AR005549A1 - DERIVATIVES OF 1-PIRAZOL-3-ILETIL-4-INDOL-3-ILPIPERIDINA, A PROCEDURE FOR PREPARING THEM, MEDICINES AND PHARMACEUTICAL PREPARATIONS THAT CONTAIN THEM, A PROCEDURE FOR PREPARING THE PHARMACEUTICAL PREPARATIONS AND USE OF THE SAME MEDICINAL PREPARATIONS FOR THE PREPARATIONS - Google Patents

DERIVATIVES OF 1-PIRAZOL-3-ILETIL-4-INDOL-3-ILPIPERIDINA, A PROCEDURE FOR PREPARING THEM, MEDICINES AND PHARMACEUTICAL PREPARATIONS THAT CONTAIN THEM, A PROCEDURE FOR PREPARING THE PHARMACEUTICAL PREPARATIONS AND USE OF THE SAME MEDICINAL PREPARATIONS FOR THE PREPARATIONS

Info

Publication number
AR005549A1
AR005549A1 ARP970100297A ARP970100297A AR005549A1 AR 005549 A1 AR005549 A1 AR 005549A1 AR P970100297 A ARP970100297 A AR P970100297A AR P970100297 A ARP970100297 A AR P970100297A AR 005549 A1 AR005549 A1 AR 005549A1
Authority
AR
Argentina
Prior art keywords
preparations
preparing
procedure
pharmaceutical preparations
indol
Prior art date
Application number
ARP970100297A
Other languages
Spanish (es)
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 AR005549A1 publication Critical patent/AR005549A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se refiere a derivados de la 1-pirazol-3-iletil-4-indol-3-ilpiperidina de fórmula (I), en donde, R1 es H o A; R2 es H, fenilo monosustituido atrisustituido con Hal, NO2, CON(R4)2, SO2N(R4)2, ciano, A o R4-O; R3 es H, Hal, A, A-O-, amino,ciano , carboxamida, NO2, SO2N(R4)2; R4 es H o A; R5 esH o A; A es alquilo de 1 a 6 átomos de C, o bien alquilo de 1 a 6 átomos de C mono a trisustituido con flúor; Hal es F, Cl, Br o I; y a sus sales.También se refiere a un procedimiento parapreparar estos compuestos y sus sales, a preparaciones farmacéuticas que los contienen y al empleo de losmismos para el tratamiento de enfermedades ocasionadas por un funcionamiento defectuoso y por alteraciones del sistema nervioso central.Estos co mpuestos ysus sales han demostrado poseer una actividad farmacéutica ventajosa, pues actúan selectivamente sobre el sistema nervioso central, pero al mismo tiempotienen pocos efectos colaterales y un potencial de dependencia nulo o muy baj o.Refers to 1-pyrazol-3-ylethyl-4-indol-3-ylpiperidine derivatives of formula (I), wherein, R1 is H or A; R2 is H, monosubstituted phenyl atrisubstituted with Hal, NO2, CON (R4) 2, SO2N (R4) 2, cyano, A or R4-O; R3 is H, Hal, A, A-O-, amino, cyano, carboxamide, NO2, SO2N (R4) 2; R4 is H or A; R5 is H or A; A is alkyl of 1 to 6 carbon atoms, or alkyl of 1 to 6 carbon atoms mono to tri-substituted with fluorine; Hal is F, Cl, Br, or I; and their salts. It also refers to a process to prepare these compounds and their salts, to pharmaceutical preparations that contain them and to the use of them for the treatment of diseases caused by a malfunction and by alterations of the central nervous system. These compounds and their Salts have been shown to have an advantageous pharmaceutical activity, since they act selectively on the central nervous system, but at the same time they have few side effects and a zero or very low dependence potential.

ARP970100297A 1996-01-25 1997-01-24 DERIVATIVES OF 1-PIRAZOL-3-ILETIL-4-INDOL-3-ILPIPERIDINA, A PROCEDURE FOR PREPARING THEM, MEDICINES AND PHARMACEUTICAL PREPARATIONS THAT CONTAIN THEM, A PROCEDURE FOR PREPARING THE PHARMACEUTICAL PREPARATIONS AND USE OF THE SAME MEDICINAL PREPARATIONS FOR THE PREPARATIONS AR005549A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19602505A DE19602505A1 (en) 1996-01-25 1996-01-25 1- (pyrazol-4-indol-3-yl) piperidines

Publications (1)

