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ES2528404T3 - Formas cristalinas de (S)-7-([1,2,4]triazol[1,5-a]piridin-6-il)-4-(3,4-diclorofenil)-1,2,3,4-tetrahidroisoquinolina y sus usos - Google Patents

Formas cristalinas de (S)-7-([1,2,4]triazol[1,5-a]piridin-6-il)-4-(3,4-diclorofenil)-1,2,3,4-tetrahidroisoquinolina y sus usos Download PDF

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ES2528404T3
ES2528404T3 ES10775425.1T ES10775425T ES2528404T3 ES 2528404 T3 ES2528404 T3 ES 2528404T3 ES 10775425 T ES10775425 T ES 10775425T ES 2528404 T3 ES2528404 T3 ES 2528404T3
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Chenkou Wei
Victor W. Rosso
Qi Gao
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Bristol Myers Squibb Co
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Abstract

Forma cristalina SA-1 de**Fórmula** en la que: el átomo de carbono designado * está en la configuración S; o una sal de este farmacéuticamente aceptable o un solvato del mismo.

Description

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DESCRIPCIÓN
Formas cristalinas de (S)-7-([1,2,4]triazol[1,5-a]piridin-6-il)-4-(3,4-diclorofenil)-1,2,3,4-tetrahidroisoquinolina y sus usos
Campo de la invención
La presente invención se refiere a los compuestos, las formas cristalinas, las composiciones, y usos para el tratamiento de diversos trastornos neurológicos y psicológicos. En particular, la presente invención se refiere a tales compuestos, formas cristalinas, composiciones y usos, donde los compuestos son novedosos derivados de tetrahidroisoquinolina [1,2,4]triazolo[1,5-a]piridinil-6-il-sustituida. La invención también se refiere a un método de fabricación de estos compuestos. Particularmente, en la presente invención se describen las formas cristalinas SA-1 y N-2.
Antecedentes de la invención
Los inhibidores de la reabsorción de monoamina elevan los niveles extracelulares de serotonina (5-HT), norepinefrina (NE) y/o dopamina (DA) en el cerebro mediante la unión a uno o más de los transportadores responsables de la reabsorción, a
saber, el transportador de serotonina (SERT), el transportador de norepinefrina (NET) y el transportador de dopamina (DAT), bloqueando así la reabsorción del(los) neurotransmisor(es) de la hendidura sináptica. Los inhibidores de la reabsorción de monoaminas son una clase de fármaco establecida que ha demostrado ser de utilidad para el tratamiento de un número de trastornos del SNC, especialmente el trastorno depresivo mayor (MDD).

Desde la introducción de los antidepresivos tricíclicos (TCAs) hace casi 50 años, los inhibidores selectivos de la reabsorción de monoaminas con perfiles de seguridad muy mejorados han mejorado significativamente el tratamiento de la depresión. Aunque los TCAs son antidepresivos muy eficaces, los efectos secundarios, cardiovasculares, anticolinérgicos y sedantes
son comunes debido a la interacción de los TCAs con los receptores muscarínicos, histamínicos y adrenérgicos. La introducción revolucionaria de los inhibidores selectivos de la reabsorción de serotonina (SSRIs) en la década de 1980
permitió que una población de pacientes mucho más grande se tratara debido al perfil de seguridad muy mejorado. Durante las últimas décadas, los inhibidores que bloquean selectivamente la reabsorción de NE o DA, o dos de los tres
neurotransmisores simultáneamente, se han vuelto disponibles para el tratamiento de trastornos del SNC, incluyendo la depresión, ansiedad, trastorno obsesivo compulsivo (OCD), trastorno de déficit de atención con hiperactividad (ADHD), el dolor y la incontinencia urinaria. Dos revisiones recientes representativas (Liu and Molino, Annual Reports in Medicinal Chemistry, 42:13 (2007); Walter, Drug Dev. Res., 65:97 (2005)) sobre los inhibidores de la reabsorción de monoaminas resumen la historia y el desarrollo reciente en el área de inhibidores de reabsorción de la monoamina.
