BR0115480A - Derivados de pirimidina - Google Patents

Derivados de pirimidina

Info

Publication number
BR0115480A
BR0115480A BR0115480-0A BR0115480A BR0115480A BR 0115480 A BR0115480 A BR 0115480A BR 0115480 A BR0115480 A BR 0115480A BR 0115480 A BR0115480 A BR 0115480A
Authority
BR
Brazil
Prior art keywords
lower alkyl
hydrogen
independently
trifluoromethyl
receptor
Prior art date
Application number
BR0115480-0A
Other languages
English (en)
Inventor
Heinz Stadler
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR0115480A publication Critical patent/BR0115480A/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/06—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
    • 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
    • A61P25/24—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
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56—One oxygen atom and one sulfur 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

"DERIVADOS DE PIRIMIDINA". A invenção refere-se a compostos da fórmula geral (I) em que R^ 1^ é alquila inferior, alcóxi inferior, piridinila, pirimidinila, fenila, -S-alquila inferior, -S(O)~ 2~-alquila inferior, -N(R)-(CH~ 2~)~ n~-N(R)~ 2~, -O-(CH~ 2~)~ n~-N(R)~ 2~, -N(R)~ 2~ ou uma amina terciária cíclica do grupo que pode conter um heteroátomo adicional, selecionado de N, O ou S e em que este grupo pode estar conectado com o anel de pirimidina através do ligante -O-(CH~ 2~)~ n~-; R^ 2^ é hidrogênio, alquila inferior, alcóxi inferior, halogênio ou trifluorometila; R^ 3^/R^ 3'^ é, independentemente um do outro, hidrogênio ou alquila inferior; R^ 4^ é, independentemente um do outro, halogênio, trifluorometila ou alcóxi inferior; R^ 5^ é hidrogênio ou alquila inferior; R é, independentemente um do outro, hidrogênio, ou alquila inferior; X é -C(O)N(R)- ou N(R)C(O)-; Y é -O-, -S-, -SO~ 2~-, ou -N(R)-; n é 1, 2, 3 ou 4; e m é 0, 1 ou 2; e a sais de adição ácidos farmaceuticamente aceitáveis dos mesmos. Eles possuem boa afinidade com o receptor de NK1 e são, portanto, adequados no tratamento de doenças relacionadas com este receptor.
BR0115480-0A 2000-11-22 2001-11-13 Derivados de pirimidina BR0115480A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP00125529 2000-11-22
PCT/EP2001/013084 WO2002042280A2 (en) 2000-11-22 2001-11-13 Pyrimidine derivatives

Publications (1)

Publication Number Publication Date
BR0115480A true BR0115480A (pt) 2003-10-21

Family

ID=8170446

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0115480-0A BR0115480A (pt) 2000-11-22 2001-11-13 Derivados de pirimidina

Country Status (31)

