RU2434871C2 - Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы - Google Patents

Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы Download PDF

Info

Publication number
RU2434871C2
RU2434871C2 RU2007132908/04A RU2007132908A RU2434871C2 RU 2434871 C2 RU2434871 C2 RU 2434871C2 RU 2007132908/04 A RU2007132908/04 A RU 2007132908/04A RU 2007132908 A RU2007132908 A RU 2007132908A RU 2434871 C2 RU2434871 C2 RU 2434871C2
Authority
RU
Russia
Prior art keywords
optionally substituted
compound
compound according
groups
group
Prior art date
Application number
RU2007132908/04A
Other languages
English (en)
Russian (ru)
Other versions
RU2007132908A (ru
Inventor
Марк В. ЛЕДЕБУР (US)
Марк В. Ледебур
Альберт К. ПИРС (US)
Альберт К. ПИРС
Гай У. БЕМИС (US)
Гай У. БЕМИС
Люк Дж. ФАРМЕР (US)
Люк Дж. Фармер
Тяньшэн ВАН (US)
Тяньшэн Ван
Дэвид МЕССЕРСМИТ (US)
Дэвид МЕССЕРСМИТ
Джон П. ДАФФИ (US)
Джон П. Даффи
Цзянь ВАН (US)
Цзянь ВАН
Франческо Г. САЛИТУРО (US)
Франческо Г. САЛИТУРО
Original Assignee
Вертекс Фармасьютикалз Инкорпорейтед
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
Application filed by Вертекс Фармасьютикалз Инкорпорейтед filed Critical Вертекс Фармасьютикалз Инкорпорейтед
Publication of RU2007132908A publication Critical patent/RU2007132908A/ru
Application granted granted Critical
Publication of RU2434871C2 publication Critical patent/RU2434871C2/ru

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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06—Antiabortive agents; Labour repressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
RU2007132908/04A 2005-02-03 2006-02-02 Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы RU2434871C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US64978105P 2005-02-03 2005-02-03
US60/649,781 2005-02-03

Publications (2)

Publication Number Publication Date
RU2007132908A RU2007132908A (ru) 2009-03-10
RU2434871C2 true RU2434871C2 (ru) 2011-11-27

Family

ID=36498734

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2007132908/04A RU2434871C2 (ru) 2005-02-03 2006-02-02 Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы

Country Status (16)

Country Link
US (2) US8633205B2 (enExample)
EP (1) EP1844050B1 (enExample)
JP (2) JP5227032B2 (enExample)
KR (1) KR20070104641A (enExample)
CN (1) CN101142218B (enExample)
AT (1) ATE420883T1 (enExample)
AU (1) AU2006221065A1 (enExample)
CA (1) CA2596830A1 (enExample)
DE (1) DE602006004844D1 (enExample)
ES (1) ES2320487T3 (enExample)
IL (1) IL184898A0 (enExample)
MX (1) MX2007009429A (enExample)
NO (1) NO20074431L (enExample)
RU (1) RU2434871C2 (enExample)
WO (1) WO2006096270A1 (enExample)
ZA (1) ZA200707342B (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2618673C2 (ru) * 2011-12-21 2017-05-10 Цзянсу Хэнжуй Медсин Ко., Лтд. Производные пирролопиримидина, полезные в качестве ингибиторов jak-киназы
RU2665680C2 (ru) * 2013-06-07 2018-09-04 Цзянсу Хэнжуй Медсин Ко., Лтд. Бисульфат ингибитора янус-киназы (jak) и способ его получения
RU2712269C2 (ru) * 2015-07-31 2020-01-28 Тайхо Фармасьютикал Ко., Лтд. Пирроло[2,3-d]пиримидиновое соединение или его соль
RU2716260C2 (ru) * 2014-11-05 2020-03-11 Цзянсу Хэнжуй Медсин Ко., Лтд. Кристаллическая форма бисульфатного ингибитора jak-киназы и способ ее получения
RU2810252C1 (ru) * 2023-05-25 2023-12-25 Федеральное государственное автономное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" 5-Амино-1-(2-оксо-2-фенилэтилиден)-3-(пирролидин-1-карбонил)-6,7,8,9-тетрагидробензо[4,5]тиено[3,2-e]пирроло[1,2-a]пиримидин-2(1Н)-он, обладающий анальгетической активностью