En la actualidad, el principal esfuerzo en el campo de los inhibidores selectivos de la reabsorción de monoaminas se centra en la mejora de la eficacia antidepresiva dado que el 30-40% de los pacientes no responden al tratamiento con antidepresivos disponibles actualmente. Un objetivo adicional importante es mejorar el inicio de acción. Los antidepresivos actuales por lo general requieren 2-6 semanas de tratamiento antes de que se vea la eficacia clínica. Los ensayos clínicos que exploran estrategias de aumento, en las que un inhibidor de la reabsorción de DA o inhibidor de la reabsorción dual de NE/DA se combina con un SSRI, han resultado en la mejora de la eficacia en pacientes con depresión refractario al tratamiento con SSRI solo (Patkar et. al, J. Clin. Psychopharmacol., 26:653 (2006); Zisook et al, Biol. Psychiat., 59:203 (2006)). Los resultados mejorados de los ensayos clínicos de este tipo sirven para justificar el enfoque considerable en el desarrollo de inhibidores que bloquean simultáneamente la reabsorción de 5-HT, NE y DA. Debido a la continua necesidad de mejores fármacos para tratar la depresión y las oportunidades para nuevas indicaciones clínicas, los esfuerzos para descubrir nuevos inhibidores selectivos de la reabsorción de monoaminas continúan sin descanso.
El metilfenidato, que se utiliza actualmente para el tratamiento del trastorno de déficit de atención con hiperactividad, es conocido por ser selectivo para la inhibición de DAT. También, la Patente de Estados Unidos No. 5,444,070 revela los inhibidores selectivos de la reabsorción de la dopamina como tratamientos para la enfermedad de Parkinson, adicción o abuso a las drogas incluyendo la cocaína y las anfetaminas.
Los inhibidores selectivos de la reabsorción de noradrenalina (NARI) también se han revelado. La Patente de Estados Unidos No. 6,352,986 describe los métodos para tratar el trastorno por déficit de atención con hiperactividad (ADHD), trastornos adictivos, y los trastornos por consumo de sustancias psicoactivas con reboxetina. También, la atomoxetina (Strattera) se comercializa actualmente como un inhibidor selectivo de la reabsorción de NET para el ADHD.
Se ha demostrado que el uso de inhibidores selectivos de la reabsorción de serotonina (SSRI) es eficaz en el tratamiento de trastornos depresivos. La sertralina, el citalopram, el escitalopram, la paroxetina, la fluoxetina y la fluvoxamina son ejemplos bien conocidos de los SSRI utilizados para tratar trastornos como la depresión, el trastorno obsesivo-compulsivo y ataques de pánico. Existen varias dificultades conocidas con la clase de SSRI de la terapéutica, incluyendo el lento comienzo de la
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Claims (5)

  1. imagen1
    1. Forma cristalina SA-1 de
    5 en la que: el átomo de carbono designado * está en la configuración S;
    o una sal de este farmacéuticamente aceptable o un solvato del mismo.

  2. 2. La forma cristalina de la reivindicación 1, caracterizada por los siguientes parámetros de célula unitaria:
    10
    Dimensiones de la célula:
    a = 11.0668(9) Å b = 7.3750(6) Å
    15 c = 15.3927(14) Å alfa = 90° beta = 100.594(7)° gamma = 90°
    20 Grupo espacial: Monocíclico, P21 Volumen: 1234.90(18) Å3 Z, Densidad calculada: 2, 1.363 mg/m3,
    en donde la medición de dicha forma cristalina es a una temperatura de entre aproximadamente 20 °C a aproximadamente 25 25 °C.
  3. 3. La forma cristalina de la reivindicación 1, caracterizada por coordenadas atómicas fraccionadas dentro de la célula unitaria como se indica en la Tabla 6.
