RU2008143361A - Деазапурины в качестве ингибиторов янус-киназ - Google Patents
Деазапурины в качестве ингибиторов янус-киназ Download PDFInfo
- Publication number
- RU2008143361A RU2008143361A RU2008143361/04A RU2008143361A RU2008143361A RU 2008143361 A RU2008143361 A RU 2008143361A RU 2008143361/04 A RU2008143361/04 A RU 2008143361/04A RU 2008143361 A RU2008143361 A RU 2008143361A RU 2008143361 A RU2008143361 A RU 2008143361A
- Authority
- RU
- Russia
- Prior art keywords
- group
- aliphatic group
- optionally substituted
- cycle
- agent
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000001931 aliphatic group Chemical group 0.000 claims abstract 30
- 150000001875 compounds Chemical class 0.000 claims abstract 25
- 125000001424 substituent group Chemical group 0.000 claims abstract 20
- 229910052736 halogen Inorganic materials 0.000 claims abstract 16
- 150000002367 halogens Chemical class 0.000 claims abstract 15
- 229910052799 carbon Inorganic materials 0.000 claims abstract 11
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims abstract 10
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 8
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 7
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims abstract 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract 6
- 239000001301 oxygen Chemical group 0.000 claims abstract 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract 4
- -1 NCH3 Chemical group 0.000 claims abstract 3
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims abstract 3
- 125000005842 heteroatom Chemical group 0.000 claims abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract 2
- 229910052717 sulfur Chemical group 0.000 claims abstract 2
- 239000011593 sulfur Chemical group 0.000 claims abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 239000003795 chemical substances by application Substances 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 125000004429 atom Chemical group 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 6
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000029462 Immunodeficiency disease Diseases 0.000 claims 2
- 108010025020 Nerve Growth Factor Proteins 0.000 claims 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 230000001028 anti-proliverative effect Effects 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 230000000973 chemotherapeutic effect Effects 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 230000002519 immonomodulatory effect Effects 0.000 claims 2
- 239000003018 immunosuppressive agent Substances 0.000 claims 2
- 229940125721 immunosuppressive agent Drugs 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 239000003900 neurotrophic factor Substances 0.000 claims 2
- 206010065040 AIDS dementia complex Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000020446 Cardiac disease Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010020880 Hypertrophy Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 231100000360 alopecia Toxicity 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000004413 cardiac myocyte Anatomy 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 230000001066 destructive effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 208000019622 heart disease Diseases 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 230000036210 malignancy Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920000136 polysorbate Polymers 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 230000010410 reperfusion Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 4
- 101100054666 Streptomyces halstedii sch3 gene Proteins 0.000 abstract 2
- 0 Cc1c[n]c(*)c1 Chemical compound Cc1c[n]c(*)c1 0.000 description 8
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
- 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
- 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
- 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
