CA2303846A1 - Antagoniste du recepteur de vitronectine - Google Patents
Antagoniste du recepteur de vitronectine Download PDFInfo
- Publication number
- CA2303846A1 CA2303846A1 CA002303846A CA2303846A CA2303846A1 CA 2303846 A1 CA2303846 A1 CA 2303846A1 CA 002303846 A CA002303846 A CA 002303846A CA 2303846 A CA2303846 A CA 2303846A CA 2303846 A1 CA2303846 A1 CA 2303846A1
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- Prior art keywords
- compound
- mmol
- cells
- compound according
- medicament
- 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.)
- Abandoned
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- VVWRJUBEIPHGQF-UHFFFAOYSA-N propan-2-yl n-propan-2-yloxycarbonyliminocarbamate Chemical compound CC(C)OC(=O)N=NC(=O)OC(C)C VVWRJUBEIPHGQF-UHFFFAOYSA-N 0.000 description 1
- FVSKHRXBFJPNKK-UHFFFAOYSA-N propionitrile Chemical compound CCC#N FVSKHRXBFJPNKK-UHFFFAOYSA-N 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 238000010926 purge Methods 0.000 description 1
- ILVXOBCQQYKLDS-UHFFFAOYSA-N pyridine N-oxide Chemical group [O-][N+]1=CC=CC=C1 ILVXOBCQQYKLDS-UHFFFAOYSA-N 0.000 description 1
- 230000009257 reactivity Effects 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 238000007634 remodeling Methods 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 238000002390 rotary evaporation Methods 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 238000013391 scatchard analysis Methods 0.000 description 1
- 238000007790 scraping Methods 0.000 description 1
- 230000036303 septic shock Effects 0.000 description 1
- 238000010898 silica gel chromatography Methods 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 230000015590 smooth muscle cell migration Effects 0.000 description 1
- 239000003998 snake venom Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- HELHAJAZNSDZJO-OLXYHTOASA-L sodium L-tartrate Chemical compound [Na+].[Na+].[O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O HELHAJAZNSDZJO-OLXYHTOASA-L 0.000 description 1
- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- IHQKEDIOMGYHEB-UHFFFAOYSA-M sodium dimethylarsinate Chemical compound [Na+].C[As](C)([O-])=O IHQKEDIOMGYHEB-UHFFFAOYSA-M 0.000 description 1
- 238000002415 sodium dodecyl sulfate polyacrylamide gel electrophoresis Methods 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- 235000010265 sodium sulphite Nutrition 0.000 description 1
- 239000001433 sodium tartrate Substances 0.000 description 1
- 229960002167 sodium tartrate Drugs 0.000 description 1
- 235000011004 sodium tartrates Nutrition 0.000 description 1
- 238000000527 sonication Methods 0.000 description 1
- 230000009870 specific binding Effects 0.000 description 1
- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical compound C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 230000007480 spreading Effects 0.000 description 1
- 238000003892 spreading Methods 0.000 description 1
- 230000010473 stable expression Effects 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 229960002317 succinimide Drugs 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- OGBMKVWORPGQRR-UMXFMPSGSA-N teriparatide Chemical compound C([C@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)C1=CNC=N1 OGBMKVWORPGQRR-UMXFMPSGSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- YDLIGFUPCAQSBU-UHFFFAOYSA-N tert-butyl n-[(2-methylpropan-2-yl)oxycarbonyl]carbamate;potassium Chemical compound [K].CC(C)(C)OC(=O)NC(=O)OC(C)(C)C YDLIGFUPCAQSBU-UHFFFAOYSA-N 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 230000009424 thromboembolic effect Effects 0.000 description 1
