JP2005501091A - アリールピペラジンとアリールピペリジン、およびメタロプロテイナーゼ阻害剤としてのそれらの使用 - Google Patents
アリールピペラジンとアリールピペリジン、およびメタロプロテイナーゼ阻害剤としてのそれらの使用 Download PDFInfo
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- JP2005501091A JP2005501091A JP2003519060A JP2003519060A JP2005501091A JP 2005501091 A JP2005501091 A JP 2005501091A JP 2003519060 A JP2003519060 A JP 2003519060A JP 2003519060 A JP2003519060 A JP 2003519060A JP 2005501091 A JP2005501091 A JP 2005501091A
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- compound
- alkyl
- pharmaceutically acceptable
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- 239000003475 metalloproteinase inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 117
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- 150000003839 salts Chemical class 0.000 claims description 36
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- 238000001727 in vivo Methods 0.000 claims description 33
- 125000000217 alkyl group Chemical group 0.000 claims description 32
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 20
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- 108010006035 Metalloproteases Proteins 0.000 claims description 18
- 201000010099 disease Diseases 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 17
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 5
- 239000002243 precursor Substances 0.000 claims description 5
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- MHKMIMPCEDHDDQ-QHCPKHFHSA-N n-hydroxy-n-[(2s)-1-[4-[5-(2-pyridin-2-ylethynyl)pyrimidin-2-yl]piperazin-1-yl]sulfonyl-5-pyrimidin-2-ylpentan-2-yl]formamide Chemical compound C([C@H](N(C=O)O)CS(=O)(=O)N1CCN(CC1)C=1N=CC(=CN=1)C#CC=1N=CC=CC=1)CCC1=NC=CC=N1 MHKMIMPCEDHDDQ-QHCPKHFHSA-N 0.000 claims description 3
- MHKMIMPCEDHDDQ-UHFFFAOYSA-N n-hydroxy-n-[1-[4-[5-(2-pyridin-2-ylethynyl)pyrimidin-2-yl]piperazin-1-yl]sulfonyl-5-pyrimidin-2-ylpentan-2-yl]formamide Chemical compound C1CN(C=2N=CC(=CN=2)C#CC=2N=CC=CC=2)CCN1S(=O)(=O)CC(N(C=O)O)CCCC1=NC=CC=N1 MHKMIMPCEDHDDQ-UHFFFAOYSA-N 0.000 claims description 3
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- YMWUJEATGCHHMB-UHFFFAOYSA-N methylene chloride Substances ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 21
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- RJHWOWJRQNENIC-UHFFFAOYSA-N tert-butyl 4-(5-iodopyridin-2-yl)piperazine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCN1C1=CC=C(I)C=N1 RJHWOWJRQNENIC-UHFFFAOYSA-N 0.000 description 1
- SLSRNBMIDCMDFO-UHFFFAOYSA-N tert-butyl 4-[5-(2-trimethylsilylethynyl)pyridin-2-yl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCN1C1=CC=C(C#C[Si](C)(C)C)C=N1 SLSRNBMIDCMDFO-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
- C07D295/26—Sulfur atoms
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- 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
-
- 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
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0119474.5A GB0119474D0 (en) | 2001-08-09 | 2001-08-09 | Compounds |
| PCT/SE2002/001436 WO2003014111A1 (en) | 2001-08-09 | 2002-08-08 | Arylpiperazines and arylpiperidines and their use as metalloproteinase inhibiting agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005501091A true JP2005501091A (ja) | 2005-01-13 |
