AU2009223640B2 - Azetidine and cyclobutane derivatives as jak inhibitors - Google Patents

Azetidine and cyclobutane derivatives as jak inhibitors Download PDF

Info

Publication number
AU2009223640B2
AU2009223640B2 AU2009223640A AU2009223640A AU2009223640B2 AU 2009223640 B2 AU2009223640 B2 AU 2009223640B2 AU 2009223640 A AU2009223640 A AU 2009223640A AU 2009223640 A AU2009223640 A AU 2009223640A AU 2009223640 B2 AU2009223640 B2 AU 2009223640B2
Authority
AU
Australia
Prior art keywords
mol
compound
pyrrolo
pyrazol
mixture
Prior art date
Legal status (The legal status 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 status listed.)
Active, expires
Application number
AU2009223640A
Other languages
English (en)
Other versions
AU2009223640A1 (en
Inventor
Yun-Long Li
Pingli Liu
David Meloni
James D. Rodgers
Stacey Shepard
Michael Xia
Jiacheng Zhou
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Incyte Holdings Corp
Original Assignee
Incyte Holdings 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=AU2009223640(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of AU2009223640A1 publication Critical patent/AU2009223640A1/en
Priority to AU2013201219A priority Critical patent/AU2013201219A1/en
Application granted granted Critical
Publication of AU2009223640B2 publication Critical patent/AU2009223640B2/en
Assigned to INCYTE HOLDINGS CORPORATION reassignment INCYTE HOLDINGS CORPORATION Request for Assignment Assignors: INCYTE CORPORATION
Active legal-status Critical Current
Adjusted expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B60VEHICLES IN GENERAL
    • B60QARRANGEMENT OF SIGNALLING OR LIGHTING DEVICES, THE MOUNTING OR SUPPORTING THEREOF OR CIRCUITS THEREFOR, FOR VEHICLES IN GENERAL
    • B60Q3/00Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors
    • B60Q3/70Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors characterised by the purpose
    • B60Q3/76Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors characterised by the purpose for spotlighting, e.g. reading lamps
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B60VEHICLES IN GENERAL
    • B60QARRANGEMENT OF SIGNALLING OR LIGHTING DEVICES, THE MOUNTING OR SUPPORTING THEREOF OR CIRCUITS THEREFOR, FOR VEHICLES IN GENERAL
    • B60Q3/00Arrangement of lighting devices for vehicle interiors; Lighting devices specially adapted for vehicle interiors
    • B60Q3/80Circuits; Control arrangements
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S362/00Illumination
    • Y10S362/80Light emitting diode
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S362/00Illumination
    • Y10S362/802Position or condition responsive switch

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Mechanical Engineering (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Surgery (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU2009223640A 2008-03-11 2009-03-10 Azetidine and cyclobutane derivatives as jak inhibitors Active 2033-01-23 AU2009223640B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2013201219A AU2013201219A1 (en) 2008-03-11 2013-03-04 Azetidine and cyclobutane derivatives as jak inhibitors

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US3566208P 2008-03-11 2008-03-11
US61/035,662 2008-03-11
US14498209P 2009-01-15 2009-01-15
US61/144,982 2009-01-15
PCT/US2009/036635 WO2009114512A1 (en) 2008-03-11 2009-03-10 Azetidine and cyclobutane derivatives as jak inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2013201219A Division AU2013201219A1 (en) 2008-03-11 2013-03-04 Azetidine and cyclobutane derivatives as jak inhibitors

Publications (2)

Publication Number Publication Date
AU2009223640A1 AU2009223640A1 (en) 2009-09-17
AU2009223640B2 true AU2009223640B2 (en) 2013-07-04

Family

ID=40591836

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009223640A Active 2033-01-23 AU2009223640B2 (en) 2008-03-11 2009-03-10 Azetidine and cyclobutane derivatives as jak inhibitors

Country Status (43)

Country Link
US (3) US8158616B2 (forum.php)
EP (1) EP2288610B8 (forum.php)
JP (2) JP5275371B2 (forum.php)
KR (2) KR101240882B1 (forum.php)
CN (2) CN102026999B (forum.php)
AR (1) AR070828A1 (forum.php)
AU (1) AU2009223640B2 (forum.php)
BR (1) BRPI0909040B8 (forum.php)
CA (1) CA2718271C (forum.php)
CL (1) CL2009000576A1 (forum.php)
CO (1) CO6290658A2 (forum.php)
CY (2) CY1118176T1 (forum.php)
DK (1) DK2288610T3 (forum.php)
DO (2) DOP2010000270A (forum.php)
EA (1) EA017218B1 (forum.php)
EC (1) ECSP10010475A (forum.php)
ES (1) ES2602577T3 (forum.php)
HN (1) HN2010001761A (forum.php)
HR (1) HRP20161390T1 (forum.php)
HU (2) HUE029767T2 (forum.php)
IL (1) IL208023A (forum.php)
LT (2) LT2288610T (forum.php)
LU (1) LUC00027I2 (forum.php)
MA (1) MA32219B1 (forum.php)
MX (1) MX2010010012A (forum.php)
MY (1) MY165582A (forum.php)
NL (1) NL300886I2 (forum.php)
NO (1) NO2017033I2 (forum.php)
NZ (1) NZ587928A (forum.php)
PA (1) PA8819201A1 (forum.php)
PE (2) PE20091712A1 (forum.php)
PL (1) PL2288610T3 (forum.php)
PT (1) PT2288610T (forum.php)
RS (1) RS55263B1 (forum.php)
SG (1) SG191660A1 (forum.php)
SI (1) SI2288610T1 (forum.php)
SV (1) SV2010003662A (forum.php)
TN (1) TN2010000415A1 (forum.php)
TW (1) TWI444382B (forum.php)
UA (1) UA101493C2 (forum.php)
UY (1) UY31705A1 (forum.php)
WO (1) WO2009114512A1 (forum.php)
ZA (1) ZA201006000B (forum.php)

