UA41251C2 - Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі - Google Patents

Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі

Info

Publication number
UA41251C2
UA41251C2 UA5010406A UA5010406A UA41251C2 UA 41251 C2 UA41251 C2 UA 41251C2 UA 5010406 A UA5010406 A UA 5010406A UA 5010406 A UA5010406 A UA 5010406A UA 41251 C2 UA41251 C2 UA 41251C2
Authority
UA
Ukraine
Prior art keywords
hydrogen
phenyl
methyl
optionally substituted
containing heterocyclic
Prior art date
Application number
UA5010406A
Other languages
English (en)
Russian (ru)
Inventor
Манодж С. Десай
Террі Дж. Росен
Терри Дж. Росен
Original Assignee
Пфайзер, Інк.
Пфайзер, Инк.
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 Пфайзер, Інк., Пфайзер, Инк. filed Critical Пфайзер, Інк.
Publication of UA41251C2 publication Critical patent/UA41251C2/uk

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20—Spiro-condensed ring systems
    • 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
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • A61P9/08—Vasodilators for multiple indications
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Винахід належить до нових похідних 3-амінопіперидину та споріднених сполук, а також фармацевтичних композицій. Пропонуються гідровані азотовмісні гетероциклічні сполуки формули (I): m – ціле число від 0 до 6; R1 – водень або (С1-С6)алкіл, необов’язково заміщений гідрокси- або алкокси-групами або фтором; R2 – радикал, який обрано з групи, до якої входять водень, метил, трет-бутил, (C5-С6)циклоалкіл, бензил, бензгідрил, нафтил, тієніл, фураніл, інданіл або феніл, який може бути необов’язково заміщений трифторметилом, одним або двома атомами галогену, алкокси, (С1-С3)гідроксиалкілом, фенілом або -NН(С1-С3)алкілом; R3 – феніл, який може бути заміщений одним, двома або трьома замісниками, обраними серед метилу, (С1-С4)алкоксилу, галогену, трифторметилу, діалкіламіну; тієніл або 2-метоксинафтил; R4 – водень, метил, метокси, галоген; R5 – водень; R6- водень, феніл, гідроксил, фенокси, аміно, ціано, карбокси, карбоетокси, ацетамідо, бензамідо, бензоїл, 4-фторбензоїл, альфа-оксибензил, альфа-окси-4-фторбензил, оксімінобензил, 4,4'-дифторбензгідрил, карбоксамідо, М-метилкарбоксамідо, п-толілсульфонамідо, тіофеніл, 2-нафтамідо- або нафтил-2-метиламіно; R7 – водень; R8 – водень або гідроксил.
UA5010406A 1990-01-04 1990-01-04 Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі UA41251C2 (uk)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1990/000116 WO1991009844A1 (en) 1990-01-04 1990-01-04 Substance p antagonists

Publications (1)

Publication Number Publication Date
UA41251C2 true UA41251C2 (uk) 2001-09-17

Family

ID=22220614

Family Applications (1)

Application Number Title Priority Date Filing Date
UA5010406A UA41251C2 (uk) 1990-01-04 1990-01-04 Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі

Country Status (27)

Country Link
EP (2) EP0436334B1 (uk)
JP (1) JPH0757748B2 (uk)
KR (1) KR930009441B1 (uk)
CN (2) CN1035944C (uk)
AT (1) ATE115127T1 (uk)
AU (1) AU625511B2 (uk)
BR (1) BR9100016A (uk)
CA (1) CA2033497C (uk)
CZ (1) CZ289485B6 (uk)
DE (1) DE69014848T2 (uk)
DK (1) DK0436334T3 (uk)
ES (1) ES2064667T3 (uk)
FI (2) FI114096B (uk)
GR (1) GR3014940T3 (uk)
HU (5) HUT60719A (uk)
IE (1) IE63770B1 (uk)
IL (3) IL112348A (uk)
MY (1) MY105438A (uk)
NO (1) NO178187C (uk)
NZ (1) NZ236581A (uk)
PL (5) PL164244B1 (uk)
PT (1) PT96405B (uk)
RU (1) RU2105758C1 (uk)
UA (1) UA41251C2 (uk)
WO (1) WO1991009844A1 (uk)
YU (1) YU48026B (uk)
ZA (1) ZA9136B (uk)