    30 4. La forma cristalina de la reivindicación 1, que tiene los picos característicos en un patrón de difracción de rayos X en polvo a valores de 2 theta de 5.8 ± 0.1, 8.1 ± 0.1, 9.1 ± 0.1, 10.8 ± 0.1, 11.7 ± 0.1, 13.0 ± 0.1, 13.3 ± 0.1, 14.5 ± 0.1, 15.1 ± 0.1, 15.4 ± 0.1, 16.2 ± 0.1, y 16.8 ± 0.1, a una temperatura entre aproximadamente 20 °C y aproximadamente 25 °C.
  4. 5. La forma cristalina de la reivindicación 1, caracterizada por una endotermia de fusión con descomposición con la 35 aparición de aproximadamente 85 °C.
  5. 6. Una composición farmacéutica que comprende un portador farmacéuticamente aceptable y una cantidad terapéuticamente eficaz de la forma cristalina de acuerdo con la reivindicación 1.
    40 7. Una forma cristalina de acuerdo con la reivindicación 1 o una sal de este farmacéuticamente aceptable para uso en el tratamiento de un trastorno seleccionado del grupo que consiste de trastorno de déficit de atención con hiperactividad (ADHD), deterioro cognitivo, trastornos de ansiedad, trastorno de ansiedad generalizada (GAD), trastorno de pánico, trastorno bipolar o depresión maníaca o trastorno manicodepresivo, trastorno obsesivo compulsivo (OCD), el trastorno de estrés postraumático (PTSD), trastorno de estrés agudo, la fobia social, fobias simples, trastorno disfórico premenstrual
    45 (PMDD), trastorno de ansiedad social (SAD), trastorno depresivo mayor (MDD), la depresión postnatal, distimia, depresión asociada con la enfermedad de Alzheimer, enfermedad de Parkinson, o psicosis, parálisis supranuclear, trastornos de la alimentación, la obesidad, la anorexia nerviosa, la bulimia nerviosa, el trastorno por atracón, la diabetes, las enfermedades isquémicas, dolor, trastornos de abuso de sustancias, dependencias químicas, la adicción a la nicotina, adicción a la cocaína, adicción a las anfetaminas, adicción al alcohol, síndrome de Lesch-Nyhan, enfermedades neurodegenerativas,
    50 enfermedad de Parkinson, el síndrome de la fase lútea tardía o la narcolepsia, los síntomas psiquiátricos, la ira, la
    34
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ES10775425.1T 2009-05-12 2010-05-11 Formas cristalinas de (S)-7-([1,2,4]triazol[1,5-a]piridin-6-il)-4-(3,4-diclorofenil)-1,2,3,4-tetrahidroisoquinolina y sus usos Active ES2528404T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17748609P 2009-05-12 2009-05-12
US177486P 2009-05-12
PCT/US2010/034428 WO2010132487A1 (en) 2009-05-12 2010-05-11 CRYSTALLINE FORMS OF (S)-7-([1,2,4]TRIAZOLO[1,5-a]PYRIDIN-6-YL)-4-(3,4-DICHLOROHPHENYL)-1,2,3,4-TETRAHYDROISOQUINOLINE AND USE THEREOF

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Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101389246B1 (ko) 2004-07-15 2014-04-24 브리스톨-마이어스스퀴브컴파니 아릴- 및 헤테로아릴-치환된 테트라히드로이소퀴놀린, 및 이것의 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
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
ES2446971T3 (es) 2009-05-12 2014-03-11 Albany Molecular Research, Inc. Tetrahidroisoquinolinas sustituidas con arilo, heteroarilo, y heterociclo y su uso
ES2528404T3 (es) 2009-05-12 2015-02-10 Bristol-Myers Squibb Company Formas cristalinas de (S)-7-([1,2,4]triazol[1,5-a]piridin-6-il)-4-(3,4-diclorofenil)-1,2,3,4-tetrahidroisoquinolina y sus usos