| JP2005501091A5 JP2005501091A5 (enExample) | 2006-01-12 |
Family
ID=9920126
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003519060A Pending JP2005501091A (ja) | 2001-08-09 | 2002-08-08 | アリールピペラジンとアリールピペリジン、およびメタロプロテイナーゼ阻害剤としてのそれらの使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US7153857B2 (enExample) |
| EP (1) | EP1417201A1 (enExample) |
| JP (1) | JP2005501091A (enExample) |
| GB (1) | GB0119474D0 (enExample) |
| WO (1) | WO2003014111A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006511492A (ja) * | 2002-10-31 | 2006-04-06 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Mch拮抗活性を有する新規アルキン化合物及びこれらの化合物を含む薬物 |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7452911B2 (en) | 2002-10-31 | 2008-11-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
| US7351719B2 (en) | 2002-10-31 | 2008-04-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds |
| US7592373B2 (en) | 2003-12-23 | 2009-09-22 | Boehringer Ingelheim International Gmbh | Amide compounds with MCH antagonistic activity and medicaments comprising these compounds |
| US20050245529A1 (en) * | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim International Gmbh | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
| DE102004017934A1 (de) | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| DE102004017930A1 (de) * | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| US7524862B2 (en) | 2004-04-14 | 2009-04-28 | Boehringer Ingelheim International Gmbh | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
| US7776869B2 (en) | 2004-10-18 | 2010-08-17 | Amgen Inc. | Heteroaryl-substituted alkyne compounds and method of use |
| EP2120964A2 (en) | 2006-12-15 | 2009-11-25 | Abraxis BioScience, Inc. | Triazine derivatives and their therapeutical applications |
| JP2012529517A (ja) | 2009-06-09 | 2012-11-22 | アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー | ベンジル置換トリアジン誘導体類及びそれらの治療応用 |
| KR101457027B1 (ko) | 2009-06-09 | 2014-10-31 | 캘리포니아 캐피탈 에쿼티, 엘엘씨 | 트리아진 유도체와 이들의 치료적 용도 |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH27291A (en) | 1989-01-31 | 1993-05-04 | Takeda Chemical Industries Ltd | Imidazolpyrimidazines their production and use |
| US5506242A (en) | 1993-01-06 | 1996-04-09 | Ciba-Geigy Corporation | Arylsufonamido-substituted hydroxamic acids |
| US5646167A (en) | 1993-01-06 | 1997-07-08 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamix acids |
| US5552419A (en) | 1993-01-06 | 1996-09-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| US5817822A (en) | 1994-06-24 | 1998-10-06 | Novartis Corporation | Certain alpha-azacycloalkyl substituted arylsulfonamido acetohydroxamic acids |
| CA2263154A1 (en) | 1996-08-07 | 1998-02-12 | Darwin Discovery Limited | Hydroxamic and carboxylic acid derivatives having mmp and tnf inhibitory activity |
| AU743901B2 (en) | 1996-10-16 | 2002-02-07 | Wyeth Holdings Corporation | Ortho-sulfonamido bicyclic heteroaryl hydroxamic acids as matrix metalloprote inase and tace inhibitors |
| WO1998032748A1 (en) | 1997-01-23 | 1998-07-30 | F. Hoffmann-La Roche Ag | Sulfamide-metalloprotease inhibitors |
| US6376506B1 (en) | 1997-01-23 | 2002-04-23 | Syntex (U.S.A.) Llc | Sulfamide-metalloprotease inhibitors |
| ZA98376B (en) | 1997-01-23 | 1998-07-23 | Hoffmann La Roche | Sulfamide-metalloprotease inhibitors |
