AR017019A1 - COMPOUNDS DERIVED FROM 2- (4-ARIL OR HETEROARILPIPERAZIN-1-ILMETIL) -1H-INDOL, COMPOSITIONS AND ITS USE IN THE MANUFACTURE OF MEDICINES - Google Patents
COMPOUNDS DERIVED FROM 2- (4-ARIL OR HETEROARILPIPERAZIN-1-ILMETIL) -1H-INDOL, COMPOSITIONS AND ITS USE IN THE MANUFACTURE OF MEDICINESInfo
- Publication number
- AR017019A1 AR017019A1 ARP980104021A ARP980104021A AR017019A1 AR 017019 A1 AR017019 A1 AR 017019A1 AR P980104021 A ARP980104021 A AR P980104021A AR P980104021 A ARP980104021 A AR P980104021A AR 017019 A1 AR017019 A1 AR 017019A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- cyano
- nitrogen
- trifluoromethyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
- A61K31/495—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
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
Un compuesto derivado de 2-(4-aril o heteroarilpiperazin-1-ilmetil)-1H-indol de formula (I) o sal farmacéuticamente aceptable del mismo, donde lalínea discontinua representa un doble enlace opcional; a es 0 o 1, en el que cuando a es 0, X puedeforma r un doble enlace opcional con el carbono adyacente aV; V es CHR10, en el que R10 es hidrogeno o alquilo C1-6; T es nitrogeno o CH; X es nitrogeno o CR11, en el que R11 es hidrogeno, alquilo C1-6, alcoxi C1-6,hidroxi o ciano; Y y Z son cadauno de el los independientemente nitrogeno o CR12, en el que R12 es hidrogeno, cloro, bromo, trifluorometilo, trifluorometoxi,ciano, alcoxi C1-6 o alquilo C1-6; R1 es hidrogeno, fluoro, cloro, bromo, trifluorometilo, trifluorometoxi, ciano o alquiloC1-6; R2, R6, R7, R8 y R9 estáncada uno de ellos independientemente seleccionados entre hidrogeno, fluoro, cloro, bromo, trifluorometilo, trifluorometoxi, ciano, alcoxi C1-6 y alquiloC1-6; R3 y R4 son cada uno de ellos independientemente hidrogeno oalquilo C1 -6; y R5 es hidrogeno, alcoxi C1-6, trifluorometilo, ciano, alquilo C1-6 oR13CO, en el que R13 es amino, alquil C1-6-amino, (alquilo C1-6)2 amino, alquilo C1-6, arilo C6-10; o cuando a es 1, R1 y R10 se pueden unir con loscarbonos a losque están uni dos para formar un compuesto de formula (II) en la que las líneas discontinuas representan enlaces opcionales; T, X, Y, Z, R2, R3,R4, R5, R6, R7, R8 y R9 son lo definido anteriormente; b es 0 o 1; y A y B son cada uno de ellosindependientemente CH, CH2,oxígeno, azufre, NH o nitrogeno;con la condicion de que cuando X es nitrogeno, el doble enlace opcional entre X y V no existe; con la condicion de que cuando b es 0, el doble enlaceopcional entre A y B no existe; y con lacondicion de que cuando b es 1, A y B no pueden ser ninguno de ellos oxígeno o azufre. Los compuestos antesmencionados son utiles para el tratamiento de trastornos del sistema de la dopamina. Se describen también composiciones y el uso de loscompuestos enla manufactura de medicamentos.A compound derived from 2- (4-aryl or heteroarylpiperazin-1-ylmethyl) -1H-indole of formula (I) or pharmaceutically acceptable salt thereof, where the broken line represents an optional double bond; a is 0 or 1, where when a is 0, X can form an optional double bond with the carbon adjacent to V; V is CHR10, wherein R10 is hydrogen or C1-6 alkyl; T is nitrogen or CH; X is nitrogen or CR11, wherein R11 is hydrogen, C1-6 alkyl, C1-6 alkoxy, hydroxy or cyano; Y and Z are each independently of the nitrogen or CR12, wherein R12 is