KR101240882B1 - Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체 - Google Patents

Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체 Download PDF

Info

Publication number
KR101240882B1
KR101240882B1 KR1020107020309A KR20107020309A KR101240882B1 KR 101240882 B1 KR101240882 B1 KR 101240882B1 KR 1020107020309 A KR1020107020309 A KR 1020107020309A KR 20107020309 A KR20107020309 A KR 20107020309A KR 101240882 B1 KR101240882 B1 KR 101240882B1
Authority
KR
South Korea
Prior art keywords
delete delete
mol
mixture
reaction
pyrrolo
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
Application number
KR1020107020309A
Other languages
English (en)
Korean (ko)
Other versions
KR20100121657A (ko
Inventor
제임스 디. 로저스
스테이시 셰퍼드
윤-롱 리
지아쳉 조우
핑리 리우
데이비드 멜로니
마이클 시아
Original Assignee
인사이트 코포레이션
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=KR101240882(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 인사이트 코포레이션 filed Critical 인사이트 코포레이션
Publication of KR20100121657A publication Critical patent/KR20100121657A/ko
Application granted granted Critical
Publication of KR101240882B1 publication Critical patent/KR101240882B1/ko
Assigned to 인사이트 홀딩스 코포레이션 reassignment 인사이트 홀딩스 코포레이션 권리의 전부이전등록 Assignors: 인사이트 코포레이션
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Mechanical Engineering (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020107020309A 2008-03-11 2009-03-10 Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체 Active KR101240882B1 (ko)

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
KR1020127020848A Division KR20120108042A (ko) 2008-03-11 2009-03-10 Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체

Publications (2)

Publication Number Publication Date
KR20100121657A KR20100121657A (ko) 2010-11-18
KR101240882B1 true KR101240882B1 (ko) 2013-03-11

Family

ID=40591836

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020107020309A Active KR101240882B1 (ko) 2008-03-11 2009-03-10 Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체
KR1020127020848A Ceased KR20120108042A (ko) 2008-03-11 2009-03-10 Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020127020848A Ceased KR20120108042A (ko) 2008-03-11 2009-03-10 Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체

Country Status (43)

Country Link
US (3) US8158616B2 (https=)
EP (1) EP2288610B8 (https=)
JP (2) JP5275371B2 (https=)
KR (2) KR101240882B1 (https=)
CN (2) CN102026999B (https=)
AR (1) AR070828A1 (https=)
AU (1) AU2009223640B2 (https=)
BR (1) BRPI0909040B8 (https=)
CA (1) CA2718271C (https=)
CL (1) CL2009000576A1 (https=)
CO (1) CO6290658A2 (https=)
CY (2) CY1118176T1 (https=)
DK (1) DK2288610T3 (https=)
DO (2) DOP2010000270A (https=)
EA (1) EA017218B1 (https=)
EC (1) ECSP10010475A (https=)
ES (1) ES2602577T3 (https=)
HN (1) HN2010001761A (https=)
HR (1) HRP20161390T1 (https=)
HU (2) HUE029767T2 (https=)
IL (1) IL208023A (https=)
LT (2) LT2288610T (https=)
LU (1) LUC00027I2 (https=)
MA (1) MA32219B1 (https=)
MX (1) MX2010010012A (https=)
MY (1) MY165582A (https=)
NL (1) NL300886I2 (https=)
NO (1) NO2017033I1 (https=)
NZ (1) NZ587928A (https=)
PA (1) PA8819201A1 (https=)
PE (2) PE20091712A1 (https=)
PL (1) PL2288610T3 (https=)
PT (1) PT2288610T (https=)
RS (1) RS55263B1 (https=)
SG (1) SG191660A1 (https=)
SI (1) SI2288610T1 (https=)
SV (1) SV2010003662A (https=)
TN (1) TN2010000415A1 (https=)
TW (1) TWI444382B (https=)
UA (1) UA101493C2 (https=)
UY (1) UY31705A1 (https=)
WO (1) WO2009114512A1 (https=)
ZA (1) ZA201006000B (https=)

Families Citing this family (316)