AU2010247763B2 (en) * 2009-05-12 2015-12-24 Albany Molecular Research, Inc. 7-([1,2,4,]triazolo[1,5,-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4- tetrahydroisoquinoline and use thereof
EP2606049A4 (en) 2010-08-17 2014-01-08 Albany Molecular Res Inc 2,5-METHANO- AND 2,5-ETHANO-TETRAHYDROBENZAZEPINE DERIVATIVES AND USES THEREOF FOR BLOCKING NOREPINEPHRINE, DOPAMINE, AND SEROTONIN REUPTAKE
GB201315846D0 (en) 2013-09-05 2013-10-23 Imp Innovations Ltd Method for treating or preventing hot flushes
KR102629310B1 (ko) * 2015-03-09 2024-01-24 더블유.알. 그레이스 앤드 캄파니-콘. 니코틴아미드 리보사이드의 결정 형태
WO2019126482A1 (en) 2017-12-22 2019-06-27 Elysium Health, Inc. Crystalline forms of nicotinamide riboside chloride
CN115304595A (zh) * 2020-01-10 2022-11-08 康圣博施医药有限公司 药物的治疗组合以及其使用方法

Family Cites Families (305)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3155669A (en) 1962-06-22 1964-11-03 Res Lab Dr C Janssen N V 2, 4, 8-triaza-spiro (4, 5) dec-2-enes
US3155670A (en) 1962-06-22 1964-11-03 Res Lab Dr C Janssen N V 1-oxo-2, 4, 8, triaza-spiro (4, 5) decanes
CH527194A (de) 1970-01-06 1972-08-31 Hoffmann La Roche Verfahren zur Herstellung von Isochinolin-Derivaten
US3947456A (en) * 1970-01-06 1976-03-30 Hoffman-La Roche Inc. Substituted 4-phenyl isoquinolines
US3666763A (en) * 1970-01-06 1972-05-30 Hoffmann La Roche 4-phenyl isoquinolines and process for preparing same
GB1504424A (en) 1975-08-09 1978-03-22 Beecham Group Ltd Isoquinoline-derived aminoethers
US4340600A (en) * 1980-05-22 1982-07-20 Smithkline Corporation Renal dilating methods and compositions using 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinolines
US4535186A (en) 1983-04-19 1985-08-13 American Home Products Corporation 2-Phenyl-2-(1-hydroxycycloalkyl or 1-hydroxycycloalk-2-enyl)ethylamine derivatives
DE3333994A1 (de) * 1983-09-21 1985-04-04 Troponwerke GmbH & Co KG, 5000 Köln Neue pyridoindolderivate, verfahren zu ihrer herstellung und ihre verwendung
US4843071A (en) 1986-12-05 1989-06-27 Serotonin Industries Of Charleston Method and composition for treating obesity, drug abuse, and narcolepsy
KR880007433A (ko) 1986-12-22 1988-08-27 메리 앤 터커 3-아릴옥시-3-치환된 프로판아민
ZA885824B (en) * 1987-08-14 1989-04-26 Merrell Dow Pharma Novel antidepressants
EP0360390A1 (en) 1988-07-25 1990-03-28 Glaxo Group Limited Spirolactam derivatives
MX18467A (es) 1988-11-23 1993-07-01 Pfizer Agentes terapeuticos de quinuclidinas
FI895821A7 (fi) 1988-12-07 1990-06-08 The Wellcome Foundation Ltd Farmaseuttisesti aktivisia CNS-yhdisteitä
US4902710A (en) * 1988-12-14 1990-02-20 Eli Lilly And Company Serotonin and norepinephrine uptake inhibitors
US5114976A (en) * 1989-01-06 1992-05-19 Norden Michael J Method for treating certain psychiatric disorders and certain psychiatric symptoms
GB8909209D0 (en) 1989-04-22 1989-06-07 Wyeth John & Brother Ltd Piperazine derivatives
EP0380223A1 (en) 1989-01-17 1990-08-01 Konica Corporation Colour filter and process for producing the same
BG49761A1 (en) 1989-04-24 1992-02-14 Vissh Khim T I 4- (4'- chalophenyl)- 2- methyl- 1, 2, 3, 4- tetrahydroisohinolines and method for its preparation