Families Citing this family (303)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105814A1 (en) * 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
PL2455382T3 (pl) 2005-12-13 2017-04-28 Incyte Holdings Corporation Podstawione heteroarylem pirolo[2,3-b]pirydyny i pirolo[2,3-b]pirymidyny jako inhibitory kinazy Janusowej
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.
EP3495369B1 (en) 2007-06-13 2021-10-27 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
NZ585139A (en) * 2007-11-16 2012-05-25 Incyte Corp 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as jak inhibitors
BRPI0906244A2 (pt) 2008-03-24 2015-06-30 Medivation Technologies Inc Composto, composição farmacêutica, método para tratar um distúrbio cognitivo, psicótico, mediado por neurotransmissores ou um distúrbio neuronal em um indivíduo, uso de um composto e kit
EP2296475A4 (en) * 2008-06-20 2014-03-05 Genentech Inc TRIAZOLOPYRIDINE COMPOUNDS JAK KINASE INHIBITORS AND METHODS
US20100048557A1 (en) * 2008-06-20 2010-02-25 Bing-Yan Zhu Triazolopyridine JAK Inhibitor Compounds and Methods
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
NZ596479A (en) * 2009-05-22 2014-01-31 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
TWI484962B (zh) 2009-05-22 2015-05-21 Incyte Corp 作為jak抑制劑之3-〔4-(7h-吡咯并〔2,3-d〕嘧啶-4-基)-1h-吡唑-1-基〕辛烷或庚腈
WO2011028685A1 (en) 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CN105541847B (zh) * 2009-10-09 2019-08-16 因西特控股公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
JP5858434B2 (ja) * 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Janusキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
HUE028723T2 (en) * 2010-03-10 2016-12-28 Incyte Holdings Corp Piperidin-4-yl azetidine derivatives as JAK-1 inhibitors
AU2015205858B2 (en) * 2010-03-10 2017-04-13 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
KR102402137B1 (ko) 2010-05-21 2022-05-30 인사이트 홀딩스 코포레이션 Jak 저해제에 대한 국소 제형
CA2818545C (en) 2010-11-19 2019-04-16 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
EA036970B1 (ru) * 2010-11-19 2021-01-21 Инсайт Холдингс Корпорейшн Применение {1-{1-[3-фтор-2-(трифтометил)изоникотиноил] пиперидин-4-ил}-3-[4-(7h-пирроло[2,3-d]пиримидин-4-ил)-1н-пиразол-1-ил]азетидин-3-ил}ацетонитрила для лечения заболеваний, связанных с активностью jak1
AU2011329734B2 (en) * 2010-11-19 2015-05-28 Incyte Holdings Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
JP5857972B2 (ja) * 2010-12-01 2016-02-10 日産化学工業株式会社 多発性骨髄腫の治療効果を有するピラゾール化合物
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
KR102024948B1 (ko) 2011-02-18 2019-11-04 노파르티스 파르마 아게 mTOR/JAK 저해제 병용 요법
NO2683684T3 (forum.php) * 2011-03-08 2018-06-02
AR086983A1 (es) 2011-06-20 2014-02-05 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
HK1198579A1 (en) 2011-08-10 2015-04-30 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
CA2849336A1 (en) * 2011-09-22 2013-03-29 Merck Sharp & Dohme Corp. Cyanomethylpyrazole carboxamides as janus kinase inhibitors
ES3018133T3 (en) 2011-11-30 2025-05-14 Univ Emory Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
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
MX361499B (es) * 2012-08-17 2018-12-06 Concert Pharmaceuticals Inc Baricitinib deuterado.
HK1214823A1 (zh) 2012-11-01 2016-08-05 Incyte Holdings Corporation 作為jak抑制劑的三環稠合噻吩衍生物
EA201590930A1 (ru) 2012-11-15 2015-08-31 Инсайт Корпорейшн Лекарственные формы руксолитиниба с замедленным высвобождением
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
UA120162C2 (uk) * 2013-03-06 2019-10-25 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки при отриманні інгібітора 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
KR102442747B1 (ko) * 2013-05-17 2022-09-14 인사이트 코포레이션 Jak 저해제로서 비피라졸 유도체
CA2928568A1 (en) 2013-07-26 2015-01-29 Update Pharma Inc. Combinatorial methods to improve the therapeutic benefit of bisantrene
PH12019502074B1 (en) * 2013-08-07 2023-10-18 Incyte Holdings Corp Sustained release dosage forms for a jak1 inhibitor
TW201529074A (zh) 2013-08-20 2015-08-01 Incyte Corp 在c-反應蛋白含量較高之實體腫瘤患者中的存活益處
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
CR20200362A (es) 2014-02-13 2020-10-26 Incyte Corp CICLOPROPILAMINA COMO INHIBIDORES DE LA LSD1 (Divisional 2016-0395)
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
SMT201900680T1 (it) 2014-02-13 2020-01-14 Incyte Corp Ciclopropilammine come inibitori di lsd1
JP6576941B2 (ja) 2014-02-28 2019-09-18 インサイト・コーポレイションIncyte Corporation 骨髄異形成症候群の治療のためのjak1阻害剤
EP3110820B1 (en) 2014-02-28 2022-04-06 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2015145286A1 (en) 2014-03-28 2015-10-01 Sun Pharmaceutical Industries Limited Amorphous form of baricitinib
EA201692193A1 (ru) 2014-04-30 2017-07-31 Инсайт Корпорейшн Способы получения ингибитора jak1 и его новых форм