* 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
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
CA2673038C (en) * 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
KR20150036210A (ko) 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염
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.
UA104849C2 (uk) * 2007-11-16 2014-03-25 Інсайт Корпорейшн 4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus
WO2009120717A2 (en) 2008-03-24 2009-10-01 Medivation Technologies, Inc. Pyrido [3, 4-b] indoles and methods of use
CN102131389A (zh) * 2008-06-20 2011-07-20 健泰科生物技术公司 三唑并吡啶jak抑制剂化合物和方法
WO2009155565A1 (en) * 2008-06-20 2009-12-23 Genentech, Inc. 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.
TWI720517B (zh) 2009-01-15 2021-03-01 美商英塞特公司 製造ｊａｋ抑制劑之方法及相關中間化合物
SI2432472T1 (sl) * 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru) 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
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
AU2015205858B2 (en) * 2010-03-10 2017-04-13 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EP3354652B1 (en) * 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
KR20130094710A (ko) 2010-04-14 2013-08-26 어레이 바이오파마 인크. Ｊａｋ 키나아제의 억제제로서 5,7-치환된-이미다조［1,2-ｃ］피리미딘
PE20130216A1 (es) 2010-05-21 2013-02-27 Incyte Corp Formulacion topica para un inhibidor de jak
EA036970B1 (ru) * 2010-11-19 2021-01-21 Инсайт Холдингс Корпорейшн Применение {1-{1-[3-фтор-2-(трифтометил)изоникотиноил] пиперидин-4-ил}-3-[4-(7h-пирроло[2,3-d]пиримидин-4-ил)-1н-пиразол-1-ил]азетидин-3-ил}ацетонитрила для лечения заболеваний, связанных с активностью jak1
PE20140146A1 (es) * 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
ES2541289T3 (es) * 2010-12-01 2015-07-17 Nissan Chemical Industries, Ltd. Compuestos de pirazol que tienen un efecto terapéutico sobre mieloma múltiple
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
US8791132B2 (en) 2011-02-18 2014-07-29 Medivation Technologies, Inc. Compounds and methods for treatment of hypertension
KR101904565B1 (ko) * 2011-03-08 2018-10-04 지이 헬쓰케어 리미티드 1-아미노-3-히드록시-시클로부탄-1-카르복실산 유도체의 제조
CN103797010B (zh) * 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) * 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
CA2849168A1 (en) * 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Cycloalkylnitrile pyrazole 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
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
JP6280546B2 (ja) 2012-06-26 2018-02-14 デル マー ファーマシューティカルズ ジアンヒドロガラクチトール、ジアセチルジアンヒドロガラクチトール、ジブロモズルシトール、又はこれらの類似体若しくは誘導体を用いた、遺伝子多型又はａｈｉ１の調節不全若しくは変異を有する患者におけるチロシンキナーゼインヒビター抵抗性悪性腫瘍を処置するための方法
BR112015002152B1 (pt) * 2012-08-02 2021-04-27 Nerviano Medical Sciences S.R.L. Compostos de pirróis substituídos ativos como inibidores de quinases, processo para a preparação de tais compostos, composição farmacêutica, método in vitro para a inibição da atividade de proteínas quinases da família jak e produto compreendendo os referidos compostos
WO2014028756A1 (en) * 2012-08-17 2014-02-20 Concert Pharmaceuticals, Inc. Deuterated baricitinib
TWI646099B (zh) 2012-11-01 2019-01-01 英塞特控股公司 作爲ｊａｋ抑制劑之三環稠合噻吩衍生物
PH12020551186B1 (en) 2012-11-15 2024-03-20 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
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
RS62867B1 (sr) 2013-03-06 2022-02-28 Incyte Holdings Corp Postupci i intermedijeri za dobijanje inhibitora jak
WO2014146249A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
KR20160061911A (ko) 2013-04-08 2016-06-01 데니스 엠. 브라운 최적하 투여된 화학 화합물의 치료 효과
HUE033587T2 (hu) 2013-05-17 2017-12-28 Incyte Corp Bipirazol-származékok mint JAK inhibitorok
CN112472699A (zh) 2013-07-26 2021-03-12 种族肿瘤学公司 改善比生群及衍生物的治疗益处的组合方法
SMT202000315T1 (it) 2013-08-07 2020-07-08 Incyte Corp Forme di dosaggio a rilascio prolungato per un inibitore di jak1
CA2921568A1 (en) 2013-08-20 2015-02-25 Incyte Corporation Survival benefit in patients with solid tumors with elevated c-reactive protein levels
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
JP6602779B2 (ja) 2014-02-13 2019-11-06 インサイト・コーポレイション Ｌｓｄ１阻害剤としてのシクロプロピルアミン類
EP3105218B1 (en) 2014-02-13 2019-09-25 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015131080A1 (en) 2014-02-28 2015-09-03 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
