YU47097B - Hinuklidin derivati i postupak za njihovo dobijanje - Google Patents

Hinuklidin derivati i postupak za njihovo dobijanje

Info

Publication number
YU47097B
YU47097B YU222289A YU222289A YU47097B YU 47097 B YU47097 B YU 47097B YU 222289 A YU222289 A YU 222289A YU 222289 A YU222289 A YU 222289A YU 47097 B YU47097 B YU 47097B
Authority
YU
Yugoslavia
Prior art keywords
carbon atoms
formula
thienyl
alkyl
alkoxy
Prior art date
Application number
YU222289A
Other languages
English (en)
Other versions
YU222289A (en
Inventor
J.A. Lowe
Original Assignee
Pfizer Inc.
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 Pfizer Inc. filed Critical Pfizer Inc.
Publication of YU222289A publication Critical patent/YU222289A/xx
Publication of YU47097B publication Critical patent/YU47097B/sh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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
    • 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
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Postupak za dobijanje hinulkidin derivata formule: ili njegove farmaceutski prihvatljive soli, u kojoj Ar je tienil, fenil, fluorofenil, hlorofenil ili bromofenil; R' je cikloalkil koji ima od pet do sedam ugljenikovih atoma, norbornil, 2,3-dihidrobenzofuranil, tienil, alkoksitienil sa jedan do tri ugljenikova atoma u alkoksi ostatku, piridil, hidroksipiridil, hinolinil, indolil, naftil, alkoksinaftil sa jedan do tri ugljenikova atoma u alkoksi ostatku, bifenil, 2,3-metilendioksifenil ili fenil opciono supstituisan sa jedan ili dva supstituenta odabranih od nitro, amino, N-monoalkilamino sa jedan do tri ugljenikova atoma u alkil ostatku, fluor, hlor, brom, tri-fluorometil, alkil sa jedan do tri ugljenikova atoma, benzil, alkoksi sa jedan do tri ugljenikova atoma, aliloksi, hidroksi, hidroksimetil, karboksi, hidroksietoksi, alkoksikarbonil i alkoksikarbonilmetoksi svaki sa jedan do tri ugljenika u alkoksi ostatku, karboksimetoksi, i R" je alkil racvastog niza sa tri do cetiri ugljenikova atoma, alkenil racvastog niza alkenil sa pet do sest ugljenikovih atoma, cikloalkil sa pet do sedam ugljenikovih atoma, furil, tienil, piridil, bifenil, ili fenil opciono supstituisan sa do dva supstituenta odabranih izmedju fluora, hlora, broma, trifluorometil, alkila sa do tri ugljenikova atoma, benzil, alkoksi sa jedan do tri ugljenikova atoma, ili karboksi, pod uslovom sto je pomenuti R" uvek razlicit od nesupstituisanog fenil grupe, fluorofenil, hlorofenil, bromofenil ili alkilfenila kada je R' nesupstituisani fenil, ili tienil a Ar je razliciti od tienil grupe, i pod daljim uslovom da je najmanje jedan od Ar, R' i R". uvek razlicit od nesupstituisanog fenila, naznacen time, sto obuhvata: (a) kondenzaciju odgovarajuceg 2-/(alfa-supstituisanog)aril-metil/hinuklidin-3-on jedinjenja formule IV: u kojoj Ar, R i R" su svaki definisan kao gore, sa (ciklicnim) metilaminom formule R'CH2, NH2, gde R' je takodje kao sto je gore definisano, radi obrazovanja -eljenog iminskog finalnog proizvoda strukturne formule II; (b) kondenzaciju odgovarajuceg 3-amino-2-/(alfa-supstituisanog)fenilmetil/hinuklidin jedinjenja formule V: u kojoj Ar, R i R" su svaki kao sto je gore definisano, sa odgovarajucim ciklicnim aldehidnim jedinjenjem formule R'CHO, pri cemu R' je takodje kao sto je definisano gore, radi obrazovanja zeljenog metilenaminskog finalnog proizvoda strukturne formule III; ili (c) kondenzaciju 3-aminohinuklidin jedinjenja formule V sa aktiviranim derivatom karboksilne kiseline formule R'COOH radi obrazovanja odgovarajuceg 3-/(ciklicno)karbonilamino(2-2/(alfa-supstituisanog)arilmetil/hinuklidin jedinjenje formule VI u kojoj R, R' i R" svi imaju isto znacenje kao gore; i d) Posle toga izlaganja jedinjenja formule II, III ili VI selektivnom redukcionom dejstvu pogodnog metalo redukcionog sredstva radi obrazovanja 3-aminohinuklidin finalnog proizvoda struktura formule I; i e) Posle toga, po potrebi, pretvaranje jedinjenja strukturne formule I u kojoj R' je nitrofenil u odgo
YU222289A 1988-11-23 1989-11-22 Hinuklidin derivati i postupak za njihovo dobijanje YU47097B (sh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1988/004205 WO1990005525A1 (en) 1988-11-23 1988-11-23 Quinuclidine derivatives as substance p antagonists