US5164372A (en) 1989-04-28 1992-11-17 Fujisawa Pharmaceutical Company, Ltd. Peptide compounds having substance p antagonism, processes for preparation thereof and pharmaceutical composition comprising the same
AU6368090A (en) 1989-10-03 1991-04-11 Warner-Lambert Company Substituted carboxytetrahydroisoquinolines and derivatives thereof having pharmaceutical activity
IE903957A1 (en) 1989-11-06 1991-05-08 Sanofi Sa Aromatic amine compounds, their method of preparation and¹pharmaceutical compositions in which they are present
FR2654725B1 (fr) 1989-11-23 1992-02-14 Rhone Poulenc Sante Nouveaux derives de l'isoindolone, leur preparation et les compositions pharmaceutiques qui les contiennent.
FR2654726B1 (fr) 1989-11-23 1992-02-14 Rhone Poulenc Sante Nouveaux derives de l'isoindolone et leur preparation.
GB8929070D0 (en) 1989-12-22 1990-02-28 Fujisawa Pharmaceutical Co Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same
US5232929A (en) 1990-11-28 1993-08-03 Pfizer Inc. 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use
WO1991009844A1 (en) 1990-01-04 1991-07-11 Pfizer Inc. Substance p antagonists
WO1991012266A1 (fr) 1990-02-15 1991-08-22 Fujisawa Pharmaceutical Co., Ltd. Compose peptidique
US5447947A (en) * 1990-02-26 1995-09-05 Arc 1 Compositions and methods of treatment of sympathetically maintained pain
AU648317B2 (en) 1990-06-01 1994-04-21 Pfizer Inc. 3-amino-2-aryl quinuclidines, process for their preparation and pharmaceutical compositions containing them
CA2086434C (en) 1990-07-23 1998-09-22 John A. Lowe, Iii Quinuclidine derivatives
ES2071334T3 (es) 1990-09-28 1995-06-16 Pfizer Analogos de anillos fusionados de nitrogeno conteniendo heterociclos no aromaticos.
GB9023116D0 (en) 1990-10-24 1990-12-05 Fujisawa Pharmaceutical Co Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same
JPH04193867A (ja) 1990-11-23 1992-07-13 Nippon Shinyaku Co Ltd イソキノリノール誘導体及び医薬
EP0498069B1 (en) 1990-12-21 1995-10-25 Fujisawa Pharmaceutical Co., Ltd. New use of peptide derivative
EP0566589A1 (en) 1991-01-10 1993-10-27 Pfizer Inc. N-alkyl quinuclidinium salts as substance p antagonists
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.
SK284185B6 (sk) 1991-03-26 2004-10-05 Pfizer Inc. Spôsob prípravy substituovaných piperidínov
FR2677361A1 (fr) 1991-06-04 1992-12-11 Adir Nouveaux peptides et pseudopeptides, derives de tachykinines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
FR2676053B1 (fr) 1991-05-03 1993-08-27 Sanofi Elf Nouveaux composes dialkylenepiperidino et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2676055B1 (fr) 1991-05-03 1993-09-03 Sanofi Elf Composes polycycliques amines et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2676447B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives du thiopyranopyrrole et leur preparation.
FR2676443B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole et leur preparation.
FR2676446B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives du thiopyranopyrrole, leur preparation et les compositions pharmaceutiques qui les contiennent.
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.
