JP2010529208A5 - - Google Patents
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- JP2010529208A5 JP2010529208A5 JP2010512341A JP2010512341A JP2010529208A5 JP 2010529208 A5 JP2010529208 A5 JP 2010529208A5 JP 2010512341 A JP2010512341 A JP 2010512341A JP 2010512341 A JP2010512341 A JP 2010512341A JP 2010529208 A5 JP2010529208 A5 JP 2010529208A5
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- Japan
- Prior art keywords
- pharmaceutical composition
- disease
- cancer
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- pharmaceutically acceptable
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 claims 19
- 201000010099 disease Diseases 0.000 claims 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 14
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 3
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 102000042838 JAK family Human genes 0.000 claims 2
- 108091082332 JAK family Proteins 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 208000037244 polycythemia vera Diseases 0.000 claims 2
- YIOHYHBNMPEYIR-UHFFFAOYSA-N 3-(2-hydroxycyclopentyl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound OC1CCCC1C(CC#N)N1N=CC(C=2C=3C=CNC=3N=CN=2)=C1 YIOHYHBNMPEYIR-UHFFFAOYSA-N 0.000 claims 1
- PEDGDCYQFZPRCX-UHFFFAOYSA-N 3-(3-hydroxycyclopentyl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound C1C(O)CCC1C(CC#N)N1N=CC(C=2C=3C=CNC=3N=CN=2)=C1 PEDGDCYQFZPRCX-UHFFFAOYSA-N 0.000 claims 1
- DBJFGIPGWLPPQS-UHFFFAOYSA-N 3-(3-oxocyclopentyl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound C1C(=O)CCC1C(CC#N)N1N=CC(C=2C=3C=CNC=3N=CN=2)=C1 DBJFGIPGWLPPQS-UHFFFAOYSA-N 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010028561 Myeloid metaplasia Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 201000002481 Myositis Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 1
- 208000022531 anorexia Diseases 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 206010061428 decreased appetite Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000005962 mycosis fungoides Diseases 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000010410 reperfusion Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94369507P | 2007-06-13 | 2007-06-13 | |
| US60/943,695 | 2007-06-13 | ||
| PCT/US2008/066658 WO2008157207A2 (en) | 2007-06-13 | 2008-06-12 | Metabolites of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-lh-pyrazol-l-yl)-3- cyclopentylpropanenitrile |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010529208A JP2010529208A (ja) | 2010-08-26 |
| JP2010529208A5 true JP2010529208A5 (OSRAM) | 2011-07-21 |
| JP5479331B2 JP5479331B2 (ja) | 2014-04-23 |
Family
ID=40029276
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010512341A Active JP5479331B2 (ja) | 2007-06-13 | 2008-06-12 | ＪＡＮＵＳキナーゼ阻害剤（Ｒ）−３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルの有効な代謝体 |
Country Status (25)
| Country | Link |
|---|---|
| US (5) | US7834022B2 (OSRAM) |
| EP (1) | EP2173751B1 (OSRAM) |
| JP (1) | JP5479331B2 (OSRAM) |
| KR (1) | KR20100049008A (OSRAM) |
| CN (1) | CN101815717B (OSRAM) |
| AR (1) | AR067024A1 (OSRAM) |
| AU (1) | AU2008266182B8 (OSRAM) |
| BR (1) | BRPI0812563A2 (OSRAM) |
| CA (1) | CA2689158C (OSRAM) |
| CL (1) | CL2008001709A1 (OSRAM) |
| CO (1) | CO6251255A2 (OSRAM) |
| CR (1) | CR11149A (OSRAM) |
| EA (1) | EA017790B1 (OSRAM) |
| EC (1) | ECSP099821A (OSRAM) |
| ES (1) | ES2448868T3 (OSRAM) |
| GE (1) | GEP20125534B (OSRAM) |
| IL (1) | IL202429A0 (OSRAM) |
| MX (2) | MX339139B (OSRAM) |
| NZ (1) | NZ581801A (OSRAM) |
| PL (1) | PL2173751T3 (OSRAM) |
| PT (1) | PT2173751E (OSRAM) |
| TW (1) | TWI426911B (OSRAM) |
| UA (1) | UA99465C2 (OSRAM) |
| WO (1) | WO2008157207A2 (OSRAM) |
| ZA (1) | ZA200908820B (OSRAM) |
Families Citing this family (87)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005105814A1 (en) * | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| EP2121692B1 (en) | 2006-12-22 | 2013-04-10 | Incyte Corporation | Substituted heterocycles as janus kinase inhibitors |
