JP2006509000A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2006509000A5 JP2006509000A5 JP2004554807A JP2004554807A JP2006509000A5 JP 2006509000 A5 JP2006509000 A5 JP 2006509000A5 JP 2004554807 A JP2004554807 A JP 2004554807A JP 2004554807 A JP2004554807 A JP 2004554807A JP 2006509000 A5 JP2006509000 A5 JP 2006509000A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- alkoxy
- alkylamino
- methyl
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 97
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 58
- 229920001577 copolymer Chemical group 0.000 claims 36
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 34
- 125000004442 acylamino group Chemical group 0.000 claims 33
- -1 hydroxy, amino Chemical group 0.000 claims 33
- 125000003545 alkoxy group Chemical group 0.000 claims 30
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 28
- 125000002252 acyl group Chemical group 0.000 claims 27
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 22
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 21
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 21
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 18
- 125000003282 alkyl amino group Chemical group 0.000 claims 18
- 229910052805 deuterium Inorganic materials 0.000 claims 18
- 125000001475 halogen functional group Chemical group 0.000 claims 18
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 15
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 14
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 13
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 12
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 125000004423 acyloxy group Chemical group 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 9
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 9
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 claims 6
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 3
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- 206010052779 Transplant rejections Diseases 0.000 claims 3
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 3
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 3
- 125000001769 aryl amino group Chemical group 0.000 claims 3
- 125000005135 aryl sulfinyl group Chemical group 0.000 claims 3
- 125000005110 aryl thio group Chemical group 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 3
- 210000000056 organ Anatomy 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- LRIZCRLAGSEHSM-YPMHNXCESA-N (3r,4r)-n,n,4-trimethyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidine-1-carboxamide Chemical compound C[C@@H]1CCN(C(=O)N(C)C)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 LRIZCRLAGSEHSM-YPMHNXCESA-N 0.000 claims 1
- KIRQFERTHYXALW-HIFRSBDPSA-N (3r,4r)-n-cyano-4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-n'-propylpiperidine-1-carboximidamide Chemical compound C1N(C(NC#N)=NCCC)CC[C@@H](C)[C@H]1N(C)C1=NC=NC2=C1C=CN2 KIRQFERTHYXALW-HIFRSBDPSA-N 0.000 claims 1
- JKTSSZQGORRDDS-PWSUYJOCSA-N 1-[(3r,4r)-3-[(5-chloro-7h-pyrrolo[2,3-d]pyrimidin-4-yl)-methylamino]-4-methylpiperidin-1-yl]propan-1-one Chemical compound C1N(C(=O)CC)CC[C@@H](C)[C@H]1N(C)C1=NC=NC2=C1C(Cl)=CN2 JKTSSZQGORRDDS-PWSUYJOCSA-N 0.000 claims 1
