BR9802482A - Derivados de 5h-tiazolo[3,2-a]pirimidina. - Google Patents

Derivados de 5h-tiazolo[3,2-a]pirimidina.

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Publication number
BR9802482A
BR9802482A BR9802482-5A BR9802482A BR9802482A BR 9802482 A BR9802482 A BR 9802482A BR 9802482 A BR9802482 A BR 9802482A BR 9802482 A BR9802482 A BR 9802482A
Authority
BR
Brazil
Prior art keywords
disease
lower alkyl
injuries
caused
cycloalkyl
Prior art date
Application number
BR9802482-5A
Other languages
English (en)
Inventor
Geo Adam
Sabine Kolczewski
Vincent Mutel
Juergen Wichmann
Thomas Johannes Woltering
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 BR9802482A publication Critical patent/BR9802482A/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/38One sulfur atom
    • C07D239/40One sulfur atom as doubly bound sulfur atom or as unsubstituted mercapto radical

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Addiction (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Patente de Invenção: <B>"DERIVADOS DE 5H-TIAZOLO[3,2-a]PIRIMIDINA"<D>. A invenção refere-se a compostos de fórmula geral: na qual: R^ 1^ representa hidrogênio, alquila inferior, fenila ou benzila, R^ 2^ representa alquila inferior, alcóxi inferior, -O(CH~ 2~)~ n~N(R^ 13^)(R^ 14^), -(CH~ 2~)~ n~N(R^ 13^)(R^ 14^) ou -N(R^ 15^)(CH~ 2~)~ n~N(R^ 13^)(R^ 14^), R^ 3^-R^ 12^ representam hidrogênio, halogênio, trifluoro metila, alquila inferior, cicloalquila, alcóxi inferior, hidróxi, nitro, ciano, -N(R^ 13^)~ 2~, fenila, fenilóxi, benzila ou benzilóxi, ou R^ 6^ e R^ 7^ representam em conjunto um anel benzeno, R^ 13^-R^ 15^ representam hidrogênio, alquila inferior ou cicloalquila, e n representa 1-5, bem como os seus sais farmaceuticamente aceitáveis. Esses compostos são adequados para o controle ou a prevenção de afecções neurológicas agudas e/ou crónicas, tais como a função cerebral limitada causada por operações de desvio ou transplantes, um débil suprimento de sangue ao cérebro, ferimentos no cordão espinhal, ferimentos na cabeça, hipoxia causada por gravidez, parada cardíaca, hipoglicemia, doença de Alzheimer, coréia de Hintington, ELA (esclerose lateral amiotrópica), demência causada pela AIDS, ferimentos nos olhos, retinopatia, distúrbios de cognição, doença de Parkinson idiopática ou doença de Parkinson causada por medicamentos, bem como as condições que levam a funções de deficiência de glutamato tais como, por exemplo, espasmos nos músculos, convulsões, enxaqueca, incontinência urinária, dependência de nicotina, psicoses, dependências de narcóticos, ansiedade, vómitos, dor crónica, disquinésia e depressões.
BR9802482-5A 1997-07-18 1998-07-16 Derivados de 5h-tiazolo[3,2-a]pirimidina. BR9802482A (pt)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP97112324 1997-07-18

Publications (1)

Publication Number Publication Date
BR9802482A true BR9802482A (pt) 2000-03-14

Family

ID=8227080

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9802482-5A BR9802482A (pt) 1997-07-18 1998-07-16 Derivados de 5h-tiazolo[3,2-a]pirimidina.

Country Status (33)

Country Link
US (1) US5958931A (pt)
EP (1) EP0891978B1 (pt)
JP (1) JP3100573B2 (pt)
KR (1) KR100296837B1 (pt)
CN (1) CN1102596C (pt)
AR (1) AR016129A1 (pt)
AT (1) ATE214704T1 (pt)
AU (1) AU738207B2 (pt)
BR (1) BR9802482A (pt)
CA (1) CA2243234C (pt)
CO (1) CO5210884A1 (pt)
CZ (1) CZ288944B6 (pt)
DE (1) DE69804273T2 (pt)
DK (1) DK0891978T3 (pt)
ES (1) ES2172840T3 (pt)
HK (1) HK1018439A1 (pt)
HR (1) HRP980398B1 (pt)
HU (1) HUP9801587A3 (pt)
ID (1) ID21824A (pt)
IL (1) IL125358A (pt)
MA (1) MA26520A1 (pt)
NO (1) NO310512B1 (pt)
NZ (1) NZ330988A (pt)
PE (1) PE97499A1 (pt)
PL (1) PL190218B1 (pt)
PT (1) PT891978E (pt)
RU (1) RU2197493C2 (pt)
SI (1) SI0891978T1 (pt)
TR (1) TR199801367A2 (pt)
TW (1) TW523518B (pt)
UY (1) UY25095A1 (pt)
YU (1) YU29798A (pt)
ZA (1) ZA986250B (pt)

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CA2438582C (en) * 2001-01-31 2012-06-26 Synaptic Pharmaceutical Corporation Use of gal3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
WO2002102807A1 (fr) * 2001-06-14 2002-12-27 Banyu Pharmaceutical Co., Ltd. Nouveaux derives d'isoxazolopyridone et leur utilisation
US7329662B2 (en) * 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
RU2378277C2 (ru) * 2004-06-21 2010-01-10 Ф. Хоффманн-Ля Рош Аг Производные пиразолпиримидина
KR100847160B1 (ko) * 2004-06-21 2008-07-17 에프. 호프만-라 로슈 아게 피라졸로 피리미딘 유도체
ES2365406T3 (es) 2005-02-11 2011-10-04 F. Hoffmann-La Roche Ag Derivados de pirazolo-pirimidina como antagonistas de mglur2.
MX2007011483A (es) 2005-03-23 2007-10-12 Hoffmann La Roche Derivados de acetilenil-pirazolo-pirimidina como antagonistas de glutamato metabotropico 2.
CA2623721C (en) 2005-09-27 2014-05-13 F. Hoffmann-La Roche Ag Oxadiazolyl pyrazolo-pyrimidines as mglur2 antagonists
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EA019085B1 (ru) 2007-09-14 2014-01-30 Янссен Фармасьютикалз, Инк. 1',3-двузамещенные 4-(арил-х-фенил)-1н-пиридин-2-оны
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MY161325A (en) 2009-05-12 2017-04-14 Janssen Pharmaceuticals Inc 1, 2, 4-triazolo[4,3-a]pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
CA2760259C (en) 2009-05-12 2018-05-01 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
ES2536433T3 (es) 2010-11-08 2015-05-25 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
JP5852664B2 (ja) 2010-11-08 2016-02-03 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド 1,2,4−トリアゾロ[4,3−a]ピリジン誘導体およびmGluR2受容体のポジティブアロステリックモジュレーターとしてのそれらの使用
CN103298809B (zh) 2010-11-08 2016-08-31 杨森制药公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途
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JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
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Also Published As

Publication number Publication date
ATE214704T1 (de) 2002-04-15
HRP980398A2 (en) 1999-04-30
EP0891978A3 (en) 1999-02-03
CZ288944B6 (cs) 2001-10-17
HU9801587D0 (en) 1998-09-28
EP0891978A2 (en) 1999-01-20
DK0891978T3 (da) 2002-07-01
IL125358A0 (en) 1999-03-12
DE69804273T2 (de) 2002-10-31
CZ223998A3 (cs) 1999-02-17
CA2243234C (en) 2007-09-18
CN1206010A (zh) 1999-01-27
TR199801367A3 (tr) 1999-02-22
IL125358A (en) 2002-09-12
ZA986250B (en) 1999-01-22
NO983244D0 (no) 1998-07-14
PE97499A1 (es) 1999-10-12
HUP9801587A3 (en) 2001-09-28
KR19990013919A (ko) 1999-02-25
RU2197493C2 (ru) 2003-01-27
NO983244L (no) 1999-01-19
ID21824A (id) 1999-07-29
HUP9801587A2 (hu) 1999-11-29
JP3100573B2 (ja) 2000-10-16
PT891978E (pt) 2002-07-31
AR016129A1 (es) 2001-06-20
CA2243234A1 (en) 1999-01-18
PL190218B1 (pl) 2005-11-30
TW523518B (en) 2003-03-11
EP0891978B1 (en) 2002-03-20
NO310512B1 (no) 2001-07-16
CO5210884A1 (es) 2002-10-30
UY25095A1 (es) 2001-01-31
CN1102596C (zh) 2003-03-05
PL327532A1 (en) 1999-02-01
ES2172840T3 (es) 2002-10-01
HRP980398B1 (en) 2002-06-30
SI0891978T1 (en) 2002-06-30
HK1018439A1 (en) 1999-12-24
YU29798A (sh) 2001-12-26
JPH1171380A (ja) 1999-03-16
US5958931A (en) 1999-09-28
KR100296837B1 (ko) 2001-10-26
MA26520A1 (fr) 2004-12-20
NZ330988A (en) 1999-03-29
DE69804273D1 (de) 2002-04-25
AU7730298A (en) 1999-01-28
AU738207B2 (en) 2001-09-13
TR199801367A2 (xx) 1999-02-22

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