JP2005535731A5 - - Google Patents
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- Publication number
- JP2005535731A5 JP2005535731A5 JP2004549842A JP2004549842A JP2005535731A5 JP 2005535731 A5 JP2005535731 A5 JP 2005535731A5 JP 2004549842 A JP2004549842 A JP 2004549842A JP 2004549842 A JP2004549842 A JP 2004549842A JP 2005535731 A5 JP2005535731 A5 JP 2005535731A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- alkyl
- alkenyl
- phenyl
- substituted
- 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
- 125000005843 halogen group Chemical group 0.000 claims 113
- 150000001875 compounds Chemical class 0.000 claims 96
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 89
- 125000000623 heterocyclic group Chemical group 0.000 claims 86
- 125000001475 halogen functional group Chemical group 0.000 claims 78
- 125000006370 trihalo methyl group Chemical group 0.000 claims 47
- 125000003118 aryl group Chemical group 0.000 claims 40
- 125000000217 alkyl group Chemical group 0.000 claims 39
- 125000001072 heteroaryl group Chemical group 0.000 claims 38
- -1 -OH Chemical group 0.000 claims 34
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 33
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 29
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 29
- 125000006375 C2-C10 alkynyl group Chemical group 0.000 claims 29
- 125000003342 alkenyl group Chemical group 0.000 claims 29
- 150000001602 bicycloalkyls Chemical group 0.000 claims 29
- 150000003839 salts Chemical class 0.000 claims 21
- 125000001309 chloro group Chemical group Cl* 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 10
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 230000001668 ameliorated effect Effects 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 231100000397 ulcer Toxicity 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39196202P | 2002-06-28 | 2002-06-28 | |
| US41103002P | 2002-09-17 | 2002-09-17 | |
| US41314802P | 2002-09-25 | 2002-09-25 | |
| US41658202P | 2002-10-08 | 2002-10-08 | |
| PCT/US2003/020509 WO2004002983A2 (en) | 2002-06-28 | 2003-06-27 | Therapeutic piperazine derivatives useful for treating pain |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005535731A JP2005535731A (ja) | 2005-11-24 |
| JP2005535731A5 true JP2005535731A5 (enExample) | 2006-03-09 |
| JP4621502B2 JP4621502B2 (ja) | 2011-01-26 |
Family
ID=30003987
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004549842A Expired - Fee Related JP4621502B2 (ja) | 2002-06-28 | 2003-06-27 | 疼痛の治療に有用な治療剤 |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US7279493B2 (enExample) |
| EP (1) | EP1556354B1 (enExample) |
| JP (1) | JP4621502B2 (enExample) |
| CN (1) | CN100457735C (enExample) |
| AT (1) | ATE384698T1 (enExample) |
| AU (1) | AU2003247829A1 (enExample) |
| BR (1) | BR0312322A (enExample) |
| CA (1) | CA2491079C (enExample) |
| CY (1) | CY1107411T1 (enExample) |
| DE (1) | DE60318875T2 (enExample) |
| DK (1) | DK1556354T3 (enExample) |
| EA (1) | EA200500114A1 (enExample) |
| ES (1) | ES2300613T3 (enExample) |
| IL (1) | IL165862A0 (enExample) |
| MX (1) | MXPA04012748A (enExample) |