Families Citing this family (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7884109B2 (en) 2005-04-05 2011-02-08 Wyeth Llc Purine and imidazopyridine derivatives for immunosuppression
JP2008545660A (ja) * 2005-05-20 2008-12-18 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阻害剤として有用なピロロピリジン化合物
WO2007038215A1 (en) * 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic inhibitors of janus kinases
SI1966202T1 (sl) * 2005-12-13 2012-01-31 Incyte Corp S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze
AU2015201850B2 (en) * 2005-12-13 2017-03-02 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
RU2453548C2 (ru) 2006-01-17 2012-06-20 Вертекс Фармасьютикалз Инкорпорейтед Азаиндолы, полезные в качестве ингибиторов янус-киназ
US7989459B2 (en) 2006-02-17 2011-08-02 Pharmacopeia, Llc Purinones and 1H-imidazopyridinones as PKC-theta inhibitors
SG170828A1 (en) * 2006-04-05 2011-05-30 Vertex Pharmaceuticals Inc Us Deazapurines useful as inhibitors of janus kinases
AR063141A1 (es) 2006-10-04 2008-12-30 Pharmacopeia Inc Derivados de 2- ( benzimidazolil ) purina 8- sustituida para inmunosupresion
WO2008043031A1 (en) 2006-10-04 2008-04-10 Pharmacopeia, Inc. 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
CN101568540A (zh) 2006-11-01 2009-10-28 沃泰克斯药物股份有限公司 用作janus激酶抑制剂的三环杂芳基化合物
KR20100014271A (ko) * 2006-11-16 2010-02-10 파마코페이아, 엘엘씨. 면역 억제를 위한 7-치환된 퓨린 유도체
US8247421B2 (en) 2006-12-21 2012-08-21 Vertex Pharmaceuticals Incorporated 5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
KR20100015353A (ko) * 2007-04-02 2010-02-12 팔라우 파르마 에스에이 Ｊａｋ３ 억제제로서의 피롤로피리미딘 유도체
EP2173752B2 (en) * 2007-06-13 2022-07-13 Incyte Holdings Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
CL2008001709A1 (es) * 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
JP5323095B2 (ja) * 2008-02-06 2013-10-23 ノバルティス アーゲー ピロロ［２，３−ｄ］ピリミジンおよびそのチロシンキナーゼ阻害剤としての使用
AU2009223640B2 (en) 2008-03-11 2013-07-04 Incyte Holdings Corporation Azetidine and cyclobutane derivatives as jak inhibitors
KR20110033223A (ko) 2008-06-20 2011-03-30 제넨테크, 인크. 트리아졸로피리딘 ｊａｋ 억제제 화합물 및 방법
KR20110031475A (ko) * 2008-06-20 2011-03-28 제넨테크, 인크. 트리아졸로피리딘 ｊａｋ 억제제 화합물 및 방법
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
EP2396004A4 (en) * 2009-02-11 2012-07-25 Reaction Biology Corp SELECTIVE KINASE HEMMER
HRP20140174T1 (hr) * 2009-02-27 2014-04-25 Ambit Biosciences Corporation Derivati kinazolina kao modulatori jak-kinaze i postupci njihove upotrebe
CA2762174C (en) 2009-05-22 2018-02-20 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CN106967070A (zh) 2009-05-22 2017-07-21 因塞特控股公司 作为jak抑制剂的化合物
SI3141252T1 (sl) 2009-06-17 2018-12-31 Vertex Pharmaceuticals Incorporated Inhibitorji replikacije virusov influence
US9346809B2 (en) 2009-07-08 2016-05-24 Leo Pharma A/S Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors
AR078012A1 (es) * 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
PL2486041T3 (pl) 2009-10-09 2014-01-31 Incyte Holdings Corp Pochodne hydroksylowe, keto i glukuronidowe 3-(4-(7H-pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo)-3-cyklopentylopropanonitrylu
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
EP3715347B1 (en) 2010-03-10 2021-12-22 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
US8518945B2 (en) * 2010-03-22 2013-08-27 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
NZ603686A (en) 2010-05-21 2014-11-28 Incyte Corp Topical formulation for a jak inhibitor
JP5951610B2 (ja) * 2010-08-27 2016-07-13 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ トリアゾロピラジン誘導体
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