Publication Number Publication Date
AR005549A1 true AR005549A1 (en) 1999-06-23

Family

ID=7783568

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP970100297A AR005549A1 (en) 1996-01-25 1997-01-24 DERIVATIVES OF 1-PIRAZOL-3-ILETIL-4-INDOL-3-ILPIPERIDINA, A PROCEDURE FOR PREPARING THEM, MEDICINES AND PHARMACEUTICAL PREPARATIONS THAT CONTAIN THEM, A PROCEDURE FOR PREPARING THE PHARMACEUTICAL PREPARATIONS AND USE OF THE SAME MEDICINAL PREPARATIONS FOR THE PREPARATIONS

Country Status (16)

Country Link
EP (1) EP0879234A1 (en)
JP (1) JP2000503972A (en)
KR (1) KR19990081970A (en)
CN (1) CN1209807A (en)
AR (1) AR005549A1 (en)
AU (1) AU715785B2 (en)
BR (1) BR9707467A (en)
CA (1) CA2244136A1 (en)
CZ (1) CZ231898A3 (en)
DE (1) DE19602505A1 (en)
HU (1) HUP9900980A2 (en)
NO (1) NO983439L (en)
PL (1) PL328228A1 (en)
SK (1) SK99298A3 (en)
WO (1) WO1997027186A1 (en)
ZA (1) ZA97572B (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2219385T3 (en) * 1999-09-09 2004-12-01 H. Lundbeck A/S INDOLES REPLACED WITH 5-AMINOALQUILO AND 5-AMINOCARBONILO.
US7179823B1 (en) 1999-11-10 2007-02-20 Takeda Pharmaceutical Company Limited 5-membered n-heterocyclic compounds with hypoglycemic and hypolipidemic activity
US7332494B2 (en) 2000-08-14 2008-02-19 Janssen Pharmaceutica, N.V. Method for treating allergies using substituted pyrazoles
CN1329392C (en) 2000-08-14 2007-08-01 奥索-麦克尼尔药品公司 Substituted pyrazoles
BR0214046A (en) * 2001-11-14 2004-10-13 Merck Patent Gmbh Pyrazole derivatives as psychopharmaceuticals
AU2006301377B2 (en) 2005-10-11 2012-03-08 F. Hoffmann-La Roche Ag Imidazo benzodiazepine derivatives
CN101541765A (en) * 2005-10-24 2009-09-23 詹森药业有限公司 3-piperidin-4-yl-indole ORL-1 receptor modulators
TWI548630B (en) * 2011-04-06 2016-09-11 Lg生命科學有限公司 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid crystalline form and the producing method thereof
TW202336015A (en) * 2020-11-04 2023-09-16 南韓商Lg化學股份有限公司 Method for preparation of 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid crystalline and pharmaceutical composition comprising the same

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2060816C3 (en) * 1970-12-10 1980-09-04 Merck Patent Gmbh, 6100 Darmstadt 4-Phenylpiperidine derivatives Process for their production and pharmaceutical preparations containing these compounds
DE2258033A1 (en) * 1972-11-27 1974-05-30 Merck Patent Gmbh 3-Heterocyclylalkyl-pyrazoles prodn. - by dehydrogenation or acid elimination from pyrazol(id)ines, useful as CNS depressants
GB8719167D0 (en) * 1987-08-13 1987-09-23 Glaxo Group Ltd Chemical compounds
US5045550A (en) * 1990-09-20 1991-09-03 Warner-Lambert Co. Substituted tetrahydropyridines as central nervous system agents
US5521196A (en) * 1994-10-05 1996-05-28 Eli Lilly And Company 5-HT1F agonists for the treatment of migraine

Also Published As

Publication number Publication date
CZ231898A3 (en) 1998-10-14
JP2000503972A (en) 2000-04-04
EP0879234A1 (en) 1998-11-25
CN1209807A (en) 1999-03-03
BR9707467A (en) 1999-07-20
AU715785B2 (en) 2000-02-10
SK99298A3 (en) 1999-01-11
NO983439L (en) 1998-09-25
NO983439D0 (en) 1998-07-24
HUP9900980A2 (en) 1999-07-28
AU1443297A (en) 1997-08-20
ZA97572B (en) 1997-08-04
WO1997027186A1 (en) 1997-07-31
CA2244136A1 (en) 1997-07-31
DE19602505A1 (en) 1997-07-31
PL328228A1 (en) 1999-01-18
KR19990081970A (en) 1999-11-15

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