| NO (1) | NO20050371L (enExample) |
| NZ (1) | NZ537292A (enExample) |
| PT (1) | PT1556354E (enExample) |
| RS (1) | RS114804A (enExample) |
| WO (1) | WO2004002983A2 (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100777169B1 (ko) | 2001-01-29 | 2007-11-16 | 시오노기세이야쿠가부시키가이샤 | 5-메틸-1-페닐-2-(1ｈ)-피리돈을 활성 성분으로서함유하는 의약 제제 |
| BR0312322A (pt) * | 2002-06-28 | 2005-04-12 | Euro Celtique Sa | Compostos, composições, métodos para o tratamento da dor em um animal, da incontinência urinária em um animal, de uma úlcera em um animal, de sìndrome de intestino irritável em um animal, da doença inflamatória do intestino em um animal, métodos para a inibição da função de vr1 em uma célula, kits e métodos para a preparação de uma composição |
| US7262194B2 (en) * | 2002-07-26 | 2007-08-28 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
| US7157462B2 (en) * | 2002-09-24 | 2007-01-02 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
| US7582635B2 (en) | 2002-12-24 | 2009-09-01 | Purdue Pharma, L.P. | Therapeutic agents useful for treating pain |
| ITMI20030151A1 (it) * | 2003-01-30 | 2004-07-31 | Recordati Ind Chimica E Farma Ceutica S P A | Uso di antagonisti selettivi del recettore mglu5 per il trattamento di disfunzioni neuromuscolari del tratto urinario inferiore. |
| SI1641775T1 (sl) * | 2003-07-03 | 2009-08-31 | Euro Celtique Sa | 2-piridin alkinski derivati, uporabni za zdravljenje bolečine |
| DE602004021206D1 (de) * | 2003-07-24 | 2009-07-02 | Euro Celtique Sa | Zur Behandlung oder Vorbeugung von Schmerzen geeignete Heteroaryl-Tetrahydropiperidyl-Verbindungen |
| PL1867644T3 (pl) * | 2003-07-24 | 2009-10-30 | Euro Celtique Sa | Związki heteroarylo-tetrahydropiperydylowe przydatne w leczeniu lub zapobieganiu bólu |
| DE602004020994D1 (de) * | 2003-07-24 | 2009-06-18 | Euro Celtique Sa | Piperidinverbindungen und pharmazeutische zusammensetzungen, die diese enthalten |
| SI1648880T1 (sl) * | 2003-08-01 | 2010-05-31 | Euro Celtique Sa | Terapevtska sredstva uporabna za zdravljenje bolečine |
| DE602004019576D1 (de) * | 2003-12-30 | 2009-04-02 | Euro Celtique Sa | Zur behandlung von schmerzen geeignete piperazine |
| KR20060087386A (ko) | 2005-01-28 | 2006-08-02 | 주식회사 대웅제약 | 신규 벤조이미다졸 유도체 및 이를 함유하는 약제학적조성물 |
| US20080051380A1 (en) | 2006-08-25 | 2008-02-28 | Auerbach Alan H | Methods and compositions for treating cancer |
| AU2011226773C1 (en) * | 2007-04-27 | 2012-07-26 | Purdue Pharma L.P. | TRPV1 antagonists and uses thereof |
| CA2685266C (en) | 2007-04-27 | 2014-01-28 | Purdue Pharma L.P. | Trpv1 antagonists and uses thereof for the treatment of prevention of pain, ui and ulcer, ibd, or ibs in an animal |
| EP2264031B1 (en) | 2008-04-18 | 2015-04-15 | Daewoong Pharmaceutical Co., Ltd. | A novel benzoxazine benzimidazole derivative, a pharmaceutical composition comprising the same, and a use thereof |
| JP5894540B2 (ja) | 2010-02-18 | 2016-03-30 | ブイティーブイ・セラピューティクス・エルエルシー | フェニル−ヘテロアリール誘導体とその使用の方法 |
| WO2011162409A1 (en) | 2010-06-22 | 2011-12-29 | Shionogi & Co., Ltd. | Compounds having trpv1 antagonistic activity and uses thereof |