KR20160136323A (ko) 2014-02-28 2016-11-29 인사이트 코포레이션 골수형성이상증후군 치료용 jak1 억제제
EP3134412A1 (en) * 2014-03-28 2017-03-01 Sun Pharmaceutical Industries Limited Amorphous form of baricitinib
MA39987A (fr) 2014-04-30 2017-03-08 Incyte Corp Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées
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
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
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
TW201618775A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑、ｐｄ－１抑制劑及／或ｐｄ－ｌ１抑制劑之治療組合物
AR101504A1 (es) 2014-08-11 2016-12-21 Acerta Pharma Bv Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6
PL3179991T3 (pl) 2014-08-11 2022-02-14 Acerta Pharma B.V. Kombinacje terapeutyczne inhibitora btk i inhibitora bcl-2
CN117088931A (zh) 2014-08-12 2023-11-21 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
CN107148425B (zh) 2014-10-29 2021-08-03 拜斯科阿迪有限公司 对mt1-mmp特异性的双环肽配体
WO2016088094A1 (en) * 2014-12-05 2016-06-09 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
WO2016125080A2 (en) * 2015-02-02 2016-08-11 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
WO2016141891A1 (zh) * 2015-03-11 2016-09-15 苏州晶云药物科技有限公司 Jak抑制剂的晶型及其制备方法
EP3277689B1 (en) 2015-04-03 2019-09-04 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
MY189367A (en) 2015-08-12 2022-02-08 Incyte Corp Salts of an lsd1 inhibitor
TWI707852B (zh) 2015-09-02 2020-10-21 美商林伯士拉克許米公司 Tyk2 抑制劑及其用途
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
AU2016342027B2 (en) 2015-10-23 2021-05-13 Navitor Pharmaceuticals, Inc. Modulators of Sestrin-GATOR2 interaction and uses thereof
RU2601410C1 (ru) * 2015-11-13 2016-11-10 ЗАО "Р-Фарм" {3-[(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)АЗОЛИЛ]АЗЕТИДИН-3-ИЛ}АЦЕТОНИТРИЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС КИНАЗ
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
ES2830446T3 (es) * 2015-12-11 2021-06-03 Sichuan Kelun Biotech Biopharmaceutical Co Ltd Derivado de azetidina, método de preparación del mismo y uso del mismo
EP3389664A4 (en) 2015-12-14 2020-01-08 Raze Therapeutics Inc. MTHFD2 CAFFEIN INHIBITORS 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
CN107641125A (zh) * 2016-02-01 2018-01-30 上海宣创生物科技有限公司 巴瑞克替尼磷酸盐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
DK3426243T3 (da) 2016-03-09 2021-07-19 Raze Therapeutics Inc 3-phosphoglyceratdehydrogenase-inhibitorer og anvendelser deraf
EP4234552A3 (en) 2016-03-09 2023-10-18 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
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
TWI833686B (zh) 2016-04-22 2024-03-01 美商英塞特公司 Lsd1 抑制劑之調配物
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
EP3472129A4 (en) 2016-06-21 2019-12-04 X4 Pharmaceuticals, Inc. CXCR4 INHIBITORS AND USES THEREOF
CN109640988A (zh) 2016-06-21 2019-04-16 X4 制药有限公司 Cxcr4抑制剂及其用途
ES2870920T3 (es) 2016-06-21 2021-10-28 X4 Pharmaceuticals Inc Inhibidores de CXCR4 y usos de los mismos
KR102598246B1 (ko) * 2016-07-26 2023-11-02 톈진 롱보진 파마시우티컬 씨오., 엘티디. Jak 저해제로서 헤테로사이클릭 화합물, 및 이의 염 및 치료학적 용도
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
US10323036B2 (en) 2016-10-14 2019-06-18 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
EP3528816A4 (en) 2016-10-21 2020-04-08 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
WO2018089499A1 (en) 2016-11-08 2018-05-17 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
CA3043768A1 (en) 2016-11-29 2018-06-07 PureTech Health LLC Exosomes for delivery of therapeutic agents
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
WO2018115203A1 (en) 2016-12-23 2018-06-28 Bicyclerd Limited Peptide derivatives having novel linkage structures
US10624968B2 (en) 2017-01-06 2020-04-21 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
TW202515876A (zh) 2017-03-08 2025-04-16 日商武田藥品工業股份有限公司 Tyk2抑制劑及其用途
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
PL3615019T3 (pl) 2017-04-26 2026-01-19 Navitor Pharmaceuticals, Inc. Modulator interakcji sestryna-gator2 do zastosowania w leczeniu depresji opornej na leczenie
US10857196B2 (en) 2017-04-27 2020-12-08 Bicycletx Limited Bicyclic peptide ligands and uses thereof
