ECSP034619A - Derivados de pirimidina - Google Patents

Derivados de pirimidina

Info

Publication number
ECSP034619A
ECSP034619A EC2003004619A ECSP034619A ECSP034619A EC SP034619 A ECSP034619 A EC SP034619A EC 2003004619 A EC2003004619 A EC 2003004619A EC SP034619 A ECSP034619 A EC SP034619A EC SP034619 A ECSP034619 A EC SP034619A
Authority
EC
Ecuador
Prior art keywords
lower alkyl
hydrogen
independently
group
receptor
Prior art date
Application number
EC2003004619A
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 ECSP034619A publication Critical patent/ECSP034619A/es

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

Abstract

La invención se refiere a compuestos de formula general en donde R1 es alquilo inferior, alcoxilo inferior, piridinilo, pirimidinilo, fenilo, -S-alquilo inferior, S (0)2- alquilo inferior, -N(®-(CH2)n-N®2, -0-(CH2)n-- N®2, -0-(CH2)n-o una amina terciaria cíclica del grupo (gráfico) que puede contener un heteroátomo adicional, seleccionado de N, Oo S, y en donde este grupo debe estar conectado con el anillo pirimidina a través del conector-0(CH2)n-; R2 es hidrógeno, alquilo inferior, alcoxilo inferior, halógeno o trifluorometilo: R3/R3 es, independientemente uno del otro, hidrógeno o alquilo inferior; R4 es independientemente uno del otro, hidrógeno o alquilo inferior; R5 es hidrógeno o alquilo inferior; R es, independientemente uno del otro, hidrógeno o alquilo inferior; x es-C(O)N(R)-o-N(R)C(O)-; Y es-O-., -S-, SO2-, -o-N(R)-; n es 1, 2, 3 o 4; y m es 0, 1 o 2; y las sales de adición ácida farmacéutica mente aceptables de los mismos. Que tienen una gran afinidad para el receptor de NKI y sonpor lo tanto, adecuados en el tratamiento de enfermedades, relacionadas con este receptor.
EC2003004619A 2000-11-22 2003-05-21 Derivados de pirimidina ECSP034619A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00125529 2000-11-22

Publications (1)

Publication Number Publication Date
ECSP034619A true ECSP034619A (es) 2003-06-25

Family

ID=8170446

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2003004619A ECSP034619A (es) 2000-11-22 2003-05-21 Derivados de pirimidina

Country Status (31)

Country Link
US (1) US6787539B2 (es)
EP (1) EP1339698A2 (es)
JP (1) JP3993100B2 (es)
KR (1) KR100571337B1 (es)
CN (1) CN1309710C (es)
AR (1) AR031486A1 (es)
AU (2) AU2792102A (es)
BG (1) BG107840A (es)
BR (1) BR0115480A (es)
CA (1) CA2429570A1 (es)
CZ (1) CZ20031666A3 (es)
EC (1) ECSP034619A (es)
GT (1) GT200100232A (es)
HK (1) HK1078079A1 (es)
HR (1) HRP20030362A2 (es)
HU (1) HUP0303045A3 (es)
IL (2) IL155705A0 (es)
JO (1) JO2307B1 (es)
MA (1) MA26967A1 (es)
MX (1) MXPA03004453A (es)
NO (1) NO324865B1 (es)
NZ (1) NZ525555A (es)
PA (1) PA8533501A1 (es)
PE (1) PE20020760A1 (es)
PL (1) PL366394A1 (es)
RU (1) RU2284997C2 (es)
SK (1) SK7612003A3 (es)
UY (1) UY27034A1 (es)
WO (1) WO2002042280A2 (es)
YU (1) YU39503A (es)
ZA (1) ZA200303517B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ20022413A3 (cs) * 2000-01-31 2003-08-13 Pfizer Products Inc. Pyrimidinkarboxamidy užitečné jako inhibitory isozymů PDE4
WO2005047268A2 (en) * 2003-11-10 2005-05-26 X-Ceptor Therapeutics, 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
JP2007534941A (ja) * 2004-04-22 2007-11-29 ザイゴ　コーポレーション 光学干渉計システムおよび光学干渉計システムを用いる方法
WO2005110416A2 (en) * 2004-05-08 2005-11-24 Neurogen Corporation 4,5-disubstituted-2-aryl pyrimidines
CA2598762A1 (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
EP2129381A1 (en) 2007-01-24 2009-12-09 Glaxo Group Limited Pharmaceutical compositions comprising 3, 5-diamin0-6- (2, 3-dichl0phenyl) -l, 2, 4-triazine or r (-) -2, 4-diamino-5- (2, 3-dichlorophenyl) -6-fluoromethyl pyrimidine and an nk1
KR101032186B1 (ko) * 2008-12-31 2011-05-02 엘에스산전 주식회사 정격 미세 조정이 가능한 과전류 계전기
WO2011053705A1 (en) * 2009-10-30 2011-05-05 Janssen Pharmaceutica Nv Pyrimidine compounds as delta opioid receptor modulators
JP5770198B2 (ja) * 2009-10-30 2015-08-26 ヤンセン ファーマシューティカ エヌ．ベー． オピオイド受容体調節因子としてのフェノキシ置換ピリミジン

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
DE3752141T2 (de) 1986-02-24 1998-03-26 Mitsui Petrochemical Ind Mittel zur behandlung von neuropathie
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
SG52217A1 (en) 1993-12-29 1998-09-28 Merck Sharp & Dohme Substituted morpholine derivatives and their use as therapeutic agents
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
CZ20022413A3 (cs) * 2000-01-31 2003-08-13 Pfizer Products Inc. Pyrimidinkarboxamidy užitečné jako inhibitory isozymů PDE4

Also Published As

Publication number Publication date
MA26967A1 (fr) 2004-12-20
UY27034A1 (es) 2002-06-20
RU2003117481A (ru) 2005-02-20
AU2002227921B2 (en) 2006-02-16
YU39503A (sh) 2006-05-25
IL155705A (en) 2008-11-26
CN1309710C (zh) 2007-04-11
PE20020760A1 (es) 2002-08-21
RU2284997C2 (ru) 2006-10-10
WO2002042280A3 (en) 2002-08-22
CA2429570A1 (en) 2002-05-30
IL155705A0 (en) 2003-11-23
CZ20031666A3 (cs) 2004-02-18
JP3993100B2 (ja) 2007-10-17
KR20030060940A (ko) 2003-07-16
AR031486A1 (es) 2003-09-24
HUP0303045A3 (en) 2004-03-29
HK1078079A1 (en) 2006-03-03
PL366394A1 (en) 2005-01-24
WO2002042280A2 (en) 2002-05-30
AU2792102A (en) 2002-06-03
GT200100232A (es) 2002-07-04
HRP20030362A2 (en) 2005-04-30
KR100571337B1 (ko) 2006-04-17
US6787539B2 (en) 2004-09-07
NZ525555A (en) 2004-10-29
NO20032291L (no) 2003-05-21
NO324865B1 (no) 2007-12-17
NO20032291D0 (no) 2003-05-21
BR0115480A (pt) 2003-10-21
ZA200303517B (en) 2004-08-10
PA8533501A1 (es) 2002-10-31
MXPA03004453A (es) 2003-08-19
US20020099207A1 (en) 2002-07-25
JO2307B1 (en) 2005-09-12
HUP0303045A2 (hu) 2003-12-29
BG107840A (bg) 2004-01-30
SK7612003A3 (en) 2004-05-04
JP2004514673A (ja) 2004-05-20
CN1628103A (zh) 2005-06-15
EP1339698A2 (en) 2003-09-03

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