EA200100710A1 - 4-(аминометил)пиперидинбензамиды для лечения желудочно-кишечных расстройств - Google Patents
4-(аминометил)пиперидинбензамиды для лечения желудочно-кишечных расстройствInfo
- Publication number
- EA200100710A1 EA200100710A1 EA200100710A EA200100710A EA200100710A1 EA 200100710 A1 EA200100710 A1 EA 200100710A1 EA 200100710 A EA200100710 A EA 200100710A EA 200100710 A EA200100710 A EA 200100710A EA 200100710 A1 EA200100710 A1 EA 200100710A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- hydrogen
- alkyl
- cycloalkyl
- alk
- aryl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Настоящее изобретение относится к соединениям формулы (I), их стереохимически изомерным формам, их N-оксидам, их пролекарствам или их фармацевтически приемлемым аддитивным солям кислот, где в указанной формуле -R-R- представляет собой двухвалентный радикал, в котором один или два атома водорода могут быть замещены C-алкилом или гидрокси; Rпредставляет собой водород или галоген; Rпредставляет собой водород или C-алкил; Rпредставляет собой водород или C-алкил; L представляет собой C-циклоалкил, оксо-C-циклоалкил или C-алкенил или L представляет собой радикал формулы -Alk-R, -Alk-X-R, -Alk-Y-C(=O)-Rили -Alk-Y-C(=O)-NRR, где каждый Alk представляет собой C-алкандиил; и Rпредставляет собой водород, амино, циано, C-алкилсульфониламино, C-циклоалкил, оксо-C-циклоалкил, арил или гетероциклическую систему; Rпредставляет собой водород, C-алкил, гидрокси-C-алкил, C-циклоалкил, арил или гетероциклическую систему; X представляет собой O, S, SOили NR; причем указанный Rпредставляет собой водород или C-алкил; Rпредставляет собой водород, C-алкил, C-циклоалкил, C-алкилокси, гидрокси или арил; Y представляет собой прямую связь или NR; причем указанный Rпредставляет собой водород или C-алкил; Rи R, каждый независимо, представляют собой водород, C-алкил, C-циклоалкил или Rи R, соединенные с атомом азота, могут образовывать необязательно замещенное пирролидинильное, пиперидинильное, пиперазинильное или 4-морфолинильное кольцо. Описываются способы получения указанных соединений, композиции, содержащие указанные продукты, и их применение в качестве лечебных средств, в частности, для лечения или профилактики желудочно-кишечных расстройств.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP98204411 | 1998-12-22 | ||
| PCT/EP1999/010064 WO2000037461A1 (en) | 1998-12-22 | 1999-12-14 | 4-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200100710A1 true EA200100710A1 (ru) | 2001-12-24 |
| EA003608B1 EA003608B1 (ru) | 2003-06-26 |
Family
ID=8234539
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200100710A EA003608B1 (ru) | 1998-12-22 | 1999-12-14 | 4-(аминометил)пиперидинбензамиды для лечения желудочно-кишечных расстройств |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US6544997B1 (ru) |
| EP (1) | EP1140915B1 (ru) |
| JP (1) | JP4615725B2 (ru) |
| KR (1) | KR100633680B1 (ru) |
| CN (1) | CN1150190C (ru) |
| AR (1) | AR024240A1 (ru) |
| AT (1) | ATE297917T1 (ru) |
| AU (1) | AU770397B2 (ru) |
| BG (1) | BG64953B1 (ru) |
| BR (1) | BR9916491A (ru) |
| CA (1) | CA2355857C (ru) |
