JP2005505550A5 - - Google Patents
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- Publication number
- JP2005505550A5 JP2005505550A5 JP2003524585A JP2003524585A JP2005505550A5 JP 2005505550 A5 JP2005505550 A5 JP 2005505550A5 JP 2003524585 A JP2003524585 A JP 2003524585A JP 2003524585 A JP2003524585 A JP 2003524585A JP 2005505550 A5 JP2005505550 A5 JP 2005505550A5
- Authority
- JP
- Japan
- Prior art keywords
- lower alkyl
- heterocyclyl
- aryl
- optionally substituted
- cycloalkyl
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 150000002148 esters Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- NIPNSKYNPDTRPC-UHFFFAOYSA-N N-[2-oxo-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethyl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical group O=C(CNC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)N1CC2=C(CC1)NN=N2 NIPNSKYNPDTRPC-UHFFFAOYSA-N 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000005257 alkyl acyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000005251 aryl acyl group Chemical group 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0121026.9A GB0121026D0 (en) | 2001-08-30 | 2001-08-30 | Organic compounds |
| GB0121024A GB0121024D0 (en) | 2001-08-30 | 2001-08-30 | Organic compounds |
| PCT/EP2002/009661 WO2003020278A1 (en) | 2001-08-30 | 2002-08-29 | Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin k inhibitory activity for the treatment of inflammations and other diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005505550A JP2005505550A (ja) | 2005-02-24 |
| JP2005505550A5 true JP2005505550A5 (https=) | 2005-11-17 |
| JP4131701B2 JP4131701B2 (ja) | 2008-08-13 |
Family
ID=26246490
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003524585A Expired - Fee Related JP4131701B2 (ja) | 2001-08-30 | 2002-08-29 | 炎症および他の疾患を処置するための、２−シアノ−４−アミノ−ピリミジン構造およびカテプシンｋ阻害活性を有するシステインプロテアーゼインヒビター |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US7112589B2 (https=) |
| EP (1) | EP1423121B1 (https=) |
| JP (1) | JP4131701B2 (https=) |
| KR (1) | KR100629834B1 (https=) |
| CN (1) | CN1549717B (https=) |
| AR (1) | AR036375A1 (https=) |
| AT (1) | ATE345136T1 (https=) |
| AU (1) | AU2002333758B2 (https=) |
| BR (1) | BR0212141A (https=) |
| CA (1) | CA2456127C (https=) |
| CO (1) | CO5560576A2 (https=) |
| DE (1) | DE60216122T2 (https=) |
| ES (1) | ES2275946T3 (https=) |
| HU (1) | HUP0401431A3 (https=) |
| IL (1) | IL160295A0 (https=) |
| MX (1) | MXPA04001930A (https=) |
| NZ (1) | NZ531287A (https=) |
| PE (1) | PE20030772A1 (https=) |
| PL (1) | PL208280B1 (https=) |
| PT (1) | PT1423121E (https=) |
| RU (1) | RU2326119C2 (https=) |
| WO (1) | WO2003020278A1 (https=) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR036375A1 (es) * | 2001-08-30 | 2004-09-01 | Novartis Ag | Compuestos pirrolo [2,3-d] pirimidina -2- carbonitrilo, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos |
| SE0201976D0 (sv) * | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| SE0201980D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| GB0220187D0 (en) * | 2002-08-30 | 2002-10-09 | Novartis Ag | Organic compounds |
| TW200510436A (en) * | 2003-07-21 | 2005-03-16 | Novartis Ag | Combinations of a cathepsin k inhibitor and a bisphosphonate in the treatment of bone metastasis, tumor growth and tumor-induced bone loss |
| WO2005011703A1 (en) * | 2003-08-04 | 2005-02-10 | Akzo Nobel N.V. | 2-cyano-1,3,5-triazine-4,6-diamine derivatives |
| WO2005030128A2 (en) * | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Pyrazole modulators of metabotropic glutamate receptors |
| CN1882343A (zh) * | 2003-11-19 | 2006-12-20 | 诺瓦提斯公司 | 组织蛋白酶k抑制剂在严重骨损失疾病中的用途 |
| JPWO2005103012A1 (ja) * | 2004-04-21 | 2008-03-13 | 小野薬品工業株式会社 | ヒドラジノ複素環ニトリル化合物およびその用途 |
| TW200614993A (en) | 2004-06-11 | 2006-05-16 | Akzo Nobel Nv | 4-phenyl-pyrimidine-2-carbonitrile derivatives |
| TW200624429A (en) * | 2004-09-07 | 2006-07-16 | Glaxo Group Ltd | Novel cysteine protease inhibitors |