EP3136857A4 (en) 2014-05-01 2017-09-20 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
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
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
RS63364B1 (sr) 2014-08-11 2022-07-29 Acerta Pharma Bv Terapeutske kombinacije btk inhibitora, pd-1 inhibitora i/ili pd-l1 inhibitora
US20170224819A1 (en) 2014-08-11 2017-08-10 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, and/or a CDK 4/6 Inhibitor
ES2900184T3 (es) 2014-08-11 2022-03-16 Acerta Pharma Bv Combinaciones terapéuticas de un inhibidor de BTK y un inhibidor de BCL-2
CN117164657A (zh) 2014-08-12 2023-12-05 莫纳什大学 定向淋巴的前药
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
PT3215518T (pt) 2014-10-29 2021-05-25 Bicyclerd Ltd Ligantes de péptido bicíclicos específicos para mt1-mmp
US9873706B2 (en) 2014-12-05 2018-01-23 Sun Pharmaceutical Industries Limited 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
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
CN105924444B (zh) * 2015-03-11 2019-06-18 苏州晶云药物科技股份有限公司 Jak抑制剂的晶型及其制备方法
EP3269719B1 (en) * 2015-03-11 2020-05-13 Crystal Pharmatech Co. Ltd. Crystal form of jak inhibitor and preparation method thereof
PE20180455A1 (es) 2015-04-03 2018-03-05 Incyte Corp Compuestos heterociclicos como inhibidores de lsd1
AR104918A1 (es) 2015-06-19 2017-08-23 Lilly Co Eli Procesos e intermediarios para la preparación de {1-(etilsulfonil)-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrilo
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
TWI765860B (zh) 2015-08-12 2022-06-01 美商英塞特公司 Lsd1抑制劑之鹽
WO2017040757A1 (en) 2015-09-02 2017-03-09 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CA2997106C (en) 2015-09-08 2024-06-04 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
MX389001B (es) 2015-10-23 2025-03-20 Navitor Pharm Inc Moduladores de interacción de sestrina-gator2 y sus usos.
RU2601410C1 (ru) * 2015-11-13 2016-11-10 ЗАО "Р-Фарм" {3-[(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)АЗОЛИЛ]АЗЕТИДИН-3-ИЛ}АЦЕТОНИТРИЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС КИНАЗ
RU2603959C1 (ru) * 2015-11-13 2016-12-10 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") ДИХЛОРАЦЕТАТ {3-[4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-ПИРАЗОЛ-1-ИЛ]-1-ЭТИЛСУЛЬФОНИЛ-АЗЕТИДИН-3-ИЛ}-АЦЕТОНИТРИЛА В КАЧЕСТВЕ ИНГИБИТОРА ЯНУС КИНАЗ
CN105294699B (zh) * 2015-12-04 2019-06-11 上海勋和医药科技有限公司 巴瑞替尼的制备方法
EP3360878B9 (en) * 2015-12-11 2021-05-05 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Azetidine derivative, preparation method therefor, and use thereof
WO2017106352A1 (en) 2015-12-14 2017-06-22 Raze Therapeutics, Inc. Caffeine inhibitors of mthfd2 and uses thereof
HU230805B1 (hu) * 2015-12-23 2018-06-28 Egis Gyógyszergyár Zrt Eljárás és köztitermék baricitinib előállítására
HU230931B1 (hu) * 2016-01-21 2019-04-29 Egis Gyógyszergyár Zrt. Baricitinib sók
CN106905322B (zh) * 2016-01-26 2019-10-15 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
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
CN107573349A (zh) * 2016-02-01 2018-01-12 上海宣创生物科技有限公司 巴瑞克替尼磷酸盐h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
HRP20211220T1 (hr) 2016-03-09 2021-10-29 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
EP3440112A4 (en) 2016-04-08 2019-10-09 X4 Pharmaceuticals, Inc. METHOD FOR THE TREATMENT OF CANCER
MY199968A (en) 2016-04-22 2023-11-30 Incyte Corp Formulations of an lsd1 inhibitor
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
CA3027500A1 (en) 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
US10988465B2 (en) 2016-06-21 2021-04-27 X4 Pharmaceuticals, Inc. CXCR4 inhibitors and uses thereof
CN109843883B (zh) 2016-07-26 2022-01-14 苏州隆博泰药业有限公司 作为选择性jak抑制剂化合物,该化合物的盐类及其治疗用途
CN106496233B (zh) * 2016-09-26 2018-05-15 东南大学 吡咯并嘧啶类化合物、其制备方法及其用途
WO2018071794A1 (en) 2016-10-14 2018-04-19 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
US10647713B2 (en) 2016-10-21 2020-05-12 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
US10414727B2 (en) 2016-11-08 2019-09-17 Navitor Pharmaceuticals, Inc. Phenyl amino piperidine mTORC inhibitors and uses thereof
CZ2016705A3 (cs) 2016-11-11 2018-05-23 Zentiva, K.S. Krystalické formy 2- [1-ethylsulfonyl-3- [4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) pyrazol-1-yl] azetidin-3-yl] acetonitrilových solí a jejich příprava
CN110177544A (zh) 2016-11-29 2019-08-27 普尔泰克健康有限公司 用于递送治疗剂的外泌体
EP3327020A1 (en) 2016-11-29 2018-05-30 Sandoz Ag Citrate salts of a janus kinase (jak) inhibitor
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
CZ2016816A3 (cs) * 2016-12-21 2018-07-04 Zentiva, K.S. Krystalické formy 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrilu s kyselinou fosforečnou a způsob jejich přípravy