| CZ (1) | CZ300851B6 (ru) |
| DE (1) | DE69925865T2 (ru) |
| DK (1) | DK1140915T3 (ru) |
| EA (1) | EA003608B1 (ru) |
| EE (1) | EE200100335A (ru) |
| ES (1) | ES2245131T3 (ru) |
| HK (1) | HK1039114B (ru) |
| HR (1) | HRP20010445A2 (ru) |
| HU (1) | HUP0104838A3 (ru) |
| ID (1) | ID28953A (ru) |
| IL (1) | IL143858A (ru) |
| MY (1) | MY121852A (ru) |
| NO (1) | NO321324B1 (ru) |
| NZ (1) | NZ512871A (ru) |
| PL (1) | PL197409B1 (ru) |
| PT (1) | PT1140915E (ru) |
| SI (1) | SI1140915T1 (ru) |
| SK (1) | SK285829B6 (ru) |
| TR (1) | TR200101962T2 (ru) |
| TW (1) | TW570920B (ru) |
| UA (1) | UA71591C2 (ru) |
| WO (1) | WO2000037461A1 (ru) |
| ZA (1) | ZA200105135B (ru) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100370983C (zh) * | 2002-09-12 | 2008-02-27 | 长濑化成株式会社 | 药物组合物 |
| EP2305254A1 (en) | 2003-06-19 | 2011-04-06 | Janssen Pharmaceutica NV | Aminosulfonyl substituted 4-(aminomethyl)-piperidine benzamides as 5HT4-antagonists for the treatment of gatrointestinal conditions |
| CA2528656C (en) * | 2003-06-19 | 2012-01-03 | Janssen Pharmaceutica N.V. | 5ht4-antagonistic 4-(aminomethyl)-piperidine benzamides |
| WO2005003121A1 (en) * | 2003-06-19 | 2005-01-13 | Janssen Pharmaceutica N.V. | Hydroxycarbonylphenyl substituted 4-(aminomethyl)-piperidine benzamides as 5ht4-antagonists |
| AU2004254190B2 (en) | 2003-06-19 | 2010-04-22 | Janssen Pharmaceutica N.V. | Heterocyclic substituted 4-(aminomethyl)-piperidine benzamides as 5HT4-antagonists |
| JO2478B1 (en) | 2003-06-19 | 2009-01-20 | جانسين فارماسوتيكا ان. في. | (Aminomethyl) -biperidine benzamides as 5 HT4 antagonists |
| PL1664036T3 (pl) * | 2003-09-03 | 2012-04-30 | Pfizer | Związki benzimidazolonu wykazujące działanie agonistyczne względem receptora 5-ht4 |
| ATE461192T1 (de) * | 2003-11-24 | 2010-04-15 | Pfizer | Chinoloncarbonsäureverbindungen mit 5-ht4- rezeptoragonistischer wirkung |
| TW200533348A (en) * | 2004-02-18 | 2005-10-16 | Theravance Inc | Indazole-carboxamide compounds as 5-ht4 receptor agonists |
| US8309575B2 (en) | 2004-04-07 | 2012-11-13 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| TWI351282B (en) | 2004-04-07 | 2011-11-01 | Theravance Inc | Quinolinone-carboxamide compounds as 5-ht4 recepto |
| US7728006B2 (en) * | 2004-04-07 | 2010-06-01 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| KR100875558B1 (ko) | 2004-06-15 | 2008-12-23 | 화이자 인코포레이티드 | 벤즈이미다졸론 카복실산 유도체 |
| US20060035890A1 (en) * | 2004-08-10 | 2006-02-16 | Amit Banerjee | Compounds and methods for the treatment of ubiquitin conjugating disorders |
| EP1807423B1 (en) * | 2004-11-05 | 2009-05-20 | Theravance, Inc. | Quinolinone-carboxamide compounds |
| ES2332808T3 (es) * | 2004-11-05 | 2010-02-12 | Theravance, Inc. | Compuestos agonistas del receptor 5-ht4. |
| NZ555180A (en) * | 2004-12-22 | 2010-09-30 | Theravance Inc | Indazole-carboxamide compounds useful as 5-HT4 receptor agonists |
| EP1871772B1 (en) * | 2005-03-02 | 2014-09-10 | Theravance, Inc. | Quinolinone compounds as 5-ht4 receptor agonists |
| US9101160B2 (en) | 2005-11-23 | 2015-08-11 | The Coca-Cola Company | Condiments with high-potency sweetener |