hydrogen, chlorine, bromine, trifluoromethyl, trifluoromethoxy, cyano, C1-6 alkoxy or C1-6 alkyl; R1 is hydrogen, fluoro, chloro, bromo, trifluoromethyl, trifluoromethoxy, cyano or C1-6 alkyl; R2, R6, R7, R8 and R9 are one of them independently selected from hydrogen, fluoro, chloro, bromo, trifluoromethyl, trifluoromethoxy, cyano, C1-6 alkoxy and C1-6 alkyl; R3 and R4 are each independently hydrogen or C1-6alkyl; and R5 is hydrogen, C1-6 alkoxy, trifluoromethyl, cyano, C1-6 alkyl or R13CO, wherein R13 is amino, C1-6 alkyl, (C1-6 alkyl) 2 amino, C1-6 alkyl, C6 aryl -10; or when a is 1, R1 and R10 can be joined with the carbons to which they are joined to form a compound of formula (II) in which the dashed lines represent optional bonds; T, X, Y, Z, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined above; b is 0 or 1; and A and B are each independently CH, CH2, oxygen, sulfur, NH or nitrogen, with the proviso that when X is nitrogen, the optional double bond between X and V does not exist; with the proviso that when b is 0, the optional double bond between A and B does not exist; and with the proviso that when b is 1, A and B cannot be any of them oxygen or sulfur. The aforementioned compounds are useful for the treatment of disorders of the dopamine system. Compositions and the use of the compounds in the manufacture of medicaments are also described.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5576497P | 1997-08-15 | 1997-08-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR017019A1 true AR017019A1 (en) | 2001-08-22 |
Family
ID=22000003
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP980104021A AR017019A1 (en) | 1997-08-15 | 1998-08-13 | COMPOUNDS DERIVED FROM 2- (4-ARIL OR HETEROARILPIPERAZIN-1-ILMETIL) -1H-INDOL, COMPOSITIONS AND ITS USE IN THE MANUFACTURE OF MEDICINES |
Country Status (30)
| Country | Link |
|---|---|
| EP (1) | EP1003739A2 (en) |
| JP (1) | JP2002536291A (en) |
| KR (1) | KR20010022507A (en) |
| CN (1) | CN1265660A (en) |
| AP (1) | AP9801321A0 (en) |
| AR (1) | AR017019A1 (en) |
| AU (1) | AU8457298A (en) |
| BG (1) | BG104069A (en) |
| BR (1) | BR9811557A (en) |
| CA (1) | CA2297486C (en) |
| CO (1) | CO4960656A1 (en) |
| DZ (1) | DZ2583A1 (en) |
| EA (1) | EA200000023A1 (en) |
| HR (1) | HRP980441A2 (en) |
| HU (1) | HUP0003425A3 (en) |
| ID (1) | ID23803A (en) |
| IL (1) | IL133960A0 (en) |
| IS (1) | IS5336A (en) |
| MA (1) | MA24632A1 (en) |
| NO (1) | NO20000722L (en) |
| OA (1) | OA11286A (en) |
| PA (1) | PA8457001A1 (en) |
| PE (1) | PE106299A1 (en) |
| PL (1) | PL338947A1 (en) |
| SK (1) | SK1352000A3 (en) |
| TN (1) | TNSN98151A1 (en) |
| TR (1) | TR200000414T2 (en) |
| UY (1) | UY25144A1 (en) |
| WO (1) | WO1999009025A2 (en) |
| ZA (1) | ZA987304B (en) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU226859B1 (en) * | 1997-10-27 | 2009-12-28 | Neurosearch As | Phenyl- or heteroaryl-homopiperazines, their use and medicaments containing them |
| EP0953567A3 (en) | 1998-04-29 | 2003-04-02 | Pfizer Products Inc. | Bicyclic substituted piperazine-, piperidine- and tetrahydropyridine derivatives, their preparation and their use as agents with central dopaminergic (dopamine D4 receptor) activity |
| CN1244577C (en) * | 1999-12-30 | 2006-03-08 | H.隆德贝克有限公司 | 4-phenyl-peiperazinyl,-piperidinyl and -tetrahydropyridyl derivatives |
| GB0017952D0 (en) * | 2000-07-22 | 2000-09-13 | Univ Manchester | Treatment of dyskinesia |