CN110603261A (zh) 2016-12-23 2019-12-20 拜斯科阿迪有限公司 具有新型键结构的肽衍生物
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
EP3572415B1 (en) * 2017-01-23 2024-03-06 Shanghai Longwood Biopharmaceuticals Co., Ltd. Jak kinase inhibitor and preparation method and use thereof
AU2018230737B2 (en) 2017-03-08 2022-09-22 Takeda Pharmaceutical Company Limited Tyk2 inhibitors, uses, and methods for production thereof
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
TWI776886B (zh) 2017-04-26 2022-09-11 美商奈維特製藥公司 Sestrin-gator2交互作用之調節劑及其用途
WO2018197893A1 (en) 2017-04-27 2018-11-01 Bicycletx Limited Bicyclic peptide ligands and uses thereof
EP3609899A1 (en) 2017-05-23 2020-02-19 Theravance Biopharma R&D IP, LLC Glucuronide prodrugs of janus kinase inhibitors
DK3636647T3 (da) * 2017-06-07 2023-02-06 Sichuan Kelun Biotech Biopharmaceutical Co Ltd Fastform af azetidinderivat og fremstillingsfremgangsmåde derfor samt anvendelse deraf
WO2018233437A1 (zh) * 2017-06-22 2018-12-27 苏州科睿思制药有限公司 巴瑞克替尼的晶型及其制备方法
WO2019002842A1 (en) 2017-06-26 2019-01-03 Bicyclerd Limited BICYCLIC PEPTIDE LIGANDS WITH DETECTABLE FRACTIONS AND USES THEREOF
WO2019003249A1 (en) 2017-06-28 2019-01-03 Mylan Laboratories Limited POLYMORPHIC FORMS OF BARICITINIB
DK3658557T3 (da) 2017-07-28 2024-07-29 Takeda Pharmaceuticals Co Tyk2-inhibitorer og anvendelser deraf
WO2019025811A1 (en) 2017-08-04 2019-02-07 Bicycletx Limited SPECIFIC BICYCLIC PEPTIDE LIGANDS OF CD137
EP3668887A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
WO2019034868A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
EP3675838A4 (en) 2017-08-29 2021-04-21 PureTech LYT, Inc. Lymphatic system-directing lipid prodrugs
US11358948B2 (en) 2017-09-22 2022-06-14 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
IL307995A (en) 2017-09-22 2023-12-01 Kymera Therapeutics Inc Protein compounds and their uses
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
CA3084589A1 (en) 2017-10-18 2019-04-25 Incyte Corporation Condensed imidazole derivatives substituted by tertiary hydroxy groups as pi3k-gamma 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
CN109867675B (zh) * 2017-12-01 2021-01-19 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
CN108129482A (zh) * 2017-12-13 2018-06-08 江苏中邦制药有限公司 一种巴瑞替尼的制备方法
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
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
WO2019126378A1 (en) 2017-12-19 2019-06-27 Ariya Therapeutics, 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
EP3502114A1 (en) 2017-12-20 2019-06-26 Sandoz AG Co-crystal of an orally available janus kinase inhibitor
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
US10766900B2 (en) 2017-12-29 2020-09-08 Formosa Laboratories, Inc. Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
SG11202006832YA (en) 2018-01-29 2020-08-28 Merck Patent Gmbh Gcn2 inhibitors and uses thereof
EP4616913A2 (en) 2018-01-29 2025-09-17 Merck Patent GmbH Gcn2 inhibitors and uses thereof
EA202091830A1 (ru) 2018-01-30 2020-12-29 Инсайт Корпорейшн Способы и промежуточные соединения для получения ингибитора jak
CN118557580A (zh) 2018-02-16 2024-08-30 因赛特公司 用于治疗细胞因子相关的病症的jak1通路抑制剂
CA3091775A1 (en) 2018-02-23 2019-08-29 Bicycletx Limited Multimeric bicyclic peptide ligands
AU2019229258B2 (en) 2018-02-27 2023-09-14 Artax Biopharma Inc. Chromene derivatives as inhibitors of TCR-Nck interaction
CN110357887B (zh) * 2018-03-26 2022-09-16 武汉誉祥医药科技有限公司 取代的7H-吡咯并[2,3-d]嘧啶衍生物及其制备方法和用途
HRP20240741T1 (hr) 2018-03-30 2024-12-06 Incyte Corporation Liječenje hidradenitis suppurativa uporabom jak inhibitora
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
US11372003B2 (en) 2018-04-13 2022-06-28 Incyte Corporation Biomarkers for graft-versus-host disease
CA3097774A1 (en) 2018-04-24 2019-10-31 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
ES2987356T3 (es) 2018-04-24 2024-11-14 Merck Patent Gmbh Compuestos antiproliferación y usos de los mismos
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
US12268681B2 (en) * 2018-05-25 2025-04-08 Kartos Therapeutics, Inc. Methods of treating myeloproliferative neoplasms
WO2019233434A1 (zh) * 2018-06-06 2019-12-12 杭州澳津生物医药技术有限公司 一种吡唑嘧啶衍生物及其用途和药物组合物
FI3813946T3 (fi) 2018-06-15 2024-06-25 Janssen Pharmaceutica Nv Rapamysiinianalogeja ja niiden käyttötapoja
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
IL279489B1 (en) 2018-06-22 2025-06-01 Bicycletx Ltd Bicyclic peptide ligands specific for nectin-4, a drug conjugate comprising the peptide ligand and a pharmaceutical composition comprising the drug conjugate
EP3817748A4 (en) 2018-07-06 2022-08-24 Kymera Therapeutics, Inc. TRICYCLIC CRBN LIGANDS AND USES THEREOF
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