Publications (2)

Publication Number Publication Date
YU222289A YU222289A (en) 1991-04-30
YU47097B true YU47097B (sh) 1994-12-28

Family

ID=22209014

Family Applications (1)

Application Number Title Priority Date Filing Date
YU222289A YU47097B (sh) 1988-11-23 1989-11-22 Hinuklidin derivati i postupak za njihovo dobijanje

Country Status (29)

Country Link
US (1) US5162339A (sh)
EP (1) EP0409931B1 (sh)
JP (1) JPH0647589B2 (sh)
KR (1) KR900701782A (sh)
CN (1) CN1026111C (sh)
AP (1) AP120A (sh)
AR (1) AR246522A1 (sh)
AT (1) ATE101608T1 (sh)
AU (1) AU617906B2 (sh)
CA (1) CA2003441C (sh)
DD (1) DD285605A5 (sh)
DE (1) DE68913194T2 (sh)
EG (1) EG19301A (sh)
ES (1) ES2062504T3 (sh)
FI (1) FI903656A0 (sh)
HU (1) HU900517D0 (sh)
IE (1) IE893730L (sh)
IL (1) IL92336A0 (sh)
MA (1) MA21682A1 (sh)
MX (1) MX18467A (sh)
MY (1) MY105061A (sh)
NZ (1) NZ231461A (sh)
OA (1) OA10023A (sh)
PH (1) PH26590A (sh)
PL (1) PL161864B1 (sh)
PT (1) PT92361B (sh)
WO (2) WO1990005525A1 (sh)
YU (1) YU47097B (sh)
ZA (1) ZA898901B (sh)