- VNFSWYNIMVHZSO-PWSUYJOCSA-N 1-[(3r,4r)-3-[(5-fluoro-7h-pyrrolo[2,3-d]pyrimidin-4-yl)-methylamino]-4-methylpiperidin-1-yl]propan-1-one Chemical compound C1N(C(=O)CC)CC[C@@H](C)[C@H]1N(C)C1=NC=NC2=C1C(F)=CN2 VNFSWYNIMVHZSO-PWSUYJOCSA-N 0.000 claims 1
- KLCACFBGIDQWHE-UHFFFAOYSA-N 1-[3-[(5-chloro-7h-pyrrolo[2,3-d]pyrimidin-4-yl)methylamino]-4-methylpiperidin-1-yl]propan-1-one Chemical compound C1N(C(=O)CC)CCC(C)C1NCC1=NC=NC2=C1C(Cl)=CN2 KLCACFBGIDQWHE-UHFFFAOYSA-N 0.000 claims 1
- DKLSBRFMPUQFLT-UHFFFAOYSA-N 1-[3-[(5-fluoro-7h-pyrrolo[2,3-d]pyrimidin-4-yl)methylamino]-4-methylpiperidin-1-yl]propan-1-one Chemical compound C1N(C(=O)CC)CCC(C)C1NCC1=NC=NC2=C1C(F)=CN2 DKLSBRFMPUQFLT-UHFFFAOYSA-N 0.000 claims 1
- MTRMACOHLXKTOY-PWSUYJOCSA-N 3,3,3-trifluoro-1-[(3r,4r)-4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]propan-1-one Chemical compound C[C@@H]1CCN(C(=O)CC(F)(F)F)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 MTRMACOHLXKTOY-PWSUYJOCSA-N 0.000 claims 1
- KWAQEXMNVBTIQE-PWSUYJOCSA-N 3,3,3-trifluoro-1-[(3r,4r)-4-methyl-3-[methyl-(5-methyl-7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]propan-1-one Chemical compound C[C@@H]1CCN(C(=O)CC(F)(F)F)C[C@@H]1N(C)C1=NC=NC2=C1C(C)=CN2 KWAQEXMNVBTIQE-PWSUYJOCSA-N 0.000 claims 1
- MTRMACOHLXKTOY-UHFFFAOYSA-N 3,3,3-trifluoro-1-[4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]propan-1-one Chemical compound CC1CCN(C(=O)CC(F)(F)F)CC1N(C)C1=NC=NC2=C1C=CN2 MTRMACOHLXKTOY-UHFFFAOYSA-N 0.000 claims 1
- UJLAWZDWDVHWOW-UHFFFAOYSA-N 3-[4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile Chemical compound CC1CCN(C(=O)CC#N)CC1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-UHFFFAOYSA-N 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- XPOHSMZMNWDIJI-UHFFFAOYSA-N methyl 4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidine-1-carboxylate Chemical compound C1N(C(=O)OC)CCC(C)C1N(C)C1=NC=NC2=C1C=CN2 XPOHSMZMNWDIJI-UHFFFAOYSA-N 0.000 claims 1
- LRIZCRLAGSEHSM-UHFFFAOYSA-N n,n,4-trimethyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidine-1-carboxamide Chemical compound CC1CCN(C(=O)N(C)C)CC1N(C)C1=NC=NC2=C1C=CN2 LRIZCRLAGSEHSM-UHFFFAOYSA-N 0.000 claims 1
- KIRQFERTHYXALW-UHFFFAOYSA-N n-cyano-4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-n'-propylpiperidine-1-carboximidamide Chemical compound C1N(C(NC#N)=NCCC)CCC(C)C1N(C)C1=NC=NC2=C1C=CN2 KIRQFERTHYXALW-UHFFFAOYSA-N 0.000 claims 1
- URCTYVNPUZEJJF-UHFFFAOYSA-N n-methyl-n-(4-methyl-1-propylsulfonylpiperidin-3-yl)-7h-pyrrolo[2,3-d]pyrimidin-4-amine Chemical compound C1N(S(=O)(=O)CCC)CCC(C)C1N(C)C1=NC=NC2=C1C=CN2 URCTYVNPUZEJJF-UHFFFAOYSA-N 0.000 claims 1
- URCTYVNPUZEJJF-OCCSQVGLSA-N n-methyl-n-[(3r,4r)-4-methyl-1-propylsulfonylpiperidin-3-yl]-7h-pyrrolo[2,3-d]pyrimidin-4-amine Chemical compound C1N(S(=O)(=O)CCC)CC[C@@H](C)[C@H]1N(C)C1=NC=NC2=C1C=CN2 URCTYVNPUZEJJF-OCCSQVGLSA-N 0.000 claims 1
- UJLAWZDWDVHWOW-YPMHNXCESA-N tofacitinib Chemical compound C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-YPMHNXCESA-N 0.000 claims 1
- 0 C*c1c(*)[n]c2ncnc(*)c12 Chemical compound C*c1c(*)[n]c2ncnc(*)c12 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42978402P | 2002-11-26 | 2002-11-26 | |