WO1992020661A1 (en) 1991-05-22 1992-11-26 Merck & Co., Inc. N, n-diacylpiperazines
FI935134L (fi) 1991-05-22 1993-11-19 Pfizer Substituerade 3-aminokinuklidiner
DE9290063U1 (de) 1991-05-31 1994-02-24 Pfizer Inc., New York, N.Y. Chinuclidin-Derivate
GB9113219D0 (en) 1991-06-19 1991-08-07 Fujisawa Pharmaceutical Co Peptide compound,processes for preparation thereof and pharmaceutical composition comprising the same
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 (es) 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
JPH06509087A (ja) 1991-07-05 1994-10-13 メルク　シヤープ　エンド　ドーム　リミテツド 芳香族化合物、それらを含む医薬組成物、及び治療におけるそれらの使用
EP0593557B1 (en) 1991-07-05 1996-01-31 MERCK SHARP & DOHME LTD. Aromatic compounds, pharmaceutical compositions containing them and their use in therapy
WO1993001159A1 (en) 1991-07-10 1993-01-21 Merck Sharp & Dohme Limited Fused tricyclic compounds, pharmaceutical compositions containing them and their use in therapy
EP0593615B1 (en) 1991-07-10 1996-01-31 MERCK SHARP & DOHME LTD. Aromatic compounds, compositions containing them and their use in therapy
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
WO1993006099A1 (en) 1991-09-16 1993-04-01 Pfizer Inc. Fused tricyclic nitrogen containing heterocycles as substance p receptor antagonists
ATE195867T1 (de) 1991-09-20 2000-09-15 Glaxo Group Ltd Neue medizinische indikation für tachykinin- antagonisten
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
FI942187L (fi) 1991-11-12 1994-05-11 Pfizer Asyklisiä etyleenidiamiinijohdannaisia aine P-reseptoriantagonisteina
CA2083891A1 (en) 1991-12-03 1993-06-04 Angus Murray Macleod Heterocyclic compounds, compositions containing them and their use in therapy
GB9200535D0 (en) 1992-01-10 1992-02-26 Fujisawa Pharmaceutical Co New compound
GB9201179D0 (en) 1992-01-21 1992-03-11 Glaxo Group Ltd Chemical compounds
US5241065A (en) * 1992-02-25 1993-08-31 Schering Corporation 2,3,4,5-tetrahydro-1h-3-benzazepines having anti-psychotic activity
US5328927A (en) 1992-03-03 1994-07-12 Merck Sharpe & Dohme, Ltd. Hetercyclic compounds, processes for their preparation and pharmaceutical compositions containing them
US5595872A (en) * 1992-03-06 1997-01-21 Bristol-Myers Squibb Company Nucleic acids encoding microsomal trigyceride transfer protein
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
FR2689888B1 (fr) 1992-04-10 1994-06-10 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent.
EP0636130A1 (en) 1992-04-15 1995-02-01 Merck Sharp & Dohme Ltd. Azacyclic compounds
GB2266529A (en) 1992-05-01 1993-11-03 Merck Sharp & Dohme Tetrahydroisoquinoline derivatives
ES2164657T3 (es) 1992-05-18 2002-03-01 Pfizer Derivados aza-biciclicos puenteados como antagonistas de la sustancia p.