| KR101293384B1 (ko) | 2010-10-13 | 2013-08-05 | 주식회사 대웅제약 | 신규 피리딜 벤조옥사진 유도체, 이를 포함하는 약학 조성물 및 이의 용도 |
| US9156830B2 (en) | 2011-05-17 | 2015-10-13 | Shionogi & Co., Ltd. | Heterocyclic compounds |
| PE20141531A1 (es) | 2011-06-22 | 2014-10-23 | Purdue Pharma Lp | Antagonistas de trpv1 que incluyen sustituyentes dihidroxi y sus usos |
| CN104540814A (zh) * | 2012-06-28 | 2015-04-22 | 艾伯维公司 | 氰基胍及其作为抗病毒剂的用途 |
| CA2937365C (en) | 2016-03-29 | 2018-09-18 | F. Hoffmann-La Roche Ag | Granulate formulation of 5-methyl-1-phenyl-2-(1h)-pyridone and method of making the same |
| CN105944083A (zh) * | 2016-05-03 | 2016-09-21 | 董桂芬 | 一种用于治疗纤维肌痛综合症的复方护理剂及其制备方法 |
| IL322013A (en) | 2016-07-29 | 2025-09-01 | Janssen Pharmaceutica Nv | Niraparib or its salts for use in the treatment of prostate cancer |
| CN112716979B (zh) * | 2021-01-26 | 2022-11-04 | 上海优祺生物医药科技有限公司 | 羊膜上皮细胞条件培养基的制药用途 |
| DE102022104759A1 (de) | 2022-02-28 | 2023-08-31 | SCi Kontor GmbH | Co-Kristall-Screening Verfahren, insbesondere zur Herstellung von Co-Kristallen |
| WO2023239415A1 (en) * | 2022-06-08 | 2023-12-14 | Angrow Company Limited | Compositions including cannabinoid and use thereof in the manufacture of a medicament for the treatment of inflammation in a subject |
Family Cites Families (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI56836C (fi) * | 1977-10-25 | 1980-04-10 | Fermion Oy | 4-substituerade piperazin-1-(n-aryl-n'-cyano)-karboximidamider som aer mellanprodukter vid framstaellningen av farmakologiskt vaerdefulla 6,7-dimetoxi- eller 6,7,8-trimetoxi-4-amino-2-(4-substituerade-piperazin-1-yl)-kinazoliner |
| US4450272A (en) * | 1982-05-06 | 1984-05-22 | American Cyanamid Company | Antiatherosclerotic 1-piperazine-thicarboxamides |
| US4439606A (en) * | 1982-05-06 | 1984-03-27 | American Cyanamid Company | Antiatherosclerotic 1-piperazinecarbonyl compounds |
| US5316759A (en) * | 1986-03-17 | 1994-05-31 | Robert J. Schaap | Agonist-antagonist combination to reduce the use of nicotine and other drugs |
| US5198459A (en) * | 1987-07-11 | 1993-03-30 | Sandoz Ltd. | Use of 5HT-3 antagonists in preventing or reducing dependency on dependency-inducing agents |
| DE3822792C2 (de) * | 1987-07-11 | 1997-11-27 | Sandoz Ag | Neue Verwendung von 5HT¶3¶-Antagonisten |
| US5075341A (en) * | 1989-12-01 | 1991-12-24 | The Mclean Hospital Corporation | Treatment for cocaine abuse |
| US6204284B1 (en) * | 1991-12-20 | 2001-03-20 | American Cyanamid Company | Use of 1-(substitutedphenyl)-3-azabicyclo[3.1.0]hexanes for the treatment of chemical dependencies |
| US5232934A (en) * | 1992-07-17 | 1993-08-03 | Warner-Lambert Co. | Method for the treatment of psychomotor stimulant addiction |
| DE4234295A1 (de) * | 1992-10-12 | 1994-04-14 | Thomae Gmbh Dr K | Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| US5321012A (en) * | 1993-01-28 | 1994-06-14 | Virginia Commonwealth University Medical College | Inhibiting the development of tolerance to and/or dependence on a narcotic addictive substance |
| GB9306578D0 (en) * | 1993-03-30 | 1993-05-26 | Merck Sharp & Dohme | Therapeutic agents |
| GB9308725D0 (en) * | 1993-04-27 | 1993-06-09 | Wyeth John & Brother Ltd | Piperazine derivatives |