- 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
-
- 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
- A61P25/14—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
- 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
- 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
- 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
- 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
- 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
- A61P9/10—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Psychology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Communicable Diseases (AREA)
- Obesity (AREA)
- Tropical Medicine & Parasitology (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US78944106P | 2006-04-05 | 2006-04-05 | |
| US60/789,441 | 2006-04-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2008143361A true RU2008143361A (ru) | 2010-05-10 |
Family
ID=38377244
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008143361/04A RU2008143361A (ru) | 2006-04-05 | 2007-04-05 | Деазапурины в качестве ингибиторов янус-киназ |
Country Status (14)
| Country | Link |
|---|---|
| US (4) | US8741912B2 (enExample) |
| EP (1) | EP2001884A1 (enExample) |
| JP (2) | JP2009532475A (enExample) |
| KR (1) | KR20090018895A (enExample) |
| CN (1) | CN101460499A (enExample) |
| AU (1) | AU2007235487A1 (enExample) |
| CA (1) | CA2648250A1 (enExample) |
| IL (1) | IL194460A0 (enExample) |
| MX (1) | MX2008012860A (enExample) |
| NO (1) | NO20084652L (enExample) |
| RU (1) | RU2008143361A (enExample) |
| SG (1) | SG170828A1 (enExample) |
| WO (1) | WO2007117494A1 (enExample) |
| ZA (1) | ZA200808536B (enExample) |
Families Citing this family (77)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2364340T3 (es) | 2004-03-30 | 2011-08-31 | Vertex Pharmaceuticals Incorporated | Azaindoles útiles como inhibidores de jak y otras proteína quinasas. |
| 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 |
| HUE028588T2 (hu) | 2005-12-13 | 2016-12-28 | Incyte Holdings Corp | Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok |
| NZ592968A (en) | 2006-01-17 | 2012-08-31 | Vertex Pharma | Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2 |
| JP2009532475A (ja) | 2006-04-05 | 2009-09-10 | 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 | ヤヌスキナーゼの阻害剤として有用なデアザプリン |
| WO2008079346A1 (en) | 2006-12-21 | 2008-07-03 | Vertex Pharmaceuticals Incorporated | 5-cyan0-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors |
| ES2415863T3 (es) | 2006-12-22 | 2013-07-29 | Incyte Corporation | Heterociclos sustituidos como inhibidores de Janus Quinasas |
| 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. |
| EP2740731B1 (en) * | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| EP2262498A2 (en) * | 2008-03-10 | 2010-12-22 | Vertex Pharmceuticals Incorporated | Pyrimidines and pyridines useful as inhibitors of protein kinases |
| MY165582A (en) | 2008-03-11 | 2018-04-05 | Incyte Holdings Corp | Azetidine and cyclobutane derivatives as jak inhibitors |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| WO2010083283A2 (en) | 2009-01-15 | 2010-07-22 | Incyte Corporation | Processes for preparing jak inhibitors and related intermediate compounds |
| BRPI1012108B8 (pt) | 2009-05-22 | 2021-05-25 | Incyte Corp | composto 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octa no- ou heptano-nitrila, sua composição, seus usos e processo para preparar um sal de ácido fosfórico |
| NZ596479A (en) * | 2009-05-22 | 2014-01-31 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| JP5719840B2 (ja) | 2009-06-08 | 2015-05-20 | 武田薬品工業株式会社 | Ｊａｋの阻害剤としてのジヒドロピロロナフチリジノン化合物 |
| GEP20207129B (en) | 2009-06-17 | 2020-07-10 | Vertex Pharma | Inhibitors of influenza viruses replication |
| UA110324C2 (en) * | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| JP5690823B2 (ja) | 2009-07-08 | 2015-03-25 | レオ ファーマ アクティーゼルスカブ | Ｊａｋ受容体およびタンパク質チロシンキナーゼ阻害薬としての複素環化合物 |