| PCT/IB2003/005229 WO2004047843A1 (en) | 2002-11-26 | 2003-11-17 | Method of treatment of transplant rejection |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006509000A JP2006509000A (ja) | 2006-03-16 |
| JP2006509000A5 true JP2006509000A5 (enExample) | 2006-12-28 |
Family
ID=32393587
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004554807A Withdrawn JP2006509000A (ja) | 2002-11-26 | 2003-11-17 | 移植片拒絶反応の処置の方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7250420B2 (enExample) |
| EP (1) | EP1572213A1 (enExample) |
| JP (1) | JP2006509000A (enExample) |
| KR (1) | KR20050086784A (enExample) |
| CN (1) | CN1717236A (enExample) |
| AU (1) | AU2003276591A1 (enExample) |
| BR (1) | BR0316487A (enExample) |
| CA (1) | CA2507392A1 (enExample) |
| MX (1) | MXPA05005576A (enExample) |
| MY (1) | MY137250A (enExample) |
| NZ (1) | NZ539901A (enExample) |
| PL (1) | PL378246A1 (enExample) |
| TW (1) | TW200418482A (enExample) |
| WO (1) | WO2004047843A1 (enExample) |
| ZA (1) | ZA200503811B (enExample) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GEP20053479B (en) | 1999-12-10 | 2005-03-25 | Pfizer Prod Inc | Pyrrolo[2,3-d]Pyrimidine Compounds, Pharmaceutical Composition Containing the Same and Use |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| RS51752B (sr) | 2002-07-29 | 2011-12-31 | Rigel Pharmaceuticals | Metode tretiranja i prevencije autoimunih oboljenja jedinjenjima 2,4-pirimidindiamina |
| AU2003276591A1 (en) | 2002-11-26 | 2004-06-18 | Pfizer Products Inc. | Method of treatment of transplant rejection |
| HRP20130602T1 (en) | 2003-07-30 | 2013-07-31 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| US20050137684A1 (en) * | 2003-12-17 | 2005-06-23 | Pfizer Inc | Stent with therapeutically active drug coated thereon |
| CA2549485A1 (en) * | 2003-12-17 | 2005-07-07 | Pfizer Products Inc. | Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection |
| 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. |
| BRPI0610514A2 (pt) * | 2005-04-05 | 2016-11-16 | Pharmacopeia Inc | composto, composição farmacêutica, e, método de tratamento de um distúrbio |
| US7884109B2 (en) * | 2005-04-05 | 2011-02-08 | Wyeth Llc | Purine and imidazopyridine derivatives for immunosuppression |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| CA2608367C (en) | 2005-06-08 | 2014-08-19 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US8163767B2 (en) | 2005-07-14 | 2012-04-24 | Astellas Pharma Inc. | Heterocyclic Janus Kinase 3 inhibitors |
| CN102127078A (zh) | 2005-07-14 | 2011-07-20 | 安斯泰来制药株式会社 | Janus激酶3的杂环类抑制剂 |
| WO2007038215A1 (en) | 2005-09-22 | 2007-04-05 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| ATE525374T1 (de) | 2005-12-13 | 2011-10-15 | Incyte Corp | Heteroarylsubstituierte pyrroloä2,3-büpyridine und pyrroloä2,3-büpyrimidine als januskinaseinhibitoren |
| US20090281075A1 (en) * | 2006-02-17 | 2009-11-12 | Pharmacopeia, Inc. | Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors |
| US7989459B2 (en) * | 2006-02-17 | 2011-08-02 | Pharmacopeia, Llc | Purinones and 1H-imidazopyridinones as PKC-theta inhibitors |
| ES2622493T3 (es) | 2006-02-24 | 2017-07-06 | Rigel Pharmaceuticals, Inc. | Composiciones y métodos para la inhibición de la ruta de JAK |
| TW200831104A (en) * | 2006-10-04 | 2008-08-01 | Pharmacopeia Inc | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
