DE60216122T2 - Cysteinprotease-hemmer mit 2-cyano-4-amino-pyrimidinstruktur und cathepsin-k-hemmender wirkung zur behandlung von entzündungen und anderen erkrankungen - Google Patents
Cysteinprotease-hemmer mit 2-cyano-4-amino-pyrimidinstruktur und cathepsin-k-hemmender wirkung zur behandlung von entzündungen und anderen erkrankungen Download PDFInfo
- Publication number
- DE60216122T2 DE60216122T2 DE60216122T DE60216122T DE60216122T2 DE 60216122 T2 DE60216122 T2 DE 60216122T2 DE 60216122 T DE60216122 T DE 60216122T DE 60216122 T DE60216122 T DE 60216122T DE 60216122 T2 DE60216122 T2 DE 60216122T2
- Authority
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- Prior art keywords
- alkyl
- heterocyclyl
- aryl
- cycloalkyl
- optionally
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- Expired - Lifetime
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- 229940124158 Protease/peptidase inhibitor Drugs 0.000 title 1
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- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
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| GB0121024 | 2001-08-30 | ||
| GBGB0121026.9A GB0121026D0 (en) | 2001-08-30 | 2001-08-30 | Organic compounds |
| GB0121024A GB0121024D0 (en) | 2001-08-30 | 2001-08-30 | Organic compounds |
| GB0121026 | 2001-08-30 | ||
| 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 (2)
| Publication Number | Publication Date |
|---|---|
| DE60216122D1 DE60216122D1 (de) | 2006-12-28 |
| DE60216122T2 true DE60216122T2 (de) | 2007-09-06 |
Family
ID=26246490
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60216122T Expired - Lifetime DE60216122T2 (de) | 2001-08-30 | 2002-08-29 | Cysteinprotease-hemmer mit 2-cyano-4-amino-pyrimidinstruktur und cathepsin-k-hemmender wirkung zur behandlung von entzündungen und anderen erkrankungen |
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| EP (1) | EP1423121B1 (enExample) |
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| AR (1) | AR036375A1 (enExample) |
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| BR (1) | BR0212141A (enExample) |
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| 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) |
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| 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 |
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| 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 |
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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
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2004
- 2004-02-25 CO CO04016657A patent/CO5560576A2/es not_active Application Discontinuation
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2005
- 2005-11-30 US US11/291,007 patent/US20060074092A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| ATE345136T1 (de) | 2006-12-15 |
| AU2002333758B2 (en) | 2006-01-19 |
| PE20030772A1 (es) | 2003-10-02 |
| KR20040029101A (ko) | 2004-04-03 |
| ES2275946T3 (es) | 2007-06-16 |
| PL367821A1 (en) | 2005-03-07 |
| KR100629834B1 (ko) | 2006-09-29 |
| IL160295A0 (en) | 2004-07-25 |
| PT1423121E (pt) | 2007-02-28 |
| EP1423121B1 (en) | 2006-11-15 |
| WO2003020278A1 (en) | 2003-03-13 |
| US20040249153A1 (en) | 2004-12-09 |
| PL208280B1 (pl) | 2011-04-29 |
| CN1549717B (zh) | 2011-08-17 |
| CO5560576A2 (es) | 2005-09-30 |
| US7112589B2 (en) | 2006-09-26 |
| MXPA04001930A (es) | 2004-06-15 |
| US20060074092A1 (en) | 2006-04-06 |
| JP2005505550A (ja) | 2005-02-24 |
| HUP0401431A3 (en) | 2004-11-29 |
| EP1423121A1 (en) | 2004-06-02 |
| RU2004109812A (ru) | 2005-10-20 |
| RU2326119C2 (ru) | 2008-06-10 |
| BR0212141A (pt) | 2004-08-24 |
| CA2456127A1 (en) | 2003-03-13 |
| CN1549717A (zh) | 2004-11-24 |
| JP4131701B2 (ja) | 2008-08-13 |
| HUP0401431A2 (hu) | 2004-10-28 |
| CA2456127C (en) | 2009-10-20 |
| NZ531287A (en) | 2005-12-23 |
| AR036375A1 (es) | 2004-09-01 |
| DE60216122D1 (de) | 2006-12-28 |
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