Families Citing this family (155)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GR1001124B (el) * 1989-11-20 1993-04-28 Pfizer Θεραπευτικοι παραγοντες κουινουκλιδινης.
WO1991009844A1 (en) * 1990-01-04 1991-07-11 Pfizer Inc. Substance p antagonists
US5332817A (en) * 1990-01-04 1994-07-26 Pfizer Inc. 3-aminopiperidine derivatives and related nitrogen containing heterocycles
US5232929A (en) * 1990-11-28 1993-08-03 Pfizer Inc. 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use
US5364943A (en) * 1991-11-27 1994-11-15 Pfizer Inc. Preparation of substituted piperidines
ES2063507T3 (es) * 1990-06-01 1995-01-01 Pfizer 3-amino-2-aril-quinuclidinas, procedimiento para su preparacion y composiciones farmaceuticas que las contienen.
JP2514137B2 (ja) * 1990-07-23 1996-07-10 フアイザー・インコーポレイテツド キヌクリジン誘導体
DK0550635T3 (da) * 1990-09-28 1995-09-04 Pfizer Cykliske forbindelser med kondeserede ringe, som er analoger til nitrogenholdige ikke-aromatiske het erocykliske forbindelser
US5216163A (en) * 1991-01-03 1993-06-01 Pfizer Inc Process for preparing azabicyclo[2.2.2]octan-3-imines
US5138060A (en) * 1991-01-03 1992-08-11 Pfizer Inc. Process and intermediates for preparing azabicyclo(2.2.2)octan-3-imines
EP0566589A1 (en) * 1991-01-10 1993-10-27 Pfizer Inc. N-alkyl quinuclidinium salts as substance p antagonists
EP0499313B1 (en) * 1991-02-11 1997-06-11 MERCK SHARP & DOHME LTD. Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
ATE115581T1 (de) * 1991-03-01 1994-12-15 Pfizer 1-azabicyclo(3.2.2>nonan-3-aminderivate.
AU647592B2 (en) * 1991-03-26 1994-03-24 Pfizer Inc. Stereoselective preparation of substituted piperidines
FR2676442B1 (fr) * 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveau derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent.
RU2092486C1 (ru) * 1991-05-22 1997-10-10 Пфайзер Инк. Замещенные 3-аминохинуклидины
WO1992020661A1 (en) * 1991-05-22 1992-11-26 Merck & Co., Inc. N, n-diacylpiperazines
US5716965A (en) * 1991-05-22 1998-02-10 Pfizer Inc. Substituted 3-aminoquinuclidines
DE69208877T2 (de) 1991-05-31 1996-07-25 Pfizer Chinuclidinderivate
CZ290475B6 (cs) * 1991-06-20 2002-07-17 Pfizer Inc. Fluoralkoxybenzylaminové deriváty heterocyklů obsahujících dusík, způsob jejich přípravy, meziprodukty tohoto postupu a pouľití těchto derivátů
TW202432B (sh) * 1991-06-21 1993-03-21 Pfizer
US5288730A (en) * 1991-06-24 1994-02-22 Merck Sharp & Dohme Limited Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
EP0536817A1 (en) * 1991-07-05 1993-04-14 MERCK SHARP & DOHME LTD. Azabicyclic compounds as tachykinin antagonists
MY110227A (en) * 1991-08-12 1998-03-31 Ciba Geigy Ag 1-acylpiperindine compounds.
US5459270A (en) * 1991-08-20 1995-10-17 Merck Sharp & Dohme Limited Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
PT533280E (pt) * 1991-09-20 2001-01-31 Glaxo Group Ltd Novas utilizacoes medicas para antagonistas de taquiquinina
HU9400728D0 (en) * 1991-09-26 1994-06-28 Pfizer Fused tricyclic nitrogen containing heterocycles as substance p receptor antagonists
JP2553020B2 (ja) * 1991-11-07 1996-11-13 吉富製薬株式会社 キヌクリジン化合物およびその医薬用途
HUT70741A (en) * 1991-11-12 1995-10-30 Pfizer Acyclic ethylenediamine derivatives as substance p receptor antagonists
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.
JP2656702B2 (ja) * 1992-03-23 1997-09-24 ファイザー製薬株式会社 ペプチド性キヌクリジン
AU675786B2 (en) * 1992-04-15 1997-02-20 Merck Sharp & Dohme Limited Azacyclic compounds
US5444074A (en) * 1992-04-15 1995-08-22 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
DK0641328T3 (da) * 1992-05-18 2002-05-21 Pfizer Broforbundne, azabicykliske derivater som substans P-antagonister
US6048859A (en) 1992-06-29 2000-04-11 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
US5637699A (en) * 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
JP2683783B2 (ja) * 1992-07-10 1997-12-03 雪印乳業株式会社 シェーグレン症候群治療剤
GB9216911D0 (en) * 1992-08-10 1992-09-23 Merck Sharp & Dohme Therapeutic agents
EP1114823A3 (en) * 1992-08-19 2001-07-18 Pfizer Inc. Substituted benzylamino nitrogen containing non-aromatic heterocycles
US5387595A (en) * 1992-08-26 1995-02-07 Merck & Co., Inc. Alicyclic compounds as tachykinin receptor antagonists
FR2695641B1 (fr) * 1992-09-11 1994-11-25 Rhone Poulenc Rorer Sa (Amino-3 phényl)-1 éthanesulfonate d'hydroquinine optiquement actif, sa préparation et son utilisation.
JP2656699B2 (ja) * 1992-10-21 1997-09-24 ファイザー製薬株式会社 置換ベンジルアミノキヌクリジン
US5604241A (en) * 1992-10-21 1997-02-18 Pfizer Inc. Substituted benzylaminoquinuclidines as substance P antagonists
US5837711A (en) * 1992-10-28 1998-11-17 Pfizer Inc. Substituted quinuclidines as substance P antagonists
JP2656700B2 (ja) * 1992-10-28 1997-09-24 ファイザー製薬株式会社 置換キヌクリジン誘導体
DE69307340T2 (de) * 1992-11-12 1997-04-24 Pfizer Chinuclidin derivat als substanz p antagonist
US5344830A (en) * 1992-12-10 1994-09-06 Merck & Co., Inc. N,N-diacylpiperazine tachykinin antagonists
PT675886E (pt) * 1992-12-10 2000-12-29 Pfizer Heterociclos nao aromaticos com substituintes aminometileno e sua utilizacao como antagonistas da substancia p
US5830854A (en) * 1992-12-14 1998-11-03 Merck Sharp & Dohme, Limited Method of treating cystic fibrosis using a tachykinin receptor antagonist
AU6226494A (en) * 1993-03-04 1994-09-26 Pfizer Inc. Spiroazacyclic derivatives as substance p antagonists
US5496833A (en) * 1993-04-13 1996-03-05 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
IL109646A0 (en) * 1993-05-19 1994-08-26 Pfizer Heteroatom substituted alkyl benzylamino-quinuclidines
JP2822274B2 (ja) * 1993-05-19 1998-11-11 ファイザー製薬株式会社 Ｐ物質拮抗剤としてのヘテロ原子置換アルキルベンジルアミノキヌクリジン類
US5393762A (en) * 1993-06-04 1995-02-28 Pfizer Inc. Pharmaceutical agents for treatment of emesis
US5348955A (en) * 1993-06-22 1994-09-20 Merck & Co., Inc. N,N-diacylpiperazines
EP0708771B1 (en) * 1993-07-15 1998-10-07 Pfizer Inc. Benzyloxyquinuclidines as substance p antagonists
US5854262A (en) * 1993-10-07 1998-12-29 Pfizer Inc. Aminomethylene substituted non-aromatic heterocycles and use as substance P antagonists
PE45195A1 (es) * 1994-03-03 1996-01-17 Boehringer Ingelheim Kg Derivado de aminoacido, procedimiento para su preparacion y composicion farmaceutica que lo contiene
US5922878A (en) * 1994-03-03 1999-07-13 Boehringer Ingelheim Gmbh Amino acid derivatives, processes for preparing them and pharmaceutical compositions containing these compounds
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
FR2719476B1 (fr) * 1994-05-05 1997-05-23 Oreal Utilisation d'un antagoniste de substance P dans une composition cosmétique et composition obtenue.
US6203803B1 (en) 1994-12-14 2001-03-20 Societe L'oreal S.A. Use of a substance P antagonist in a cosmetic composition, and the composition thus obtained
FR2719474B1 (fr) 1994-05-05 1996-05-31 Oreal Utilisation d'un antagoniste de substance P dans une composition cosmétique et composition obtenue.
TW397825B (en) * 1994-10-14 2000-07-11 Novartis Ag Aroyl-piperidine derivatives
FR2725900B1 (fr) * 1994-10-21 1997-07-18 Sanofi Sa Utilisation d'antagonistes des recepteurs nk1 pour la preparation de medicaments a action cardioregulatrice
IL116249A (en) * 1994-12-12 2003-07-06 Pfizer Nk-1 receptor antagonists for the treatment of neuronal damage and stroke
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
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
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
ATE199552T1 (de) 1995-07-07 2001-03-15 Pfizer Substituierte benzolaktamverbindungen als substanz-p-antagonisten
US6288225B1 (en) 1996-05-09 2001-09-11 Pfizer Inc Substituted benzolactam compounds as substance P antagonists
PE8798A1 (es) * 1995-07-17 1998-03-02 Pfizer Procedimiento de separacion de los enantiomeros del 1-azabiciclo[2.2.2] octan-3-amina, 2-(difenilmetil) -n- [[2-metoxi-5-(1-metiletil) fenil] metil]
TW458774B (en) 1995-10-20 2001-10-11 Pfizer Antiemetic pharmaceutical compositions
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
MX9706944A (es) * 1996-09-12 1998-08-30 Pfizer Quinuclidinas sustituidas con tetrazolilo como antagonistas de la sustancia p.
US6117855A (en) 1996-10-07 2000-09-12 Merck Sharp & Dohme Ltd. Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors antagonists for treating schizophrenic disorders
US5977104A (en) * 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
US6114315A (en) * 1996-12-02 2000-09-05 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating major depressive disorders with anxiety
CA2273806A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating substance use disorders
EP0942732B1 (en) * 1996-12-02 2004-11-17 MERCK SHARP & DOHME LTD. Use of nk-1 receptor antagonists for treating movement disorders
WO1998024442A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating sexual dysfunction
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
JP2001508412A (ja) * 1996-12-02 2001-06-26 メルク シヤープ エンド ドーム リミテツド 認識障害の治療のためのｎｋ−１受容体拮抗薬の使用
WO1998024443A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating bipolar disorders
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
US6156749A (en) * 1997-12-01 2000-12-05 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating movement disorders
US6271230B1 (en) 1997-12-01 2001-08-07 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating cognitive disorders
US6087348A (en) * 1997-12-01 2000-07-11 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating stress disorders
AU5624599A (en) * 1998-08-25 2000-03-14 Lothar Farber Pharmaceutical uses
US6387925B1 (en) * 1999-06-01 2002-05-14 Pfizer Inc. Polymorphs of a crystalline azo-bicyclo (2.2.2) oct-3-yl amine citrate and their pharmaceutical compositions
US6262067B1 (en) * 1999-06-22 2001-07-17 Pfizer Inc. Polymorphs of a crystalline azo-bicyclo 2,2,2 OCT-3-yl amine dihydrochloride and their pharmaceutical compositions
CA2324116A1 (en) * 1999-10-25 2001-04-25 Susan Beth Sobolov-Jaynes Nk-1 receptor antagonists and eletriptan for the treatment of migraine
RU2309953C2 (ru) 1999-11-03 2007-11-10 Эймр Текнолоджи, Инк. Арил- и гетероарилзамещенные тетрагидроизохинолины, фармацевтическая композиция и способ лечения на их основе
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
USRE44578E1 (en) 2000-04-10 2013-11-05 Teva Pharmaceutical Industries, Ltd. Stable pharmaceutical compositions containing 7-substituted-3,5-dihydroxyheptanoic acids or 7-substituted-3,5-dihydroxyheptenoic acids
IL142810A0 (en) * 2000-05-03 2002-03-10 Pfizer Prod Inc Pharmaceutical uses for fluoroalkoxybenzylamino derivatives of nitrogen containing heterocycles
CA2415532C (en) 2000-07-11 2010-05-11 Albany Molecular Research, Inc. Novel 4-phenyl substituted tetrahydroisoquinolines therapeutic use thereof
US20020049211A1 (en) * 2000-09-06 2002-04-25 Sobolov-Jaynes Susan Beth Combination treatment for depression and anxiety
EP1192952A3 (en) * 2000-09-28 2003-03-26 Pfizer Products Inc. Combination, for treating depression and anxiety, containing an NK-3 receptor antagonist and a CNS penetrant NK-1 receptor antagonist
PL367944A1 (en) * 2001-07-20 2005-03-07 Pfizer Products Inc. Use of nk-1 receptor antagonists to modify unwanted behavior in dogs, cats and horses
US6861526B2 (en) * 2002-10-16 2005-03-01 Pfizer Inc. Process for the preparation of (S,S)-cis-2-benzhydryl-3-benzylaminoquinuclidine
WO2004067703A2 (en) * 2003-01-31 2004-08-12 Pfizer Products Inc. 5ht7 antagonists and inverse agonists
WO2005045395A2 (en) * 2003-10-27 2005-05-19 Meyer Donald W Method of detecting bovine spongiform encephalopathy
DE602004028150D1 (de) * 2003-11-26 2010-08-26 Pfizer Prod Inc Aminopyrazolderivate als gsk-3-inhibitoren
KR101412339B1 (ko) 2004-07-15 2014-06-25 알바니 몰레큘라 리써치, 인크. 아릴- 및 헤테로아릴-치환된 테트라히드로이소퀴놀린, 및이것의 노르에피네프린, 도파민 및 세로토닌의 재흡수를차단하기 위한 용도