| WO2008043019A1 (en) * | 2006-10-04 | 2008-04-10 | Pharmacopeia, Inc | 8-substituted 2-(benzimidazolyl) purine derivatives for immunosuppression |
| US7902187B2 (en) * | 2006-10-04 | 2011-03-08 | Wyeth Llc | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
| CA2673125C (en) | 2006-10-19 | 2015-04-21 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US20080119496A1 (en) * | 2006-11-16 | 2008-05-22 | Pharmacopeia Drug Discovery, Inc. | 7-Substituted Purine Derivatives for Immunosuppression |
| JP5492565B2 (ja) | 2006-12-22 | 2014-05-14 | インサイト・コーポレイション | Ｊａｎｕｓキナーゼ阻害剤としての置換複素環 |
| 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. |
| ES2467665T5 (es) | 2007-06-13 | 2022-11-03 | Incyte Holdings Corp | Sales del inhibidor de cinasas Janus (R)-3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo |
| AU2009214440B2 (en) | 2008-02-15 | 2014-09-25 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases |
| SG191660A1 (en) | 2008-03-11 | 2013-07-31 | Incyte Corp | Azetidine and cyclobutane derivatives as jak inhibitors |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| AU2009244897B2 (en) | 2008-04-16 | 2014-11-13 | Alexion Pharmaceuticals, Inc. | 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors |
| WO2009131687A2 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| RU2011105768A (ru) * | 2008-08-01 | 2012-09-10 | Биокрист Фармасьютикалз, Инк. (Us) | Производные пиперидина в качестве ингибиторов jakз |
| PT2384326E (pt) * | 2008-08-20 | 2014-06-09 | Zoetis Llc | Compostos de pirrolo[2,3-d]pirimidina |
| EP3026052A1 (en) | 2009-04-20 | 2016-06-01 | Auspex Pharmaceuticals, Inc. | Preparation of deuterated piperidine inhibitors of janus kinase 3 |
| JP6172939B2 (ja) | 2009-05-22 | 2017-08-02 | 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阻害薬としての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］オクタン−またはヘプタン−ニトリル |
| WO2010135650A1 (en) | 2009-05-22 | 2010-11-25 | 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 |
| 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 |
| KR101805936B1 (ko) | 2009-10-09 | 2017-12-07 | 인사이트 홀딩스 코포레이션 | 3-（4-（7Ｈ-피롤로〔2,3-ｄ〕피리미딘-4-일）-1Ｈ-피라졸-1-일）-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 |
| PE20130038A1 (es) | 2010-03-10 | 2013-01-28 | Incyte Corp | Derivados de piperidin-4-il azetidina como inhibidores de jak1 |
| KR102303885B1 (ko) | 2010-05-21 | 2021-09-24 | 인사이트 홀딩스 코포레이션 | Ｊａｋ 저해제에 대한 국소 제형 |
| EP2635557A2 (en) | 2010-11-01 | 2013-09-11 | Portola Pharmaceuticals, Inc. | Nicotinamides as jak kinase modulators |
| EA026201B1 (ru) | 2010-11-19 | 2017-03-31 | Инсайт Холдингс Корпорейшн | Циклобутилзамещенные производные пирролопиридина и пирролопиримидина как ингибиторы jak |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| CN103732226B (zh) | 2011-02-18 | 2016-01-06 | 诺瓦提斯药物公司 | mTOR/JAK抑制剂组合疗法 |
| AU2012232658B2 (en) | 2011-03-22 | 2016-06-09 | Advinus Therapeutics Limited | Substituted fused tricyclic compounds, compositions and medicinal applications thereof |
| CA2839767A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| 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 |
| SG10201601352UA (en) | 2011-11-23 | 2016-03-30 | Portola Pharm Inc | Pyrazine kinase inhibitors |