RU2013132681A (ru) 2010-12-16 2015-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
RU2013136906A (ru) 2011-01-07 2015-02-20 Лео Фарма А/С Новые производные сульфамидпиперазина в качестве ингибиторов протеинтирозинкиназы и их фармацевтическое применение
JP5936628B2 (ja) 2011-02-18 2016-06-22 ノバルティス・ファルマ・アクチェンゲゼルシャフトＮｏｖａｒｔｉｓ Ｐｈａｒｍａ ＡＧ ｍＴＯＲ／ＪＡＫ阻害剤併用療法
WO2012127506A1 (en) 2011-03-22 2012-09-27 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
TWI577676B (zh) 2011-06-20 2017-04-11 英塞特控股公司 作為ｊａｋ抑制劑之吖丁啶基苯基、吡啶基或吡基羧醯胺衍生物
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
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
US10821111B2 (en) 2011-11-30 2020-11-03 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
WO2013082476A1 (en) * 2011-11-30 2013-06-06 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
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
WO2013174735A1 (en) 2012-05-21 2013-11-28 Bayer Pharma Aktiengesellschaft Substituted benzothienopyrimidines
TW201412740A (zh) * 2012-09-20 2014-04-01 Bayer Pharma AG 經取代之吡咯并嘧啶胺基苯并噻唑酮
IN2015DN02008A (enExample) 2012-09-21 2015-08-14 Advinus Therapeutics Ltd
SG11201503695XA (en) 2012-11-15 2015-06-29 Incyte Corp Sustained-release dosage forms of ruxolitinib
JP6397831B2 (ja) 2013-03-06 2018-09-26 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤の製造方法及びその中間体
WO2014145576A2 (en) 2013-03-15 2014-09-18 Northwestern University Substituted pyrrolo(2,3-d)pyrimidines for the treatment of cancer
UA120499C2 (uk) 2013-08-07 2019-12-26 Інсайт Корпорейшн Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1
PL3068776T3 (pl) 2013-11-13 2019-10-31 Vertex Pharma Inhibitory replikacji wirusów grypy
JP6618901B2 (ja) 2013-11-13 2019-12-11 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルスの複製の阻害剤を調製する方法
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
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
JP6704416B2 (ja) 2015-05-13 2020-06-03 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルスの複製の阻害剤を調製する方法
MA42422A (fr) 2015-05-13 2018-05-23 Vertex Pharma Inhibiteurs de la réplication des virus de la grippe
WO2017091681A1 (en) 2015-11-24 2017-06-01 Aclaris Therapeutics, Inc. Selective kinase inhibitors
CN107722012B (zh) * 2016-08-11 2020-05-29 斯福瑞（南通）制药有限公司 制备4-氯-7H-吡咯并[2,3-d]嘧啶的方法
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
MD3746429T2 (ro) 2018-01-30 2022-08-31 Incyte Corp Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă)
HUE067471T2 (hu) 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
KR102133595B1 (ko) 2019-05-31 2020-07-13 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
CN114008050B (zh) * 2019-06-18 2024-12-31 豪夫迈·罗氏有限公司 Jak激酶的吡唑并嘧啶芳基醚抑制剂及其用途
KR102112336B1 (ko) 2019-08-12 2020-05-18 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
JP2022549506A (ja) 2019-09-27 2022-11-25 ディスク・メディシン・インコーポレイテッド 骨髄線維症および関連状態を処置するための方法
PE20230251A1 (es) 2019-11-22 2023-02-07 Incyte Corp Terapia de combinacion que comprende un inhibidor de alk2 y un inhibidor de jak2
CN115836089A (zh) 2020-05-13 2023-03-21 迪斯克医药公司 用于治疗骨髓纤维化的抗血幼素（hjv）抗体
EP3915990A1 (en) * 2020-05-26 2021-12-01 Centre National de la Recherche Scientifique 4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridine-1-(2h)-carboxamide derivatives as limk and/or rock kinases inhibitors for use in the treatment of cancer
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2136683C1 (ru) * 1995-06-07 1999-09-10 Пфайзер Инк. Сконденсированные с гетероциклическим кольцом производные пиримидина
RU2264389C2 (ru) * 2000-10-20 2005-11-20 Эйсай Ко., Лтд. Азотсодержащие ароматические производные, их применение, лекарственное средство на их основе и способ лечения

