JP2006509000A5 - - Google Patents
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- 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.)
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- 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 (https=) | 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 (https=) |
| EP (1) | EP1572213A1 (https=) |
| JP (1) | JP2006509000A (https=) |
| KR (1) | KR20050086784A (https=) |
| CN (1) | CN1717236A (https=) |
| AU (1) | AU2003276591A1 (https=) |
| BR (1) | BR0316487A (https=) |
| CA (1) | CA2507392A1 (https=) |
| MX (1) | MXPA05005576A (https=) |
| MY (1) | MY137250A (https=) |
| NZ (1) | NZ539901A (https=) |
| PL (1) | PL378246A1 (https=) |
| TW (1) | TW200418482A (https=) |
| WO (1) | WO2004047843A1 (https=) |
| ZA (1) | ZA200503811B (https=) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60037345T2 (de) | 1999-12-10 | 2008-11-13 | Pfizer Products Inc., Groton | Pyrrolo(2,3-d)pyrimidin-Verbindungen |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| HRP20050089B1 (hr) | 2002-07-29 | 2015-06-19 | Rigel Pharmaceuticals | Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti |
| NZ539901A (en) | 2002-11-26 | 2007-09-28 | Pfizer Prod Inc | Method of treatment of transplant rejection |
| WO2005012294A1 (en) | 2003-07-30 | 2005-02-10 | 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 |
| SG133602A1 (en) * | 2003-12-17 | 2007-07-30 | Pfizer Prod 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. |
| US7884109B2 (en) * | 2005-04-05 | 2011-02-08 | Wyeth Llc | Purine and imidazopyridine derivatives for immunosuppression |
| JP2008534689A (ja) * | 2005-04-05 | 2008-08-28 | ファーマコペイア， インコーポレイテッド | 免疫抑制のためのプリン及びイミダゾピリジン誘導体 |
| BRPI0610876B8 (pt) | 2005-06-08 | 2021-05-25 | Rigel Pharmaceuticals Inc | composto, formulação farmacêutica, e métodos de inibir uma atividade de uma jak cinase, e de inibir uma cascata de transdução de sinal em que jak3 cinase desempenha um papel |
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| CA2621261C (en) | 2005-09-22 | 2014-05-20 | Incyte Corporation | Azepine inhibitors of janus kinases |
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| US7902187B2 (en) * | 2006-10-04 | 2011-03-08 | Wyeth Llc | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
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| US7919490B2 (en) * | 2006-10-04 | 2011-04-05 | Wyeth Llc | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
| JP5161233B2 (ja) | 2006-10-19 | 2013-03-13 | ライジェル ファーマシューティカルズ， インコーポレイテッド | 自己免疫疾患の処置のためのｊａｋキナーゼの阻害剤としての２，４−ピリミジンアミン誘導体 |
| US20080119496A1 (en) * | 2006-11-16 | 2008-05-22 | Pharmacopeia Drug Discovery, Inc. | 7-Substituted Purine Derivatives for Immunosuppression |
| CA2673038C (en) | 2006-12-22 | 2015-12-15 | Incyte Corporation | Substituted tricyclic heteroaryl compounds 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. |
| KR20150036210A (ko) | 2007-06-13 | 2015-04-07 | 인사이트 코포레이션 | 야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염 |
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| HUE029767T2 (en) | 2008-03-11 | 2017-04-28 | Incyte Holdings Corp | JAK inhibitor azetidine and cyclobutane derivatives |
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| JP2011529918A (ja) * | 2008-08-01 | 2011-12-15 | バイオクライスト ファーマシューティカルズ， インコーポレイテッド | Ｊａｋ３阻害剤としてのピペリジン誘導体 |
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| CN103797010B (zh) | 2011-06-20 | 2016-02-24 | 因塞特控股公司 | 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物 |
| EP2741747A1 (en) | 2011-08-10 | 2014-06-18 | Novartis Pharma AG | JAK P13K/mTOR COMBINATION THERAPY |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
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| US9593115B2 (en) | 2012-09-21 | 2017-03-14 | Advinus Therapeutics Ltd. | Substituted fused tricyclic compounds, compositions, and medicinal applications thereof |
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2003
- 2003-11-17 NZ NZ539901A patent/NZ539901A/en unknown
- 2003-11-17 PL PL378246A patent/PL378246A1/pl not_active Application Discontinuation
- 2003-11-17 AU AU2003276591A patent/AU2003276591A1/en not_active Abandoned
- 2003-11-17 CN CNA2003801042374A patent/CN1717236A/zh active Pending
- 2003-11-17 EP EP03811831A patent/EP1572213A1/en not_active Withdrawn
- 2003-11-17 BR BR0316487-0A patent/BR0316487A/pt not_active IP Right Cessation
- 2003-11-17 KR KR1020057009377A patent/KR20050086784A/ko not_active Ceased
- 2003-11-17 JP JP2004554807A patent/JP2006509000A/ja not_active Withdrawn
- 2003-11-17 MX MXPA05005576A patent/MXPA05005576A/es unknown
- 2003-11-17 WO PCT/IB2003/005229 patent/WO2004047843A1/en not_active Ceased
- 2003-11-17 CA CA002507392A patent/CA2507392A1/en not_active Abandoned
- 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
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