| US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| JP2015529242A (ja) | 2012-09-21 | 2015-10-05 | アドヴィヌス セラピューティクス リミテッドＡｄｖｉｎｕｓ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｉｍｉｔｅｄ | 置換された縮合三環式化合物、組成物およびその医薬用途 |
| EP2903970A4 (en) | 2012-10-08 | 2016-11-30 | Portola Pharm Inc | SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS |
| RS62329B1 (sr) | 2012-11-15 | 2021-10-29 | Incyte Holdings Corp | Dozni oblici ruksolitiniba sa produženim vremenom oslobađanja |
| CN103896826B (zh) * | 2012-12-26 | 2016-08-03 | 上海朴颐化学科技有限公司 | 氮保护的(3r,4r)-3-甲氨基-4-甲基哌啶的不对称合成方法、相关中间体及原料制备方法 |
| TR201820520T4 (tr) | 2013-03-06 | 2019-01-21 | Incyte Holdings Corp | Bir jak inhibitörü yapmaya yönelik prosesler ve ara ürünler. |
| DK3030227T3 (da) | 2013-08-07 | 2020-04-20 | Incyte Corp | Vedvarende frigivelses-doseringsformer for en jak1-inhibitor |
| 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 |
| CN107602569A (zh) * | 2017-10-23 | 2018-01-19 | 上海博悦生物科技有限公司 | 一种新型吡咯并[2,3‑d]嘧啶化合物及其合成方法和用途 |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| WO2019152374A1 (en) | 2018-01-30 | 2019-08-08 | Incyte Corporation | Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| CA3095487A1 (en) | 2018-03-30 | 2019-10-03 | Incyte Corporation | Treatment of hidradenitis suppurativa using jak inhibitors |
| NL2022471B1 (en) | 2019-01-29 | 2020-08-18 | Vationpharma B V | Solid state forms of oclacitinib |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3037980A (en) | 1955-08-18 | 1962-06-05 | Burroughs Wellcome Co | Pyrrolopyrimidine vasodilators and method of making them |
| GB915304A (en) | 1958-03-13 | 1963-01-09 | Wellcome Found | Pyrrolo[2,3-d]pyrimidine derivatives |
| BE640616A (enExample) | 1962-12-19 | |||
| US3492397A (en) | 1967-04-07 | 1970-01-27 | Warner Lambert Pharmaceutical | Sustained release dosage in the pellet form and process thereof |
| US4060598A (en) | 1967-06-28 | 1977-11-29 | Boehringer Mannheim G.M.B.H. | Tablets coated with aqueous resin dispersions |
| US3538214A (en) | 1969-04-22 | 1970-11-03 | Merck & Co Inc | Controlled release medicinal tablets |
| US4173626A (en) | 1978-12-11 | 1979-11-06 | Merck & Co., Inc. | Sustained release indomethacin |
| NO169490C (no) | 1988-03-24 | 1992-07-01 | Takeda Chemical Industries Ltd | Analogifremgangsmaate for fremstilling av terapeutisk aktive pyrrolopyrimidinderivater |
| JP2983254B2 (ja) | 1989-06-14 | 1999-11-29 | 武田薬品工業株式会社 | ピロロ〔２，３―ｄ〕ピリミジン誘導体の製造法およびその中間体 |
| GB9114760D0 (en) | 1991-07-09 | 1991-08-28 | Pfizer Ltd | Therapeutic agents |
| US6136595A (en) | 1993-07-29 | 2000-10-24 | St. Jude Children's Research Hospital | Jak kinases and regulations of cytokine signal transduction |
| US5389509A (en) | 1993-10-04 | 1995-02-14 | Eastman Kodak Company | Ultrathin high chloride tabular grain emulsions |
| IL112249A (en) | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| ES2109796T3 (es) | 1994-05-03 | 1998-01-16 | Ciba Geigy Ag | Derivados de pirrolopirimidilo con efecto antiproliferante. |
| ATE247469T1 (de) | 1995-06-07 | 2003-09-15 | Pfizer | Heterocyclische kondensierte pyrimidin-derivate |
| DE69618959T2 (de) | 1995-07-05 | 2002-08-29 | E.I. Du Pont De Nemours And Co., Wilmington | Pyrimidone und ihre verwendug als fungizide |
