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AR035682A1 - Piperazinilcarbonilquinolinas e -isoquinolinas, un proceso para su preparacion, las preparaciones farmaceuticas que las contienen, el uso de las mismas para preparar un medicamento, los antagonistas selectivos del receptor de 5-ht2a que conforman estos compuestos y el uso de estos antagonistas en la - Google Patents

Piperazinilcarbonilquinolinas e -isoquinolinas, un proceso para su preparacion, las preparaciones farmaceuticas que las contienen, el uso de las mismas para preparar un medicamento, los antagonistas selectivos del receptor de 5-ht2a que conforman estos compuestos y el uso de estos antagonistas en la

Info

Publication number
AR035682A1
AR035682A1 ARP020100135A ARP020100135A AR035682A1 AR 035682 A1 AR035682 A1 AR 035682A1 AR P020100135 A ARP020100135 A AR P020100135A AR P020100135 A ARP020100135 A AR P020100135A AR 035682 A1 AR035682 A1 AR 035682A1
Authority
AR
Argentina
Prior art keywords
hal
compounds
ht2a
unsubstituted
disease
Prior art date
Application number
ARP020100135A
Other languages
English (en)
Inventor
Boettcher Henning Dr
Bartoszyk Gerd Dr
Harting Juergen Dr
Van Amsterdam Christoph Dr
Seyfried Christoph Dr
Original Assignee
Merck Patent Gmbh
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR035682A1 publication Critical patent/AR035682A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Addiction (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se describen piperazinilcarbonilquinolinas e -isoquinolinas de fórmula (1), donde: R1 es un radical fenilo o naftilo, no sustituido o sustituido con R3 y/o R4, o es Het1; R2 es un radical quinolinilo o isoquinolinilo, no sustituido o sustituido con R5 y/o R6; R3 y R4 son cada uno, independientemente entre sí, H, Hal, A, OA, OH o CN; R5 y R6 son cada uno, independientemente entre sí, H, CN, acilo, Hal, A, OA, OH, CONH2, CONHA o CONA2; Het1 es un sistema de anillo heterocíclico insaturado, monocíclico o bicíclico, no sustituido o monosustituido o disustituido con Hal, A, OA u OH y que contiene 1, 2 o 3 heteroátomos idénticos o diferentes, tal como nitrógeno, oxígeno y azufre; A es alquilo C1-6; alq es alquileno C1-6; Hal es F, Cl, Br o I; y sus sales y solvatos aceptables para uso farmacéutico. Estos compuestos son antagonistas selectivos del receptor de 5-HT2A y presentan una actividad clínicamente antipsicótica con mínimos efectos secundarios o ausencia de los mismos. También se describen los procesos para preparar los compuestos de fórmula (1), las preparaciones farmacéuticas que los contienen, los antagonistas selectivos del receptor de 5-HT2A que conforman estos compuestos y el uso de estos compuestos como antagonistas 5-HT2A para preparar medicamentos destinados al tratamiento de psicosis, esquizofrenia, depresión, trastornos neurológicos, trastornos de la memoria, mal de Parkinson, esclerosis amiotrópica lateral, mal de Alzheimer, enfermedad de Huntington, trastornos de la alimentación tal como la bulimia, anorexia nerviosa, síndrome premestrual y/o a afectar positivamente el trastornos obsesivo-compulsivo (OCD):
ARP020100135A 2001-01-17 2002-01-16 Piperazinilcarbonilquinolinas e -isoquinolinas, un proceso para su preparacion, las preparaciones farmaceuticas que las contienen, el uso de las mismas para preparar un medicamento, los antagonistas selectivos del receptor de 5-ht2a que conforman estos compuestos y el uso de estos antagonistas en la AR035682A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10102053A DE10102053A1 (de) 2001-01-17 2001-01-17 Piperazinylcarbonylchinoline und -isochinoline

Publications (1)

Publication Number Publication Date
AR035682A1 true AR035682A1 (es) 2004-06-23

Family

ID=7670921

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020100135A AR035682A1 (es) 2001-01-17 2002-01-16 Piperazinilcarbonilquinolinas e -isoquinolinas, un proceso para su preparacion, las preparaciones farmaceuticas que las contienen, el uso de las mismas para preparar un medicamento, los antagonistas selectivos del receptor de 5-ht2a que conforman estos compuestos y el uso de estos antagonistas en la

Country Status (23)

