MX9306310A - ANTAGONIST COMPOUNDS OF THE 5-HT4 RECEPTOR, PROCEDURE FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM - Google Patents
ANTAGONIST COMPOUNDS OF THE 5-HT4 RECEPTOR, PROCEDURE FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEMInfo
- Publication number
- MX9306310A MX9306310A MX9306310A MX9306310A MX9306310A MX 9306310 A MX9306310 A MX 9306310A MX 9306310 A MX9306310 A MX 9306310A MX 9306310 A MX9306310 A MX 9306310A MX 9306310 A MX9306310 A MX 9306310A
- Authority
- MX
- Mexico
- Prior art keywords
- alkyl
- hydrogen
- formula
- receptor
- procedure
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 108091005482 5-HT4 receptors Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- -1 cyano, hydroxyl Chemical group 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 239000003523 serotonin 4 antagonist Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
La presente invención se relaciona con los compuestos de fórmula (I), y las sales farmacéuticamente aceptables de los mismos, y el uso de un compuesto de fórmula (I) o una sal farmacéuticamente aceptable del mismo: en donde R1 es hidrógeno o alquilo de C1-6; R2 es hidrógeno o halo; Y es 0 o NH; Z es subfórmula (i). (ii), (iii), (iv) o (v): o en donde el anillo de piperidina (i) o (ii) es reemplazado por pirrolidinilo y/o el N-sustituyente en (i) o (ii) es reemplazado por R3 en donde R3 es hidrógeno o alquilo C1-12, aralquilo o R3 es (CH2)r-R10 en donde r es 2 ó 3 y R10 es seleccionado de ciano, hidroxilo, alcoxi de C1-6, fenoxi, C(O)alquilo de C1-6, COC6H5,-CONR11R12, NR11COR12, SO2NR11R12 o NR11SO2R12 en donde R11 y R12 son hidrógeno o alquilo de C1-6; o un compuesto de fórmula (I) en donde el enlace CO-Y es reemplazado por un bioisóstero heterocíclico; que tiene actividad antagonista de receptor de 5-HT4.The present invention relates to the compounds of formula (I), and the pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is hydrogen or alkyl of C1-6; R2 is hydrogen or halo; Y is 0 or NH; Z is sub-formula (i). (ii), (iii), (iv) or (v): or wherein the piperidine ring (i) or (ii) is replaced by pyrrolidinyl and / or the N-substituent in (i) or (ii) is replaced by R3 where R3 is hydrogen or C1-12 alkyl, aralkyl or R3 is (CH2) r-R10 where r is 2 or 3 and R10 is selected from cyano, hydroxyl, C1-6 alkoxy, phenoxy, C ( O) C1-6 alkyl, COC6H5, -CONR11R12, NR11COR12, SO2NR11R12 or NR11SO2R12 where R11 and R12 are hydrogen or C1-6 alkyl; or a compound of formula (I) wherein the CO-Y bond is replaced by a heterocyclic bioisoster; having 5-HT4 receptor antagonist activity.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB929221468A GB9221468D0 (en) | 1992-10-13 | 1992-10-13 | Pharmaceuticals |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX9306310A true MX9306310A (en) | 1994-04-29 |
Family
ID=10723359
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX9306310A MX9306310A (en) | 1992-10-13 | 1993-10-11 | ANTAGONIST COMPOUNDS OF THE 5-HT4 RECEPTOR, PROCEDURE FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP0664808A1 (en) |
| JP (1) | JPH08502274A (en) |
| CN (1) | CN1092775A (en) |
| AU (1) | AU5177093A (en) |
| CA (1) | CA2146928A1 (en) |
| GB (1) | GB9221468D0 (en) |
| MX (1) | MX9306310A (en) |
| WO (1) | WO1994008998A1 (en) |
| ZA (1) | ZA937505B (en) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5998409A (en) * | 1992-03-12 | 1999-12-07 | Smithkline Beecham Plc | Condensed indole derivatives as 5HT4 -receptor antagonists |