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
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
WO2020051424A1 (en) 2018-09-07 2020-03-12 Pic Therapeutics Eif4e inhibitors and uses thereof
WO2020072870A1 (en) 2018-10-05 2020-04-09 Johnson Matthey Public Limited Company Co-crystal forms of baricitinib
WO2020081508A1 (en) 2018-10-15 2020-04-23 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
AR116592A1 (es) 2018-10-17 2021-05-26 Lilly Co Eli Tratamiento de la colangitis biliar primaria y la colangitis esclerosante primaria con baricitinib
US10919937B2 (en) 2018-10-23 2021-02-16 Bicycletx Limited Bicyclic peptide ligands and uses thereof
CA3117336A1 (en) 2018-10-24 2020-04-30 Navitor Pharmaceuticals, Inc. Polymorphs of (s)-2-amino-5,5-difluoro-4,4-dimethylpentanoic acid for use in modulating mtorc1
WO2020092726A1 (en) 2018-10-31 2020-05-07 Incyte Corporation Combination therapy for treatment of hematological diseases
US11053241B2 (en) 2018-11-30 2021-07-06 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
BR112021010484A2 (pt) 2018-11-30 2021-08-24 Kymera Therapeutics, Inc. Degradadores de irak e usos dos mesmos
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
GB201820325D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for psma
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
BR112021011894A2 (pt) 2018-12-21 2021-09-08 Daiichi Sankyo Company, Limited Composição farmacêutica
WO2020154474A1 (en) 2019-01-23 2020-07-30 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CN111499641B (zh) * 2019-01-30 2021-06-04 格格巫(珠海)生物科技有限公司 一种jak抑制剂及其制备方法
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
CN113508114B (zh) * 2019-02-27 2024-03-26 四川科伦博泰生物医药股份有限公司 以氮杂环丁烷衍生物为活性成分的口服药物组合物、其制备方法及用途
JP7248256B2 (ja) 2019-03-14 2023-03-29 上海華匯拓医薬科技有限公司 Jakキナーゼ阻害剤及びその調製方法、並びにその医薬分野での使用
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
AU2020253990A1 (en) 2019-04-02 2021-10-28 Bicycletx Limited Bicycle toxin conjugates and uses thereof
MX2021012216A (es) 2019-04-05 2022-01-24 Kymera Therapeutics Inc Degradadores de transductores de señal y activadores de transcripción (stat) y usos de los mismos.
EP3725305A1 (en) 2019-04-17 2020-10-21 Zentiva K.S. Pharmaceutical composition containing baricitinib hydrobromide
JP7241916B2 (ja) * 2019-04-24 2023-03-17 エランコ・ユーエス・インコーポレイテッド 7h-ピロロ[2,3-d]ピリミジンjak-阻害剤
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
WO2020243423A1 (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
TWI860386B (zh) 2019-07-30 2024-11-01 英商拜西可泰克斯有限公司 異質雙環肽複合物
EP3771716A1 (en) 2019-08-02 2021-02-03 Zaklady Farmaceutyczne "Polpharma" S.A. Low hygroscopic amorphous form of baricitinib
EP3771715A1 (en) 2019-08-02 2021-02-03 Zaklady Farmaceutyczne "Polpharma" S.A. Crystalline forms of baricitinib
CN115038688A (zh) 2019-09-11 2022-09-09 文森雷生物科学股份有限公司 Usp30抑制剂及其用途
JP2022547719A (ja) 2019-09-13 2022-11-15 ニンバス サターン, インコーポレイテッド Hpk1アンタゴニストおよびその使用
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021072116A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
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
MX2022005215A (es) 2019-11-01 2022-06-08 Navitor Pharm Inc Metodos de tratamiento que usan un modulador de la diana mecanicista del complejo 1 de rapamicina (mtorc1).
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
EP4061367A1 (en) 2019-11-22 2022-09-28 Incyte Corporation Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
WO2021110805A1 (en) * 2019-12-04 2021-06-10 Idorsia Pharmaceuticals Ltd Combination of an azetidine lpa1 receptor antagonist with pirfenidone and/or nintedanib for use in the treatment of fibrotic diseases
US11819476B2 (en) 2019-12-05 2023-11-21 Janssen Pharmaceutica Nv Rapamycin analogs and uses thereof
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
US11779578B2 (en) 2019-12-17 2023-10-10 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
CA3162502A1 (en) 2019-12-23 2021-07-01 Yi Zhang Smarca degraders and uses thereof
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN115348864A (zh) 2020-02-05 2022-11-15 纯技术Lyt股份有限公司 神经甾体的脂质前药
AR121506A1 (es) 2020-03-03 2022-06-08 Pic Therapeutics Inc Inhibidores del eif4e y sus usos
PH12022552458A1 (en) 2020-03-19 2024-01-22 Kymera Therapeutics Inc Mdm2 degraders and uses thereof
CN113443986A (zh) * 2020-03-27 2021-09-28 南京药石科技股份有限公司 一种合成3-氧代-1-环丁烷羧酸的中间体的制备方法
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
CN113582901A (zh) * 2020-05-01 2021-11-02 浙江瑞博制药有限公司 一种氧化反应氧化醇制备醛或酮的方法
AU2021270458A1 (en) 2020-05-13 2022-11-10 AbbVie Deutschland GmbH & Co. KG Anti-hemojuvelin (HJV) antibodies for treating myelofibrosis
PT4157831T (pt) 2020-06-02 2024-12-20 Incyte Corp Processos de preparação de um inibidor de jak1
