HUP0003931A2 - Vitronectin receptor antagonist and pharmaceutical compositions containing the compounds - Google Patents
Vitronectin receptor antagonist and pharmaceutical compositions containing the compoundsInfo
- Publication number
- HUP0003931A2 HUP0003931A2 HU0003931A HUP0003931A HUP0003931A2 HU P0003931 A2 HUP0003931 A2 HU P0003931A2 HU 0003931 A HU0003931 A HU 0003931A HU P0003931 A HUP0003931 A HU P0003931A HU P0003931 A2 HUP0003931 A2 HU P0003931A2
- Authority
- HU
- Hungary
- Prior art keywords
- compounds
- vitronectin receptor
- pharmaceutical compositions
- compositions containing
- receptor antagonist
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 102100022337 Integrin alpha-V Human genes 0.000 title abstract 3
- 108010048673 Vitronectin Receptors Proteins 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000002464 receptor antagonist Substances 0.000 title 1
- 229940044551 receptor antagonist Drugs 0.000 title 1
- 208000006386 Bone Resorption Diseases 0.000 abstract 2
- 230000024279 bone resorption Effects 0.000 abstract 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 101000781681 Protobothrops flavoviridis Disintegrin triflavin Proteins 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 210000002997 osteoclast Anatomy 0.000 abstract 1
- 230000001599 osteoclastic effect Effects 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A találmány (I) képletű vegyületre, azaz (S)-4-(karboxi-metil)-8-{3-[(2-piridil)-amino]-1-propoxi}-3-oxo-2-(2,3,4-trifluor-benzil)-2,3,4,5-tetrahidro-lH-2-benzazepinre és gyógyászatilag elfogadhatósóira vonatkozik. A találmány szerinti vegyület gátolja avitronektinnek és más RGD-tartalmú peptideknek a vitronektinreceptorhoz történő kötődését. Az osteoclastokon lévő vitronektinreceptor inhibíciója gátolja az osteoclasticus csontreszorpciót és ígyfelhasználható az olyan betegségek kezelésére, amelyekben acsontreszorpció egy patológiás állapottal, például osteoporosisszalvagy osteoarthritisszel áll összefüggésben. A találmány kiterjed avegyületek új intermediereire, valamint a vegyületeket tartalmazógyógyszerkészítményekre és a vegyületek gyógyászati alkalmazására is. ÓThe invention relates to the compound of formula (I), i.e. (S)-4-(carboxymethyl)-8-{3-[(2-pyridyl)amino]-1-propoxy}-3-oxo-2-(2, It refers to 3,4-trifluorobenzyl)-2,3,4,5-tetrahydro-1H-2-benzazepine and its pharmaceutically acceptable salts. The compound according to the invention inhibits the binding of avitronectin and other RGD-containing peptides to the vitronectin receptor. Inhibition of the vitronectin receptor on osteoclasts inhibits osteoclastic bone resorption and can thus be used to treat diseases in which bone resorption is associated with a pathological condition, such as osteoporosis or osteoarthritis. The invention also covers new intermediates of the compounds, as well as pharmaceutical preparations containing the compounds and the medicinal use of the compounds. HE
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5986797P | 1997-09-24 | 1997-09-24 | |
| PCT/US1998/019987 WO1999015178A1 (en) | 1997-09-24 | 1998-09-24 | Vitronectin receptor antagonist |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HUP0003931A2 true HUP0003931A2 (en) | 2001-10-28 |
Family
ID=22025805
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0003931A HUP0003931A2 (en) | 1997-09-24 | 1998-09-24 | Vitronectin receptor antagonist and pharmaceutical compositions containing the compounds |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1023073A1 (en) |
| JP (1) | JP2002500162A (en) |
| KR (1) | KR20010024249A (en) |
| CN (1) | CN1271284A (en) |
| AU (1) | AU9578798A (en) |
| BR (1) | BR9813214A (en) |
| CA (1) | CA2304000A1 (en) |
| HU (1) | HUP0003931A2 (en) |
| IL (1) | IL135188A0 (en) |
| NO (1) | NO20001515L (en) |
| PL (1) | PL339414A1 (en) |
| TR (1) | TR200000786T2 (en) |
| WO (1) | WO1999015178A1 (en) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2358855A1 (en) | 1999-02-03 | 2000-08-10 | Merck & Co., Inc. | Benzazepine derivatives as alpha-v integrin receptor antagonists |