PH12019502605A1 (en) 2017-05-23 2020-10-26 Theravance Biopharma R&D Ip Llc Glucuronide prodrugs of janus kinase inhibitors
JP7120505B2 (ja) * 2017-06-07 2022-08-17 シチュアン ケルン－バイオテック バイオファーマシューティカル カンパニー リミテッド アゼチジン誘導体の固体形態並びにその調製方法及びその使用
CN121318982A (zh) * 2017-06-22 2026-01-13 礼来公司 巴瑞克替尼的晶型及其制备方法
EP3645549A1 (en) 2017-06-26 2020-05-06 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
SI3658557T1 (sl) 2017-07-28 2024-10-30 Takeda Pharmaceutical Company Limited Zaviralci TYK2 in njihova uporaba
JP7670481B2 (ja) 2017-08-04 2025-04-30 バイスクルテクス・リミテッド Ｃｄ１３７に対して特異的な二環式ペプチドリガンド
WO2019034868A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF
WO2019034866A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited BICYCLIC PEPTIDE LIGANDS CONJUGATES AND USES THEREOF
CA3077739A1 (en) 2017-08-29 2019-03-07 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
US11358948B2 (en) 2017-09-22 2022-06-14 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
WO2019060742A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc AGENTS FOR DEGRADING PROTEINS 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
KR102717072B1 (ko) 2017-10-18 2024-10-15 인사이트 코포레이션 Pi3k-감마 저해제로서의 3차 하이드록시기로 치환된 축합된 이미다졸 유도체
KR102821964B1 (ko) * 2017-11-03 2025-06-19 어클라리스 쎄라퓨틱스, 인코포레이티드 치환된 피롤로피리미딘 jak 억제제 및 이의 제조 및 사용 방법
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
WO2019113487A1 (en) 2017-12-08 2019-06-13 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
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID PRODRUGS AND THEIR USES
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
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
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
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
JP7229257B2 (ja) 2018-01-29 2023-02-28 メルク パテント ゲーエムベーハー Ｇｃｎ２阻害剤およびその使用
BR112020015396A2 (pt) 2018-01-29 2020-12-08 Merck Patent Gmbh Inididores de gcn2 e usos dos mesmos
SG11202007164UA (en) 2018-01-30 2020-08-28 Incyte Corp Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
KR102925957B1 (ko) 2018-02-16 2026-02-11 인사이트 코포레이션 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
CN111902429A (zh) 2018-02-23 2020-11-06 拜斯科技术开发有限公司 多聚体双环肽配体
EP3759086A1 (en) 2018-02-27 2021-01-06 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
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
CA3097025A1 (en) 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
HRP20241163T1 (hr) 2018-04-24 2024-11-22 Merck Patent Gmbh Antiproliferacijski spojevi i njihova uporaba
ES2969982T3 (es) 2018-04-24 2024-05-23 Vertex Pharma Compuestos de pteridinona 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
MX2020012503A (es) * 2018-05-25 2021-08-11 Kartos Therapeutics Inc Métodos de tratamiento de neoplasias mieloproliferativas.
EP3805219A4 (en) * 2018-06-06 2022-03-23 Gengle Therapeutics, Inc. PYRAZOLOPYRIMIDI DERIVATIVE, ITS USE AND PHARMACEUTICAL COMPOSITION
WO2019241789A1 (en) 2018-06-15 2019-12-19 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
IL279489B2 (en) 2018-06-22 2025-10-01 Bicycletx Ltd Bicyclic peptide ligands specific for nectin-4, a drug conjugate containing the peptide ligands and a pharmaceutical composition containing the drug conjugate
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
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
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
WO2020051424A1 (en) 2018-09-07 2020-03-12 Pic Therapeutics Eif4e inhibitors and uses thereof
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
WO2020072870A1 (en) 2018-10-05 2020-04-09 Johnson Matthey Public Limited Company Co-crystal forms of baricitinib
CN113271940A (zh) 2018-10-15 2021-08-17 林伯士拉克许米公司 Tyk2抑制剂和其用途
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
WO2020084305A1 (en) 2018-10-23 2020-04-30 Bicycletx Limited Bicyclic peptide ligands and uses thereof
EP3870158A4 (en) 2018-10-24 2022-08-10 Navitor Pharmaceuticals, Inc. Polymorphic compounds and uses thereof
CA3117969A1 (en) 2018-10-31 2020-05-07 Incyte Corporation Combination therapy for treatment of hematological diseases
CA3119773A1 (en) 2018-11-30 2020-06-04 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CA3120866A1 (en) 2018-11-30 2020-06-04 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
