AR043838A1 - Pirazoles sustituidos - Google Patents

Pirazoles sustituidos

Info

Publication number
AR043838A1
AR043838A1 ARP040101120A ARP040101120A AR043838A1 AR 043838 A1 AR043838 A1 AR 043838A1 AR P040101120 A ARP040101120 A AR P040101120A AR P040101120 A ARP040101120 A AR P040101120A AR 043838 A1 AR043838 A1 AR 043838A1
Authority
AR
Argentina
Prior art keywords
het
hal
cycloalkyl
mono
organic radical
Prior art date
Application number
ARP040101120A
Other languages
English (en)
Inventor
Schiemann Kai Dr
Schadt Oliver Dr
Van Amsterdam Cristoph Dr
Seyfried Christoph 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 AR043838A1 publication Critical patent/AR043838A1/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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/22—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
    • A61P25/34—Tobacco-abuse
    • 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
    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • 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
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/14—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
    • C07D409/14—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Rheumatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Toxicology (AREA)
  • Pulmonology (AREA)
  • Nutrition Science (AREA)
  • Urology & Nephrology (AREA)

Abstract

Los compuestos de la fórmula (1) donde R1, R2 son, de forma independiente entre sí, H, A, Hal, (CH2)nHet, (CH2)nAr, cicloalquilo C3-7, CF3, NO2, CN, C(NH)NOH u OCF3, OH, OA, NH2, NHA, NA2; Q es NR3R4 o Het; R3, R4 son H, (CH2)nHet, (CH2)nAr, cicloalquilo C3-7 o CF3; R5 es A, Ar o Het; A es alquilo o alcoxi lineal o ramificado con 1 a 10 átomos de C, alquenilo o alcoxialquilo C2-10; Het es un radical orgánico que contiene heteroátomos, en especial un radical heterocíclico mono- o bicíclico insustituido o mono o polisustituido con A, cicloalquilo C3-7, OH, OA, NH2, NAH, NA2, NO2, CN y/o Hal, saturado, insaturado o aromático o un radical orgánico lineal o ramificado que contiene uno o varios heteroátomos; Ar es un radical orgánico aromático, en especial un radical fenilo insustituido o mono o polisustituido con A y/o al, OR5, OOCR5, COOR5, CON(R5)2, CN, NO2, NH2, NHCOR5, CF3, SO2CH3 o un grupo que lleva un anillo -OCH2O-, -OC(CH3)2O, -OCH2CH2O; n es 0, 1, 2, 3, 4 o 5; m es 1, 2 o 3; Hal es F, Cl, Br o I y es N o CH, así como sus sales y solvatos, enantiómeros, racematos y otras mezclas enantioméricas, en especial sus sales y solvatos de tolerancia fisiológica. Son apropiados como ligandos de receptores 5 HT.
ARP040101120A 2003-04-05 2004-04-02 Pirazoles sustituidos AR043838A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE2003115573 DE10315573A1 (de) 2003-04-05 2003-04-05 Substituierte Pyrazole

Publications (1)

Publication Number Publication Date
AR043838A1 true AR043838A1 (es) 2005-08-17

Family

ID=32981074

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040101120A AR043838A1 (es) 2003-04-05 2004-04-02 Pirazoles sustituidos

Country Status (16)

Country Link
US (1) US7566709B2 (es)
EP (1) EP1611107B1 (es)
JP (1) JP4740116B2 (es)
KR (1) KR20050119194A (es)
CN (1) CN1768043A (es)
AR (1) AR043838A1 (es)
AT (1) ATE478052T1 (es)
AU (1) AU2004228121B2 (es)
BR (1) BRPI0409002A (es)
CA (1) CA2521202A1 (es)
DE (2) DE10315573A1 (es)
ES (1) ES2349922T3 (es)
MX (1) MXPA05010646A (es)
RU (1) RU2005133990A (es)
WO (1) WO2004089910A1 (es)
ZA (1) ZA200508951B (es)

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DE10315569A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazolverbindungen
DE10315571A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Pyrazolverbindungen
DE10315572A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
WO2006089076A2 (en) * 2005-02-18 2006-08-24 Neurogen Corporation Thiazole amides, imidazole amides and related analogues
KR20080028964A (ko) 2005-06-27 2008-04-02 엑셀리시스, 인코포레이티드 피라졸계 ｌｘｒ 변조제
SG162803A1 (en) * 2005-06-27 2010-07-29 Exelixis Inc Imidazole based lxr modulators
EP1919895A2 (en) 2005-08-02 2008-05-14 Lexicon Pharmaceuticals, Inc. 2-aminoaryl pyridines as protein kinases inhibitors
JP2008169191A (ja) * 2006-02-20 2008-07-24 Eisai R & D Management Co Ltd 運動ニューロン疾患治療剤
JP5399262B2 (ja) 2006-12-08 2014-01-29 エグゼリクシス パテント カンパニー エルエルシー Ｌｘｒおよびｆｘｒのモジュレーター
US8524909B2 (en) * 2010-02-02 2013-09-03 Hoffmann-La Roche Inc. Tetrahydro-pyran derivatives
TW201321367A (zh) * 2011-10-25 2013-06-01 Du Pont 經１，３－二芳基取代之雜環殺蟲劑
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GB201312800D0 (en) 2013-07-17 2013-08-28 Heptares Therapeutics Ltd mGlu5 modulators
WO2015022293A2 (en) * 2013-08-12 2015-02-19 Basf Se 1,3-(het)aryl-substituted pyrazole compounds
TW201601632A (zh) 2013-11-20 2016-01-16 杜邦股份有限公司 １－芳基－３－烷基吡唑殺蟲劑
LT3762368T (lt) 2018-03-08 2022-06-10 Incyte Corporation Aminopirazindiolio junginiai, kaip pi3k-γ inhibitoriai
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof

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Also Published As

Publication number Publication date
JP2006522036A (ja) 2006-09-28
RU2005133990A (ru) 2006-03-20
DE10315573A1 (de) 2004-10-14
US7566709B2 (en) 2009-07-28
AU2004228121A1 (en) 2004-10-21
DE502004011551D1 (de) 2010-09-30
ZA200508951B (en) 2007-03-28
EP1611107B1 (de) 2010-08-18
WO2004089910A1 (de) 2004-10-21
CA2521202A1 (en) 2004-10-21
JP4740116B2 (ja) 2011-08-03
CN1768043A (zh) 2006-05-03
AU2004228121B2 (en) 2010-11-04
KR20050119194A (ko) 2005-12-20
ES2349922T3 (es) 2011-01-13
BRPI0409002A (pt) 2006-03-28
MXPA05010646A (es) 2005-12-12
ATE478052T1 (de) 2010-09-15
EP1611107A1 (de) 2006-01-04
US20070105871A1 (en) 2007-05-10

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