| US5461047A (en) * | 1993-06-16 | 1995-10-24 | G. D. Searle & Co. | 2-,3-,4-,5-,6-,7-,8-,9- and/or 10-substituted dibenzoxazepine and dibenzthiazepine compounds, pharmaceutical compositions and methods of use |
| US5464788A (en) * | 1994-03-24 | 1995-11-07 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| FR2722788B1 (fr) * | 1994-07-20 | 1996-10-04 | Pf Medicament | Nouvelles piperazides derivees d'aryl piperazine, leurs procedes de preparation, leur utilisation a titre de medicament et les compositions pharmaceutiques les comprenant |
| US5556837A (en) * | 1994-08-01 | 1996-09-17 | Regeneron Pharmaceuticals Inc. | Methods for treating addictive disorders |
| US5762925A (en) * | 1994-11-03 | 1998-06-09 | Sagen; Jacqueline | Preventing opiate tolerance by cellular implantation |
| US5780472A (en) | 1995-01-11 | 1998-07-14 | Samjin Pharmaceuticazl Co., Ltd. | Piperazine derivatives and methods for the preparation thereof and compositions containing the same |
| US5792769A (en) * | 1995-09-29 | 1998-08-11 | 3-Dimensional Pharmaceuticals, Inc. | Guanidino protease inhibitors |
| RU2146254C1 (ru) * | 1996-06-29 | 2000-03-10 | Самдзин Фармасьютикал Ко., Лтд. | Производные пиперазина и способ их получения |
| JP2001502712A (ja) * | 1996-10-31 | 2001-02-27 | ノボ ノルディスク アクティーゼルスカブ | 束縛されたソマトスタチン・アゴニスト及びアンタゴニスト |
| WO1999007672A1 (en) | 1997-08-05 | 1999-02-18 | Novo Nordisk A/S | Derivatives of 2,5- and 3,5-disubstituted anilines, their preparation and use |
| ATE496035T1 (de) * | 1998-03-31 | 2011-02-15 | Kyowa Hakko Kirin Co Ltd | Stickstoffenthaltende heterocyclische verbindungen |
| US6329395B1 (en) * | 1998-06-08 | 2001-12-11 | Schering Corporation | Neuropeptide Y5 receptor antagonists |
| BR9914018A (pt) | 1998-09-22 | 2001-07-03 | Yamanouchi Pharmaceuticals Co | Derivado de cianofenila |
| DE60010988T2 (de) | 1999-03-03 | 2005-06-09 | Samjin Pharmaceutical Co., Ltd. | Piperazinderivate und verfahren zu ihrer herstellung |
| US6109269A (en) * | 1999-04-30 | 2000-08-29 | Medtronic, Inc. | Method of treating addiction by brain infusion |
| AU2001264376A1 (en) * | 2000-06-15 | 2001-12-24 | Chaconne Nsi Co., Ltd. | Urea derivative useful as an anti-cancer agent and process for preparing same |
| WO2002005819A1 (en) | 2000-07-15 | 2002-01-24 | Smithkline Beecham Corporation | Compounds and methods |
| ES2266227T3 (es) * | 2000-08-21 | 2007-03-01 | Pacific Corporation | Nuevos compuestos de (tio)urea y composiciones farmaceuticas que los contienen. |
| EP1303483B1 (en) * | 2000-08-21 | 2008-04-23 | Pacific Corporation | Novel thiourea derivatives and the pharmaceutical compositions containing the same |
| AU2001280187A1 (en) | 2000-08-28 | 2002-03-13 | Toray Industries, Inc. | Cyclic amine derivatives |
| PE20030417A1 (es) | 2001-09-13 | 2003-08-06 | Smithkline Beecham Plc | Derivados de urea como antagonistas del receptor vainilloide |
| RS63204A (sr) | 2002-01-17 | 2006-10-27 | Neurogen Corporation | Supstituisani analozi hinazolin-4-ilamina kao modulatori kapsaicina |
| JP2005526723A (ja) | 2002-02-15 | 2005-09-08 | グラクソ グループ リミテッド | バニロイド受容体モジュレーター |