| EP1177792A3 (en) | 2000-07-27 | 2002-10-23 | Pfizer Products Inc. | Dopamine D4 Ligands for the treatment of novelty-seeking disorders |
| EP1373204B1 (en) | 2001-03-09 | 2016-10-26 | Janssen Pharmaceuticals, Inc. | Heterocyclic compounds |
| CA2497827A1 (en) | 2002-09-06 | 2004-03-18 | Janssen Pharmaceutica, N.V. | (1h-benzoimidazol-2-yl)-(piperazinyl)-methanone derivatives and related compounds as histamine h4-receptor antagonists for the treatment of inflammatory and allergic disorders |
| WO2004108671A1 (en) * | 2003-06-06 | 2004-12-16 | Suven Life Sciences Limited | Substituted indoles with serotonin receptor affinity, process for their preparation and pharmaceutical compositions containing them |
| JP4859665B2 (en) | 2004-03-30 | 2012-01-25 | 武田薬品工業株式会社 | Alkoxyphenylpropanoic acid derivatives |
| US7572805B2 (en) | 2004-07-14 | 2009-08-11 | Bristol-Myers Squibb Company | Pyrrolo(oxo)isoquinolines as 5HT ligands |
| US7618980B2 (en) | 2004-07-14 | 2009-11-17 | Bristol-Myers Squibb Company | Pyrrolo(oxo)quinolines as 5HT ligands |
| JO2769B1 (en) | 2005-10-26 | 2014-03-15 | جانسين فارماسوتيكا ان. في | Fast Dissociting Dopamine 2 Receptor Antagonists |
| JO2642B1 (en) | 2006-12-08 | 2012-06-17 | جانسين فارماسوتيكا ان. في | Fast Dissociating Dopamine 2 Receptor Antagonists |
| JO2849B1 (en) * | 2007-02-13 | 2015-03-15 | جانسين فارماسوتيكا ان. في | Fast -Dissociating Dopamine 2 Receptor Antagonists |
| JP5431305B2 (en) | 2007-04-23 | 2014-03-05 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 4-Alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists |
| AU2008240729B2 (en) | 2007-04-23 | 2012-08-23 | Janssen Pharmaceutica N.V. | Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists |
| CA2729313C (en) | 2008-07-03 | 2016-08-30 | Janssen Pharmaceutica Nv | Substituted 6-(1-piperazinyl)-pyridazines as 5-ht6 receptor antagonists |
| DK2307374T3 (en) | 2008-07-31 | 2017-05-01 | Janssen Pharmaceutica Nv | PIPERAZIN-1-YLTRIFLUORMETHYL-SUBSTITUTED PYRIDINES AS QUICK DISSOCATING DOPAMIN-2 RECEPTOR ANTAGONISTS |
| WO2019057123A1 (en) * | 2017-09-20 | 2019-03-28 | 杭州英创医药科技有限公司 | Polycyclic compound acting as ido inhibitor and/or ido-hdac dual inhibitor |
| JP2023523176A (en) * | 2020-04-22 | 2023-06-02 | アニマ バイオテック インコーポレイテッド | COLLAGEN 1 TRANSLATION INHIBITOR AND METHOD OF USE THEREOF |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB944443A (en) * | 1959-09-25 | 1900-01-01 | ||
| KR100236808B1 (en) * | 1991-07-03 | 2000-02-01 | 로렌스 티. 마이젠헬더 | Substituted indoles as anti-aids pharmaceuticals |
| JPH05255089A (en) * | 1991-12-18 | 1993-10-05 | Sanwa Kagaku Kenkyusho Co Ltd | Antiviral agent |
| US5670522A (en) * | 1992-10-23 | 1997-09-23 | Merck Sharp & Dohme Limited | Dopamine receptor subtype ligands |
| GB9305644D0 (en) * | 1993-03-18 | 1993-05-05 | Merck Sharp & Dohme | Therapeutic agents |
| AU6215594A (en) * | 1993-03-18 | 1994-10-11 | Merck Sharp & Dohme Limited | Indole derivatives as dopamine d4 antagonists |
| WO1994024105A1 (en) * | 1993-04-15 | 1994-10-27 | Merck Sharp & Dohme Limited | Indole derivatives as dopamine d4 antagonists |
| DE4414113A1 (en) * | 1994-04-22 | 1995-10-26 | Merck Patent Gmbh | 3-indolylpiperidines |
| TW406075B (en) * | 1994-12-13 | 2000-09-21 | Upjohn Co | Alkyl substituted piperidinyl and piperazinyl anti-AIDS compounds |