| 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 |
| WO2011076734A1 (en) * | 2009-12-21 | 2011-06-30 | Euroscreen S.A. | Compounds, pharmaceutical composition and methods for use in treating inflammatory diseases |
| KR20120124428A (ko) | 2009-12-30 | 2012-11-13 | 아르퀼 인코포레이티드 | 치환된 피롤로-아미노피리미딘 화합물 |
| US20110207754A1 (en) * | 2010-02-18 | 2011-08-25 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
| AU2015205858B2 (en) * | 2010-03-10 | 2017-04-13 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| CA2792508C (en) * | 2010-03-10 | 2018-01-16 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| EA202091303A3 (ru) | 2010-05-21 | 2021-05-31 | Инсайт Холдингс Корпорейшн | Композиция ингибитора jak для местного применения |
| WO2012066488A2 (en) * | 2010-11-17 | 2012-05-24 | Actelion Pharmaceuticals Ltd | Bridged spiro[2.4]heptane ester derivatives |
| 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 |
| CA2818542A1 (en) * | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2536415T3 (es) * | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| WO2012078802A1 (en) * | 2010-12-08 | 2012-06-14 | Takeda Pharmaceutical Company Limited | PREPARATION OF SUBSTITUTED-4,5-DIHYDROPYRROLO[4,3,2-de][2,6]NAPHTHYRIDIN-3(1H)-ONES |
| RU2013132681A (ru) | 2010-12-16 | 2015-01-27 | Вертекс Фармасьютикалз Инкорпорейтед | Ингибиторы репликации вирусов гриппа |
| CN103298817A (zh) * | 2011-01-07 | 2013-09-11 | 利奥制药有限公司 | 作为蛋白酪氨酸激酶抑制剂的新磺酰胺哌嗪衍生物及其药物用途 |
| WO2012112847A1 (en) | 2011-02-18 | 2012-08-23 | Novartis Pharma Ag | mTOR/JAK INHIBITOR COMBINATION THERAPY |
| AU2012232658B2 (en) | 2011-03-22 | 2016-06-09 | Advinus Therapeutics Limited | Substituted fused tricyclic compounds, compositions and medicinal applications thereof |
| MX2013013331A (es) * | 2011-05-17 | 2014-10-17 | Principia Biopharma Inc | Derivados de azaindol como inhibidores de tirosina-cinasas. |
| US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| WO2013023119A1 (en) | 2011-08-10 | 2013-02-14 | 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 |
| 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 |
| WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
| WO2014045305A1 (en) | 2012-09-21 | 2014-03-27 | Advinus Therapeutics Limited | Substituted fused tricyclic compounds, compositions and medicinal applications thereof |
| KR102242077B1 (ko) | 2012-11-15 | 2021-04-20 | 인사이트 홀딩스 코포레이션 | 룩솔리티니브의 서방성 제형 |
| EP3489239B1 (en) | 2013-03-06 | 2021-09-15 | Incyte Holdings Corporation | Processes and intermediates for making a jak inhibitor |
| MX376856B (es) | 2013-08-07 | 2025-03-07 | Incyte Holdings Corp | Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1). |
| HUE038820T2 (hu) | 2013-11-13 | 2018-11-28 | Vertex Pharma | Eljárás influenzavírusok replikációjának inhibitorai elõállítására |
| PT3068776T (pt) | 2013-11-13 | 2019-08-26 | Vertex Pharma | Inibidores da replicação de vírus da gripe |
| 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 |
| 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 |
| EP3294717B1 (en) | 2015-05-13 | 2020-07-29 | Vertex Pharmaceuticals Inc. | Methods of preparing inhibitors of influenza viruses replication |
| WO2016183120A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| EP3492468B1 (en) * | 2016-07-26 | 2022-02-23 | Suzhou Longbiotech Pharmaceuticals Co., Ltd. | Heterocyclic compound as jak inhibitor, and salts and therapeutic use thereof |
| WO2018041989A1 (en) | 2016-09-02 | 2018-03-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating refractory celiac disease type 2 |
| TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
| MD3746429T2 (ro) | 2018-01-30 | 2022-08-31 | Incyte Corp | Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă) |
| KR20260080448A (ko) | 2018-03-30 | 2026-06-02 | 인사이트 코포레이션 | Jak 억제제를 사용하는 화농성 한선염의 치료 |
| CN108586341B (zh) * | 2018-05-25 | 2020-05-08 | 天津商业大学 | 酰胺类化合物和其药用盐及其制备方法和药物用途 |