| KR100437582B1 (ko) | 1995-07-06 | 2004-12-17 | 노파르티스 아게 | 피롤로피리미딘및그들의제조방법 |
| AR004010A1 (es) | 1995-10-11 | 1998-09-30 | Glaxo Group Ltd | Compuestos heterociclicos |
| CN1168138A (zh) | 1995-11-14 | 1997-12-17 | 法玛西雅厄普约翰公司 | 芳基和杂芳基嘌呤化合物 |
| ES2177925T3 (es) | 1996-01-23 | 2002-12-16 | Novartis Ag | Pirrolopirimidinas y procedimientos para su preparacion. |
| CH690773A5 (de) | 1996-02-01 | 2001-01-15 | Novartis Ag | Pyrrolo(2,3-d)pyrimide und ihre Verwendung. |
| GB9604361D0 (en) | 1996-02-29 | 1996-05-01 | Pharmacia Spa | 4-Substituted pyrrolopyrimidine compounds as tyrosine kinase inhibitors |
| AU1794697A (en) | 1996-03-06 | 1997-09-22 | Novartis Ag | 7-alkyl-pyrrolo{2,3-d}pyrimidines |
| WO1997049706A1 (en) | 1996-06-25 | 1997-12-31 | Novartis Ag | SUBSTITUTED 7-AMINO-PYRROLO[3,2-d]PYRIMIDINES AND THE USE THEREOF |
| HRP970371A2 (en) | 1996-07-13 | 1998-08-31 | Kathryn Jane Smith | Heterocyclic compounds |
| ID19430A (id) | 1996-07-13 | 1998-07-09 | Glaxo Group Ltd | Senyawa senyawa heterosiklik |
| DE69738468T2 (de) | 1996-08-23 | 2009-01-08 | Novartis Ag | Substituierte pyrrolopyrimidine und verfahren zu ihrer herstellung |
| IL129825A0 (en) | 1996-11-27 | 2000-02-29 | Pfizer | Fused bicyclic pyrimidine derivatives |
| ES2301194T3 (es) | 1997-02-05 | 2008-06-16 | Warner-Lambert Company Llc | Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular. |
| JP2001520748A (ja) | 1997-03-24 | 2001-10-30 | ファルマシア・アンド・アップジョン・カンパニー | Ｊａｋ２／サイトカイン受容体結合の阻害剤を同定する方法 |
| AU3378799A (en) | 1998-04-02 | 1999-10-25 | Neurogen Corporation | Aminoalkyl substituted pyrrolo(2,3-b)pyridine and pyrrolo(2,3-d)pyrimidine derivatives: modulators of crf1 receptors |
| AU4317399A (en) | 1998-05-28 | 1999-12-13 | Parker Hughes Institute | Quinazolines for treating brain tumor |
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| WO1999065908A1 (en) | 1998-06-19 | 1999-12-23 | Pfizer Products Inc. | PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS |
| CA2337999A1 (en) | 1998-06-30 | 2000-01-06 | Parker Hughes Institute | Method for inhibiting c-jun expression using jak-3 inhibitors |
| KR20010089171A (ko) | 1998-08-21 | 2001-09-29 | 추후제출 | 퀴나졸린 유도체 |
| PL346700A1 (en) | 1998-09-18 | 2002-02-25 | Basf Ag | Pyrrolopyrimidines as protein kinase inhibitors |
| US6080747A (en) | 1999-03-05 | 2000-06-27 | Hughes Institute | JAK-3 inhibitors for treating allergic disorders |
| GEP20053479B (en) * | 1999-12-10 | 2005-03-25 | Pfizer Prod Inc | Pyrrolo[2,3-d]Pyrimidine Compounds, Pharmaceutical Composition Containing the Same and Use |
| EA006153B1 (ru) | 2000-06-26 | 2005-10-27 | Пфайзер Продактс Инк. | СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ |
| US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| GT200200234A (es) | 2001-12-06 | 2003-06-27 | Compuestos cristalinos novedosos | |
| KR20040006555A (ko) | 2002-07-12 | 2004-01-24 | 삼성전자주식회사 | 액정 표시 장치 |
| AU2003276591A1 (en) | 2002-11-26 | 2004-06-18 | Pfizer Products Inc. | Method of treatment of transplant rejection |
| CA2549485A1 (en) | 2003-12-17 | 2005-07-07 | Pfizer Products Inc. | Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection |
-
2003