| US8017168B2 (en) | 2006-11-02 | 2011-09-13 | The Coca-Cola Company | High-potency sweetener composition with rubisco protein, rubiscolin, rubiscolin derivatives, ace inhibitory peptides, and combinations thereof, and compositions sweetened therewith |
| US8377968B2 (en) | 2008-06-02 | 2013-02-19 | Zalicus Pharmaceuticals, Ltd. | N-piperidinyl acetamide derivatives as calcium channel blockers |
| WO2014134306A1 (en) | 2013-03-01 | 2014-09-04 | Zalicus Pharmaceuticals, Ltd. | Heterocyclic inhibitors of the sodium channel |
| CA3001857A1 (en) * | 2015-10-14 | 2017-04-20 | Aquinnah Pharmaceuticals, Inc. | Compounds, compositions and methods of use against stress granules |
| WO2021007487A1 (en) | 2019-07-11 | 2021-01-14 | Praxis Precision Medicines, Inc. | Formulations of t-type calcium channel modulators and methods of use thereof |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ225152A (en) * | 1987-07-17 | 1990-04-26 | Janssen Pharmaceutica Nv | Heterocyclically substituted piperidinyl benzamides as pharmaceuticals |
| CA1317940C (en) * | 1987-09-25 | 1993-05-18 | Georges H. P. Van Daele | Substituted n-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides |
| US5374637A (en) * | 1989-03-22 | 1994-12-20 | Janssen Pharmaceutica N.V. | N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives |
| JPH06510283A (ja) | 1991-08-20 | 1994-11-17 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | ５−ｈｔ４レセプター拮抗薬 |
| DE69229674T2 (de) * | 1991-09-12 | 2000-04-06 | Smithkline Beecham Plc | 5-ht4 rezeptor antagonisten |
| ATE172201T1 (de) * | 1992-01-23 | 1998-10-15 | Toray Industries | Morphinan-derivate und medizinische verwendung |
| CA2129112A1 (en) * | 1992-02-06 | 1993-08-19 | Francis David King | Benzopyran, benzothiopyran and benzofuran derivatives as 5-ht4 antagonists |
| WO1994008994A1 (en) | 1992-10-13 | 1994-04-28 | Smithkline Beecham Plc | Heterocyclic -esters or -amides used as 5-ht4 receptor antagonists |
| GB9219163D0 (en) | 1992-09-10 | 1992-10-28 | Smithkline Beecham Plc | Pharmaceuticals |
| MX9306311A (es) | 1992-10-13 | 1994-04-29 | Smithkline Beecham Plc | Compuestos antagonistas del receptor de 5-ht4, procedimiento para su preparacion y composiciones farmaceuticas que los contienen |
| US5705498A (en) | 1992-11-05 | 1998-01-06 | Smithkline Beecham Plc. | Piperidine derivatives as 5-HT4 receptor antagonists |
| GB9301660D0 (en) | 1993-01-28 | 1993-03-17 | Smithkline Beecham Plc | Pharmaceuticals |
| GB9312348D0 (en) | 1993-06-16 | 1993-07-28 | Smithkline Beecham Plc | Pharmaceuticals |
| ES2103675B1 (es) * | 1995-01-10 | 1998-07-01 | Almirall Lab | Nuevas piperidinas sustituidas. |
| IT1275903B1 (it) | 1995-03-14 | 1997-10-24 | Boehringer Ingelheim Italia | Esteri e ammidi della 1,4-piperidina disostituita |
| GB9507882D0 (en) * | 1995-04-18 | 1995-05-31 | Pharmacia Spa | Substituted dihydrobenzofuran derivatives as 5-ht4 agonists |
| WO1997029739A2 (en) * | 1996-02-15 | 1997-08-21 | Janssen Pharmaceutica N.V. | Use of 5ht4 receptor antagonists for overcoming gastrointestinal effects of serotonin reuptake inhibitors |