| CA3129665A1 (en) | 2019-03-21 | 2020-09-24 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| WO2020201362A2 (en) | 2019-04-02 | 2020-10-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
| WO2020212395A1 (en) | 2019-04-16 | 2020-10-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels |
| EP3725305A1 (en) | 2019-04-17 | 2020-10-21 | Zentiva K.S. | Pharmaceutical composition containing baricitinib hydrobromide |
| CA3156007A1 (en) | 2019-09-27 | 2021-04-01 | Disc Medicine, Inc. | METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| AU2021273014A1 (en) | 2020-05-13 | 2022-11-17 | AbbVie Deutschland GmbH & Co. KG | Anti-hemojuvelin (HJV) antibodies for treating anemia of chronic disease |
| ES3075793T3 (en) | 2020-05-13 | 2026-08-07 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| 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 |
| CN112979635A (zh) * | 2021-02-06 | 2021-06-18 | 绍兴文理学院 | 一种噻唑类化合物及其制备方法和应用 |
| CN112979634A (zh) * | 2021-02-06 | 2021-06-18 | 绍兴文理学院 | 一种含酰胺结构的噻唑类化合物及其制备方法和应用 |
| US20250283174A1 (en) | 2022-05-16 | 2025-09-11 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation |
| CN116478172B (zh) * | 2023-06-20 | 2023-09-05 | 英矽智能科技(上海)有限公司 | 吡咯并[3,2-d]嘧啶类化合物及其应用 |
| WO2026093435A1 (en) | 2024-10-31 | 2026-05-07 | Institut National de la Santé et de la Recherche Médicale | Use of jak inhibitors for enhancing the potency of immunotherapy in the treament of cancer |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8474101A1 (es) * | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| OA12118A (en) | 1999-12-10 | 2006-05-04 | Pfizer Prod Inc | PyrroloÄ2,3-dÜpyrimidine compounds. |
| US6610688B2 (en) * | 1999-12-21 | 2003-08-26 | Sugen, Inc. | 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors |
| WO2003053336A2 (en) * | 2001-12-19 | 2003-07-03 | The Quigley Corporation | Methods for the treatment of peripheral neural and vascular ailments |
| CA2515132C (en) * | 2003-02-07 | 2012-01-03 | Vertex Pharmaceuticals Incorporated | Heteroaryl substituted pyrroles useful as inhibitors of protein kinases |
| TWI339206B (en) * | 2003-09-04 | 2011-03-21 | Vertex Pharma | Compositions useful as inhibitors of protein kinases |
| CA2547080A1 (en) * | 2003-12-02 | 2005-07-28 | Vertex Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
| ES2364340T3 (es) * | 2004-03-30 | 2011-08-31 | Vertex Pharmaceuticals Incorporated | Azaindoles útiles como inhibidores de jak y otras proteína quinasas. |
| US7514448B2 (en) * | 2004-04-02 | 2009-04-07 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of rock and other protein kinases |
| WO2005117909A2 (en) * | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| US20060122213A1 (en) * | 2004-06-30 | 2006-06-08 | Francoise Pierard | Azaindoles useful as inhibitors of protein kinases |
| US8633205B2 (en) * | 2005-02-03 | 2014-01-21 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein kinases |
| WO2006101783A2 (en) * | 2005-03-15 | 2006-09-28 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| 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 |
| CN101801971A (zh) * | 2005-09-30 | 2010-08-11 | 沃泰克斯药物股份有限公司 | 可用作janus激酶抑制剂的脱氮嘌呤 |
| HUE028588T2 (hu) * | 2005-12-13 | 2016-12-28 | Incyte Holdings Corp | Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok |
| NZ592968A (en) * | 2006-01-17 | 2012-08-31 | Vertex Pharma | Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2 |
| JP2009532475A (ja) | 2006-04-05 | 2009-09-10 | 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 | ヤヌスキナーゼの阻害剤として有用なデアザプリン |
-
2007
- 2007-04-05 JP JP2009504273A patent/JP2009532475A/ja active Pending
- 2007-04-05 US US11/732,845 patent/US8741912B2/en not_active Expired - Fee Related
- 2007-04-05 SG SG201102383-5A patent/SG170828A1/en unknown
- 2007-04-05 MX MX2008012860A patent/MX2008012860A/es not_active Application Discontinuation
- 2007-04-05 AU AU2007235487A patent/AU2007235487A1/en not_active Abandoned