- 2003-11-17 AU AU2003276591A patent/AU2003276591A1/en not_active Abandoned
- 2003-11-17 EP EP03811831A patent/EP1572213A1/en not_active Withdrawn
- 2003-11-17 JP JP2004554807A patent/JP2006509000A/ja not_active Withdrawn
- 2003-11-17 MX MXPA05005576A patent/MXPA05005576A/es unknown
- 2003-11-17 CN CNA2003801042374A patent/CN1717236A/zh active Pending
- 2003-11-17 CA CA002507392A patent/CA2507392A1/en not_active Abandoned
- 2003-11-17 KR KR1020057009377A patent/KR20050086784A/ko not_active Ceased
- 2003-11-17 BR BR0316487-0A patent/BR0316487A/pt not_active IP Right Cessation
- 2003-11-17 NZ NZ539901A patent/NZ539901A/en unknown
- 2003-11-17 WO PCT/IB2003/005229 patent/WO2004047843A1/en not_active Ceased
- 2003-11-17 PL PL378246A patent/PL378246A1/pl not_active Application Discontinuation
- 2003-11-20 TW TW092132613A patent/TW200418482A/zh unknown
- 2003-11-21 MY MYPI20034496A patent/MY137250A/en unknown
- 2003-11-24 US US10/720,600 patent/US7250420B2/en not_active Expired - Fee Related
-
2005
- 2005-05-11 ZA ZA200503811A patent/ZA200503811B/en unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2006509000A5 (enExample) | ||
| RU2006120956A (ru) | Пирроло{2, 3-d}пиримидиновые соединения для лечения отторжения трансплантата | |
| US20150290212A1 (en) | Therapeutic uses of selected pyrazolopyrimidine compounds with anti-mer tyrosine kinase activity | |
| ES2661583T3 (es) | Métodos y composiciones usando inhibidores de PDE4 para el tratamiento y gestión de enfermedades autoinmunes e inflamatorias | |
| GEP20105025B (en) | Pharmaceutical compositions for treatent of atherosclerosis and related conditions and use thereof for treatment of these diseases | |
| EP3687997A1 (en) | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors | |
| WO2006069155A3 (en) | Inhibitors of protein arginine methyl transferases | |
| EP2275107A3 (en) | Combinations for the treatment of diseases involving cell proliferation | |
| JP2009542721A5 (enExample) | ||
| KR20160006668A (ko) | 브루톤 티로신 키나제 억제제와 cyp3a4 억제제의 배합물 | |
| JP2010513458A5 (enExample) | ||
| DE602004024375D1 (de) | Carboxamidderivate | |
| JP2009504763A5 (enExample) | ||
| TW200745111A (en) | New compounds | |
| JP2010521483A5 (enExample) | ||
| JP2010532387A5 (enExample) | ||
| NO20071197L (no) | Sulfonamidderivater, deres fremstilling og deres terapeutiske anvendelse | |
| NO20070837L (no) | Pyrido-pyrido pyrimidinderivater, fremstilling derav samt terapeutisk anvendelse for behandling av cancer. | |
| MY145465A (en) | Diaminopyrimidines as p2x3 and p2x2/3 antagonists. | |
| KR20160067118A (ko) | (ｓ)-3-(4-((4-(모르폴리노메틸)벤질)옥시)-1-옥소이소인돌린-2-일)피페리딘-2,6-디온의 제제 | |
| EA013973B1 (ru) | Способы лечения кожной волчанки при помощи аминоизоиндолиновых соединений | |
| WO2008002244A8 (en) | Imidazol-pyrimidine derivatives for treatment of diseases related to glycogen synthase kinase (gsk3) | |
| CY1114803T1 (el) | Παραγωγα πυριμιδινο σουλφοναμιδιου ως ρυθμιστες υποδοχεων χημειοκινης | |
| JP2018090566A5 (enExample) | ||
| WO2005011594A3 (en) | Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with a tyrosine kinase inhibitor, delta opioid receptor antagonist, neurokinin receptor antagonist, or vcam inhibitor for treatment of asthma or chronic obstructive pulmonary disease |