Country Link
US (1) US6787539B2 (pt)
EP (1) EP1339698A2 (pt)
JP (1) JP3993100B2 (pt)
KR (1) KR100571337B1 (pt)
CN (1) CN1309710C (pt)
AR (1) AR031486A1 (pt)
AU (2) AU2002227921B2 (pt)
BG (1) BG107840A (pt)
BR (1) BR0115480A (pt)
CA (1) CA2429570A1 (pt)
CZ (1) CZ20031666A3 (pt)
EC (1) ECSP034619A (pt)
GT (1) GT200100232A (pt)
HK (1) HK1078079A1 (pt)
HR (1) HRP20030362A2 (pt)
HU (1) HUP0303045A3 (pt)
IL (2) IL155705A0 (pt)
JO (1) JO2307B1 (pt)
MA (1) MA26967A1 (pt)
MX (1) MXPA03004453A (pt)
NO (1) NO324865B1 (pt)
NZ (1) NZ525555A (pt)
PA (1) PA8533501A1 (pt)
PE (1) PE20020760A1 (pt)
PL (1) PL366394A1 (pt)
RU (1) RU2284997C2 (pt)
SK (1) SK7612003A3 (pt)
UY (1) UY27034A1 (pt)
WO (1) WO2002042280A2 (pt)
YU (1) YU39503A (pt)
ZA (1) ZA200303517B (pt)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2223772T3 (es) * 2000-01-31 2005-03-01 Pfizer Products Inc. Pirimidincarboxamidas utiles como inhibidores de las isozimas pde4.
US8455489B2 (en) * 2003-11-10 2013-06-04 Exelixis, Inc. Substituted pyrimidine compositions and methods of use
JP4613501B2 (ja) 2004-03-17 2011-01-19 味の素株式会社 ５−保護アミノピリミジン化合物の製造方法
JP4501015B2 (ja) 2004-03-17 2010-07-14 味の素株式会社 アミノピリミジン化合物の製造方法
US7280223B2 (en) * 2004-04-22 2007-10-09 Zygo Corporation Interferometry systems and methods of using interferometry systems
JP4906715B2 (ja) * 2004-05-08 2012-03-28 ニューロジェン・コーポレーション ４，５−ジ置換−２−アリールピリミジン類
WO2006089674A2 (en) 2005-02-25 2006-08-31 F.Hoffmann-La Roche Ag Tablets with improved drug substance dispersibility
DE102005027150A1 (de) * 2005-03-12 2006-09-28 Bayer Healthcare Ag Pyrimidincarbonsäure-Derivate und ihre Verwendung
EA200970706A1 (ru) 2007-01-24 2010-02-26 Глэксо Груп Лимитед Новые фармацевтические композиции
KR101032186B1 (ko) * 2008-12-31 2011-05-02 엘에스산전 주식회사 정격 미세 조정이 가능한 과전류 계전기
BR112012010220A2 (pt) 2009-10-30 2021-02-23 Janssen Pharmaceutical N.V. piridinas fenóxi-substituídas como modulares do receptor opioide
CN102741240B (zh) * 2009-10-30 2015-05-06 詹森药业有限公司 用作δ阿片类受体调节剂的嘧啶化合物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS57131771A (en) * 1981-02-10 1982-08-14 Mitsubishi Yuka Yakuhin Kk Novel pyrimidine derivative
FR2536071B1 (fr) * 1982-11-12 1986-07-11 Sanofi Sa Sels acides de 2-piperazinopyrimidine, procede pour leur preparation et compositions pharmaceutiques en contenant
WO1987004928A1 (en) 1986-02-24 1987-08-27 Mitsui Petrochemical Industries, Ltd. Agents for treating neurophathy
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
NZ277839A (en) 1993-12-29 1998-01-26 Merck Sharp & Dohme Substituted morpholine derivatives, preparation and pharmaceutical compositions thereof
IL112778A0 (en) 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
US5972938A (en) 1997-12-01 1999-10-26 Merck & Co., Inc. Method for treating or preventing psychoimmunological disorders
ES2223772T3 (es) 2000-01-31 2005-03-01 Pfizer Products Inc. Pirimidincarboxamidas utiles como inhibidores de las isozimas pde4.

Also Published As

Publication number Publication date
NO324865B1 (no) 2007-12-17
RU2003117481A (ru) 2005-02-20
PA8533501A1 (es) 2002-10-31
WO2002042280A3 (en) 2002-08-22
WO2002042280A2 (en) 2002-05-30
EP1339698A2 (en) 2003-09-03
RU2284997C2 (ru) 2006-10-10
HRP20030362A2 (en) 2005-04-30
US20020099207A1 (en) 2002-07-25
JP3993100B2 (ja) 2007-10-17
JP2004514673A (ja) 2004-05-20
NO20032291D0 (no) 2003-05-21
CA2429570A1 (en) 2002-05-30
US6787539B2 (en) 2004-09-07
PE20020760A1 (es) 2002-08-21
PL366394A1 (en) 2005-01-24
BG107840A (bg) 2004-01-30
NO20032291L (no) 2003-05-21
CN1309710C (zh) 2007-04-11
ZA200303517B (en) 2004-08-10
AU2792102A (en) 2002-06-03
CN1628103A (zh) 2005-06-15
IL155705A (en) 2008-11-26
MA26967A1 (fr) 2004-12-20
SK7612003A3 (en) 2004-05-04
ECSP034619A (es) 2003-06-25
MXPA03004453A (es) 2003-08-19
JO2307B1 (en) 2005-09-12
UY27034A1 (es) 2002-06-20
AR031486A1 (es) 2003-09-24
YU39503A (sh) 2006-05-25
IL155705A0 (en) 2003-11-23
KR100571337B1 (ko) 2006-04-17
NZ525555A (en) 2004-10-29
KR20030060940A (ko) 2003-07-16
HUP0303045A3 (en) 2004-03-29
HK1078079A1 (en) 2006-03-03
HUP0303045A2 (hu) 2003-12-29
GT200100232A (es) 2002-07-04
CZ20031666A3 (cs) 2004-02-18
AU2002227921B2 (en) 2006-02-16

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Legal Events

Date Code Title Description
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

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