Country Link
US (1) US7329749B2 (es)
EP (1) EP1366039B1 (es)
JP (1) JP4417624B2 (es)
KR (1) KR100854481B1 (es)
CN (1) CN1249055C (es)
AR (1) AR035682A1 (es)
AT (1) ATE304010T1 (es)
BR (1) BR0116774A (es)
CA (1) CA2434773C (es)
CZ (1) CZ304144B6 (es)
DE (2) DE10102053A1 (es)
DK (1) DK1366039T3 (es)
ES (1) ES2248230T3 (es)
HK (1) HK1061849A1 (es)
HU (1) HU230250B1 (es)
MX (1) MXPA03006360A (es)
MY (1) MY127293A (es)
PL (1) PL212087B1 (es)
RU (1) RU2280034C2 (es)
SI (1) SI1366039T1 (es)
SK (1) SK287333B6 (es)
WO (1) WO2002057256A1 (es)
ZA (1) ZA200306331B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002057435A2 (en) * 2001-01-18 2002-07-25 Merck Patent Gmbh Bifunctional fusion proteins with glucocerebrosidase activity
ATE404200T1 (de) * 2002-04-22 2008-08-15 Univ Johns Hopkins Med Modulatoren von hedgehog signalpfaden, zusammensetzungen und verwandte verwendungen
WO2004002965A1 (de) * 2002-06-29 2004-01-08 Zentaris Gmbh Aryl- und heteroarylcarbonylpiperazine und deren verwendung zur behandlung gutartiger und bösartiger tumorerkrankungen
US20090311242A1 (en) * 2004-07-29 2009-12-17 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with 5-hydroxytryptamine 2a receptor (5ht2a)
GB2497476B (en) 2010-09-06 2018-01-10 Guangzhou Inst Biomed & Health Amide Compounds

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4970714A (en) * 1989-01-05 1990-11-13 International Business Machines Corp. Adaptive data link protocol
EP0957100B1 (en) 1997-07-07 2004-10-27 Kowa Co., Ltd. Diamine derivatives and pharmaceutical containing the same
EP1107758A2 (en) * 1998-08-28 2001-06-20 Scios Inc. Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase
DE19934433A1 (de) * 1999-07-22 2001-01-25 Merck Patent Gmbh N-(Indolcarbonyl-)piperazinderivate

Also Published As

Publication number Publication date
DK1366039T3 (da) 2006-01-02
HUP0401038A2 (hu) 2004-08-30
JP2004517145A (ja) 2004-06-10
JP4417624B2 (ja) 2010-02-17
EP1366039B1 (en) 2005-09-07
SI1366039T1 (sl) 2006-02-28
BR0116774A (pt) 2004-01-06
MY127293A (en) 2006-11-30
CZ20031861A3 (cs) 2003-09-17
SK287333B6 (sk) 2010-07-07
MXPA03006360A (es) 2003-10-06
KR20030068579A (ko) 2003-08-21
DE60113300T2 (de) 2006-06-29
WO2002057256A9 (en) 2005-12-08
US20040077657A1 (en) 2004-04-22
SK8652003A3 (en) 2003-11-04
US7329749B2 (en) 2008-02-12
EP1366039A1 (en) 2003-12-03
CA2434773A1 (en) 2002-07-25
ATE304010T1 (de) 2005-09-15
HU230250B1 (hu) 2015-11-30
CN1249055C (zh) 2006-04-05
ZA200306331B (en) 2005-01-26
CZ304144B6 (cs) 2013-11-20
DE60113300D1 (de) 2005-10-13
HUP0401038A3 (en) 2011-08-29
PL212087B1 (pl) 2012-08-31
CA2434773C (en) 2011-10-04
ES2248230T3 (es) 2006-03-16
RU2280034C2 (ru) 2006-07-20
KR100854481B1 (ko) 2008-08-26
RU2003124077A (ru) 2005-01-10
CN1486308A (zh) 2004-03-31
WO2002057256A1 (en) 2002-07-25
PL361741A1 (en) 2004-10-04
DE10102053A1 (de) 2002-07-18
HK1061849A1 (en) 2004-10-08

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AR035682A1 (es) Piperazinilcarbonilquinolinas e -isoquinolinas, un proceso para su preparacion, las preparaciones farmaceuticas que las contienen, el uso de las mismas para preparar un medicamento, los antagonistas selectivos del receptor de 5-ht2a que conforman estos compuestos y el uso de estos antagonistas en la

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