| ZA968661B (en) * | 1995-11-17 | 1998-04-14 | Upjohn Co | Oxazolidinone antibacterial agent with tricyclic substituents. |
| TW504510B (en) * | 1996-05-10 | 2002-10-01 | Janssen Pharmaceutica Nv | 2,4-diaminopyrimidine derivatives |
-
1998
- 1998-08-05 WO PCT/IB1998/001198 patent/WO1999009025A2/en not_active Application Discontinuation
- 1998-08-05 AU AU84572/98A patent/AU8457298A/en not_active Abandoned
- 1998-08-05 TR TR2000/00414T patent/TR200000414T2/en unknown
- 1998-08-05 BR BR9811557-0A patent/BR9811557A/en not_active IP Right Cessation
- 1998-08-05 HU HU0003425A patent/HUP0003425A3/en unknown
- 1998-08-05 IL IL13396098A patent/IL133960A0/en unknown
- 1998-08-05 PL PL98338947A patent/PL338947A1/en unknown
- 1998-08-05 CN CN98807831A patent/CN1265660A/en active Pending
- 1998-08-05 EA EA200000023A patent/EA200000023A1/en unknown
- 1998-08-05 KR KR1020007001093A patent/KR20010022507A/en not_active Application Discontinuation
- 1998-08-05 CA CA002297486A patent/CA2297486C/en not_active Expired - Fee Related
- 1998-08-05 SK SK135-2000A patent/SK1352000A3/en unknown
- 1998-08-05 JP JP2000509706A patent/JP2002536291A/en active Pending
- 1998-08-05 EP EP98935229A patent/EP1003739A2/en not_active Withdrawn
- 1998-08-05 AP APAP/P/1998/001321A patent/AP9801321A0/en unknown
- 1998-08-05 ID IDW20000197A patent/ID23803A/en unknown
- 1998-08-10 PE PE1998000717A patent/PE106299A1/en not_active Application Discontinuation
- 1998-08-10 PA PA19988457001A patent/PA8457001A1/en unknown
- 1998-08-12 DZ DZ980193A patent/DZ2583A1/en active
- 1998-08-12 TN TNTNSN98151A patent/TNSN98151A1/en unknown
- 1998-08-12 MA MA25210A patent/MA24632A1/en unknown
- 1998-08-13 AR ARP980104021A patent/AR017019A1/en unknown
- 1998-08-14 ZA ZA9807304A patent/ZA987304B/en unknown
- 1998-08-14 CO CO98046788A patent/CO4960656A1/en unknown
- 1998-08-14 HR HR60/055,764A patent/HRP980441A2/en not_active Application Discontinuation
- 1998-08-17 UY UY25144A patent/UY25144A1/en not_active Application Discontinuation
-
2000
- 2000-01-10 BG BG104069A patent/BG104069A/en unknown
- 2000-01-11 IS IS5336A patent/IS5336A/en unknown
- 2000-02-08 OA OA1200000030A patent/OA11286A/en unknown
- 2000-02-14 NO NO20000722A patent/NO20000722L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP1003739A2 (en) | 2000-05-31 |
| AU8457298A (en) | 1999-03-08 |
| BG104069A (en) | 2001-05-31 |
| CA2297486C (en) | 2005-05-03 |
| PE106299A1 (en) | 1999-11-02 |
| PL338947A1 (en) | 2000-12-04 |
| SK1352000A3 (en) | 2000-08-14 |
| HRP980441A2 (en) | 1999-04-30 |
| CN1265660A (en) | 2000-09-06 |
| WO1999009025A2 (en) | 1999-02-25 |
| IL133960A0 (en) | 2001-04-30 |
| TNSN98151A1 (en) | 2005-03-15 |
| CA2297486A1 (en) | 1999-02-25 |
| NO20000722D0 (en) | 2000-02-14 |
| BR9811557A (en) | 2000-08-22 |
| WO1999009025A3 (en) | 1999-04-15 |
| MA24632A1 (en) | 1999-04-01 |
| IS5336A (en) | 2000-01-11 |
| HUP0003425A2 (en) | 2001-10-28 |
| NO20000722L (en) | 2000-02-14 |
| UY25144A1 (en) | 2000-12-29 |
| ID23803A (en) | 2000-05-11 |
| TR200000414T2 (en) | 2000-08-21 |
| OA11286A (en) | 2003-10-22 |
| JP2002536291A (en) | 2002-10-29 |
| EA200000023A1 (en) | 2000-08-28 |
| DZ2583A1 (en) | 2003-02-22 |
| CO4960656A1 (en) | 2000-09-25 |
| HUP0003425A3 (en) | 2002-02-28 |
| AP9801321A0 (en) | 2000-02-14 |
| PA8457001A1 (en) | 2000-09-29 |
| KR20010022507A (en) | 2001-03-15 |
| ZA987304B (en) | 2000-02-14 |
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