| US6514964B1 (en) | 1999-09-27 | 2003-02-04 | Amgen Inc. | Fused cycloheptane and fused azacycloheptane compounds and their methods of use |
| DK1381384T3 (en) | 2001-04-24 | 2011-07-25 | Merck Patent Gmbh | Combination therapy using anti-angiogenic agents and TNFalfa |
| KR20040058229A (en) | 2001-10-22 | 2004-07-03 | 더 스크립스 리서치 인스티튜트 | Antibody targeting compounds |
| WO2004089890A2 (en) * | 2003-04-04 | 2004-10-21 | Smithkline Beecham Corporation | Process and intermediates for preparing benzazepines |
| US7579529B2 (en) | 2004-02-02 | 2009-08-25 | Pioneer Hi-Bred International, Inc. | AP2 domain transcription factor ODP2 (ovule development protein 2) and methods of use |
| UA87854C2 (en) | 2004-06-07 | 2009-08-25 | Мерк Энд Ко., Инк. | N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators |
| ES2425396T3 (en) | 2006-01-18 | 2013-10-15 | Merck Patent Gmbh | Specific therapy using integrin ligands for cancer treatment |
| MX2009007597A (en) | 2007-01-18 | 2009-07-22 | Merck Patent Gmbh | Specific therapy and medicament using integrin ligands for treating cancer. |
| JP5359879B2 (en) | 2007-11-16 | 2013-12-04 | 宇部興産株式会社 | Benzazepinone compounds |
| EP2257538B1 (en) * | 2008-03-06 | 2016-04-27 | GlaxoSmithKline LLC | Process for the preparation of benzodiazepine derivatives |
| JP2012517447A (en) | 2009-02-10 | 2012-08-02 | ザ スクリプス リサーチ インスティチュート | Chemically programmed vaccination methods |
| CN102427816A (en) | 2009-03-30 | 2012-04-25 | 宇部兴产株式会社 | Pharmaceutical composition for treatment or prevention of ophthalmic diseases |
| KR20120104491A (en) | 2009-05-25 | 2012-09-21 | 메르크 파텐트 게엠베하 | Continuous administration of cilengitide in cancer treatments |
| AU2010339404B2 (en) | 2009-12-30 | 2016-01-28 | Pioneer Hi-Bred International, Inc. | Methods and compositions for the introduction and regulated expression of genes in plants |
| WO2011082310A2 (en) | 2009-12-30 | 2011-07-07 | Pioneer Hi-Bred International, Inc. | Methods and compositions for targeted polynucleotide modification |
| US10328082B2 (en) | 2014-05-30 | 2019-06-25 | Pfizer Inc. | Methods of use and combinations |
| WO2023275715A1 (en) | 2021-06-30 | 2023-01-05 | Pfizer Inc. | Metabolites of selective androgen receptor modulators |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA60311C2 (en) * | 1996-10-02 | 2003-10-15 | Смітклайн Бічам Корпорейшн | Vitronectin receptor antagonists |
-
1998
- 1998-09-24 CA CA002304000A patent/CA2304000A1/en not_active Abandoned
- 1998-09-24 IL IL13518898A patent/IL135188A0/en unknown
- 1998-09-24 KR KR1020007003093A patent/KR20010024249A/en not_active Application Discontinuation
- 1998-09-24 WO PCT/US1998/019987 patent/WO1999015178A1/en not_active Application Discontinuation
- 1998-09-24 BR BR9813214-8A patent/BR9813214A/en not_active Application Discontinuation
- 1998-09-24 EP EP98949471A patent/EP1023073A1/en active Pending
- 1998-09-24 PL PL98339414A patent/PL339414A1/en unknown
- 1998-09-24 JP JP2000512547A patent/JP2002500162A/en not_active Withdrawn
- 1998-09-24 HU HU0003931A patent/HUP0003931A2/en unknown
- 1998-09-24 AU AU95787/98A patent/AU9578798A/en not_active Abandoned
- 1998-09-24 CN CN98809494A patent/CN1271284A/en active Pending
- 1998-09-24 TR TR2000/00786T patent/TR200000786T2/en unknown
-
2000
- 2000-03-23 NO NO20001515A patent/NO20001515L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| NO20001515D0 (en) | 2000-03-23 |
| JP2002500162A (en) | 2002-01-08 |
| NO20001515L (en) | 2000-03-23 |
| EP1023073A1 (en) | 2000-08-02 |
| WO1999015178A1 (en) | 1999-04-01 |
| CN1271284A (en) | 2000-10-25 |
| AU9578798A (en) | 1999-04-12 |
| BR9813214A (en) | 2000-08-29 |
| CA2304000A1 (en) | 1999-04-01 |
| PL339414A1 (en) | 2000-12-18 |
| KR20010024249A (en) | 2001-03-26 |
| TR200000786T2 (en) | 2000-08-21 |
| IL135188A0 (en) | 2001-05-20 |
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