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US20230250110A1 (en) 2020-06-03 2023-08-10 Kymera Therapeutics, Inc. Deuterated irak degraders and uses thereof
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
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
LT4175719T (lt) 2020-07-02 2025-08-25 Incyte Corporation Tricikliniai karbamido dariniai kaip jak2 v617f inhibitoriai
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
CN111999400B (zh) * 2020-07-15 2022-07-01 安徽联创生物医药股份有限公司 一种用hplc分离测定巴瑞替尼原料药杂质的方法
CN111875534B (zh) * 2020-08-10 2022-06-17 烟台大学 1,8-二甲酰基咔唑的安全高效制备方法
CN111848491B (zh) * 2020-08-10 2022-06-17 烟台大学 1-甲酰基咔唑的制备方法
CA3186504A1 (en) 2020-08-17 2022-02-24 Stephen J. Blakemore Bicycle conjugates specific for nectin-4 and uses thereof
KR20230095923A (ko) 2020-08-18 2023-06-29 인사이트 코포레이션 Jak1 억제제를 제조하기 위한 공정 및 중간체
US11905292B2 (en) 2020-08-18 2024-02-20 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
CN116601131A (zh) 2020-10-23 2023-08-15 林伯士克洛索有限公司 Ctps1抑制剂及其用途
MX2023004591A (es) 2020-10-23 2023-07-06 Elanco Us Inc Inhibidores de janus cinasas (jak) que tienen una distribución de tamaño de partícula específica.
CN114437079B (zh) * 2020-10-30 2024-11-01 杭州邦顺制药有限公司 吡咯嘧啶五元氮杂环化合物的晶型
WO2022120354A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
US11957661B2 (en) 2020-12-08 2024-04-16 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
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
JP2024503300A (ja) 2020-12-30 2024-01-25 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
CN117098757A (zh) 2021-02-02 2023-11-21 里米诺生物科学有限公司 Gpr84拮抗剂和其用途
CA3206499A1 (en) 2021-02-02 2022-08-11 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
CN118420621A (zh) * 2021-02-07 2024-08-02 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
CN114907353A (zh) * 2021-02-09 2022-08-16 明慧医药(杭州)有限公司 一种前药化合物及其制备方法和用途
JP2024506909A (ja) 2021-02-12 2024-02-15 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
AU2022220043A1 (en) 2021-02-15 2023-08-31 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
JP2024506657A (ja) 2021-02-15 2024-02-14 カイメラ セラピューティクス, インコーポレイテッド Irak4分解剤およびその使用
AR125273A1 (es) 2021-02-25 2023-07-05 Incyte Corp Lactamas espirocíclicas como inhibidores de jak2 v617f
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
WO2022187856A1 (en) 2021-03-05 2022-09-09 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
WO2022213062A1 (en) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
EP4319756A4 (en) 2021-04-09 2025-02-26 Nimbus Clio, Inc. CBL-B MODULATORS AND USES THEREOF
IL307673A (en) 2021-04-16 2023-12-01 Ikena Oncology Inc MEK inhibitors and their use
MX2023013052A (es) 2021-05-03 2024-01-12 Incyte Corp Inhibidores de la via de la cinasa jano 1 (jak1) para el tratamiento del prurigo nodularis.
CA3217792A1 (en) 2021-05-07 2022-11-10 Kymera Therapeutics, Inc Cdk2 degraders and uses thereof
EP4370504A1 (en) 2021-07-12 2024-05-22 Incyte Corporation Process and intermediates for preparing baricitinib
CA3224068A1 (en) 2021-07-30 2023-02-02 Eli Lilly And Company Treatment of hand eczema with baricitinib
EP4392422A1 (en) 2021-08-25 2024-07-03 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
WO2023028238A1 (en) 2021-08-25 2023-03-02 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
CN118302168A (zh) 2021-10-29 2024-07-05 凯麦拉医疗公司 Irak4降解剂和其制备
CN114373808B (zh) * 2021-11-26 2023-11-10 江苏科来材料科技有限公司 一种高效晶硅电池
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CN114149437A (zh) * 2021-12-24 2022-03-08 安徽大学 一种吡咯并嘧啶五元氮杂环衍生物及其制备方法和用途
AU2023214044A1 (en) 2022-01-31 2024-08-08 Kymera Therapeutics, Inc. Irak degraders and uses thereof
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
TW202337453A (zh) 2022-03-17 2023-10-01 美商英塞特公司 作為jak2 v617f抑制劑之三環脲化合物
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
EP4532470A1 (en) 2022-05-25 2025-04-09 Ikena Oncology, Inc. Mek inhibitors and uses thereof
CN117384163A (zh) * 2022-07-05 2024-01-12 盛世泰科生物医药技术(苏州)股份有限公司 一种含偕二氟基的化合物及其制备方法和用途
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
IL318577A (en) 2022-08-02 2025-03-01 Liminal Biosciences Ltd ARYL-TRIAZOLYL AND RELATED GPR84 ANTAGONISTS AND THEIR USES
JP2025527248A (ja) 2022-08-02 2025-08-20 リミナル・バイオサイエンシーズ・リミテッド 置換ピリドンgpr84アンタゴニスト及びその使用
CN115181103B (zh) * 2022-08-16 2023-11-07 上海博悦生物科技有限公司 一种巴瑞替尼的制备方法
TW202430148A (zh) 2022-11-22 2024-08-01 美商皮克醫療公司 eIF4E抑制劑及其用途
CN118255769A (zh) * 2022-12-28 2024-06-28 格格巫(珠海)生物科技有限公司 一种立体异构体的制备方法及中间体
WO2024193496A1 (zh) * 2023-03-17 2024-09-26 北京普祺医药科技股份有限公司 吡咯并嘧啶化合物或其可药用盐的制备方法
CN116444529B (zh) * 2023-06-16 2023-12-05 药康众拓(江苏)医药科技有限公司 一种氘代氮杂环丁烷类jak抑制剂及其用途
WO2025062372A1 (en) 2023-09-21 2025-03-27 Takeda Pharmaceutical Company Limited Tyk2 inhibitors for use in the treatment of inflammatory bowel disease