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9604361D0 (en) * 1996-02-29 1996-05-01 Pharmacia Spa 4-Substituted pyrrolopyrimidine compounds as tyrosine kinase inhibitors
EA006227B1 (ru) * 1999-12-10 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2136683C1 (ru) * 1995-06-07 1999-09-10 Пфайзер Инк. Сконденсированные с гетероциклическим кольцом производные пиримидина
RU2264389C2 (ru) * 2000-10-20 2005-11-20 Эйсай Ко., Лтд. Азотсодержащие ароматические производные, их применение, лекарственное средство на их основе и способ лечения

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Online!: Chem Abstr., KHACHATRYAN et al. "Synthesis and mass spectra of some furo-, thieno-, and pyrrolo[2,3-d]pyrimidines", 1989:135185, CAS RN119707-35-6, abstracs. *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2618673C2 (ru) * 2011-12-21 2017-05-10 Цзянсу Хэнжуй Медсин Ко., Лтд. Производные пирролопиримидина, полезные в качестве ингибиторов jak-киназы
RU2665680C2 (ru) * 2013-06-07 2018-09-04 Цзянсу Хэнжуй Медсин Ко., Лтд. Бисульфат ингибитора янус-киназы (jak) и способ его получения
RU2716260C2 (ru) * 2014-11-05 2020-03-11 Цзянсу Хэнжуй Медсин Ко., Лтд. Кристаллическая форма бисульфатного ингибитора jak-киназы и способ ее получения
RU2712269C2 (ru) * 2015-07-31 2020-01-28 Тайхо Фармасьютикал Ко., Лтд. Пирроло[2,3-d]пиримидиновое соединение или его соль
RU2810252C1 (ru) * 2023-05-25 2023-12-25 Федеральное государственное автономное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" 5-Амино-1-(2-оксо-2-фенилэтилиден)-3-(пирролидин-1-карбонил)-6,7,8,9-тетрагидробензо[4,5]тиено[3,2-e]пирроло[1,2-a]пиримидин-2(1Н)-он, обладающий анальгетической активностью

Also Published As

Publication number Publication date
ZA200707342B (en) 2009-03-25
EP1844050B1 (en) 2009-01-14
EP1844050A1 (en) 2007-10-17
WO2006096270A1 (en) 2006-09-14
ES2320487T3 (es) 2009-05-22
DE602006004844D1 (de) 2009-03-05
IL184898A0 (en) 2007-12-03
RU2007132908A (ru) 2009-03-10
CN101142218B (zh) 2013-02-06
JP5227032B2 (ja) 2013-07-03
CN101142218A (zh) 2008-03-12
JP2009102361A (ja) 2009-05-14
CA2596830A1 (en) 2006-09-14
US8633205B2 (en) 2014-01-21
AU2006221065A1 (en) 2006-09-14
JP2008528705A (ja) 2008-07-31
NO20074431L (no) 2007-08-31
KR20070104641A (ko) 2007-10-26
US20060183761A1 (en) 2006-08-17
HK1116349A1 (en) 2008-12-19
US20140171454A1 (en) 2014-06-19
US20070004762A9 (en) 2007-01-04
MX2007009429A (es) 2008-03-18
ATE420883T1 (de) 2009-01-15

Similar Documents

Publication Publication Date Title
RU2434871C2 (ru) Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы
EP1881983B1 (en) Pyrrolopyridines useful as inhibitors of protein kinase
JP2008528705A5 (enExample)
US7998987B2 (en) Inhibitors of c-Met and uses thereof
JP2009532475A (ja) ヤヌスキナーゼの阻害剤として有用なデアザプリン
JP5112317B2 (ja) 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン
CA3176140A1 (en) Phd inhibitor compounds, compositions, and use
US20240327376A1 (en) Picolinamide compounds as selective phd1 inhibitors, compositions, and methods of use
EP4447963A1 (en) Selective phd1 inhibitor compounds, compositions, and methods of use
HK1116349B (en) Pyrrolopyrimidines useful as inhibitors of protein kinase
HK1122794A (en) Pyrrolopyridines useful as inhibitors of protein kinase
HK1122559A (en) 3,5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases
HK1155440A (en) Inhibitors of phosphatidylinositol 3-kinase

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20130203