UY26051A1 - Derivados de bifenilos antagonistas del receptor de nk-1 - Google Patents

Derivados de bifenilos antagonistas del receptor de nk-1

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Publication number
UY26051A1
UY26051A1 UY26051A UY26051A UY26051A1 UY 26051 A1 UY26051 A1 UY 26051A1 UY 26051 A UY26051 A UY 26051A UY 26051 A UY26051 A UY 26051A UY 26051 A1 UY26051 A1 UY 26051A1
Authority
UY
Uruguay
Prior art keywords
hydrogen
lower alkyl
trifluoromethyl
halogen
biphenyl derivatives
Prior art date
Application number
UY26051A
Other languages
English (en)
Inventor
Bos Michael
Galley Guido
Godel Tierry
Hoffmann Torsten
Hunkeler Walter
Schnider Patrick
Stadler Heinz
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 UY26051A1 publication Critical patent/UY26051A1/es

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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)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (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

Derivados de bifenilos de fórmula general I en donde: R es hidrógeno, alquilo inferior, alcoxi inferior, halógeno, amino, -N(R6)2 ó trifluorometilo; R1 es hidrógeno, alcoxi inferior o halógeno; R y R1 pueden ser conjuntamente -CH=CH-CH=CH-; R2 es halógeno, alquilo inferior o trifluorometilo; R3 es hidrógeno o alquilo inferior; R4 es hidrógeno o una amina terciaria cíclica, sustituida opcionalmente por alquilo inferior; R5 es hidrógeno, nitro, amino ó -N(R6)2; R6 es hidrógeno o alquilo inferior; X es -C(O)N(R6)-, -(CH2)nO-, -(CH2)nN(R6)-, N(R6)C(O)- ó -N(R6)(CH2)n; y n es 1-2; y sales derivadas de una adición ácida farmacéuticamente aceptables. Los compuestos de la fórmula I se pueden usar para el tratamiento de enfermedades relacionadas con el receptor de NK-1 (Neuroquinina-1), tales como trastornos del sistema nervioso central (ej: ansiedad, depresión y psicosis), y otros. Ej. no limitante: 2-(3,5-bis-trifluorometil-fenil)-N-metil-N-(2'-metil-bifenil-2-il)-isobutiramida.
UY26051A 1999-03-09 2000-03-08 Derivados de bifenilos antagonistas del receptor de nk-1 UY26051A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP99104626 1999-03-09

Publications (1)

Publication Number Publication Date
UY26051A1 true UY26051A1 (es) 2000-09-29

Family

ID=8237723

Family Applications (1)

Application Number Title Priority Date Filing Date
UY26051A UY26051A1 (es) 1999-03-09 2000-03-08 Derivados de bifenilos antagonistas del receptor de nk-1

Country Status (33)