GB201820295D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands 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
WO2020128527A1 (en) 2018-12-21 2020-06-25 Bicyclerd Limited Bicyclic peptide ligands specific for pd-l1
US12492224B2 (en) 2018-12-21 2025-12-09 Bicycletx Limited Bicyclic peptide ligands specific for PD-L1
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
CN113348021B (zh) 2019-01-23 2025-07-11 武田药品工业株式会社 Tyk2抑制剂和其用途
MX2021008984A (es) 2019-01-30 2021-09-08 Felicamed Biotechnology Co Ltd Inhibidor jak y metodo de preparacion del mismo.
US20220135566A1 (en) 2019-02-05 2022-05-05 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
EP3939979A4 (en) 2019-03-14 2022-04-06 Shanghai Synergy Pharmaceutical Sciences Co., Ltd Jak kinase inhibitor, preparation method for same, and applications thereof in field of medicine
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
SG11202110828UA (en) 2019-04-02 2021-10-28 Bicycletx Ltd Bicycle toxin conjugates and uses thereof
CN120574283A (zh) 2019-04-05 2025-09-02 凯麦拉医疗公司 Stat降解剂和其用途
EP3725305A1 (en) 2019-04-17 2020-10-21 Zentiva K.S. Pharmaceutical composition containing baricitinib hydrobromide
US11548895B2 (en) * 2019-04-24 2023-01-10 Elanco Us Inc. Process for making crystalline 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl)azetidin-3-yl)acetonitrile
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
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders 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
PH12022500002A1 (en) 2019-06-28 2023-04-03 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
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
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
US11845724B2 (en) 2019-09-11 2023-12-19 Vincere Biosciences, Inc. USP30 inhibitors and uses thereof
MX2022002877A (es) 2019-09-13 2022-08-08 Nimbus Saturn Inc Antagonistas de cinasa progenitora hematopoyetica 1 (hpk1) y sus usos.
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
EP4041204A1 (en) 2019-10-10 2022-08-17 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021072098A1 (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
US11723890B2 (en) 2019-11-01 2023-08-15 Navitor Pharmaceuticals, Inc. Methods of treatment using an mTORC1 modulator
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
JP7717065B2 (ja) 2019-11-22 2025-08-01 インサイト コーポレーション Ａｌｋ２阻害剤及びｊａｋ２阻害剤を含む併用療法
JP7665619B2 (ja) * 2019-12-04 2025-04-21 イドルシア・ファーマシューティカルズ・リミテッド 線維性疾患の治療に使用するためのアゼチジンｌｐａ１受容体アンタゴニストのピルフェニドン及び／又はニンテダニブとの合剤
AU2020397938A1 (en) 2019-12-05 2022-06-23 Janssen Pharmaceutica Nv Rapamycin analogs and uses thereof
WO2021119159A1 (en) 2019-12-10 2021-06-17 Kymera Therapeutics, Inc. Irak degraders and uses thereof
KR20220145325A (ko) 2019-12-17 2022-10-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
CA3162302A1 (en) 2019-12-19 2021-06-24 Lyne Gagnon Cycloalkyl-containing carboxylic acids and uses thereof
WO2021133917A1 (en) 2019-12-23 2021-07-01 Kymera Therapeutics, Inc. Smarca inhibitors and uses thereof
EP4081308A4 (en) 2019-12-23 2024-01-24 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
IL295362A (en) 2020-02-05 2022-10-01 Puretech Lyt Inc Lipid drug inhibitors of neurosteroids
TW202146393A (zh) 2020-03-03 2021-12-16 美商皮克醫療公司 Eif4e抑制劑及其用途
KR20230005160A (ko) 2020-03-19 2023-01-09 카이메라 쎄라퓨틱스 인코포레이티드 Mdm2 분해제 및 이의 용도
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
US20230218644A1 (en) 2020-04-16 2023-07-13 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
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
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
MX2022015221A (es) 2020-06-02 2023-03-08 Incyte Corp Procesos para preparar un inhibidor de cinasa jano 1 (jak1).
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
US20230250110A1 (en) 2020-06-03 2023-08-10 Kymera Therapeutics, Inc. Deuterated irak degraders and uses thereof
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
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
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 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
AU2021322934A1 (en) 2020-08-03 2023-03-30 Bicycletx Limited Peptide-based linkers