- 229940034208 thyroxine Drugs 0.000 description 1
- XUIIKFGFIJCVMT-UHFFFAOYSA-N thyroxine-binding globulin Natural products IC1=CC(CC([NH3+])C([O-])=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-UHFFFAOYSA-N 0.000 description 1
- 238000001890 transfection Methods 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 238000009901 transfer hydrogenation reaction Methods 0.000 description 1
- 108091007466 transmembrane glycoproteins Proteins 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 210000004509 vascular smooth muscle cell Anatomy 0.000 description 1
- 229960001134 von willebrand factor Drugs 0.000 description 1
- 230000029663 wound healing Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
-
- 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
- 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
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
-
- 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
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Inorganic Chemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
L'invention concerne un composé représenté par la formule (I) qui est un antagoniste du récepteur de vitronectine, utile pour le traitement de l'ostéoporose: (I), ou un sel pharmaceutiquement acceptable de ce composé.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5983297P | 1997-09-24 | 1997-09-24 | |
| US60/059,832 | 1997-09-24 | ||
| PCT/US1998/019949 WO1999015170A1 (fr) | 1997-09-24 | 1998-09-24 | Antagoniste du recepteur de vitronectine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2303846A1 true CA2303846A1 (fr) | 1999-04-01 |
Family
ID=22025570
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002303846A Abandoned CA2303846A1 (fr) | 1997-09-24 | 1998-09-24 | Antagoniste du recepteur de vitronectine |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1017387A4 (fr) |
| JP (1) | JP2002528380A (fr) |
| KR (1) | KR20010024247A (fr) |
| CN (1) | CN1273529A (fr) |
| AU (1) | AU9577498A (fr) |
| BR (1) | BR9813208A (fr) |
| CA (1) | CA2303846A1 (fr) |
| HU (1) | HUP0003949A2 (fr) |
| IL (1) | IL135189A0 (fr) |
| NO (1) | NO20001514L (fr) |
| PL (1) | PL339413A1 (fr) |
| TR (1) | TR200000792T2 (fr) |
| WO (1) | WO1999015170A1 (fr) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1150965A4 (fr) | 1999-02-03 | 2002-05-15 | Merck & Co Inc | Derives de la benzazepine utilises comme antagonistes du recepteur alpha-v de l'integrine |
| US6514964B1 (en) * | 1999-09-27 | 2003-02-04 | Amgen Inc. | Fused cycloheptane and fused azacycloheptane compounds and their methods of use |
| AU2001288485A1 (en) * | 2000-08-29 | 2002-03-13 | Balekudru Devadas | Compounds containing a bicyclic ring system useful as alpha v beta 3 antagonists |
| US6531494B1 (en) | 2001-08-29 | 2003-03-11 | Pharmacia Corporation | Gem-substituted αvβ3 antagonists |
| PL365729A1 (en) * | 2000-08-30 | 2005-01-10 | Pharmacia Corporation | Gem-substituted alpha v beta 3 integrin antagonists |
| ES2366775T3 (es) | 2001-04-24 | 2011-10-25 | Merck Patent Gmbh | POLITERAPIA UTILIZANDO AGENTES ANTIANGIOGÉNICOS Y TNF(alfa). |
| WO2003059251A2 (fr) | 2001-10-22 | 2003-07-24 | The Scripps Research Institute | Composes de ciblage d'anticorps |