| US6482827B1 (en) | 1997-07-10 | 2002-11-19 | Pharmacia & Upjohn S.P.A. | Matrix metalloproteinase inhibitors |
| JP2001500533A (ja) | 1997-07-10 | 2001-01-16 | フアルマシア・エ・アツプジヨン・エツセ・ピー・アー | マトリックスメタロプロテイナーゼ・インヒビター |
| US6235786B1 (en) | 1997-08-06 | 2001-05-22 | Abbott Laboratories | Reverse hydroxamate inhibitors of matrix metalloproteinases |
| US6294573B1 (en) | 1997-08-06 | 2001-09-25 | Abbott Laboratories | Reverse hydroxamate inhibitors of matrix metalloproteinases |
| US6403632B1 (en) | 2000-03-01 | 2002-06-11 | Bristol Myers Squibb Pharma Co | Lactam metalloprotease inhibitors |
| ZA988967B (en) | 1997-10-03 | 2000-04-03 | Du Pont Pharm Co | Lactam metalloprotease inhibitors. |
| US6130220A (en) | 1997-10-16 | 2000-10-10 | Syntex (Usa) Inc. | Sulfamide-metalloprotease inhibitors |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| US6100266A (en) | 1998-01-30 | 2000-08-08 | Darwin Discovery Limited | Hydroxamic and carboxylic acid derivatives |
| JP2002523492A (ja) | 1998-08-29 | 2002-07-30 | ブリティッシュ バイオテック ファーマシューティカルズ リミテッド | タンパク質分解酵素阻害剤としてのヒドロキサム酸誘導体 |
| GB9919776D0 (en) * | 1998-08-31 | 1999-10-27 | Zeneca Ltd | Compoujnds |
| JP2002536373A (ja) * | 1999-02-08 | 2002-10-29 | ジー・ディー・サール・アンド・カンパニー | スルファメトヒドロキサム酸メタロプロテアーゼ阻害剤 |
| US6511993B1 (en) * | 1999-06-03 | 2003-01-28 | Kevin Neil Dack | Metalloprotease inhibitors |
| CN1159295C (zh) | 1999-06-04 | 2004-07-28 | 阿斯特拉曾尼卡有限公司 | 金属蛋白酶抑制剂 |
| AU2001232113A1 (en) | 2000-02-21 | 2001-09-03 | Astrazeneca Ab | Arylpiperazines and their use as metalloproteinase inhibiting agents (mmp) |
| CA2396965C (en) | 2000-02-21 | 2010-03-16 | Astrazeneca Ab | Piperidine- and piperazine substituted n-hydroxyformamides as inhibitors of metalloproteinases |
| US20030139419A1 (en) | 2000-02-21 | 2003-07-24 | Bernard Barlaam | Arylpiperazines and arylpiperidines and their use as metalloproteinase inhibiting agents |
| JP2003533521A (ja) | 2000-05-15 | 2003-11-11 | ダーウィン・ディスカバリー・リミテッド | ヒドロキサム酸誘導体 |
| GB0119473D0 (en) | 2001-08-09 | 2001-10-03 | Astrazeneca | Compounds |
| GB0119472D0 (en) | 2001-08-09 | 2001-10-03 | Astrazeneca Ab | Compounds |
-
2001
- 2001-08-09 GB GBGB0119474.5A patent/GB0119474D0/en not_active Ceased
-
2002
- 2002-08-08 JP JP2003519060A patent/JP2005501091A/ja active Pending
- 2002-08-08 EP EP02759021A patent/EP1417201A1/en not_active Withdrawn
- 2002-08-08 US US10/485,409 patent/US7153857B2/en not_active Expired - Fee Related
- 2002-08-08 WO PCT/SE2002/001436 patent/WO2003014111A1/en not_active Ceased
-
2006
- 2006-06-12 US US11/451,683 patent/US20060229313A1/en not_active Abandoned
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006511492A (ja) * | 2002-10-31 | 2006-04-06 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Mch拮抗活性を有する新規アルキン化合物及びこれらの化合物を含む薬物 |
| JP4883909B2 (ja) * | 2002-10-31 | 2012-02-22 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Mch拮抗活性を有する新規アルキン化合物及びこれらの化合物を含む薬物 |
Also Published As
| Publication number | Publication date |
|---|---|
| US7153857B2 (en) | 2006-12-26 |
| GB0119474D0 (en) | 2001-10-03 |
| WO2003014111A1 (en) | 2003-02-20 |
| EP1417201A1 (en) | 2004-05-12 |
| US20040220185A1 (en) | 2004-11-04 |
| US20060229313A1 (en) | 2006-10-12 |
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