Families Citing this family (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5830863A (en) * 1988-06-20 1998-11-03 Merrell Pharmaceuticals Inc. Neurokinin A antagonists
US6218364B1 (en) 1988-06-20 2001-04-17 Scott L. Harbeson Fluorinated neurokinin A antagonists
US5232929A (en) * 1990-11-28 1993-08-03 Pfizer Inc. 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use
US5332817A (en) * 1990-01-04 1994-07-26 Pfizer Inc. 3-aminopiperidine derivatives and related nitrogen containing heterocycles
US5364943A (en) * 1991-11-27 1994-11-15 Pfizer Inc. Preparation of substituted piperidines
KR0160142B1 (ko) * 1990-05-31 1998-12-01 알렌 제이. 스피겔 치환된 피페리딘의 제조방법
HUT62891A (en) * 1990-06-01 1993-06-28 Pfizer Process for producing 3-amino-2-arylquinuclidine compounds and pharmaceuticql composition comprising such compounds
CA2086434C (en) * 1990-07-23 1998-09-22 John A. Lowe, Iii Quinuclidine derivatives
BR9205807A (pt) * 1991-03-26 1994-06-28 Pfizer Preparação estéreo-seletiva de piperidinas substituidas
US5716965A (en) * 1991-05-22 1998-02-10 Pfizer Inc. Substituted 3-aminoquinuclidines
UA39168C2 (uk) * 1991-06-20 2001-06-15 Пфайзер, Інк. Фторалкоксифенільні похідні піперидину або хінуклідину, що є антагоністами речовини p і фармацевтична композиція на їх основі
TW202432B (uk) * 1991-06-21 1993-03-21 Pfizer
US5459270A (en) * 1991-08-20 1995-10-17 Merck Sharp & Dohme Limited Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
EP0916346A3 (en) 1991-09-20 2000-12-06 Glaxo Group Limited NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis
GB9201179D0 (en) * 1992-01-21 1992-03-11 Glaxo Group Ltd Chemical compounds
FR2688219B1 (fr) 1992-03-03 1994-07-08 Sanofi Elf Sels d'ammonium quaternaires de composes aromatiques amines, leur preparation et compositions pharmaceutiques les contenant.
US5444074A (en) * 1992-04-15 1995-08-22 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
WO1993021181A1 (en) * 1992-04-15 1993-10-28 Merck Sharp & Dohme Limited Azacyclic compounds
CA2134964C (en) * 1992-05-18 1997-12-30 Manoj C. Desai Bridged aza-bicyclic derivatives as substance p antagonists
US5637699A (en) * 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
US6048859A (en) 1992-06-29 2000-04-11 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
CA2099233A1 (en) * 1992-06-29 1993-12-30 Conrad P. Dorn Morpholine and thiomorpholine tachykinin receptor antagonists
EP0652866B1 (en) * 1992-07-28 1998-11-25 MERCK SHARP & DOHME LTD. Azacyclic compounds
AU4396193A (en) * 1992-08-04 1994-03-03 Pfizer Inc. 3-benzylamino-2-phenyl-piperidine derivatives as substance p receptor antagonists
GB9216911D0 (en) * 1992-08-10 1992-09-23 Merck Sharp & Dohme Therapeutic agents
US5387595A (en) * 1992-08-26 1995-02-07 Merck & Co., Inc. Alicyclic compounds as tachykinin receptor antagonists
US5563161A (en) * 1992-09-10 1996-10-08 Merck Sharp & Dohme Ltd. Alcohols and ethers with aromatic substituents as tachykinin-antagonists
GB9220286D0 (en) * 1992-09-25 1992-11-11 Merck Sharp & Dohme Therapeutic agents
DE69328975T2 (de) * 1992-12-10 2000-11-09 Pfizer Inc., New York Aminomethylen substituierte heterocyclische verbindungen und ihre verwendung alssubstanz p antagonisten
US6369074B1 (en) * 1992-12-10 2002-04-09 Pfizer Inc. Aminomethylene substituted non-aromatic heterocycles and use as substance P antagonists
US5344830A (en) * 1992-12-10 1994-09-06 Merck & Co., Inc. N,N-diacylpiperazine tachykinin antagonists
US5830854A (en) * 1992-12-14 1998-11-03 Merck Sharp & Dohme, Limited Method of treating cystic fibrosis using a tachykinin receptor antagonist
GB9300051D0 (en) * 1993-01-04 1993-03-03 Merck Sharp & Dohme Therapeutic agents
CA2152925A1 (en) * 1993-02-18 1994-09-01 Raymond Baker Azacyclic compounds compositions containing them and their use as tachykinin antagonists
US5496833A (en) * 1993-04-13 1996-03-05 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
DE69404306T2 (de) * 1993-05-28 1997-10-30 Pfizer Verfahren zur herstellung und optischen auflösung von 2-phenyl-3-aminopiperidine
US5348955A (en) * 1993-06-22 1994-09-20 Merck & Co., Inc. N,N-diacylpiperazines
GB9317104D0 (en) * 1993-08-17 1993-09-29 Zeneca Ltd Therapeutic heterocycles
DE69433744T2 (de) * 1993-09-17 2004-10-14 Pfizer Inc. 3-amino-5-carboxy-substituierte piperidine und 3-amino-4-carboxy-substituierte pyrrolidine als tachykinin-antagonisten
AU7082194A (en) * 1993-09-17 1995-04-03 Pfizer Inc. Heteroarylamino and heteroarylsulfonamido substituted 3-benzylaminomethyl piperidines and related compounds
US6083943A (en) * 1993-09-17 2000-07-04 Pfizer Inc Substituted azaheterocyclecarboxylic acid
IS4208A (is) * 1993-09-22 1995-03-23 Glaxo Group Limited 3-(tetrazólýl-benzyl)amínó-piperadidín afleiður
CA2181376A1 (en) * 1994-01-28 1995-08-03 Malcolm Maccoss Aralkylamino substituted azacyclic therapeutic agents
US5610165A (en) * 1994-02-17 1997-03-11 Merck & Co., Inc. N-acylpiperidine tachykinin antagonists
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
GB9408872D0 (en) * 1994-05-03 1994-06-22 Zeneca Ltd Heterocyclic compounds
GB9418545D0 (en) * 1994-09-15 1994-11-02 Merck Sharp & Dohme Therapeutic agents
FR2725900B1 (fr) * 1994-10-21 1997-07-18 Sanofi Sa Utilisation d'antagonistes des recepteurs nk1 pour la preparation de medicaments a action cardioregulatrice
EP0709375B1 (en) * 1994-10-25 2005-05-18 AstraZeneca AB Therapeutic heterocycles
US5998444A (en) * 1995-10-24 1999-12-07 Zeneca Ltd. Piperidinyl compounds as NK1 or NK2 antagonists
US6008223A (en) * 1994-10-27 1999-12-28 Zeneca Limited Therapeutic compounds
FR2728165A1 (fr) 1994-12-19 1996-06-21 Oreal Utilisation d'un antagoniste de substance p pour le traitement des rougeurs cutanees d'origine neurogene
FR2728169A1 (fr) 1994-12-19 1996-06-21 Oreal Utilisation d'un antagoniste de substance p pour le traitement des prurits et des dysesthesies oculaires ou palpebrales
FR2728166A1 (fr) 1994-12-19 1996-06-21 Oreal Composition topique contenant un antagoniste de substance p
FR2729954B1 (fr) * 1995-01-30 1997-08-01 Sanofi Sa Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
FR2729952B1 (fr) * 1995-01-30 1997-04-18 Sanofi Sa Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
FR2741262B1 (fr) 1995-11-20 1999-03-05 Oreal Utilisation d'un antagoniste de tnf-alpha pour le traitement des rougeurs cutanees d'origine neurogene
DK0780375T3 (da) 1995-12-21 2002-10-07 Pfizer 3-((5-substitueret benzyl)amino)-2-phenylpiperidiner som substans P-antagonister
WO1998014193A1 (en) * 1996-10-04 1998-04-09 Alcon Laboratories, Inc. The use of a substance p antagonist for the manufacture of a medicament for the treatment of ocular pain
US5750549A (en) * 1996-10-15 1998-05-12 Merck & Co., Inc. Cycloalkyl tachykinin receptor antagonists
EP0977572A1 (en) * 1997-04-24 2000-02-09 Merck Sharp & Dohme Ltd. Use of nk-1 receptor antagonists for treating eating disorders
GB9716457D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
CA2298777A1 (en) * 1997-08-04 1999-02-18 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating mania
WO1999007375A1 (en) * 1997-08-04 1999-02-18 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating aggressive behaviour disorders
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
GB9816897D0 (en) * 1998-08-04 1998-09-30 Merck Sharp & Dohme Therapeutic use
WO2000010545A2 (en) * 1998-08-25 2000-03-02 Novartis Ag Use of substance p antagonists for the treatment of chronic fatigue syndrome and/or fibromyalgia and use of nk-1 receptor antagonists for the treatment of chronic fatigue syndrome
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
ES2304984T3 (es) 1999-11-03 2008-11-01 Amr Technology, Inc. Tetra-hidroisoquinolinas de sustitucion arilica y heteroarilica y su utilizacion para bloquear la recaptacion de norepinefrina, dopamina y serotonina.
NZ520588A (en) 2000-03-21 2004-06-25 Smithkline Beecham Corp Protease inhibitors
EP1299393A2 (en) 2000-07-11 2003-04-09 Bristol-Myers Squibb Pharma Company 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
AU2001292320A1 (en) * 2000-10-02 2002-04-15 Tanabe Seiyaku Co., Ltd. Benzylamine compound, process for producing the same, and intermediate therefor
US6709651B2 (en) 2001-07-03 2004-03-23 B.M.R.A. Corporation B.V. Treatment of substance P-related disorders
US20050038072A1 (en) * 2001-12-28 2005-02-17 Takeda Chemical Industries, Ltd. Nitrogeneous cyclic ketone derivative, process for producing the same, and use
NZ552397A (en) 2004-07-15 2011-04-29 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
DE602005018381D1 (de) 2004-10-18 2010-01-28 Lilly Co Eli 1-(hetero)aryl-3-aminopyrrolidinderivate zur verwendung als antagonisten des mglur3-rezeptors
GB0423356D0 (en) 2004-10-21 2004-11-24 Merck Sharp & Dohme Therapeutic agents
ATE550019T1 (de) 2005-05-17 2012-04-15 Merck Sharp & Dohme Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
KR101589551B1 (ko) 2005-07-15 2016-02-02 알바니 몰레큘라 리써치, 인크. 아릴- 및 헤테로아릴-치환된 테트라히드로벤자제핀, 및 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
BRPI0616463A2 (pt) 2005-09-29 2011-06-21 Merck & Co Inc composto, composição farmacêutica, e, uso de um composto
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
PL2109608T3 (pl) 2007-01-10 2011-08-31 Msd Italia Srl Indazole podstawione grupą amidową jako inhibitory polimerazy poli(ADP-rybozy)-(PARP)
EP2117538A1 (en) 2007-01-24 2009-11-18 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-)
CA2682727C (en) 2007-04-02 2016-03-22 Banyu Pharmaceutical Co., Ltd. Indoledione derivative
CA2690191C (en) 2007-06-27 2015-07-28 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
KR20100126467A (ko) 2008-03-03 2010-12-01 타이거 파마테크 티로신 키나아제 억제제
AR071997A1 (es) 2008-06-04 2010-07-28 Bristol Myers Squibb Co Forma cristalina de 6-((4s)-2-metil-4-(2-naftil)-1,2,3,4-tetrahidroisoquinolin-7-il)piridazin-3-amina
US9156812B2 (en) 2008-06-04 2015-10-13 Bristol-Myers Squibb Company Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
UA105182C2 (uk) 2008-07-03 2014-04-25 Ньюрексон, Інк. Бензоксазини, бензотіазини і споріднені сполуки, що мають інгібуючу nos активність
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
AU2010247735B2 (en) 2009-05-12 2015-07-16 Albany Molecular Research, Inc. Crystalline forms of (S)-7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)- 1,2,3,4-tetrahydroisoquinoline and use thereof
KR20120034644A (ko) 2009-05-12 2012-04-12 알바니 몰레큘라 리써치, 인크. 아릴, 헤테로아릴, 및 헤테로사이클 치환된 테트라하이드로이소퀴놀린 및 이의 용도
US8802696B2 (en) 2009-05-12 2014-08-12 Albany Molecular Research, Inc. 7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoqu inoli and use thereof
BR112012008849A2 (pt) 2009-10-14 2015-09-22 Schering Corp composto, composição farmacêutica, e, uso de um composto
EP2584903B1 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
CN103068980B (zh) 2010-08-02 2017-04-05 瑟纳治疗公司 使用短干扰核酸（siNA）的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1（CTNNB1）基因表达的抑制
SI2606134T1 (sl) 2010-08-17 2019-08-30 Sirna Therapeutics, Inc. RNA-INTERFERENČNO POSREDOVANO ZAVIRANJE IZRAŽANJA GENA VIRUSA HEPATITISA B (HBV) Z UPORABO KRATKE INTERFERENČNE NUKLEINSKE KISLINE (siNA)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
EP2615916B1 (en) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel erk inhibitors
DK2632472T3 (en) 2010-10-29 2018-03-19 Sirna Therapeutics Inc RNA INTERFERENCE-MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERRING NUCLEIC ACIDS (SINA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
IN2013MN02170A (uk) 2011-04-21 2015-06-12 Piramal Entpr Ltd
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP3919620A1 (en) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
JP6280554B2 (ja) 2012-09-28 2018-02-14 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｅｒｋ阻害剤である新規化合物
EP2919788A4 (en) 2012-11-14 2016-05-25 Univ Johns Hopkins METHODS AND COMPOSITIONS FOR THE TREATMENT OF SCHIZOPHRENIA
PL2925888T3 (pl) 2012-11-28 2018-03-30 Merck Sharp & Dohme Corp. Kompozycje i sposoby do stosowania w leczeniu nowotworów
WO2014100065A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
US11993602B2 (en) 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL89969C (uk) * 1954-02-05
GB1060160A (en) * 1964-08-05 1967-03-01 Allen & Hanburys Ltd 4-phenylpiperidine derivatives
US3560510A (en) * 1969-03-05 1971-02-02 Aldrich Chem Co Inc 2-benzhydrylquinuclidines
US3992389A (en) * 1970-09-03 1976-11-16 John Wyeth & Brother Limited Heterocyclic compounds
WO1990005525A1 (en) * 1988-11-23 1990-05-31 Pfizer Inc. Quinuclidine derivatives as substance p antagonists
KR0160142B1 (ko) * 1990-05-31 1998-12-01 알렌 제이. 스피겔 치환된 피페리딘의 제조방법

Also Published As

Publication number Publication date
DE69014848D1 (de) 1995-01-19
CA2033497A1 (en) 1991-07-05
NO178187C (no) 1996-02-07
JPH0757748B2 (ja) 1995-06-21
CN1045595C (zh) 1999-10-13
RU2105758C1 (ru) 1998-02-27
IL112348A0 (en) 1995-03-30
PL293390A1 (en) 1992-07-13
PL164205B1 (en) 1994-06-30
HUT68180A (en) 1995-05-29
HUT68179A (en) 1995-05-29
CZ289485B6 (cs) 2002-02-13
YU491A (sh) 1994-01-20
PT96405A (pt) 1991-10-15
FI114096B (fi) 2004-08-13
HU910006D0 (en) 1991-08-28
IL96821A0 (en) 1991-09-16
KR910014350A (ko) 1991-08-31
PL163967B1 (pl) 1994-06-30
AU6862191A (en) 1991-07-18
ZA9136B (en) 1992-08-26
CN1035944C (zh) 1997-09-24
PL164203B1 (pl) 1994-06-30
PT96405B (pt) 1998-06-30
FI20040479A (fi) 2004-04-01
HU222724B1 (hu) 2003-09-29
IL96821A (en) 1997-03-18
EP0558156A3 (en) 1993-10-06
NO910016D0 (no) 1991-01-03
PL293391A1 (en) 1992-07-13
AU625511B2 (en) 1992-07-16
GR3014940T3 (en) 1995-05-31
HUT60719A (en) 1992-10-28
PL164204B1 (pl) 1994-06-30
PL164244B1 (en) 1994-07-29
DK0436334T3 (da) 1995-02-13
CN1087083A (zh) 1994-05-25
CS1091A3 (en) 1991-08-13
BR9100016A (pt) 1991-10-22
YU48026B (sh) 1996-10-09
CN1053060A (zh) 1991-07-17
IE63770B1 (en) 1995-06-14
DE69014848T2 (de) 1995-05-04
PL293392A1 (en) 1992-07-13
NO910016L (no) 1991-07-05
ATE115127T1 (de) 1994-12-15
FI910034A0 (fi) 1991-01-03
IE910007A1 (en) 1991-07-17
HUT68130A (en) 1995-05-29
CA2033497C (en) 1997-01-07
EP0436334A3 (en) 1992-05-27
PL293389A1 (en) 1992-07-13
EP0436334A2 (en) 1991-07-10
ES2064667T3 (es) 1995-02-01
IL112348A (en) 1998-06-15
WO1991009844A1 (en) 1991-07-11
JPH04103570A (ja) 1992-04-06
MY105438A (en) 1994-10-31
NZ236581A (en) 1992-10-28
HU220602B1 (hu) 2002-03-28
FI910034A (fi) 1991-07-05
EP0436334B1 (en) 1994-12-07
PL288592A1 (en) 1992-06-15
EP0558156A2 (en) 1993-09-01
KR930009441B1 (ko) 1993-10-04
NO178187B (no) 1995-10-30

Similar Documents

Publication Publication Date Title
UA41251C2 (uk) Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі
HUP0300565A2 (hu) PDE 5 inhibitor hatású 8-kinolin-xantin- és 8-izo-kinolin-xantin-származékok, alkalmazásuk, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
AU3813095A (en) Aniline derivatives
BG100951A (en) Novel erythromycin derivatives, method for their preparation and their use as drugs
HUP9902471A2 (hu) Piperazin- és piperidinvegyületek, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítmények
AU669032B2 (en) New indole, indazole and benzisoxazole compounds, process for preparing them and pharmaceutical compositions containing them
ATE227719T1 (de) Heteroaryl-zyklische acetale
BG100154A (en) Carbazole derivatibes having inhibiting effect to 17,20-lyase
FR2673427B1 (fr) Derives heterocycliques diazotes n-substitues par un groupement biphenylmethyle, leur preparation, les compositions pharmaceutiques en contenant.
BG104287A (en) Halogensubstituted tetracyclic derivatives of tetrahydrofuran
CA2067758A1 (en) Piperidine and pyrrolidine derivatives
CS621987A2 (en) Coating composition
DE69511260D1 (en) Bicyclische amidinderivate als no-synthetase inhibitoren
BG101538A (en) Fungicidal mixture
NO994659L (no) Nye pyridinderivater og farmasöytiske preparater inneholdende slike
NO20043951L (no) 3-cyklyl-5-(nitrogenholdig 5-leddet ring) metyl-oksazolidinon-derivater og deres anvendelse som antibakterielle midler
AU6615686A (en) Antihypertensive combination product
DE69414112D1 (de) Pyridazinon derivate mit pharmazeutischer wirkung
IL81933A (en) Asymmetrical ester derivatives of 1,4-dihydro-2,6-dimethyl-4-phenyl-pyridine-3,5-dicarboxylic acid,their preparation and pharmaceutical compositions containing them
UA72934C2 (uk) Феніл- і піридилтетрагідропіридини, що інгібують фактор некрозу пухлин, спосіб їх одержання та фармацевтична композиція
TW333525B (en) New perhydroisoindole derivatives, their preparation and the pharmaceutical compositions which contain them the invention relates to perhydroisoindole derivatives of general formula (I), and their salts when they exist advantageously as neurokinin A antagonists.
NO982549L (no) 5-naftalen-1-yl-1,3-dioksan-derivater, fremstilling og terapeutisk anvendelse derav
ES2103675A1 (es) Nuevas piperidinas sustituidas.
IL115085A0 (en) Bicyclic carboxamide derivatives their preparation and pharmaceutical compositions containing them
AU5489598A (en) Diphenylalkyl-tetrahydropyridines, process for their preparation and pharmaceutical composition containing them