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
CA3186504A1 (en) 2020-08-17 2022-02-24 Stephen J. Blakemore Bicycle conjugates specific for nectin-4 and uses thereof
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
IL300557A (en) 2020-08-18 2023-04-01 Incyte Corp Process and intermediates for preparing a JAK1 inhibitor
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
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.
US12331046B2 (en) 2020-10-23 2025-06-17 Nimbus Clotho, Inc. CTPS1 inhibitors and uses thereof
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
CA3200814A1 (en) 2020-12-02 2022-06-09 Alfredo C. Castro Tead inhibitors and uses thereof
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CA3204374A1 (en) 2020-12-08 2022-06-16 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
EP4259144A4 (en) 2020-12-09 2025-08-20 Kymera Therapeutics Inc SMARCA DEGRADING AGENTS AND THEIR USES
MX2023007150A (es) 2020-12-18 2023-09-04 Boehringer Ingelheim Animal Health Usa Inc Compuestos de pirazol que contienen boro, composiciones que los comprenden, métodos y usos de los mismos.
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
CN116867758A (zh) 2020-12-30 2023-10-10 凯麦拉医疗公司 Irak降解剂和其用途
US12378229B2 (en) 2021-02-02 2025-08-05 Liminal Biosciences Limited GPR84 antagonists and uses thereof
MX2023009060A (es) 2021-02-02 2023-09-29 Liminal Biosciences Ltd Antagonistas de gpr84 y usos de estos.
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
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
EP4291235A4 (en) 2021-02-12 2025-01-08 Nimbus Saturn, Inc. HPK1 ANTAGONISTS AND USES THEREOF
CN116867494A (zh) 2021-02-15 2023-10-10 凯麦拉医疗公司 Irak4降解剂和其用途
US12171768B2 (en) 2021-02-15 2024-12-24 Kymera Therapeutics, Inc. IRAK4 degraders and uses thereof
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
US11926625B2 (en) 2021-03-05 2024-03-12 Nimbus Saturn, Inc. HPK1 antagonists and uses thereof
WO2022213062A1 (en) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
US12325697B2 (en) 2021-04-09 2025-06-10 Nimbus Clio, Inc. CBL-B modulators and uses thereof
WO2022221866A1 (en) 2021-04-16 2022-10-20 Ikena Oncology, Inc. Mek inhibitors and uses thereof
UA129643C2 (uk) 2021-05-03 2025-06-18 Інсайт Корпорейшн Інгібітори шляху jak1 для лікування вузлуватого свербця
KR20240020735A (ko) 2021-05-07 2024-02-15 카이메라 쎄라퓨틱스 인코포레이티드 Cdk2 분해제 및 그 용도
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
US20250041304A1 (en) 2021-07-30 2025-02-06 Eli Lilly And Company Treatment of Hand Eczema with Baricitinib
CA3229560A1 (en) 2021-08-25 2023-03-02 Christopher L. Vandeusen Eif4e inhibitors and uses thereof
US12157732B2 (en) 2021-08-25 2024-12-03 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
CA3236265A1 (en) 2021-10-29 2023-05-04 William Leong Irak4 degraders and synthesis 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
CA3243560A1 (en) 2022-01-31 2023-08-03 Kymera Therapeutics, Inc. Iraqi Degradation Agents and Their Uses
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
AU2023235313A1 (en) 2022-03-17 2024-10-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
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
US11878958B2 (en) 2022-05-25 2024-01-23 Ikena Oncology, Inc. MEK inhibitors and uses thereof
CN117384163B (zh) * 2022-07-05 2026-02-17 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
KR20250056924A (ko) 2022-08-02 2025-04-28 리미널 바이오사이언시스 리미티드 치환된 피리돈 gpr84 길항제 및 이의 용도
IL318577A (en) 2022-08-02 2025-03-01 Liminal Biosciences Ltd ARYL-TRIAZOLYL AND RELATED GPR84 ANTAGONISTS AND THEIR USES
US20260028330A1 (en) 2022-08-02 2026-01-29 Liminal Biosciences Limited Heteroaryl carboxamide 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
WO2024112894A1 (en) 2022-11-22 2024-05-30 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
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
CN120882718A (zh) * 2023-03-17 2025-10-31 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
AU2024312190A1 (en) 2023-06-23 2025-07-03 Kymera Therapeutics, Inc. Irak degraders and uses thereof
AU2024344754A1 (en) 2023-09-21 2026-04-02 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
WO2007117494A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases

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
JP4010563B2 (ja) 1995-07-05 2007-11-21 イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー 殺菌・殺カビ性のピリミジノン類
SI9620103A (sl) 1995-07-06 1998-10-31 Novartis Ag Pirolopirimidini in postopki za njihovo pripravo
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
AU4231299A (en) 1998-06-04 1999-12-20 Abbott Laboratories Cell adhesion-inhibiting antinflammatory compounds
SK286640B6 (sk) 1998-06-19 2009-03-05 Pfizer Products Inc. Pyrol [2,3-d] pyrimidínová zlúčenina, jej použitie na výrobu liečiva, farmaceutická kompozícia s jej obsahom, použitie jej kombinácie s ďalšími činidlami a súpravy s jej obsahom na výrobu liečiva
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
PT1107964E (pt) 1998-08-11 2010-06-11 Novartis Ag Derivados de isoquinolina com actividade inibidora da angiogénese
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
DE60037345T2 (de) 1999-12-10 2008-11-13 Pfizer Products Inc., Groton Pyrrolo(2,3-d)pyrimidin-Verbindungen
WO2001047922A2 (en) * 1999-12-24 2001-07-05 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
CN100548375C (zh) * 2000-06-23 2009-10-14 田边三菱制药株式会社 抗肿瘤作用增效剂
ATE423120T1 (de) 2000-06-26 2009-03-15 Pfizer Prod Inc Pyrroloä2,3-düpyrimidin verbindungen als immunosuppressive wirkstoffe
KR100786927B1 (ko) 2000-06-28 2007-12-17 스미스클라인비이참피이엘시이 습식 분쇄방법
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
EP1414443B1 (en) 2001-08-01 2006-11-15 Merck & Co., Inc. BENZIMIDAZO 4,5-f|ISOQUINOLINONE DERIVATIVES
BR0212760A (pt) 2001-09-19 2004-12-07 Aventis Pharma Sa Compostos quìmicos
DE60213842T2 (de) 2001-10-30 2007-09-06 Novartis Ag Staurosporin-derivate als hemmer der flt3-rezeptor-tyrosinkinase-wirkung
PY0228255A (es) 2001-12-06 2004-06-01 Pfizer Prod Inc 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
BR0309844A (pt) * 2002-05-07 2005-02-15 Control Delivery Sys Inc Processos para formação de um dispositivo para a distribuição de droga
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
AU2003252478A1 (en) * 2002-07-10 2004-02-02 Ono Pharmaceutical Co., Ltd. Ccr4 antagonist and medicinal use thereof
US7259161B2 (en) 2002-11-04 2007-08-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
NZ539901A (en) 2002-11-26 2007-09-28 Pfizer Prod 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
JP2006518381A (ja) 2003-02-07 2006-08-10 バーテックス　ファーマシューティカルズ　インコーポレイテッド プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール
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
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
EP1689407A1 (en) 2003-11-25 2006-08-16 Pfizer Products Inc. Method of treatment of atherosclerosis
SG133602A1 (en) 2003-12-17 2007-07-30 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
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
ES2364340T3 (es) 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
AU2005237254B2 (en) 2004-05-03 2010-02-04 Novartis Ag Combinations comprising a S1P receptor agonist and a JAK3 kinase inhibitor
WO2005110410A2 (en) 2004-05-14 2005-11-24 Abbott Laboratories 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
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
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
AU2005309019A1 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of 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.
KR20070104641A (ko) 2005-02-03 2007-10-26 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로 유용한 피롤로피리미딘
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
EP2354140A1 (en) 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
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
CA2621261C (en) * 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
ZA200802685B (en) 2005-09-30 2009-10-28 Vertex Pharma Deazapurines useful as inhibitors of janus kinases
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
WO2007076423A2 (en) 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
UA95940C2 (uk) 2006-01-17 2011-09-26 Вертекс Фармасьютикалс Інкорпорейтед Азаіндоли як інгібітори кіназ януса
TW200805992A (en) * 2006-07-04 2008-01-16 Benq Corp Method and apparatus for barring short message
CA2673038C (en) * 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
KR20150036210A (ko) * 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염
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
WO2007117494A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases

Also Published As

Publication number Publication date
AU2009223640B2 (en) 2013-07-04
PT2288610T (pt) 2016-10-17
RS55263B1 (sr) 2017-02-28
LUC00027I1 (https=) 2017-07-12
LTC2288610I2 (lt) 2019-02-25
HUE029767T2 (en) 2017-04-28
EA017218B1 (ru) 2012-10-30
TN2010000415A1 (en) 2011-12-29
BRPI0909040A8 (pt) 2017-12-12
ZA201006000B (en) 2012-01-25
LUC00027I2 (https=) 2017-09-25
KR20100121657A (ko) 2010-11-18
NZ587928A (en) 2012-08-31
CA2718271A1 (en) 2009-09-17
MA32219B1 (fr) 2011-04-01
BRPI0909040B1 (pt) 2019-10-22
US20090233903A1 (en) 2009-09-17
AR070828A1 (es) 2010-05-05
PE20091712A1 (es) 2009-11-21
US20120077798A1 (en) 2012-03-29
WO2009114512A1 (en) 2009-09-17
CN102026999A (zh) 2011-04-20
MY165582A (en) 2018-04-05
IL208023A0 (en) 2010-12-30
JP5275371B2 (ja) 2013-08-28
CY2017024I2 (el) 2017-11-14
CY1118176T1 (el) 2017-06-28
DOP2010000270A (es) 2010-10-15
BRPI0909040A2 (https=) 2017-09-19
KR20120108042A (ko) 2012-10-04
US20130225556A1 (en) 2013-08-29
EP2288610B1 (en) 2016-08-31
TWI444382B (zh) 2014-07-11
DK2288610T3 (en) 2016-11-28
US8158616B2 (en) 2012-04-17
CL2009000576A1 (es) 2009-06-19
IL208023A (en) 2015-08-31
MX2010010012A (es) 2010-10-20
LT2288610T (lt) 2016-12-12
CO6290658A2 (es) 2011-06-20
EA201071057A1 (ru) 2011-02-28
HN2010001761A (es) 2013-09-02
EP2288610B8 (en) 2016-10-12
ECSP10010475A (es) 2010-10-30
PA8819201A1 (es) 2010-07-27
UY31705A1 (es) 2009-08-03
ES2602577T3 (es) 2017-02-21
BRPI0909040B8 (pt) 2021-05-25
CY2017024I1 (el) 2017-11-14
HK1149005A1 (zh) 2011-09-23
UA101493C2 (ru) 2013-04-10
CN103788098A (zh) 2014-05-14
JP2011514909A (ja) 2011-05-12
CA2718271C (en) 2014-05-06
NO2017033I2 (no) 2017-07-11
HUS1700031I1 (hu) 2017-09-28
NO2017033I1 (no) 2017-07-11
SG191660A1 (en) 2013-07-31
LTPA2017023I1 (lt) 2017-08-10
TW200942545A (en) 2009-10-16
US8420629B2 (en) 2013-04-16
AU2009223640A1 (en) 2009-09-17
SV2010003662A (es) 2011-03-17
PE20140099A1 (es) 2014-02-06
EP2288610A1 (en) 2011-03-02
JP2013155179A (ja) 2013-08-15
PL2288610T3 (pl) 2017-12-29
HRP20161390T1 (hr) 2016-12-02
CN102026999B (zh) 2014-03-05
NL300886I2 (nl) 2017-10-24
DOP2013000036A (es) 2013-03-15
SI2288610T1 (sl) 2016-11-30

Similar Documents

Publication Publication Date Title
KR101240882B1 (ko) Ｊａｋ 억제제로서의 아제티딘 및 시클로부탄 유도체
US11851442B2 (en) Tricyclic fused thiophene derivatives as JAK inhibitors
CN107698569B (zh) 作为jak抑制剂的联吡唑衍生物
CN102844317B (zh) 作为Janus激酶抑制剂的环丁烷和甲基环丁烷衍生物
JP5876146B2 (ja) Ｊａｋ阻害剤としてのアゼチジニルフェニル、ピリジル、またはピラジニルカルボキサミド誘導体
AU2013201219A1 (en) Azetidine and cyclobutane derivatives as jak inhibitors
HK1149005B (en) Azetidine and cyclobutane derivatives as jak inhibitors

Legal Events

Date Code Title Description
A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

R15-X000 Change to inventor requested

St.27 status event code: A-3-3-R10-R15-oth-X000

R16-X000 Change to inventor recorded

St.27 status event code: A-3-3-R10-R16-oth-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

A107 Divisional application of patent
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

PN2301 Change of applicant

St.27 status event code: A-5-5-R10-R11-asn-PN2301

PN2301 Change of applicant

St.27 status event code: A-5-5-R10-R14-asn-PN2301

FPAY Annual fee payment

Payment date: 20151230

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

FPAY Annual fee payment

Payment date: 20161229

Year of fee payment: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

FPAY Annual fee payment

Payment date: 20171228

Year of fee payment: 6

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

S17-X000 Non-exclusive voluntary license recorded

St.27 status event code: A-4-4-S10-S17-lic-X000

A101 Application to extend term of patent right by permit
PA0101 Application to register extension of term of patent right by permit, etc.

St.27 status event code: A-4-4-G10-G18-tex-PA0101

Protection beyond ip right term event data comment text: Claim Total Quantity : 3, Claim Number : 14, 24, 33, Period Limitation Text : 1230, Comment Text : 91

FPAY Annual fee payment

Payment date: 20181227

Year of fee payment: 7

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 7

PE0702 Decision to register extension of term of patent right by permit, etc.

St.27 status event code: A-4-4-G10-G20-tex-PE0702

Protection beyond ip right term event data comment text: Claim Total Quantity : 3, Claim Number : 14, 24, 33, Period Limitation Text : 1230, Comment Text : 91

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 8

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 9

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 10

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 11

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 12

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 13

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000