| TW445263B (en) | 1996-02-29 | 2001-07-11 | Janssen Pharmaceutica Nv | Novel esters of 1,4-disubstituted piperidine derivatives |
| TW548103B (en) * | 1997-07-11 | 2003-08-21 | Janssen Pharmaceutica Nv | Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives |
| JP3366323B2 (ja) * | 1998-09-10 | 2003-01-14 | エフ．ホフマン−ラ ロシュ アーゲー | ５−ｈｔ４受容体アンタゴニストとしてのジヒドロベンゾジオキシンカルボキサミド及びケトン誘導体 |
| DE10217868A1 (de) * | 2002-04-22 | 2003-10-30 | Jomed N V | Ballon-Katheter |
-
1999
- 1999-12-03 TW TW088121125A patent/TW570920B/zh not_active IP Right Cessation
- 1999-12-14 JP JP2000589532A patent/JP4615725B2/ja not_active Expired - Fee Related
- 1999-12-14 TR TR2001/01962T patent/TR200101962T2/xx unknown
- 1999-12-14 ES ES99967956T patent/ES2245131T3/es not_active Expired - Lifetime
- 1999-12-14 DE DE69925865T patent/DE69925865T2/de not_active Expired - Lifetime
- 1999-12-14 DK DK99967956T patent/DK1140915T3/da active
- 1999-12-14 ID IDW00200101336A patent/ID28953A/id unknown
- 1999-12-14 CA CA002355857A patent/CA2355857C/en not_active Expired - Fee Related
- 1999-12-14 PL PL348417A patent/PL197409B1/pl unknown
- 1999-12-14 US US09/857,905 patent/US6544997B1/en not_active Expired - Lifetime
- 1999-12-14 IL IL14385899A patent/IL143858A/xx not_active IP Right Cessation
- 1999-12-14 EP EP99967956A patent/EP1140915B1/en not_active Expired - Lifetime
- 1999-12-14 NZ NZ512871A patent/NZ512871A/xx unknown
- 1999-12-14 AU AU24328/00A patent/AU770397B2/en not_active Ceased
- 1999-12-14 EA EA200100710A patent/EA003608B1/ru not_active IP Right Cessation
- 1999-12-14 SI SI9930822T patent/SI1140915T1/sl unknown
- 1999-12-14 PT PT99967956T patent/PT1140915E/pt unknown
- 1999-12-14 CZ CZ20012117A patent/CZ300851B6/cs not_active IP Right Cessation
- 1999-12-14 WO PCT/EP1999/010064 patent/WO2000037461A1/en active IP Right Grant
- 1999-12-14 CN CNB998147699A patent/CN1150190C/zh not_active Expired - Fee Related
- 1999-12-14 BR BR9916491-4A patent/BR9916491A/pt not_active Application Discontinuation
- 1999-12-14 AT AT99967956T patent/ATE297917T1/de not_active IP Right Cessation
- 1999-12-14 SK SK859-2001A patent/SK285829B6/sk not_active IP Right Cessation
- 1999-12-14 KR KR1020017005055A patent/KR100633680B1/ko not_active IP Right Cessation
- 1999-12-14 EE EEP200100335A patent/EE200100335A/xx unknown
- 1999-12-14 HU HU0104838A patent/HUP0104838A3/hu unknown
- 1999-12-14 UA UA2001064399A patent/UA71591C2/uk unknown
- 1999-12-17 MY MYPI99005534A patent/MY121852A/en unknown
- 1999-12-21 AR ARP990106644A patent/AR024240A1/es active IP Right Grant
-
2001
- 2001-06-07 BG BG105571A patent/BG64953B1/bg unknown
- 2001-06-08 NO NO20012858A patent/NO321324B1/no not_active IP Right Cessation
- 2001-06-14 HR HR20010445A patent/HRP20010445A2/hr not_active Application Discontinuation
- 2001-06-21 ZA ZA200105135A patent/ZA200105135B/en unknown
-
2002
- 2002-01-29 HK HK02100161.1A patent/HK1039114B/zh not_active IP Right Cessation
-
2003
- 2003-01-29 US US10/353,307 patent/US7205410B2/en not_active Expired - Fee Related
Also Published As
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |