BR0008862A - Derivados de bifenila como antagonistas do receptor neuroquinina-1 - Google Patents

Derivados de bifenila como antagonistas do receptor neuroquinina-1

Info

Publication number
BR0008862A
BR0008862A BR0008862-5A BR0008862A BR0008862A BR 0008862 A BR0008862 A BR 0008862A BR 0008862 A BR0008862 A BR 0008862A BR 0008862 A BR0008862 A BR 0008862A
Authority
BR
Brazil
Prior art keywords
hydrogen
lower alkyl
halogen
compounds
neurokinin
Prior art date
Application number
BR0008862-5A
Other languages
English (en)
Inventor
Michael Boes
Guido Galley
Thierry Godel
Torsten Hoffmann
Walter Hunkeler
Patrick Schnider
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 BR0008862A publication Critical patent/BR0008862A/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • A61P1/04Drugs 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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/06Antimigraine agents
    • 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
    • A61P25/28Drugs 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
    • A61P25/36Opioid-abuse
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/12Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • C07C233/15Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/42Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/44Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/66Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Patente de Invenção: "DERIVADOS DE BIFENILA COMO ANTAGONISTAS DO RECEPTOR NEUROQUININA-1". A invenção refere-se a compostos da fórmula geral (I) em que R é hidrogênio, alquila inferior, alcóxi inferior, halogênio, amino, -N(R^ 6^)~ 2~ ou trifluorometila; R^ 1^ é hidrogênio, alcóxi inferior ou halogênio; R e R^ 1^ podem ser, juntos, -CH=CH-CH=CH-; R^ 2^ é halogênio, alquila inferior ou tri-fluorometila; R^ 3^ é hidrogênio ou alquila inferior; R^ 4^ é hidrogênio ou uma amina cíclica terciária, opcionalmente substituída por alquila inferior; R^ 5^ é hidrogênio, nitro, amino ou -N(R^ 6^)~ 2~; R^ 6^ é hidrogênio ou alquila inferior; X é -C(O) N(R^ 6^)-, -(CH~ 2~)~ n~O-, -(CH~ 2~)~ n~N(R^ 6^)-, -N(R^ 6^)C(O)- ou -N(R^ 6^)(CH~ 2~)~ n~-; e n é 1 ou 2; e a sais ácidos de adição destes compostos, farmaceuticamente aceitáveis. Os compostos da fórmula 1 podem ser usados para o tratamento de doenças relacionadas ao receptor NK-1.
BR0008862-5A 1999-03-09 2000-02-28 Derivados de bifenila como antagonistas do receptor neuroquinina-1 BR0008862A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP99104626 1999-03-09
PCT/EP2000/001668 WO2000053572A1 (en) 1999-03-09 2000-02-28 Biphenyl derivatives as antagonists of the neurokinine-1 receptor

Publications (1)

Publication Number Publication Date
BR0008862A true BR0008862A (pt) 2002-01-02

Family

ID=8237723

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0008862-5A BR0008862A (pt) 1999-03-09 2000-02-28 Derivados de bifenila como antagonistas do receptor neuroquinina-1

Country Status (33)

Country Link
US (2) US6291465B1 (pt)
EP (1) EP1171419B1 (pt)
JP (1) JP3839668B2 (pt)
KR (1) KR100473247B1 (pt)
CN (1) CN1152006C (pt)
AR (1) AR043273A1 (pt)
AT (1) ATE286018T1 (pt)
AU (1) AU767449B2 (pt)
BR (1) BR0008862A (pt)
CA (1) CA2366205C (pt)
CO (1) CO5160261A1 (pt)
CZ (1) CZ20013190A3 (pt)
DE (1) DE60017110T2 (pt)
ES (1) ES2233338T3 (pt)
HK (1) HK1045684B (pt)
HR (1) HRP20010629A2 (pt)
HU (1) HUP0201710A3 (pt)
IL (2) IL145166A0 (pt)
JO (1) JO2235B1 (pt)
MA (1) MA26778A1 (pt)
MY (1) MY121145A (pt)
NO (1) NO20014356D0 (pt)
NZ (1) NZ513824A (pt)
PE (1) PE20001549A1 (pt)
PL (1) PL201681B1 (pt)
PT (1) PT1171419E (pt)
RU (1) RU2238266C2 (pt)
SI (1) SI1171419T1 (pt)
TR (1) TR200102585T2 (pt)
UY (1) UY26051A1 (pt)
WO (1) WO2000053572A1 (pt)
YU (1) YU64901A (pt)
ZA (1) ZA200107259B (pt)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0008489A (pt) 1999-02-24 2002-02-05 Hoffmann La Roche Derivados de fenil- e piridinila
AUPQ514600A0 (en) 2000-01-18 2000-02-10 James Cook University Brain injury treatment
TWI287003B (en) * 2000-07-24 2007-09-21 Hoffmann La Roche 4-phenyl-pyridine derivatives
US6642226B2 (en) * 2001-02-06 2003-11-04 Hoffman-La Roche Inc. Substituted phenyl-piperidine methanone compounds
US6531597B2 (en) * 2001-02-13 2003-03-11 Hoffmann-La Roche Inc. Process for preparation of 2-phenyl acetic acid derivatives
EP1483233A4 (en) 2002-03-13 2005-12-21 Univ Tennessee Res Corp SUBSTITUTED TETRAHYDROISOQUINOLEINE COMPOUNDS, METHODS OF PREPARATION AND USE THEREOF
WO2006124865A2 (en) * 2005-05-19 2006-11-23 Vertex Pharmaceuticals Incorporated Biaryls derivatives useful as modulators of ion channels
WO2006130493A2 (en) 2005-05-31 2006-12-07 Vertex Pharmaceuticals Incorporated Heterocycles useful as modulators of ion channels
WO2013004766A1 (en) 2011-07-04 2013-01-10 Ferrari Giulio Nk-1 receptor antagonists for treating corneal neovascularisation
KR102364344B1 (ko) * 2016-05-23 2022-02-18 인스티튜드 오브 머테리아 메디카, 차이니스 아케데미 오브 메디컬 싸이언시스 니코티닐 알콜 에테르 유도체, 그의 제조 방법, 및 그의 약학적 조성물 및 용도
CA3091944A1 (en) 2018-02-26 2019-08-29 Ospedale San Raffaele S.R.L. Nk-1 antagonists for use in the treatment of ocular pain
US20230134843A1 (en) 2020-03-11 2023-05-04 Ospedale San Raffaele S.R.L. Treatment of stem cell deficiency
CN115466195B (zh) * 2022-09-15 2024-04-19 中国科学院成都生物研究所 一类联苯类酰胺化合物及其制备方法和应用