Country Link
US (2) US6291465B1 (es)
EP (1) EP1171419B1 (es)
JP (1) JP3839668B2 (es)
KR (1) KR100473247B1 (es)
CN (1) CN1152006C (es)
AR (1) AR043273A1 (es)
AT (1) ATE286018T1 (es)
AU (1) AU767449B2 (es)
BR (1) BR0008862A (es)
CA (1) CA2366205C (es)
CO (1) CO5160261A1 (es)
CZ (1) CZ20013190A3 (es)
DE (1) DE60017110T2 (es)
ES (1) ES2233338T3 (es)
HK (1) HK1045684B (es)
HR (1) HRP20010629A2 (es)
HU (1) HUP0201710A3 (es)
IL (2) IL145166A0 (es)
JO (1) JO2235B1 (es)
MA (1) MA26778A1 (es)
MY (1) MY121145A (es)
NO (1) NO20014356L (es)
NZ (1) NZ513824A (es)
PE (1) PE20001549A1 (es)
PL (1) PL201681B1 (es)
PT (1) PT1171419E (es)
RU (1) RU2238266C2 (es)
SI (1) SI1171419T1 (es)
TR (1) TR200102585T2 (es)
UY (1) UY26051A1 (es)
WO (1) WO2000053572A1 (es)
YU (1) YU64901A (es)
ZA (1) ZA200107259B (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2238264C2 (ru) 1999-02-24 2004-10-20 Ф.Хоффманн-Ля Рош Аг Производные бензола или пиридина и фармацевтическая композиция на их основе
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
US7241774B2 (en) 2002-03-13 2007-07-10 University Of Tennessee Research Foundation Substituted tetrahydroisoquinoline compounds, methods of making, and their use
JP2008540665A (ja) * 2005-05-19 2008-11-20 バーテックス ファーマシューティカルズ インコーポレイテッド イオンチャネルのモジュレーターとして有用なビアリール
EP1904491A2 (en) 2005-05-31 2008-04-02 Vertex Pharmaceuticals Incorporated Heterocycles useful as modulators of ion channels
DK2729147T3 (en) 2011-07-04 2017-12-18 Irbm - Science Park S P A NK-1 RECEPTOR ANTAGONISTS FOR TREATMENT OF CORNOVA
US10975049B2 (en) 2016-05-23 2021-04-13 Institute Of Materia Medica, Chinese Academy Of Medical Sciences Nicotinyl alcohol ether derivative, preparation method therefor, and pharmaceutical composition and uses thereof
RU2020131446A (ru) 2018-02-26 2022-03-28 Оспедале Сан Раффаэле С.Р.Л. Антагонисты nk-1 для применения в лечении глазной боли
EP4117673A1 (en) 2020-03-11 2023-01-18 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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
JP3839518B2 (ja) * 1996-03-27 2006-11-01 ポーラ化成工業株式会社 抗真菌剤
WO1998047875A1 (en) 1997-04-18 1998-10-29 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
PT1394150E (pt) * 1999-02-24 2011-02-17 Hoffmann La Roche Derivados de 4-fenilpiridina e a sua utilização como antagonistas dos receptores de nc-1

Also Published As

Publication number Publication date
CO5160261A1 (es) 2002-05-30
JO2235B1 (en) 2004-10-07
ZA200107259B (en) 2002-12-02
US20020040060A1 (en) 2002-04-04
IL145166A (en) 2006-10-05
MY121145A (en) 2005-12-30
HRP20010629A2 (en) 2002-08-31
AU3161200A (en) 2000-09-28
YU64901A (sh) 2005-07-19
CA2366205A1 (en) 2000-09-14
NZ513824A (en) 2004-01-30
EP1171419B1 (en) 2004-12-29
KR100473247B1 (ko) 2005-03-08
ATE286018T1 (de) 2005-01-15
KR20010111271A (ko) 2001-12-17
HUP0201710A2 (en) 2002-10-28
PL350536A1 (en) 2002-12-16
BR0008862A (pt) 2002-01-02
AU767449B2 (en) 2003-11-13
US6291465B1 (en) 2001-09-18
HK1045684B (zh) 2004-11-26
PL201681B1 (pl) 2009-04-30
HK1045684A1 (en) 2002-12-06
AR043273A1 (es) 2005-07-27
JP2002539112A (ja) 2002-11-19
EP1171419A1 (en) 2002-01-16
SI1171419T1 (en) 2005-06-30
NO20014356D0 (no) 2001-09-07
CZ20013190A3 (cs) 2002-02-13
CA2366205C (en) 2008-09-09
MA26778A1 (fr) 2004-12-20
US6552088B2 (en) 2003-04-22
PE20001549A1 (es) 2001-01-09
PT1171419E (pt) 2005-04-29
NO20014356L (no) 2001-09-07
ES2233338T3 (es) 2005-06-16
WO2000053572A1 (en) 2000-09-14
IL145166A0 (en) 2002-06-30
CN1152006C (zh) 2004-06-02
TR200102585T2 (tr) 2002-01-21
CN1343197A (zh) 2002-04-03
DE60017110D1 (de) 2005-02-03
JP3839668B2 (ja) 2006-11-01
RU2238266C2 (ru) 2004-10-20
DE60017110T2 (de) 2006-01-26
HUP0201710A3 (en) 2002-11-28

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