| UA87854C2 (en) | 2004-06-07 | 2009-08-25 | Мерк Энд Ко., Инк. | N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators |
| AU2007207465B2 (en) | 2006-01-18 | 2012-12-06 | Merck Patent Gmbh | Specific therapy using integrin ligands for treating cancer |
| BRPI0806596A2 (pt) | 2007-01-18 | 2013-07-23 | Merck Patent Ges Mit Berchraenkter Haftung | medicamento e terapia especÍfica usando-se ligantes de integrina para o tratamento de cÂncer |
| AU2008321770B2 (en) * | 2007-11-16 | 2012-09-06 | Ube Industries, Ltd. | Benzazepinone compound |
| US8076475B2 (en) * | 2008-03-06 | 2011-12-13 | Glaxosmithkline Llc | Process |
| WO2010093706A2 (fr) | 2009-02-10 | 2010-08-19 | The Scripps Research Institute | Vaccination programmée chimiquement |
| WO2010113958A1 (fr) | 2009-03-30 | 2010-10-07 | 宇部興産株式会社 | Composition pharmaceutique pour la prévention ou le traitement de maladies ophtalmiques |
| JP5572996B2 (ja) * | 2009-05-15 | 2014-08-20 | 宇部興産株式会社 | ベンズアゼピノン化合物を有効成分として含有する医薬 |
| EP2445534A2 (fr) | 2009-05-25 | 2012-05-02 | Merck Patent GmbH | Administration continue du cilengitide dans des traitements du cancer |
| CN103864765B (zh) * | 2014-03-05 | 2016-02-10 | 天津药物研究院 | 含有五元杂环的苯并氮杂卓类衍生物、其制备方法和用途 |
| ES2864079T3 (es) | 2014-05-30 | 2021-10-13 | Pfizer | Derivados de carbonitrilo como moduladores selectivos del receptor de andrógenos |
| WO2023275715A1 (fr) | 2021-06-30 | 2023-01-05 | Pfizer Inc. | Métabolites de modulateurs sélectifs du récepteur des androgènes |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA955391B (en) * | 1994-06-29 | 1996-02-09 | Smithkline Beecham Corp | Vitronectin receptor antagonists |
| UA60311C2 (uk) * | 1996-10-02 | 2003-10-15 | Смітклайн Бічам Корпорейшн | Антагоністи рецептора вітронектину, спосіб одержання цих сполук та фармацевтична композиція |
| EP0946180A4 (fr) * | 1996-10-07 | 2003-07-23 | Smithkline Beecham Corp | Procede de stimulation de la formation osseuse |
-
1998
- 1998-09-24 AU AU95774/98A patent/AU9577498A/en not_active Abandoned
- 1998-09-24 IL IL13518998A patent/IL135189A0/xx unknown
- 1998-09-24 CA CA002303846A patent/CA2303846A1/fr not_active Abandoned
- 1998-09-24 BR BR9813208-3A patent/BR9813208A/pt not_active Application Discontinuation
- 1998-09-24 CN CN98809495A patent/CN1273529A/zh active Pending
- 1998-09-24 EP EP98949454A patent/EP1017387A4/fr not_active Withdrawn
- 1998-09-24 TR TR2000/00792T patent/TR200000792T2/xx unknown
- 1998-09-24 PL PL98339413A patent/PL339413A1/xx unknown
- 1998-09-24 WO PCT/US1998/019949 patent/WO1999015170A1/fr not_active Ceased
- 1998-09-24 HU HU0003949A patent/HUP0003949A2/hu unknown
- 1998-09-24 JP JP2000512539A patent/JP2002528380A/ja not_active Withdrawn
- 1998-09-24 KR KR1020007003088A patent/KR20010024247A/ko not_active Withdrawn
-
2000
- 2000-03-23 NO NO20001514A patent/NO20001514L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| KR20010024247A (ko) | 2001-03-26 |
| NO20001514D0 (no) | 2000-03-23 |
| TR200000792T2 (tr) | 2000-09-21 |
| BR9813208A (pt) | 2000-08-22 |
| PL339413A1 (en) | 2000-12-18 |
| IL135189A0 (en) | 2001-05-20 |
| CN1273529A (zh) | 2000-11-15 |
| NO20001514L (no) | 2000-03-23 |
| WO1999015170A1 (fr) | 1999-04-01 |
| EP1017387A1 (fr) | 2000-07-12 |
| EP1017387A4 (fr) | 2004-08-18 |
| HUP0003949A2 (hu) | 2001-10-28 |
| JP2002528380A (ja) | 2002-09-03 |
| AU9577498A (en) | 1999-04-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |