-17 烟台大学 1-甲酰基咔唑的制备方法
CN111875534B (zh) * 2020-08-10 2022-06-17 烟台大学 1,8-二甲酰基咔唑的安全高效制备方法
AU2021327130A1 (en) 2020-08-17 2023-03-02 Bicycletx Limited Bicycle conjugates specific for Nectin-4 and uses thereof
US11905292B2 (en) 2020-08-18 2024-02-20 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
CA3192055A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak1 inhibitor
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
JP2023548052A (ja) 2020-10-23 2023-11-15 エランコ・ユーエス・インコーポレイテッド 特定の粒径分布を有するｊａｋ阻害剤
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
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
AU2021392040A1 (en) 2020-12-02 2023-06-29 Ikena Oncology, Inc. Tead inhibitors and uses thereof
US11827657B2 (en) 2020-12-18 2023-11-28 Boehringer Ingelheim Animal Health USA Inc. Boron containing pyrazole compounds, compositions comprising them, methods and uses thereof
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
WO2022167445A1 (en) 2021-02-02 2022-08-11 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
EP4288427A1 (en) 2021-02-02 2023-12-13 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
CN114907354B (zh) * 2021-02-07 2024-04-09 南京知和医药科技有限公司 一种磺酰胺类多环化合物及其制备方法与用途
TW202245789A (zh) 2021-02-15 2022-12-01 美商凱麥拉醫療公司 Irak4降解劑及其用途
CN114957260B (zh) * 2021-02-26 2024-04-09 南京知和医药科技有限公司 一种巴瑞替尼衍生物及其制备方法与用途
JP2024509192A (ja) 2021-03-05 2024-02-29 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
KR20230172548A (ko) 2021-04-16 2023-12-22 이케나 온콜로지, 인코포레이티드 Mek 억제제 및 이의 용도
CA3226714A1 (en) * 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
WO2023009767A1 (en) 2021-07-30 2023-02-02 Eli Lilly And Company Treatment of hand eczema with baricitinib
IL310924A (en) 2021-08-25 2024-04-01 Pic Therapeutics Inc EIF4E inhibitors and their uses
WO2023028238A1 (en) 2021-08-25 2023-03-02 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
CN114373808B (zh) * 2021-11-26 2023-11-10 江苏科来材料科技有限公司 一种高效晶硅电池
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CN114149437A (zh) * 2021-12-24 2022-03-08 安徽大学 一种吡咯并嘧啶五元氮杂环衍生物及其制备方法和用途
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023194842A1 (en) 2022-04-05 2023-10-12 Unichem Laboratories Limited Substituted tricyclic compounds and their use in rheumatoid arthritis
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2024028363A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Heteroaryl carboxamide and related gpr84 antagonists and uses thereof
WO2024028365A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Substituted pyridone gpr84 antagonists and uses thereof
WO2024028364A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Aryl-triazolyl and related gpr84 antagonists and uses thereof
CN115181103B (zh) * 2022-08-16 2023-11-07 上海博悦生物科技有限公司 一种巴瑞替尼的制备方法
CN116444529B (zh) * 2023-06-16 2023-12-05 药康众拓(江苏)医药科技有限公司 一种氘代氮杂环丁烷类jak抑制剂及其用途

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3036390A1 (de) 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
US4548990A (en) * 1983-08-15 1985-10-22 Ciba-Geigy Corporation Crosslinked, porous polymers for controlled drug delivery
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
AU6478396A (en) 1995-07-05 1997-02-05 E.I. Du Pont De Nemours And Company Fungicidal pyrimidinones
CA2224435C (en) 1995-07-06 2008-08-05 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
CA2333770A1 (en) 1998-06-04 1999-12-09 Abbott Laboratories Cell adhesion-inhibiting antinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
CZ20004727A3 (cs) 1998-06-19 2002-03-13 Pfizer Products Inc. Deriváty pyrrolo[2,3-d] pyrimidinu
DE69942097D1 (de) 1998-08-11 2010-04-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
AU3565999A (en) 1999-04-16 2000-11-02 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
PL218519B1 (pl) 1999-12-10 2014-12-31 Pfizer Prod Inc Związki pirolo [2,3-d] pirymidynowe, środek farmaceutyczny zawierający te związki oraz ich zastosowanie
CA2699568C (en) * 1999-12-24 2013-03-12 Aventis Pharma Limited Azaindoles
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
KR20030011106A (ko) * 2000-06-23 2003-02-06 미쯔비시 웰 파마 가부시키가이샤 항종양 작용 강화제
ATE423120T1 (de) 2000-06-26 2009-03-15 Pfizer Prod Inc Pyrroloä2,3-düpyrimidin verbindungen als immunosuppressive wirkstoffe
PT1294358E (pt) 2000-06-28 2004-12-31 Smithkline Beecham Plc Processo de moagem por via humida
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
US6852727B2 (en) 2001-08-01 2005-02-08 Merck & Co., Inc. Benzimisazo[4,5-f]isoquinolinone derivatives
AU2002337142B2 (en) 2001-09-19 2007-10-11 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
JP4959918B2 (ja) 2001-10-30 2012-06-27 ノバルティス アーゲー Ｆｌｔ３レセプター・チロシン・キナーゼ活性インヒビターとしてのスタウロスポリン誘導体
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
US20040019066A1 (en) * 2002-05-06 2004-01-29 Institut Pasteur Methionine salvage pathway in bacillus
AU2003234439A1 (en) * 2002-05-07 2003-11-11 Control Delivery Systems, Inc. Processes for forming a drug delivery device
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US20060004010A1 (en) * 2002-07-10 2006-01-05 Hiromu Habashita Ccr4 antagonist and medical use thereof
EP1562938B1 (en) 2002-11-04 2007-08-29 Vertex Pharmaceuticals Incorporated Heteroaryl-pyrimidine derivatives as jak inhibitors
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
MXPA05005576A (es) 2002-11-26 2005-07-27 Pfizer Prod Inc Procedimiento de tratamiento del rechazo a un trasplante.
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
EP1611125A1 (en) 2003-02-07 2006-01-04 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
MXPA06005882A (es) 2003-11-25 2006-06-27 Pfizer Prod Inc Metodo de tratamiento de la aterosclerosis.
RU2006120956A (ru) 2003-12-17 2008-01-27 Пфайзер Продактс Инк. (Us) Пирроло{2, 3-d}пиримидиновые соединения для лечения отторжения трансплантата
US20050239806A1 (en) * 2004-01-13 2005-10-27 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
MXPA06011327A (es) 2004-03-30 2006-12-15 Vertex Pharma Azaindoles utiles como inhibidores de jak y otras proteinas cinasas.
AU2005249380C1 (en) 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
EP2363149A1 (en) 2004-05-03 2011-09-07 Novartis AG Combinations comprising a S1P receptor agonist and a JAK3 kinase inhibitor
EP1753428A4 (en) 2004-05-14 2010-09-15 Abbott Lab INHIBITORS OF KINASES AS THERAPEUTIC AGENTS
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
JP5315611B2 (ja) * 2004-06-23 2013-10-16 小野薬品工業株式会社 Ｓ１ｐ受容体結合能を有する化合物およびその用途
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
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
EP1885352A2 (en) 2004-11-24 2008-02-13 Novartis AG Combinations comprising jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
ATE420883T1 (de) 2005-02-03 2009-01-15 Vertex Pharma Pyrrolopyrimidine verwendbar als protein kinase inhibitoren
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
CA2609126A1 (en) 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
EP2270014A1 (en) * 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
EP2532667A1 (en) 2005-09-30 2012-12-12 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
WO2007070514A1 (en) * 2005-12-13 2007-06-21 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
CA2636189A1 (en) 2006-01-17 2007-07-26 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of janus kinases
SG170828A1 (en) * 2006-04-05 2011-05-30 Vertex Pharmaceuticals Inc Us Deazapurines useful as inhibitors of janus kinases
TW200805992A (en) * 2006-07-04 2008-01-16 Benq Corp Method and apparatus for barring short message
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.
RS58449B1 (sr) * 2007-06-13 2019-04-30 Incyte Holdings Corp Upotreba soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h- pirazol-1-il)-3-ciklopentilpropionitrila

Also Published As

Publication number Publication date
PE20140099A1 (es) 2014-02-06
MY165582A (en) 2018-04-05
PE20091712A1 (es) 2009-11-21
CN102026999B (zh) 2014-03-05
KR101240882B1 (ko) 2013-03-11
DOP2013000036A (es) 2013-03-15
IL208023A (en) 2015-08-31
LTPA2017023I1 (lt) 2017-08-10
JP5275371B2 (ja) 2013-08-28
HUS1700031I1 (hu) 2017-09-28
HK1149005A1 (zh) 2011-09-23
HUE029767T2 (en) 2017-04-28
KR20120108042A (ko) 2012-10-04
US20130225556A1 (en) 2013-08-29
US20120077798A1 (en) 2012-03-29
MA32219B1 (fr) 2011-04-01
EA201071057A1 (ru) 2011-02-28
CN103788098A (zh) 2014-05-14
US20090233903A1 (en) 2009-09-17
ZA201006000B (en) 2012-01-25
CN102026999A (zh) 2011-04-20
BRPI0909040B8 (pt) 2021-05-25
NO2017033I2 (no) 2017-07-11
HN2010001761A (es) 2013-09-02
DK2288610T3 (en) 2016-11-28
RS55263B1 (sr) 2017-02-28
NZ587928A (en) 2012-08-31
CO6290658A2 (es) 2011-06-20
PA8819201A1 (es) 2010-07-27
UY31705A1 (es) 2009-08-03
CA2718271C (en) 2014-05-06
EA017218B1 (ru) 2012-10-30
LTC2288610I2 (lt) 2019-02-25
TN2010000415A1 (en) 2011-12-29
TW200942545A (en) 2009-10-16
US8158616B2 (en) 2012-04-17
BRPI0909040A8 (pt) 2017-12-12
LUC00027I2 (es) 2017-09-25
BRPI0909040A2 (es) 2017-09-19
NL300886I2 (nl) 2017-10-24
AU2009223640B2 (en) 2013-07-04
CY2017024I2 (el) 2017-11-14
UA101493C2 (ru) 2013-04-10
TWI444382B (zh) 2014-07-11
JP2011514909A (ja) 2011-05-12
EP2288610B1 (en) 2016-08-31
CY1118176T1 (el) 2017-06-28
PT2288610T (pt) 2016-10-17
SI2288610T1 (sl) 2016-11-30
HRP20161390T1 (hr) 2016-12-02
NO2017033I1 (no) 2017-07-11
WO2009114512A1 (en) 2009-09-17
JP2013155179A (ja) 2013-08-15
SV2010003662A (es) 2011-03-17
DOP2010000270A (es) 2010-10-15
LUC00027I1 (es) 2017-07-12
SG191660A1 (en) 2013-07-31
PL2288610T3 (pl) 2017-12-29
KR20100121657A (ko) 2010-11-18
EP2288610A1 (en) 2011-03-02
MX2010010012A (es) 2010-10-20
CL2009000576A1 (es) 2009-06-19
LT2288610T (lt) 2016-12-12
IL208023A0 (en) 2010-12-30
EP2288610B8 (en) 2016-10-12
US8420629B2 (en) 2013-04-16
CY2017024I1 (el) 2017-11-14
BRPI0909040B1 (pt) 2019-10-22
AU2009223640A1 (en) 2009-09-17
ECSP10010475A (es) 2010-10-30
ES2602577T3 (es) 2017-02-21
CA2718271A1 (en) 2009-09-17

Similar Documents

Publication Publication Date Title
AR070828A1 (es) Derivados de azetidina y ciclobutano como inhibidores de jak
AR076435A1 (es) Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos
AR119698A2 (es) Compuesto amida n-urea sustituida derivado de aminoácido
AR085960A1 (es) 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
PE20140192A1 (es) Derivados de bencimidazol como inhibidores de cinasa pi3
AR086198A1 (es) Inhibidores sustituidos de acetil-coa carboxilasa y composiciones farmaceuticas que los contienen
PE20181272A1 (es) Heterociclilaminas como inhibidores de pi3k
PE20151602A1 (es) SALES DE DERIVADOS DE 2-AMINO-1-HIDROXIETIL-8-HIDROXIQUINOLIN-2(1H)-ONA QUE TIENEN ACTIVIDAD AGONISTA DEL RECEPTOR B(beta)2 ADRENERGICO ASI COMO ACTIVIDAD ANTAGONISTA DEL RECEPTOR MUSCARINICO M3
CO6170361A2 (es) Composiciones y metodos para modular receptores de c-kit y pdgfr
AR057109A1 (es) Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis
CL2009000127A1 (es) Compuestos derivados de [indol, azaindol]-2-carboxamida sustituidos con un grupo silanilo; procedimiento de preparacion; compuestos intermediarios; composicion farmaceutica; y su uso en el tratamiento del dolor, inflamacion, trastornos metabolicos, entre otras enfermedades mediadas por la modulacion del receptor trpv1.
AR046085A1 (es) Agonistas etilamino amino sustituidos del receptor beta 2 adrenergico
PE20150194A1 (es) Novedosas n-piridinil amidas ciclicas sustituidas como inhibidores de quinasa
AR084152A1 (es) Compuestos de triazolopirimidina como inhibidores de pde10a, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades del snc
ECSP11010901A (es) Compuestos de amida útiles en terapia
PE20141352A1 (es) Fenil-3-aza-biciclo[3,1,0]hex-3-il-metanonas y su uso como medicamento
AR087915A1 (es) N-(3-(2-amino-6,6-difluor-4,4a,5,6,7,7a-hexahidro-ciclopenta-[e][1,3]oxazin-4-il)-fenil)-amidas como inhibidores de la bace1
AR077080A1 (es) Compuestos de 2,3-dihidro-1h-indeno
UY32004A (es) Derivados de carbamatos de alquiltiazoles, su preparación y su aplicación en terapéutica
AR073043A1 (es) Compuestos de azetidinas polisustituidos, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de los mismos en el tratamiento de enfermedades respiratorias, metabolicas y del sistema nervioso central, entre otras.
CO6341621A2 (es) Piperidinas arilamino y heteroarilamino sustituidas como inhibidores de glyt-1
AR081966A1 (es) Derivados aminoester de alcaloides y composicion medicinal de los mismos
AR072880A1 (es) Derivados nitrogenados de la pancratistatina
AR085428A1 (es) (3r,4r)-4-ciano-3,4-difenilbutanoatos sustituidos, procedimiento para su preparacion y su uso como herbicidas y reguladores de crecimiento de plantas

Legal Events

Date Code Title Description
FG Grant, registration