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AR043835A1 - Pirazoles sustituidos, un procedimiento para su preparacion, el uso de los mismos para preparar un medicamento, las preparaciones farmaceuticas que los contienen y un procedimiento para obtener dichas preparaciones farmaceuticas - Google Patents

Pirazoles sustituidos, un procedimiento para su preparacion, el uso de los mismos para preparar un medicamento, las preparaciones farmaceuticas que los contienen y un procedimiento para obtener dichas preparaciones farmaceuticas

Info

Publication number
AR043835A1
AR043835A1 ARP040101117A ARP040101117A AR043835A1 AR 043835 A1 AR043835 A1 AR 043835A1 AR P040101117 A ARP040101117 A AR P040101117A AR P040101117 A ARP040101117 A AR P040101117A AR 043835 A1 AR043835 A1 AR 043835A1
Authority
AR
Argentina
Prior art keywords
hal
pharmaceutical preparations
procedure
nhet
mono
Prior art date
Application number
ARP040101117A
Other languages
English (en)
Inventor
Seyfried Christoph Dr
Schadt Oliver Dr
Arlt Michael Dr
Finsinger Dirk Dr
Schiemann Kai Dr
Van Amsterdam Cristoph Dr
Bartoszyk Gerd 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 AR043835A1 publication Critical patent/AR043835A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P25/14—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
    • A61P25/18—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
    • A61P25/22—Anxiolytics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/10—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 carbon chain containing aromatic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Nutrition Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Pirazoles sustituidos de fórmula (1) en la que: R1 representa H, A, Hal, (CH2)nHet, (CH2)nAr, cicloalquilo C3-7, CF3, NO2, CN, C(NH)NOH o OCF3; R2 representa (CH2)nHet, (CH2)nAr, cicloalquilo C3-7, CF3; R3, R4 representan H, (CH2)nCO2R5, (CH2)nCOHet, CHO, (CH2)nOR5, (CH2)nHet, (CH2)nN(R5)2, CH=N-OA, CH2CH=N-OA, (CH2)nNHOA, (CH2)N(R5)Het, (CH2)nCH=N-Het, (CH2)nOCOR5, (CH2)nN(R5)CH2CH2OR5, (CH2)nN(R5)CH2CH2OCF3, (CH2)nN(R5)C(R5)HCOOR5, (CH2)nN(R5)CH2COHet, (CH2)nN(R5)CH2Het, (CH2)nN(R5)CH2CH2Het, (CH2)nN(R5)CH2CH2N(R5)CH2COOR5, (CH2)nN(R5)CH2CH2N(R5)2, CH=CHCOOR5, CH=CHCH2NR5Het, CH=CHCH2N(R5)2, CH=CHCH2OR5 o (CH2)nN(R5)Ar, teniendo en cada caso uno de los restos R3 o R4 el significado de H; R5 representa H o A; A representa alquilo de cadena recta o ramificada o alcoxi C1-10, alquenilo o alcoxialquilo C2-10; Het representa un radical orgánico con uno o varios heteroátomos, de cadena recta o ramificada o heterocíclico, mono o bicíclico, saturado, insaturado o aromático, que no está sustituido o está mono o polisustituido con A y/o Hal; Ar representa un radical fenilo no sustituido o mono o polisustituido con A y/o Hal, OR5, OOCR5, COOR5, CON(R5)2, CN, NO2, NH2, NHCOR5, CF3 o SO2CH3, n es 0,1 , 2, 3, 4, o 5; Hal representa F, Cl, Br o I; y X representa N o cuando R1 significa cualquiera de los restos de fórmulas (2) en donde R es H o un grupo alquilo C1-6, y/o R2 presenta uno de los siguientes significados de restos de fórmulas (3), en donde R es H o un grupo alquilo C1-6, entonces también representa CH, y sus sales o solvatos, enantiómeros, racematos y otras mezclas de enantiómeros, en particular sus sales y solvatos aceptables desde el punto de vista fisiológico. Estos compuestos son adecuados como ligandos de receptores 5-HT, en particular de receptores 5-HT2A y/o receptores 5-HT2C. También se describe un procedimiento para preparar los compuestos de fórmula (1), las preparaciones farmacéuticas que los contienen y el uso de los mismos para la preparación de un medicamento destinado, en particular, a la profilaxis y/o el tratamiento de la psicosis, los trastornos neurológicos, la esclerosis lateral amiotrófica, los trastornos alimenticios tales como la bulimia, la anorexia nerviosa, el síndrome premenstrual y/o para ejercer una influencia positiva en los trastornos obsesivo-compulsivos (obsessive-compulsive disorder, OCD).
ARP040101117A 2003-04-05 2004-04-02 Pirazoles sustituidos, un procedimiento para su preparacion, el uso de los mismos para preparar un medicamento, las preparaciones farmaceuticas que los contienen y un procedimiento para obtener dichas preparaciones farmaceuticas AR043835A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE2003115569 DE10315569A1 (de) 2003-04-05 2003-04-05 Substituierte Pyrazolverbindungen

Publications (1)

Publication Number Publication Date
AR043835A1 true AR043835A1 (es) 2005-08-17

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ARP040101117A AR043835A1 (es) 2003-04-05 2004-04-02 Pirazoles sustituidos, un procedimiento para su preparacion, el uso de los mismos para preparar un medicamento, las preparaciones farmaceuticas que los contienen y un procedimiento para obtener dichas preparaciones farmaceuticas

Country Status (15)

Country Link
US (1) US7842695B2 (es)
EP (1) EP1611122B1 (es)
JP (2) JP4740117B2 (es)
KR (1) KR20050119192A (es)
CN (1) CN1768052A (es)
AR (1) AR043835A1 (es)
AT (1) ATE364601T1 (es)
BR (1) BRPI0408986A (es)
CA (1) CA2521227A1 (es)
DE (2) DE10315569A1 (es)
ES (1) ES2287710T3 (es)
MX (1) MXPA05010650A (es)
PL (1) PL377604A1 (es)
WO (1) WO2004089932A1 (es)
ZA (1) ZA200508923B (es)

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ATE364601T1 (de) 2007-07-15
JP2011153144A (ja) 2011-08-11
US7842695B2 (en) 2010-11-30
AU2004228124A1 (en) 2004-10-21
JP4740117B2 (ja) 2011-08-03
ZA200508923B (en) 2007-02-28
ES2287710T3 (es) 2007-12-16
EP1611122B1 (de) 2007-06-13
BRPI0408986A (pt) 2006-03-28
MXPA05010650A (es) 2005-12-12
CA2521227A1 (en) 2004-10-21
KR20050119192A (ko) 2005-12-20
JP2006522039A (ja) 2006-09-28
WO2004089932A1 (de) 2004-10-21
DE10315569A1 (de) 2004-10-14
US20070010531A1 (en) 2007-01-11
DE502004004089D1 (de) 2007-07-26
PL377604A1 (pl) 2006-02-06
CN1768052A (zh) 2006-05-03
EP1611122A1 (de) 2006-01-04

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