| WO2006040300A1 (en) * | 2004-10-12 | 2006-04-20 | N.V. Organon | 4-cycloalkyl-pyrimidine-2-carbonitrile derivatives |
| IL164942A0 (en) * | 2004-10-31 | 2005-12-18 | Yeda Res & Dev | The use of a protease or a protease inhibitor for the manufacture of medicaments |
| GB0514684D0 (en) * | 2005-07-18 | 2005-08-24 | Novartis Ag | Organic compounds |
| CA2617725C (en) * | 2005-08-05 | 2012-04-03 | Hybrigenics Sa | Novel cysteine protease inhibitors and their therapeutic applications |
| AR057110A1 (es) * | 2005-09-02 | 2007-11-14 | Glaxo Group Ltd | DERIVADOS DE HETEROARIL-NITRILOS SUSTITUíDOS QUE SON INHIBIDORES DE PROTEASAS |
| US7326715B2 (en) | 2005-09-23 | 2008-02-05 | N.V. Organon | 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives |
| TW200745055A (en) * | 2005-09-23 | 2007-12-16 | Organon Nv | 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives |
| US7687515B2 (en) | 2006-01-17 | 2010-03-30 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| AU2007253796A1 (en) * | 2006-05-22 | 2007-11-29 | Velcura Therapeutics, Inc. | Use of Cathepsin K antagonists in bone production |
| US20090227579A1 (en) * | 2006-06-23 | 2009-09-10 | Astrazeneca Ab | Pteridine Derivatives and their Use as Cathespin Inhibitors |
| EP1947091A1 (en) * | 2007-01-16 | 2008-07-23 | Glaxo Group Limited | Pyrimidyl nitrile derivatives as cysteine protease inhibitors |
| US7932251B2 (en) | 2007-07-16 | 2011-04-26 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| KR101595238B1 (ko) | 2007-12-21 | 2016-02-18 | 리간드 파마슈티칼스 인코포레이티드 | 선택적 안드로겐 수용체 조절제(ｓａｒｍ) 및 이의 용도 |
| EP2719700A1 (en) | 2008-01-09 | 2014-04-16 | Amura Therapeutics Limited | Tetrahydrofuro(3,2-b)pyrrol-3-one derivatives as inhibitors of cysteine proteinases |
| TW201035094A (en) | 2009-01-16 | 2010-10-01 | Organon Nv | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| US8026236B2 (en) | 2009-01-16 | 2011-09-27 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| EP2316820A1 (en) * | 2009-10-28 | 2011-05-04 | Dompe S.p.A. | 2-aryl-propionamide derivatives useful as bradykinin receptor antagonists and pharmaceutical compositions containing them |
| WO2011086125A1 (en) | 2010-01-15 | 2011-07-21 | N.V. Organon | 1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES |
| CN108192972B (zh) | 2010-10-06 | 2022-09-09 | 生物医学研究机构基金会 | 用于乳腺癌转移的诊断、预后和治疗的方法 |
| US8524710B2 (en) * | 2010-11-05 | 2013-09-03 | Hoffmann-La Roche Inc. | Pyrrolidine derivatives |
| EP2650682A1 (en) | 2012-04-09 | 2013-10-16 | Fundació Privada Institut de Recerca Biomèdica | Method for the prognosis and treatment of cancer metastasis |
| BR112014030750A2 (pt) | 2012-06-06 | 2017-08-22 | Inst Catalana Recerca Estudis Avancats | Método para diagnóstico, prognóstico e tratamento da metástase do câncer pulmonar |
| ES2906586T3 (es) | 2012-10-12 | 2022-04-19 | Inbiomotion Sl | Método para el diagnóstico, pronóstico y tratamiento de metástasis de cáncer de próstata |
| US10119171B2 (en) | 2012-10-12 | 2018-11-06 | Inbiomotion S.L. | Method for the diagnosis, prognosis and treatment of prostate cancer metastasis |
| WO2014184679A2 (en) | 2013-03-15 | 2014-11-20 | Inbiomotion S.L. | Method for the prognosis and treatment of renal cell carcinoma metastasis |
| CA2906394A1 (en) | 2013-03-15 | 2014-09-18 | Fundacio Institut De Recerca Biomedica (Irb Barcelona) | Method for the prognosis and treatment of cancer metastasis |
| DK3055429T3 (en) | 2013-10-09 | 2019-04-23 | Fundacio Inst De Recerca Biomedica Irb Barcelona | Procedure for the prognosis and treatment of metastatic bone cancer resulting from breast cancer |
| EP3094323A4 (en) | 2014-01-17 | 2017-10-11 | Ligand Pharmaceuticals Incorporated | Methods and compositions for modulating hormone levels |
| KR20170093182A (ko) | 2014-12-11 | 2017-08-14 | 인바이오모션 에스.엘. | 인간 c-maf에 대한 결합 구성원 |
| US11596642B2 (en) | 2016-05-25 | 2023-03-07 | Inbiomotion S.L. | Therapeutic treatment of breast cancer based on c-MAF status |