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070135461A1 (en) * 2005-12-13 2007-06-14 Rodgers James D Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors

Family Cites Families (73)

* 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
PL324486A1 (en) 1995-07-05 1998-05-25 Du Pont Fungicidal pyrimidinones
DK0836605T3 (da) 1995-07-06 2002-05-13 Novartis Ag Pyrrolopyrimidiner og fremgangsmåder til deres fremstilling
JP2002517396A (ja) 1998-06-04 2002-06-18 アボット・ラボラトリーズ 細胞接着阻害抗炎症性化合物
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
CZ20004727A3 (cs) 1998-06-19 2002-03-13 Pfizer Products Inc. Deriváty pyrrolo[2,3-d] pyrimidinu
CN1152031C (zh) 1998-08-11 2004-06-02 诺瓦提斯公司 具有血管生成抑制活性的异喹啉衍生物
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
WO2000063168A1 (en) 1999-04-16 2000-10-26 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
NZ518884A (en) 1999-12-10 2004-02-27 Pfizer Prod Inc Pyrrolo[2,3-d]pyrimidine compounds
KR100755622B1 (ko) 1999-12-24 2007-09-04 아벤티스 파마 리미티드 아자인돌
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
AU2001274598A1 (en) 2000-06-23 2002-01-02 Mitsubishi Pharma Corporation Antitumor effect potentiators
PL359563A1 (en) 2000-06-26 2004-08-23 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine compounds as immunosuppressive agents
DE60105023T2 (de) 2000-06-28 2005-08-18 Smithkline Beecham P.L.C., Brentford Nassvermahlungsverfahren
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
US20040102455A1 (en) 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
ES2274986T3 (es) 2001-08-01 2007-06-01 MERCK & CO., INC. Derivados de benzimidazo 4,5-f/isoquinolinona.
ATE420879T1 (de) 2001-09-19 2009-01-15 Aventis Pharma Sa Indolizine als kinaseproteinhemmer
DE60213842T2 (de) 2001-10-30 2007-09-06 Novartis Ag Staurosporin-derivate als hemmer der flt3-rezeptor-tyrosinkinase-wirkung
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
TW200406374A (en) 2002-05-29 2004-05-01 Novartis Ag Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
EP1541563A4 (en) 2002-07-10 2007-11-07 Ono Pharmaceutical Co ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE
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
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
EP1572213A1 (en) 2002-11-26 2005-09-14 Pfizer Products Inc. Method of treatment of transplant rejection
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
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
JP2007512316A (ja) 2003-11-25 2007-05-17 ファイザー・プロダクツ・インク アテローム性動脈硬化症の治療方法
JP2007514729A (ja) 2003-12-17 2007-06-07 ファイザー・プロダクツ・インク 移植拒絶反応の治療方法
US20050153989A1 (en) 2004-01-13 2005-07-14 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
NZ584499A (en) 2004-03-30 2011-08-26 Vertex Pharma Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods 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
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
RU2415678C2 (ru) 2004-05-03 2011-04-10 Новартис Аг Комбинации, включающие агонист рецептора s1p и ингибитор киназы jak3
US20060074102A1 (en) 2004-05-14 2006-04-06 Kevin Cusack Kinase inhibitors as therapeutic agents
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
EP1760071A4 (en) 2004-06-23 2008-03-05 Ono Pharmaceutical Co COMPOUND WITH S1P RECEPTOR BINDING ABILITY AND USE THEREOF
WO2006013114A1 (en) 2004-08-06 2006-02-09 Develogen Aktiengesellschaft Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
KR20070085433A (ko) 2004-11-24 2007-08-27 노파르티스 아게 Jak 저해제들과 bcr-abl, flt-3, fak 또는raf 키나제 저해제들 중 하나 이상의 조합물
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.
RU2434871C2 (ru) 2005-02-03 2011-11-27 Вертекс Фармасьютикалз Инкорпорейтед Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
CN101228161B (zh) 2005-05-20 2012-10-10 沃泰克斯药物股份有限公司 适用作蛋白激酶抑制剂的吡咯并吡啶类
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
EP1926735A1 (en) 2005-09-22 2008-06-04 Incyte Corporation Tetracyclic inhibitors of janus kinases
EP1931674B1 (en) 2005-09-30 2012-12-12 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
WO2007076423A2 (en) 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
UA95940C2 (uk) 2006-01-17 2011-09-26 Вертекс Фармасьютикалс Інкорпорейтед Азаіндоли як інгібітори кіназ януса
CN101460499A (zh) 2006-04-05 2009-06-17 沃泰克斯药物股份有限公司 可用作janus激酶抑制剂的去氮杂嘌呤
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
EP3495369B1 (en) 2007-06-13 2021-10-27 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070135461A1 (en) * 2005-12-13 2007-06-14 Rodgers James D Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors

Also Published As

Publication number Publication date
CY2017024I1 (el) 2017-11-14
ES2602577T3 (es) 2017-02-21
KR20100121657A (ko) 2010-11-18
KR101240882B1 (ko) 2013-03-11
PA8819201A1 (es) 2010-07-27
UY31705A1 (es) 2009-08-03
PE20140099A1 (es) 2014-02-06
CL2009000576A1 (es) 2009-06-19
JP2011514909A (ja) 2011-05-12
BRPI0909040B8 (pt) 2021-05-25
EP2288610B1 (en) 2016-08-31
PE20091712A1 (es) 2009-11-21
EA017218B1 (ru) 2012-10-30
DK2288610T3 (en) 2016-11-28
NZ587928A (en) 2012-08-31
US20090233903A1 (en) 2009-09-17
MX2010010012A (es) 2010-10-20
IL208023A (en) 2015-08-31
CO6290658A2 (es) 2011-06-20
BRPI0909040B1 (pt) 2019-10-22
PT2288610T (pt) 2016-10-17
EA201071057A1 (ru) 2011-02-28
RS55263B1 (sr) 2017-02-28
LT2288610T (lt) 2016-12-12
DOP2010000270A (es) 2010-10-15
UA101493C2 (ru) 2013-04-10
HN2010001761A (es) 2013-09-02
HUS1700031I1 (hu) 2017-09-28
KR20120108042A (ko) 2012-10-04
LTPA2017023I1 (lt) 2017-08-10
NO2017033I1 (no) 2017-07-11
IL208023A0 (en) 2010-12-30
US20130225556A1 (en) 2013-08-29
HRP20161390T1 (hr) 2016-12-02
LUC00027I2 (forum.php) 2017-09-25
SG191660A1 (en) 2013-07-31
TW200942545A (en) 2009-10-16
US8420629B2 (en) 2013-04-16
WO2009114512A1 (en) 2009-09-17
EP2288610B8 (en) 2016-10-12
MY165582A (en) 2018-04-05
NO2017033I2 (no) 2017-07-11
ECSP10010475A (es) 2010-10-30
TN2010000415A1 (en) 2011-12-29
LUC00027I1 (forum.php) 2017-07-12
JP2013155179A (ja) 2013-08-15
TWI444382B (zh) 2014-07-11
CA2718271A1 (en) 2009-09-17
JP5275371B2 (ja) 2013-08-28
MA32219B1 (fr) 2011-04-01
CN103788098A (zh) 2014-05-14
SI2288610T1 (sl) 2016-11-30
CY2017024I2 (el) 2017-11-14
HK1149005A1 (zh) 2011-09-23
US20120077798A1 (en) 2012-03-29
AU2009223640A1 (en) 2009-09-17
PL2288610T3 (pl) 2017-12-29
SV2010003662A (es) 2011-03-17
DOP2013000036A (es) 2013-03-15
NL300886I2 (nl) 2017-10-24
CN102026999A (zh) 2011-04-20
HUE029767T2 (en) 2017-04-28
EP2288610A1 (en) 2011-03-02
LTC2288610I2 (lt) 2019-02-25
CY1118176T1 (el) 2017-06-28
ZA201006000B (en) 2012-01-25
US8158616B2 (en) 2012-04-17
BRPI0909040A8 (pt) 2017-12-12
BRPI0909040A2 (forum.php) 2017-09-19
CN102026999B (zh) 2014-03-05
CA2718271C (en) 2014-05-06
AR070828A1 (es) 2010-05-05

Similar Documents

Publication Publication Date Title
AU2009223640B2 (en) Azetidine and cyclobutane derivatives as jak inhibitors
US11851442B2 (en) Tricyclic fused thiophene derivatives as JAK inhibitors
CN107698569B (zh) 作为jak抑制剂的联吡唑衍生物
EP2721028B1 (en) Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
EP2640725B1 (en) Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
WO2011028685A1 (en) Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
AU2013201219A1 (en) Azetidine and cyclobutane derivatives as jak inhibitors
HK1149005B (en) Azetidine and cyclobutane derivatives as jak inhibitors
HK1197056B (en) Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
PC Assignment registered

Owner name: INCYTE HOLDINGS CORPORATION

Free format text: FORMER OWNER WAS: INCYTE CORPORATION

NC Extension of term for standard patent requested (sect. 70)

Free format text: PRODUCT NAME: OLUMIANT BARICITINIB

Filing date: 20180123

NDB Extension of term for standard patent granted (sect.76)

Free format text: PRODUCT NAME: OLUMIANT BARICITINIB

Filing date: 20180123

Extension date: 20330123