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JPH06227913A (ja) * 1993-02-03 1994-08-16 Sumitomo Chem Co Ltd 安息香酸誘導体を有効成分とする植物病害防除剤
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
ES2164758T3 (es) 1993-12-29 2002-03-01 Merck Sharp & Dohme Derivados de morfolina sustituidos y su uso como agentes terapeuticos.
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
JP3839518B2 (ja) * 1996-03-27 2006-11-01 ポーラ化成工業株式会社 抗真菌剤
AU6415998A (en) 1997-04-18 1998-11-13 Pfizer Inc. Process and intermediates for the preparation of 4'-trifluoromethyl-biphenyl-2-carboxylic acid (1,2,3,4-tetrahydro-isoquinolin-6-yl)-amide
US5972938A (en) 1997-12-01 1999-10-26 Merck & Co., Inc. Method for treating or preventing psychoimmunological disorders
DK1394150T3 (da) * 1999-02-24 2011-03-21 Hoffmann La Roche 4-phenylpyridinderivater og deres anvendelse som NK-1-receptorantagonister

Also Published As

Publication number Publication date
JP3839668B2 (ja) 2006-11-01
MA26778A1 (fr) 2004-12-20
RU2238266C2 (ru) 2004-10-20
HUP0201710A3 (en) 2002-11-28
NO20014356L (no) 2001-09-07
PT1171419E (pt) 2005-04-29
UY26051A1 (es) 2000-09-29
EP1171419B1 (en) 2004-12-29
DE60017110D1 (de) 2005-02-03
CA2366205A1 (en) 2000-09-14
JO2235B1 (en) 2004-10-07
NO20014356D0 (no) 2001-09-07
WO2000053572A1 (en) 2000-09-14
US6552088B2 (en) 2003-04-22
ATE286018T1 (de) 2005-01-15
PE20001549A1 (es) 2001-01-09
CN1343197A (zh) 2002-04-03
AU3161200A (en) 2000-09-28
SI1171419T1 (en) 2005-06-30
NZ513824A (en) 2004-01-30
HK1045684A1 (en) 2002-12-06
IL145166A0 (en) 2002-06-30
TR200102585T2 (tr) 2002-01-21
CO5160261A1 (es) 2002-05-30
PL201681B1 (pl) 2009-04-30
CN1152006C (zh) 2004-06-02
CA2366205C (en) 2008-09-09
ES2233338T3 (es) 2005-06-16
AR043273A1 (es) 2005-07-27
DE60017110T2 (de) 2006-01-26
MY121145A (en) 2005-12-30
KR20010111271A (ko) 2001-12-17
JP2002539112A (ja) 2002-11-19
CZ20013190A3 (cs) 2002-02-13
KR100473247B1 (ko) 2005-03-08
US20020040060A1 (en) 2002-04-04
AU767449B2 (en) 2003-11-13
HUP0201710A2 (en) 2002-10-28
US6291465B1 (en) 2001-09-18
HRP20010629A2 (en) 2002-08-31
YU64901A (sh) 2005-07-19
IL145166A (en) 2006-10-05
HK1045684B (zh) 2004-11-26
EP1171419A1 (en) 2002-01-16
PL350536A1 (en) 2002-12-16
ZA200107259B (en) 2002-12-02

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