| CL2008001709A1 (es) * | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| DK2740731T3 (en) | 2007-06-13 | 2016-04-11 | Incyte Holdings Corp | CRYSTALLINE SALTS OF JANUSKINASEINHIBITOREN (R) -3- (4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-CYCLOPENTYLPROPANNITRIL |
| WO2009064835A1 (en) * | 2007-11-16 | 2009-05-22 | Incyte Corporation | 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors |
| CA2714177A1 (en) | 2008-02-06 | 2009-08-13 | Novartis Ag | Pyrrolo [2,3-d] pyridines and use thereof as tyrosine kinase inhibitors |
| BRPI0909040B8 (pt) | 2008-03-11 | 2021-05-25 | Incyte Holdings Corp | derivados de azetidina e ciclobutano, seus usos, e composição |
| 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 |
| CN102395576A (zh) | 2009-02-27 | 2012-03-28 | 埃姆比特生物科学公司 | 调控jak激酶的喹唑啉衍生物和其使用方法 |
| AU2010249443B2 (en) | 2009-05-22 | 2015-08-13 | Incyte Holdings Corporation | 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as JAK inhibitors |
| MY156727A (en) * | 2009-05-22 | 2016-03-15 | 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 |
| 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 |
| US20120034226A1 (en) * | 2009-09-16 | 2012-02-09 | Riken | Diagnostic method of skin inflammatory disease |
| KR101921850B1 (ko) * | 2009-10-09 | 2018-11-23 | 인사이트 홀딩스 코포레이션 | 3-（4-（7Ｈ-피롤로〔2,3-ｄ〕피리미딘-4-일）-1Ｈ-피라졸-1-일）-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 |
| CA2790070C (en) * | 2010-02-18 | 2018-03-06 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
| AU2011224484A1 (en) | 2010-03-10 | 2012-09-27 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
| US8962596B2 (en) * | 2010-04-14 | 2015-02-24 | Array Biopharma Inc. | 5,7-substituted-imidazo[1,2-C]pyrimidines as inhibitors of JAK kinases |
| MY161078A (en) * | 2010-05-21 | 2017-04-14 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| CA2810024A1 (en) | 2010-09-01 | 2012-03-08 | Ambit Biosciences Corporation | Quinazoline compounds and methods of use thereof |
| CN103370076A (zh) * | 2010-11-02 | 2013-10-23 | 纽约市哥伦比亚大学托管会 | 治疗毛发脱落疾病的方法 |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| EP2640723A1 (en) | 2010-11-19 | 2013-09-25 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2547916T3 (es) | 2011-02-18 | 2015-10-09 | Novartis Pharma Ag | Terapia de combinación de inhibidores de mTOR/JAK |
| KR20140040819A (ko) | 2011-06-20 | 2014-04-03 | 인사이트 코포레이션 | Ｊａｋ 저해제로서의 아제티디닐 페닐, 피리딜 또는 피라지닐 카르복스아미드 유도체 |
| HK1198579A1 (en) | 2011-08-10 | 2015-04-30 | Novartis Pharma Ag | Jak p13k/mtor combination therapy |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| AU2012323399A1 (en) * | 2011-10-12 | 2014-05-29 | Array Biopharma Inc. | 5,7-substituted-imidazo[1,2-c]pyrimidines |
| US10821111B2 (en) | 2011-11-30 | 2020-11-03 | Emory University | Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections |
| US9089574B2 (en) | 2011-11-30 | 2015-07-28 | Emory University | Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections |
| WO2013173720A1 (en) | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| EA201492287A1 (ru) | 2012-06-15 | 2015-07-30 | Консерт Фармасьютикалс, Инк. | Дейтерированные производные руксолитиниба |
| WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
| WO2014016396A1 (en) | 2012-07-27 | 2014-01-30 | Ratiopharm Gmbh | Oral dosage forms for modified release comprising ruxolitinib |
| UA117572C2 (uk) | 2012-11-01 | 2018-08-27 | Інсайт Холдинґс Корпорейшн | Трициклічні конденсовані похідні тіофену як інгібітори jak |
| PH12020551186B1 (en) | 2012-11-15 | 2024-03-20 | Incyte Holdings 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 |
| TWI719401B (zh) | 2013-05-17 | 2021-02-21 | 美商英塞特公司 | 作為jak抑制劑之聯吡唑衍生物 |
| KR20160045081A (ko) | 2013-08-07 | 2016-04-26 | 인사이트 코포레이션 | Jak1 억제제용 지속 방출 복용 형태 |
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