| US11160801B2 (en) * | 2017-01-27 | 2021-11-02 | Genfit | RORgamma modulators and uses thereof |
| CN108586356B (zh) * | 2017-03-16 | 2021-02-19 | 杭州科巢生物科技有限公司 | 瑞博西尼新中间体及其制备瑞博西尼的合成方法 |
| KR20200104298A (ko) | 2017-11-22 | 2020-09-03 | 인바이오모션 에스.엘. | c-MAF 상태에 기반한 유방암의 요법 치료 |
| CN109467536B (zh) * | 2018-12-23 | 2020-06-05 | 沧州普瑞东方科技有限公司 | 2-氯/羟基嘧啶-5-羧酸的合成方法 |
| AU2020250933A1 (en) | 2019-04-05 | 2021-10-28 | Centre Hospitalier Régional Et Universitaire De Brest | Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning |
| AU2020257397B2 (en) | 2019-04-19 | 2026-02-26 | Ligand Pharmaceuticals Inc. | Crystalline forms and methods of producing crystalline forms of a compound |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE609808A (https=) | 1960-11-02 | |||
| NL295648A (https=) * | 1962-07-26 | |||
| BR6915234D0 (pt) | 1969-05-22 | 1973-06-07 | American Cyanamid Co | Novos derivados de melamina e processo para sua preparaca |
| CH627919A5 (de) * | 1977-04-14 | 1982-02-15 | Ciba Geigy Ag | Herbizide mittel. |
| CA2230894A1 (en) * | 1995-09-01 | 1997-03-13 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions |
| US6313127B1 (en) | 1996-02-02 | 2001-11-06 | Zeneca Limited | Heterocyclic compounds useful as pharmaceutical agents |
| DE19817459A1 (de) | 1998-04-20 | 1999-10-21 | Basf Ag | Neue heterozyklische substituierte Amide, Herstellung und Anwendung |
| YU17402A (sh) | 1999-09-13 | 2004-11-25 | Boehringer Ingelheim Pharmaceuticals Inc. | Nova spiroheterociklična jedinjenja upotrebljiva kao reverzibilni inhibitori cisteinskih proteaza |
| EP1219609B1 (en) * | 1999-09-16 | 2007-04-04 | Tanabe Seiyaku Co., Ltd. | Aromatic nitrogenous six-membered ring compounds |
| NZ522217A (en) * | 2000-04-28 | 2004-04-30 | Tanabe Seiyaku Co | Cyclic compounds |
| GB0013383D0 (en) | 2000-06-01 | 2000-07-26 | Glaxo Group Ltd | Therapeutic benzamide derivatives |
| AR036375A1 (es) * | 2001-08-30 | 2004-09-01 | Novartis Ag | Compuestos pirrolo [2,3-d] pirimidina -2- carbonitrilo, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos |
| SE0201976D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| SE0201980D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
-
2002
- 2002-08-28 AR ARP020103230A patent/AR036375A1/es not_active Application Discontinuation
- 2002-08-29 CA CA002456127A patent/CA2456127C/en not_active Expired - Fee Related
- 2002-08-29 PE PE2002000834A patent/PE20030772A1/es not_active Application Discontinuation
- 2002-08-29 PT PT02797650T patent/PT1423121E/pt unknown
- 2002-08-29 AT AT02797650T patent/ATE345136T1/de active
- 2002-08-29 PL PL367821A patent/PL208280B1/pl not_active IP Right Cessation
- 2002-08-29 US US10/487,741 patent/US7112589B2/en not_active Expired - Fee Related
- 2002-08-29 BR BR0212141-7A patent/BR0212141A/pt not_active IP Right Cessation
- 2002-08-29 EP EP02797650A patent/EP1423121B1/en not_active Expired - Lifetime
- 2002-08-29 KR KR1020047002973A patent/KR100629834B1/ko not_active Expired - Fee Related
- 2002-08-29 NZ NZ531287A patent/NZ531287A/en unknown
- 2002-08-29 CN CN028169638A patent/CN1549717B/zh not_active Expired - Fee Related
- 2002-08-29 JP JP2003524585A patent/JP4131701B2/ja not_active Expired - Fee Related
- 2002-08-29 IL IL16029502A patent/IL160295A0/xx unknown
- 2002-08-29 AU AU2002333758A patent/AU2002333758B2/en not_active Ceased
- 2002-08-29 RU RU2004109812/04A patent/RU2326119C2/ru not_active IP Right Cessation
- 2002-08-29 HU HU0401431A patent/HUP0401431A3/hu unknown
- 2002-08-29 ES ES02797650T patent/ES2275946T3/es not_active Expired - Lifetime
- 2002-08-29 DE DE60216122T patent/DE60216122T2/de not_active Expired - Lifetime
- 2002-08-29 WO PCT/EP2002/009661 patent/WO2003020278A1/en not_active Ceased
- 2002-08-29 MX MXPA04001930A patent/MXPA04001930A/es active IP Right Grant
-
2004
- 2004-02-25 CO CO04016657A patent/CO5560576A2/es not_active Application Discontinuation
-
2005
- 2005-11-30 US US11/291,007 patent/US20060074092A1/en not_active Abandoned
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