| US5852014A (en) * | 1992-03-12 | 1998-12-22 | Smithkline Beecham P.L.C. | Condensed indole derivatives as 5HT4 -receptor antagonists |
| WO1994008965A1 (en) * | 1992-10-16 | 1994-04-28 | Smithkline Beecham Plc | N-alkylpiperidinyl-4-methyl carboxylic esters/amides of condensed ring systems as 5-ht4 receptor antagonists |
| EP0977558B1 (en) * | 1996-02-15 | 2003-10-01 | Janssen Pharmaceutica N.V. | Use of 5ht4 receptor antagonists for overcoming gastrointestinal effects of serotonin reuptake inhibitors |
| FR2797630B1 (en) * | 1999-08-20 | 2005-04-29 | Univ Caen Basse Normandie | PYRROLO [1,2-a] QUINOXALINE ETHER DERIVATIVES, PROCESS FOR PREPARING THEM AND THEIR THERAPEUTIC APPLICATION |
| JP2005526003A (en) * | 2001-10-22 | 2005-09-02 | ファイザー株式会社 | Imidazopyridine compounds as 5-HT4 receptor modulators |
| US6624162B2 (en) | 2001-10-22 | 2003-09-23 | Pfizer Inc. | Imidazopyridine compounds as 5-HT4 receptor modulators |
| MXPA03000145A (en) | 2002-01-07 | 2003-07-15 | Pfizer | Oxo or oxy-pyridine compounds as 5-ht4 receptor modulators. |
| GB0211230D0 (en) | 2002-05-16 | 2002-06-26 | Medinnova Sf | Treatment of heart failure |
| DOP2003000703A (en) | 2002-09-20 | 2004-03-31 | Pfizer | IMIDAZOPIRADINE COMPOUNDS AS 5-HT4 RECEIVER AGONISTS |
| WO2004026868A1 (en) | 2002-09-20 | 2004-04-01 | Pfizer Japan Inc. | N-substituted piperidinyl-imidazopyridine compounds as 5-ht4 receptor modulators |
| WO2004094418A1 (en) * | 2003-04-21 | 2004-11-04 | Pfizer Inc. | Imidazopyridine compounds having 5-ht4 receptor agonistic activity and 5-ht3 receptor antagonistic activity |
| EP1758891A2 (en) | 2004-06-15 | 2007-03-07 | Pfizer Japan Inc. | Benzimidazolone carboxylic acid derivatives |
| US7737163B2 (en) | 2004-06-15 | 2010-06-15 | Pfizer Inc. | Benzimidazolone carboxylic acid derivatives |
| CN104761551A (en) * | 2015-03-31 | 2015-07-08 | 山东友帮生化科技有限公司 | Method for synthesizing 6-iodo-8-carboxylimidazo(1,2-a)pyridine |
| CN104725376A (en) * | 2015-03-31 | 2015-06-24 | 山东友帮生化科技有限公司 | Synthetic method of 6-chlorine-8-carboxyl imidazo [1,2-a] pyridine |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9103862D0 (en) * | 1991-02-25 | 1991-04-10 | Glaxo Group Ltd | Chemical compounds |
| US5260303A (en) * | 1991-03-07 | 1993-11-09 | G. D. Searle & Co. | Imidazopyridines as serotonergic 5-HT3 antagonists |
-
1992
- 1992-10-13 GB GB929221468A patent/GB9221468D0/en active Pending
-
1993
- 1993-10-11 MX MX9306310A patent/MX9306310A/en unknown
- 1993-10-11 ZA ZA937505A patent/ZA937505B/en unknown
- 1993-10-12 WO PCT/EP1993/002808 patent/WO1994008998A1/en not_active Ceased
- 1993-10-12 CA CA002146928A patent/CA2146928A1/en not_active Abandoned
- 1993-10-12 JP JP6509615A patent/JPH08502274A/en active Pending
- 1993-10-12 AU AU51770/93A patent/AU5177093A/en not_active Abandoned
- 1993-10-12 EP EP93922942A patent/EP0664808A1/en not_active Withdrawn
- 1993-10-12 CN CN93114853A patent/CN1092775A/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| ZA937505B (en) | 1994-07-22 |
| GB9221468D0 (en) | 1992-11-25 |
| WO1994008998A1 (en) | 1994-04-28 |
| CA2146928A1 (en) | 1994-04-28 |
| CN1092775A (en) | 1994-09-28 |
| JPH08502274A (en) | 1996-03-12 |
| AU5177093A (en) | 1994-05-09 |
| EP0664808A1 (en) | 1995-08-02 |
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