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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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 (154)

* 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.
UA41251C2 (uk) * 1990-01-04 2001-09-17 Пфайзер, Інк. Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі
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
ATE113947T1 (de) * 1990-06-01 1994-11-15 Pfizer 3-amino-2-arylchinuclidine, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zubereitungen.
EP0540526B1 (en) * 1990-07-23 1994-12-28 Pfizer Inc. Quinuclidine derivatives
EP0550635B1 (en) * 1990-09-28 1995-04-19 Pfizer Inc. Fused ring analogs of nitrogen containing nonaromatic heterocycles
US5138060A (en) * 1991-01-03 1992-08-11 Pfizer Inc. Process and intermediates for preparing azabicyclo(2.2.2)octan-3-imines
US5216163A (en) * 1991-01-03 1993-06-01 Pfizer Inc Process for preparing azabicyclo[2.2.2]octan-3-imines
HUT65612A (en) * 1991-01-10 1994-07-28 Pfizer Process n-alcyl-quinuclidinium salts of p-antagonistic activity
DE69220258T2 (de) * 1991-02-11 1997-12-18 Merck Sharp & Dohme Azabicyclische Verbindungen, diese enthaltende pharmazeutische Zubereitungen und ihre therapeutische Verwendung
ES2065175T3 (es) * 1991-03-01 1995-02-01 Pfizer Derivados de 1-azabiciclo(3.2.2)nonan-3-amina.
BR9205807A (pt) * 1991-03-26 1994-06-28 Pfizer Preparação estéreo-seletiva de piperidinas substituidas
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.
US5716965A (en) * 1991-05-22 1998-02-10 Pfizer Inc. Substituted 3-aminoquinuclidines
WO1992020661A1 (en) * 1991-05-22 1992-11-26 Merck & Co., Inc. N, n-diacylpiperazines
HUT65771A (en) * 1991-05-22 1994-07-28 Pfizer Process for producing substituted 3-amino-quinuclidine derivatives and pharmaceutical compositions containing them
UA27776C2 (uk) * 1991-05-31 2000-10-16 Пфайзер Інк. Похідні хінуклідину та їх фармацевтично прийнятні солі, що є антагоністами речовини р у ссавців, фармацевтична композиція, що має антагоністичну дію на речовину р у ссавців
KR0154882B1 (ko) * 1991-06-20 1998-11-16 알렌 제이. 스피겔 질소 함유 헤테로사이클릭 화합물의 플루오로알콕시벤질아미노 유도체
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.
EP0600952B1 (en) * 1991-08-20 1996-04-17 MERCK SHARP & DOHME LTD. Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
EP1082959A1 (en) * 1991-09-20 2001-03-14 Glaxo Group Limited NK1 Antagonists for the treatment of depression
US5527808A (en) * 1991-09-26 1996-06-18 Pfizer Inc. Fused tricyclic nitrogen containing heterocycles
WO1993009116A1 (en) * 1991-11-07 1993-05-13 Yoshitomi Pharmaceutical Industries, Ltd. Quinuclidine compound and medicinal use thereof
DK0613458T3 (da) * 1991-11-12 1998-02-09 Pfizer Acykliske ethylendiaminderivater som substans P receptorantagonister
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
WO1993021181A1 (en) * 1992-04-15 1993-10-28 Merck Sharp & Dohme Limited Azacyclic compounds
US5444074A (en) * 1992-04-15 1995-08-22 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
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
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
US6048859A (en) 1992-06-29 2000-04-11 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
US5721255A (en) * 1992-08-19 1998-02-24 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
ES2096312T3 (es) * 1992-11-12 1997-03-01 Pfizer Derivado de quinuclidina como antagonista de la sustancia p.
US5344830A (en) * 1992-12-10 1994-09-06 Merck & Co., Inc. N,N-diacylpiperazine tachykinin antagonists
WO1994013663A1 (en) * 1992-12-10 1994-06-23 Pfizer Inc. Aminomethylene substituted non-aromatic heterocycles and use as substance p antagonists
US5830854A (en) * 1992-12-14 1998-11-03 Merck Sharp & Dohme, Limited Method of treating cystic fibrosis using a tachykinin receptor antagonist
ATE166650T1 (de) * 1993-03-04 1998-06-15 Pfizer Spiroazacyclischderivate als substanz p antagonisten
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
ES2121213T3 (es) * 1993-07-15 1998-11-16 Pfizer Benciloxiquinuclidinas como antagonistas de la sustancia p.
US5854262A (en) * 1993-10-07 1998-12-29 Pfizer Inc. Aminomethylene substituted non-aromatic heterocycles and use as substance P antagonists
US5922878A (en) * 1994-03-03 1999-07-13 Boehringer Ingelheim Gmbh Amino acid derivatives, processes for preparing them and pharmaceutical compositions containing these compounds
PE45195A1 (es) * 1994-03-03 1996-01-17 Boehringer Ingelheim Kg Derivado de aminoacido, procedimiento para su preparacion y composicion farmaceutica que lo contiene
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
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.
FR2719476B1 (fr) * 1994-05-05 1997-05-23 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
FR2728166A1 (fr) 1994-12-19 1996-06-21 Oreal Composition topique contenant un antagoniste de substance p
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
FR2729954B1 (fr) 1995-01-30 1997-08-01 Sanofi Sa Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
JP3042894B2 (ja) 1995-07-07 2000-05-22 ファイザー製薬株式会社 サブスタンスpアンタゴニストとしての置換ベンゾラクタム化合物
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
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive 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
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
JP2001504851A (ja) * 1996-12-02 2001-04-10 メルク シヤープ エンド ドーム リミテツド 性的機能不全の治療のためのnk−1受容体拮抗薬の使用
CA2273853A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating cognitive disorders
CA2273856A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating bipolar disorders
JP2001507678A (ja) * 1996-12-02 2001-06-12 メルク シヤープ エンド ドーム リミテツド 運動障害の治療のためのnk−1受容体拮抗薬の使用
JP2001504853A (ja) * 1996-12-02 2001-04-10 メルク シヤープ エンド ドーム リミテツド 物質使用障害の治療のためのnk−1受容体拮抗薬の使用
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
US6087348A (en) * 1997-12-01 2000-07-11 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating stress disorders
US6271230B1 (en) 1997-12-01 2001-08-07 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating cognitive disorders
US6156749A (en) * 1997-12-01 2000-12-05 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating movement disorders
ATE238044T1 (de) * 1998-08-25 2003-05-15 Novartis Pharma Gmbh Verwendung von substanz p antagonisten zur behandlung des chronischen ermüdungssyndroms und/oder der fibromyalgie
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
KR100821410B1 (ko) 2000-07-11 2008-04-10 에이엠알 테크놀로지, 인크. 4-페닐 치환된 테트라하이드로이소퀴놀린 및 이의치료학적 용도
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
US20050136487A1 (en) * 2003-10-27 2005-06-23 Meyer Donald W. Transmissible spongiform encephalopathy detection in cervids, sheep and goats
WO2005051919A1 (en) * 2003-11-26 2005-06-09 Pfizer Products Inc. Aminopyrazole derivatives as gsk-3 inhibitors
ZA200701232B (en) 2004-07-15 2008-08-27 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
EP1904069B1 (en) 2005-07-15 2018-06-13 Albany Molecular Research, Inc. Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
US8293900B2 (en) 2005-09-29 2012-10-23 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
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
BRPI0806245B1 (pt) 2007-01-10 2022-01-25 Msd Italia S.R.L. Compostos de fórmula i e seus usos
KR20090112722A (ko) 2007-01-24 2009-10-28 글락소 그룹 리미티드 3,5-디아미노-6-(2,3-디클로로페닐)-1,2,4-트리아진 또는 r(-)-2,4-디아미노-5-(2,3-디클로로페닐)-6-플루오로메틸 피리미딘 및 nk1을 포함하는 제약 조성물
CA2682727C (en) 2007-04-02 2016-03-22 Banyu Pharmaceutical Co., Ltd. Indoledione derivative
EP2170076B1 (en) 2007-06-27 2016-05-18 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
US8598184B2 (en) 2008-03-03 2013-12-03 Tiger Pharmatech Protein kinase inhibitors
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
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
UA105182C2 (ru) 2008-07-03 2014-04-25 Ньюрексон, Інк. Бензоксазины, бензотиазины и родственные соединения, которые имеют ингибирующую nos активность
MX2011004551A (es) 2008-10-30 2011-05-25 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
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
KR20120034644A (ko) 2009-05-12 2012-04-12 알바니 몰레큘라 리써치, 인크. 아릴, 헤테로아릴, 및 헤테로사이클 치환된 테트라하이드로이소퀴놀린 및 이의 용도
CN102638982B (zh) 2009-05-12 2015-07-08 百时美施贵宝公司 (S)-7-([1,2,4]三唑并[1,5-a]吡啶-6-基)-4-(3,4-二氯苯基)-1,2,3,4-四氢异喹啉的晶型及其用途
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
WO2011046771A1 (en) 2009-10-14 2011-04-21 Schering Corporation SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
CA2805265A1 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
WO2012024170A2 (en) 2010-08-17 2012-02-23 Merck Sharp & Dohme Corp. 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
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. 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
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
JP2014514321A (ja) 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション インスリン様増殖因子1受容体阻害剤
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US10154988B2 (en) 2012-11-14 2018-12-18 The Johns Hopkins University Methods and compositions for treating schizophrenia
MX363243B (es) 2012-11-28 2019-03-14 Merck Sharp & Dohme Composiciones para tratar cáncer y usos de dichas composiciones.
RU2690663C2 (ru) 2012-12-20 2019-06-05 Мерк Шарп И Доум Корп. Замещенные имидазопиридины в качестве ингибиторов hdm2
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.
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833668A4 (en) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. 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
AU2021329805B2 (en) 2020-08-18 2024-02-29 Merck Sharp & Dohme Llc Bicycloheptane pyrrolidine orexin receptor agonists

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
EP0272052B1 (en) * 1986-12-16 1992-07-08 A.H. ROBINS COMPANY, INCORPORATED (a Delaware corporation) Anxiolytic-N-(1-Azabicyclo[2.2.2]Oct-3-yl) Benzamides and Thobenzamides
EP0289170B1 (en) * 1987-04-25 1993-06-23 Beecham Group Plc Azabicyclic compounds, process for their preparation and pharmaceutical compositions containing them

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DE68913194T2 (de) 1994-05-19
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WO1990005525A1 (en) 1990-05-31
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MY105061A (en) 1994-07-30
AU4661989A (en) 1990-06-12
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IL92336A0 (en) 1990-07-26
PL161864B1 (pl) 1993-08-31
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