- 2007-04-05 WO PCT/US2007/008367 patent/WO2007117494A1/en not_active Ceased
- 2007-04-05 RU RU2008143361/04A patent/RU2008143361A/ru not_active Application Discontinuation
- 2007-04-05 EP EP07754825A patent/EP2001884A1/en not_active Withdrawn
- 2007-04-05 KR KR1020087027078A patent/KR20090018895A/ko not_active Ceased
- 2007-04-05 CN CNA200780020405XA patent/CN101460499A/zh active Pending
- 2007-04-05 CA CA002648250A patent/CA2648250A1/en not_active Abandoned
-
2008
- 2008-10-02 IL IL194460A patent/IL194460A0/en unknown
- 2008-10-03 US US12/245,069 patent/US20090227607A1/en not_active Abandoned
- 2008-10-07 ZA ZA2008/08536A patent/ZA200808536B/en unknown
- 2008-11-05 NO NO20084652A patent/NO20084652L/no not_active Application Discontinuation
-
2012
- 2012-02-23 US US13/403,169 patent/US20120316186A1/en not_active Abandoned
-
2013
- 2013-11-01 JP JP2013228595A patent/JP2014024869A/ja not_active Ceased
-
2014
- 2014-04-11 US US14/250,668 patent/US20140315931A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2007117494A1 (en) | 2007-10-18 |
| AU2007235487A1 (en) | 2007-10-18 |
| IL194460A0 (en) | 2009-08-03 |
| EP2001884A1 (en) | 2008-12-17 |
| SG170828A1 (en) | 2011-05-30 |
| US20090227607A1 (en) | 2009-09-10 |
| KR20090018895A (ko) | 2009-02-24 |
| CA2648250A1 (en) | 2007-10-18 |
| US20140315931A1 (en) | 2014-10-23 |
| MX2008012860A (es) | 2009-01-07 |
| JP2009532475A (ja) | 2009-09-10 |
| US8741912B2 (en) | 2014-06-03 |
| US20090088445A1 (en) | 2009-04-02 |
| CN101460499A (zh) | 2009-06-17 |
| NO20084652L (no) | 2008-12-03 |
| JP2014024869A (ja) | 2014-02-06 |
| ZA200808536B (en) | 2012-07-25 |
| US20120316186A1 (en) | 2012-12-13 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2009532475A5 (enExample) | ||
| RU2008133613A (ru) | Азаиндолы, полезные в качестве ингибиторов янус-киназ | |
| RU2008117151A (ru) | Деазапурины, пригодные в качестве ингибиторов янус-киназ | |
| RU2010129928A (ru) | Пиразоло[1, 5-а]пиримидины, используемые в качестве ингибиторов jak2 | |
| JP2008545660A5 (enExample) | ||
| RU2008136854A (ru) | Дигидродиазепины, которые можно использовать в качестве ингибиторов протеинкиназ | |
| RU2012142550A (ru) | Производные пирролопиразина и их применение в качестве ингибиторов jak и syk | |
| CA2765015C (en) | Deuterated isoindoline-1,3-dione derivatives as pde4 and tnf-alpha inhibitors | |
| JP2005519932A5 (enExample) | ||
| RU2006138621A (ru) | Азаиндолы, полезные в качестве ингибиторов rock и других протеинкиназ | |
| RU2011133825A (ru) | Пирролопиридины, полезные в качестве ингибиторов протеинкиназы | |
| RU2013114351A (ru) | Пестицидные композиции | |
| JP2009526849A5 (enExample) | ||
| RU2008144584A (ru) | 4,5-дигидро-[1,2,4]триазоло[4,3-f]птеридины в качестве ингибиторов протеинкиназы plk1 для лечения пролиферативных заболеваний | |
| CA2446756A1 (en) | Thiazole compounds useful as inhibitors of protein kinase | |
| RU2008116844A (ru) | Ацилированные производные спиропиперидина как модуляторы рецептора меланокортина-4 | |
| CA2510534A1 (en) | Compositions useful as inhibitors of protein kinases | |
| RU2004126671A (ru) | Гетероарилсоединения, полезные в качестве ингибиторов gsk-3 | |
| AR046297A1 (es) | Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo | |
| JP2005504789A5 (enExample) | ||
| RU2004120553A (ru) | Производные никотинамида, полезные в качестве р38-ингибиторов | |
| RU2003117476A (ru) | Аминотиазолы и их применение в качестве антагонистов рецептора аденозина | |
| RU2005111225A (ru) | Производные триазаспиро[5.5]ундекана и лекарственные средства, содержащие их в качестве активного ингредиента | |
| RU2005106353A (ru) | Производные гидантоина и их применение в качестве ингибиторов тасе | |
| RU2003105278A (ru) | Производные хинолина, способ их получения и их применение, лекарственное средство и способ лечения опухолевого заболевания млекопитающего |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20120528 |