US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
CN101495184A (zh) 2005-07-15 2009-07-29 Amr科技公司 芳基和杂芳基取代的四氢苯并氮杂及其在阻断去甲肾上腺素多巴胺和血清素的重摄取中的应用
AU2006297443B2 (en) 2005-09-29 2010-08-12 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP2083831B1 (en) 2006-09-22 2013-12-25 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
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
SI2805945T1 (sl) 2007-01-10 2019-09-30 Msd Italia S.R.L. Amid substituirani indazoli, kot inhibitorji poli(ADP-riboza)polimeraze(PARP)
WO2008090117A1 (en) 2007-01-24 2008-07-31 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
AU2008233662B2 (en) 2007-04-02 2012-08-23 Msd K.K. Indoledione derivative
CA2690191C (en) 2007-06-27 2015-07-28 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
CA2717509A1 (en) 2008-03-03 2009-09-11 Tiger Pharmatech Tyrosine kinase inhibitors
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 (ru) 2008-07-03 2014-04-25 Ньюрексон, Інк. Бензоксазины, бензотиазины и родственные соединения, которые имеют ингибирующую nos активность
PE20110852A1 (es) 2008-10-30 2011-11-25 Merck Sharp & Dohme Antagonistas del receptor de orexina de isonicotinamida
TW201031664A (en) * 2009-01-26 2010-09-01 Targacept Inc Preparation and therapeutic applications of (2S,3R)-N-2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)-3,5-difluorobenzamide
EP2413932A4 (en) 2009-04-01 2012-09-19 Merck Sharp & Dohme INHIBITORS OF AKT ACTIVITY
CA2760837C (en) 2009-05-12 2018-04-03 Albany Molecular Research, Inc. 7-([1,2,4]triazolo[1,5-.alpha.]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof
US8815894B2 (en) 2009-05-12 2014-08-26 Bristol-Myers Squibb Company 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
US9034899B2 (en) 2009-05-12 2015-05-19 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
CA2777043C (en) 2009-10-14 2015-12-15 Schering Corporation Substituted piperidines that increase p53 activity and the uses thereof
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
US8518907B2 (en) 2010-08-02 2013-08-27 Merck Sharp & Dohme Corp. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
EP2606134B1 (en) 2010-08-17 2019-04-10 Sirna Therapeutics, Inc. RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (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
WO2012036997A1 (en) 2010-09-16 2012-03-22 Schering Corporation Fused pyrazole derivatives as novel erk inhibitors
EP3766975A1 (en) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acid (sina)
US9351965B2 (en) 2010-12-21 2016-05-31 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
WO2012143879A1 (en) 2011-04-21 2012-10-26 Piramal Healthcare Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2013165816A2 (en) 2012-05-02 2013-11-07 Merck Sharp & Dohme Corp. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
AU2013323508B2 (en) 2012-09-28 2017-11-02 Merck Sharp & Dohme Corp. Novel compounds that are ERK inhibitors
WO2014078568A1 (en) 2012-11-14 2014-05-22 The Johns Hopkins University Methods and compositions for treating schizophrenia
ES2651347T3 (es) 2012-11-28 2018-01-25 Merck Sharp & Dohme Corp. Composiciones y métodos para el tratamiento del cáncer
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
US9540377B2 (en) 2013-01-30 2017-01-10 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
NL2015865B1 (en) 2015-11-27 2017-06-13 Le Vet B V Maropitant Formulation.
EP3525785A4 (en) 2016-10-12 2020-03-25 Merck Sharp & Dohme Corp. KDM5 INHIBITORS
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
US11098029B2 (en) 2019-02-13 2021-08-24 Merck Sharp & Dohme Corp. 5-alkyl pyrrolidine orexin receptor agonists
EP4010314B1 (en) 2019-08-08 2024-02-28 Merck Sharp & Dohme LLC Heteroaryl pyrrolidine and piperidine orexin receptor agonists
TW202227417A (zh) 2020-08-18 2022-07-16 美商默沙東藥廠 雙環庚烷吡咯啶之食慾素受體促效劑

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3534053A (en) * 1967-05-24 1970-10-13 American Home Prod Quinuclidine derivatives
US3506673A (en) * 1968-03-29 1970-04-14 Aldrich Chem Co Inc 2-(4'halo)-benzhydryl-3-quinuclidinols
US3506672A (en) * 1968-03-29 1970-04-14 Aldrich Chem Co Inc 2-(4,4'-dihalo)-benzhydryl-3-quinuclidinols
US3560510A (en) * 1969-03-05 1971-02-02 Aldrich Chem Co Inc 2-benzhydrylquinuclidines
US3917612A (en) * 1971-07-27 1975-11-04 Hoffmann La Roche 1,1-Dichloro-3-(4-piperidinyl)propan-2-ols
BE789679A (fr) * 1971-10-05 1973-04-04 Leo Pharm Prod Ltd Nouveaux derives d'acide amino-5 isophtalique et leurs procedesde preparation
US3933906A (en) * 1972-10-13 1976-01-20 Ciba-Geigy Corporation 3,4-Bisamino-5-sulfamoylbenzoic acids
FR2529548A1 (fr) * 1982-07-02 1984-01-06 Delalande Sa Nouveaux derives de l'amino-3 quinuclidine, leur procede et leur application en therapeutique
PH23937A (en) * 1986-12-16 1990-01-23 Robins Co Inc A H Anxiolytic-n-(1-azabicyclo(2.2.2.)oct-3-yl)benzamides and thiobenzamides
EP0289170B1 (en) * 1987-04-25 1993-06-23 Beecham Group Plc Azabicyclic compounds, process for their preparation and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
NZ231461A (en) 1991-01-29
YU222289A (en) 1991-04-30
MY105061A (en) 1994-07-30
CA2003441C (en) 1998-04-07
JPH0647589B2 (ja) 1994-06-22
MA21682A1 (fr) 1990-07-01
PL161864B1 (pl) 1993-08-31
CN1043130A (zh) 1990-06-20
WO1990005729A1 (en) 1990-05-31
JPH03503768A (ja) 1991-08-22
ZA898901B (en) 1991-10-30
IE893730L (en) 1990-05-23
AR246522A1 (es) 1994-08-31
KR900701782A (ko) 1990-12-04
PT92361A (pt) 1990-05-31
DE68913194D1 (en) 1994-03-24
CA2003441A1 (en) 1990-05-23
PT92361B (pt) 1995-07-18
PH26590A (en) 1992-08-19
US5162339A (en) 1992-11-10
OA10023A (en) 1996-10-14
MX18467A (es) 1993-07-01
DD285605A5 (de) 1990-12-19
CN1026111C (zh) 1994-10-05
AP8900152A0 (en) 1990-01-31
EG19301A (en) 1994-10-30
AU4661989A (en) 1990-06-12
EP0409931A1 (en) 1991-01-30
DE68913194T2 (de) 1994-05-19
FI903656A0 (fi) 1990-07-19
HU900517D0 (en) 1991-05-28
ATE101608T1 (de) 1994-03-15
AP120A (en) 1991-02-20
WO1990005525A1 (en) 1990-05-31
ES2062504T3 (es) 1994-12-16
EP0409931B1 (en) 1994-02-16
IL92336A0 (en) 1990-07-26
AU617906B2 (en) 1991-12-05

