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 (enExample) | 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 (enExample) |
| EP (1) | EP1423121B1 (enExample) |
| JP (1) | JP4131701B2 (enExample) |
| KR (1) | KR100629834B1 (enExample) |
| CN (1) | CN1549717B (enExample) |
| AR (1) | AR036375A1 (enExample) |
| AT (1) | ATE345136T1 (enExample) |
| AU (1) | AU2002333758B2 (enExample) |
| BR (1) | BR0212141A (enExample) |
| CA (1) | CA2456127C (enExample) |
| CO (1) | CO5560576A2 (enExample) |
| DE (1) | DE60216122T2 (enExample) |
| ES (1) | ES2275946T3 (enExample) |
| HU (1) | HUP0401431A3 (enExample) |
| IL (1) | IL160295A0 (enExample) |
| MX (1) | MXPA04001930A (enExample) |
| NZ (1) | NZ531287A (enExample) |
| PE (1) | PE20030772A1 (enExample) |
| PL (1) | PL208280B1 (enExample) |
| PT (1) | PT1423121E (enExample) |
| RU (1) | RU2326119C2 (enExample) |
| WO (1) | WO2003020278A1 (enExample) |
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 |
| SE0201980D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| SE0201976D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| GB0220187D0 (en) | 2002-08-30 | 2002-10-09 | Novartis Ag | Organic compounds |
| US20060281714A1 (en) * | 2003-07-21 | 2006-12-14 | Johann Zimmermann | 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 |
| US20060281803A1 (en) * | 2003-09-23 | 2006-12-14 | Lindsley Craig W | Pyrazole modulators of metabotropic glutamate receptors |
| EP1686995A1 (en) * | 2003-11-19 | 2006-08-09 | Novartis AG | Use of cathepsin k inhibitors for treating of severe bone loss diseases |
| WO2005103012A1 (ja) * | 2004-04-21 | 2005-11-03 | Ono Pharmaceutical Co., Ltd. | 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 |
| AR050858A1 (es) * | 2004-09-07 | 2006-11-29 | Glaxo Group Ltd | Compuesto de heteroaril-nitrilo sustituido, su uso para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para la preparacion del mismo |
| 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 |
| RU2424234C2 (ru) * | 2005-08-05 | 2011-07-20 | Ибриженикс Са | Новые ингибиторы цистеиновых протеаз и их терапевтическое применение |
| AR057110A1 (es) * | 2005-09-02 | 2007-11-14 | Glaxo Group Ltd | DERIVADOS DE HETEROARIL-NITRILOS SUSTITUíDOS QUE SON INHIBIDORES DE PROTEASAS |
| TW200745055A (en) * | 2005-09-23 | 2007-12-16 | Organon Nv | 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives |
| US7326715B2 (en) | 2005-09-23 | 2008-02-05 | N.V. Organon | 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 |
| WO2007137149A2 (en) * | 2006-05-22 | 2007-11-29 | Velcura Therapeutics, Inc. | Use of cathepsin k antagonists in bone production |
| CN101479269A (zh) * | 2006-06-23 | 2009-07-08 | 阿斯利康(瑞典)有限公司 | 蝶啶衍生物及其作为组织蛋白酶抑制剂的用途 |
| 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 |
| CN101945853B (zh) | 2007-12-21 | 2014-08-20 | 配体药物公司 | 选择性雄激素受体调节剂(sarm)及其应用 |
| JP5587790B2 (ja) | 2008-01-09 | 2014-09-10 | アミュラ セラピューティクス リミティド | 化合物 |
| US8026236B2 (en) | 2009-01-16 | 2011-09-27 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
| TW201035094A (en) | 2009-01-16 | 2010-10-01 | Organon Nv | 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 |
| EP2523954B1 (en) | 2010-01-15 | 2014-04-16 | Merck Sharp & Dohme B.V. | 1h-[1,2,3]triazolo[4,5-c]pyridine-4- carbonitrile derivatives as cathepsin s inhibitors |
| ES2562274T3 (es) | 2010-10-06 | 2016-03-03 | Fundació Institut De Recerca Biomèdica (Irb Barcelona) | Procedimiento para el diagnóstico, pronóstico y tratamiento de metástasis de cáncer de mama |
| 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 |
| EP3467124A1 (en) | 2012-06-06 | 2019-04-10 | Fundació Institut de Recerca Biomèdica IRB (Barcelona) | Method for the diagnosis, prognosis and treatment of lung cancer metastasis |
| CA2888122A1 (en) | 2012-10-12 | 2014-04-17 | Inbiomotion S.L. | Method for the diagnosis, prognosis and treatment of prostate cancer metastasis using c-maf |