| US7074805B2 (en) * | 2002-02-20 | 2006-07-11 | Abbott Laboratories | Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor |
| US20030158188A1 (en) * | 2002-02-20 | 2003-08-21 | Chih-Hung Lee | Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor |
| US7105505B2 (en) * | 2002-04-18 | 2006-09-12 | Schering Corporation | Benzimidazole derivatives useful as histamine H3 antagonists |
| NZ535764A (en) * | 2002-04-18 | 2007-10-26 | Schering Corp | 1-(4-piperidinyl) benzimidazolones as histamine H3 antagonists |
| US7220862B2 (en) * | 2002-06-05 | 2007-05-22 | Bristol-Myers Squibb Company | Calcitonin gene related peptide receptor antagonists |
| EP1539742B1 (en) * | 2002-06-24 | 2006-11-08 | Schering Corporation | Indole derivatives useful as histamine h3 antagonists |
| BR0312322A (pt) | 2002-06-28 | 2005-04-12 | Euro Celtique Sa | Compostos, composições, métodos para o tratamento da dor em um animal, da incontinência urinária em um animal, de uma úlcera em um animal, de sìndrome de intestino irritável em um animal, da doença inflamatória do intestino em um animal, métodos para a inibição da função de vr1 em uma célula, kits e métodos para a preparação de uma composição |
| ES2298545T3 (es) * | 2002-08-21 | 2008-05-16 | Astrazeneca Ab | Compuestos de tieno-pirrol como antagonistas de la hormona liberadora de gonadotropina. |
| TW200418835A (en) | 2003-01-24 | 2004-10-01 | Tanabe Seiyaku Co | A pyrazolopyrimidine compound and a process for preparing the same |
-
2003
- 2003-06-27 BR BR0312322-7A patent/BR0312322A/pt not_active Application Discontinuation
- 2003-06-27 NZ NZ537292A patent/NZ537292A/en not_active IP Right Cessation
- 2003-06-27 DK DK03762220T patent/DK1556354T3/da active
- 2003-06-27 CA CA2491079A patent/CA2491079C/en not_active Expired - Fee Related
- 2003-06-27 DE DE60318875T patent/DE60318875T2/de not_active Expired - Lifetime
- 2003-06-27 JP JP2004549842A patent/JP4621502B2/ja not_active Expired - Fee Related
- 2003-06-27 AU AU2003247829A patent/AU2003247829A1/en not_active Abandoned
- 2003-06-27 ES ES03762220T patent/ES2300613T3/es not_active Expired - Lifetime
- 2003-06-27 RS YU114804A patent/RS114804A/sr unknown
- 2003-06-27 US US10/607,563 patent/US7279493B2/en not_active Expired - Lifetime
- 2003-06-27 IL IL16586203A patent/IL165862A0/xx unknown
- 2003-06-27 EA EA200500114A patent/EA200500114A1/ru unknown
- 2003-06-27 WO PCT/US2003/020509 patent/WO2004002983A2/en not_active Ceased
- 2003-06-27 CN CNB038201372A patent/CN100457735C/zh not_active Expired - Fee Related
- 2003-06-27 AT AT03762220T patent/ATE384698T1/de active
- 2003-06-27 PT PT03762220T patent/PT1556354E/pt unknown
- 2003-06-27 EP EP03762220A patent/EP1556354B1/en not_active Expired - Lifetime
- 2003-06-27 MX MXPA04012748A patent/MXPA04012748A/es active IP Right Grant
-
2005
- 2005-01-24 NO NO20050371A patent/NO20050371L/no unknown
-
2007
- 2007-09-04 US US11/899,379 patent/US7799786B2/en not_active Expired - Lifetime
-
2008
- 2008-04-15 CY CY20081100417T patent/CY1107411T1/el unknown
-
2010
- 2010-09-10 US US12/879,885 patent/US20110281885A1/en not_active Abandoned
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