Similar Documents

Publication Publication Date Title
YU47097B (sh) Hinuklidin derivati i postupak za njihovo dobijanje
Gupton et al. Application of 2-substituted vinamidinium salts to the synthesis of 2, 4-disubstituted pyrroles
US6025494A (en) Tetracyclic derivatives, process of preparation and use
YU60198A (sh) Supstituisani derivati indazola i njihova upotreba kao fosfodiesteraze (pde) tipa iv i inhibitora faktora nekroze tumora (tnf)
KR910011890A (ko) N-(피롤로[2,3-d]피리미딘-3-일아크릴)-글루타민산 유도체
DK157861C (da) Analogifremgangsmaade til fremstilling af 4-substituerede fenylalkylimidazolderivater eller ugiftige, farmaceutisk acceptable syreadditionssalte deraf
NO155884C (no) Analogifremgangsmaate for fremstilling av terapeutisk aktive imidazol-derivater.
DK157926C (da) Analogifremgangsmaade til fremstilling af 4-(substitueret aminometyl)-imidazoler eller ugiftige, farmaceutisk acceptable syreadditionssalte deraf
DK249781A (da) Frmgangsmaade til fremstilling af pyrrolopyrrolcarboxylsyrer
US4189496A (en) 2,3-Dihydro-5-thienylmethyl and furylmethyl-6-substituted and 6,7-disubstituted-benzofuran-2-carboxylic acid
AR010984A1 (es) Nuevos esteres de la pleuromutilina, y el acido 1-azabiciclo-4- carbanilcarbanico; procedimiento para su preparacion y composicionesfarmaceuticas que los contienen.
DE2705778A1 (de) Kondensierte pyrimidinderivate, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DK493185A (da) Benzenkondenserede heterocykliske forbindelser
DD270902A5 (de) Verfahren zur herstellung von neuen sulfanamide-aethylverbindungen
KR840005147A (ko) 신규 티에노-피리디논 유도체의 제조방법
US4160844A (en) Composition for treating skin mast cells and/or delayed cellular hypersensitivity reactions
EP0323146A3 (en) Dopamine-beta-hydroxylase inhibitors
US4169149A (en) Use of α-mercapto-β-arylacrylic acid derivatives in heavy metal poisoning
DE2954566C2 (sh)
US4226882A (en) Use of α,α'-dithiobis-(β-arylacrylic acid) derivatives in the treatment of hypertension
US4210665A (en) Use of α,α'-dithiobis(β-arylacrylic acid) derivatives in heavy metal poisoning
US5409940A (en) 3,4-dehydropiperidine derivatives
DE1795490C (de) 3-(p-Methoxyphenyl)-5-(2-morpholinoäthyi)isoxazol und Verfahren zu dessen Herstellung. Ausscheidung aus: 1470258
US4210664A (en) Use of α,α'-dithiobis(β-arylacrylic acid) derivatives to enhance zinc serum and tissue concentrations
IE33870B1 (en) Benzobenzofuranooxepine compounds and process for preparing the same