| US10119171B2 (en) | 2012-10-12 | 2018-11-06 | Inbiomotion S.L. | Method for the diagnosis, prognosis and treatment of prostate cancer metastasis |
| US20160032400A1 (en) | 2013-03-15 | 2016-02-04 | Fundació Institut De Recerca Biomèdica (Irb Barcelona) | Method for the prognosis and treatment of cancer metastasis |
| US20160032399A1 (en) | 2013-03-15 | 2016-02-04 | Inbiomotion S.L. | Method for the Prognosis and Treatment of Renal Cell Carcinoma Metastasis |
| EP3524698A1 (en) | 2013-10-09 | 2019-08-14 | Fundació Institut de Recerca Biomèdica IRB (Barcelona) | Method for the prognosis and treatment of cancer metastasis |
| EP3613418A1 (en) | 2014-01-17 | 2020-02-26 | Ligand Pharmaceuticals, Inc. | Methods and compositions for modulating hormone levels |
| KR20170093182A (ko) | 2014-12-11 | 2017-08-14 | 인바이오모션 에스.엘. | 인간 c-maf에 대한 결합 구성원 |
| CA3025264A1 (en) | 2016-05-25 | 2017-11-30 | Inbiomotion S.L. | Therapeutic treatment of breast cancer based on c-maf status |
| KR20190112009A (ko) * | 2017-01-27 | 2019-10-02 | 장피트 | Ror감마 조절제 및 이의 용도 |
| 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 |
| CA3082728A1 (en) | 2017-11-22 | 2019-05-31 | Inbiomotion S.L. | Therapeutic treatment of breast cancer based on c-maf status |
| 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 |
|---|---|---|---|---|
| NL270922A (enExample) | 1960-11-02 | |||
| NL295648A (enExample) * | 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. |
| JPH11512399A (ja) * | 1995-09-01 | 1999-10-26 | シグナル ファーマシューティカルズ，インコーポレイテッド | ピリミジンカルボキサミドおよび関連化合物ならびに炎症状態を処置するための方法 |
| 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 |
| HUP0302380A2 (hu) * | 1999-09-13 | 2004-03-01 | Boehringer Ingelheim Pharmaceuticals, Inc. | Cisztein-proteázok reverzibilis inhibitoraiként alkalmazható új spiroheterociklusos vegyületek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények |
| CA2383466C (en) * | 1999-09-16 | 2009-08-25 | Tanabe Seiyaku Co., Ltd. | Aromatic nitrogen-containing 6-membered cyclic compounds |
| KR100711042B1 (ko) | 2000-04-28 | 2007-04-24 | 다나베 세이야꾸 가부시키가이샤 | 환상 화합물 |
| 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 |
| SE0201980D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| SE0201976D0 (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 HU HU0401431A patent/HUP0401431A3/hu unknown
- 2002-08-29 CN CN028169638A patent/CN1549717B/zh not_active Expired - Fee Related
- 2002-08-29 PL PL367821A patent/PL208280B1/pl not_active IP Right Cessation
- 2002-08-29 CA CA002456127A patent/CA2456127C/en not_active Expired - Fee Related
- 2002-08-29 DE DE60216122T patent/DE60216122T2/de not_active Expired - Lifetime
- 2002-08-29 RU RU2004109812/04A patent/RU2326119C2/ru not_active IP Right Cessation
- 2002-08-29 ES ES02797650T patent/ES2275946T3/es not_active Expired - Lifetime
- 2002-08-29 AU AU2002333758A patent/AU2002333758B2/en not_active Ceased
- 2002-08-29 EP EP02797650A patent/EP1423121B1/en not_active Expired - Lifetime
- 2002-08-29 PT PT02797650T patent/PT1423121E/pt unknown
- 2002-08-29 NZ NZ531287A patent/NZ531287A/en unknown
- 2002-08-29 MX MXPA04001930A patent/MXPA04001930A/es active IP Right Grant
- 2002-08-29 WO PCT/EP2002/009661 patent/WO2003020278A1/en not_active Ceased
- 2002-08-29 KR KR1020047002973A patent/KR100629834B1/ko not_active Expired - Fee Related
- 2002-08-29 IL IL16029502A patent/IL160295A0/xx unknown
- 2002-08-29 PE PE2002000834A patent/PE20030772A1/es not_active Application Discontinuation
- 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 JP JP2003524585A patent/JP4131701B2/ja not_active Expired - Fee Related
- 2002-08-29 AT AT02797650T patent/ATE345136T1/de active
-
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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