GB9211193D0 (en) 1992-05-27 1992-07-08 Merck Sharp & Dohme Therapeutic agents
US5637699A (en) 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
CA2099233A1 (en) 1992-06-29 1993-12-30 Conrad P. Dorn Morpholine and thiomorpholine tachykinin receptor antagonists
AU4713293A (en) 1992-07-13 1994-01-31 Merck Sharp & Dohme Limited Heterocyclic amide derivatives as tachykinin derivatives
JPH07509133A (ja) 1992-07-17 1995-10-12 リボザイム・ファーマシューティカルズ・インコーポレイテッド 動物疾患の処置のための方法および剤
GB2268931A (en) 1992-07-22 1994-01-26 Merck Sharp & Dohme Azabicyclic tachykinin-receptor antagonists
EP0652866B1 (en) 1992-07-28 1998-11-25 MERCK SHARP & DOHME LTD. Azacyclic compounds
GB2269170A (en) 1992-07-29 1994-02-02 Merck Sharp & Dohme Azatricyclic tachykinin antagonists
AU4718093A (en) 1992-07-31 1994-03-03 Merck Sharp & Dohme Limited Substituted amines as tachykinin receptor antagonists
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
CA2140640A1 (en) 1992-08-13 1994-03-03 David C. Horwell Tachykinin antagonists
US5212185A (en) * 1992-08-14 1993-05-18 G. D. Searle & Co. Piperidinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
ATE208376T1 (de) 1992-08-19 2001-11-15 Pfizer Substituierte benzylamin-stickstoff enthaltende nichtaromatische heterocyclen
US5387595A (en) 1992-08-26 1995-02-07 Merck & Co., Inc. Alicyclic compounds as tachykinin receptor antagonists
NO179904C (no) 1992-09-04 1997-01-08 Takeda Chemical Industries Ltd Kondenserte heterocykliske forbindelser og deres anvendelse
AU4973693A (en) 1992-09-10 1994-03-29 Merck Sharp & Dohme Limited Alcohols and ethers with aromatic substituents as tachykinin-antagonists
GB9220286D0 (en) 1992-09-25 1992-11-11 Merck Sharp & Dohme Therapeutic agents
GB2271566A (en) 1992-10-14 1994-04-20 Merck & Co Inc HIV integrase inhibitors
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
GB9222262D0 (en) 1992-10-23 1992-12-09 Merck Sharp & Dohme Therapeutic agents
GB9222486D0 (en) 1992-10-26 1992-12-09 Merck Sharp & Dohme Therapeutic agents
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
AU678409B2 (en) 1992-10-28 1997-05-29 Merck Sharp & Dohme Limited 4-arylmethyloxymethyl piperidines as tachykinin antagonists
AU5342894A (en) 1992-10-30 1994-05-24 Merck Sharp & Dohme Limited Tachykinin antagonists
ATE147385T1 (de) 1992-11-12 1997-01-15 Pfizer Chinuclidin derivat als substanz p antagonist
US5261188A (en) 1992-11-23 1993-11-16 The Standard Products Company Belt weatherstrip with bulb
JPH06153997A (ja) 1992-11-27 1994-06-03 Canon Inc 検出信号増幅による標的核酸の検出方法
DK0675886T3 (da) 1992-12-10 2000-09-18 Pfizer Aminomethylensubstituerede ikke-aromatiske heterocykler og deres anvendelse som substance P-antagonister
JPH08504435A (ja) 1992-12-14 1996-05-14 メルク シヤープ エンド ドーム リミテツド タキキニン受容体拮抗剤としての４−アミノメチル／チオメチル／スルホニルメチル−４−フェニルピペリジン
GB9226581D0 (en) 1992-12-21 1993-02-17 Merck Sharp & Dohme Therapeutic agents
DK154192D0 (da) * 1992-12-23 1992-12-23 Neurosearch As Heterocycliske forbindelser
GB9300051D0 (en) 1993-01-04 1993-03-03 Merck Sharp & Dohme Therapeutic agents
US5466689A (en) 1993-02-08 1995-11-14 Takeda Chemical Industries, Ltd. Morpholine derivatives and their use
JPH08506823A (ja) 1993-02-18 1996-07-23 メルク シヤープ エンド ドーム リミテツド アザ環式化合物、該化合物を含む組成物及びタキキニン拮抗剤としての該化合物の使用
US5674889A (en) 1993-02-22 1997-10-07 Merck, Sharp & Dohme, Ltd. Aromatic compounds, compositions containing them and their use in therapy
DE69318854T2 (de) 1993-03-04 1998-10-08 Pfizer Spiroazacyclischderivate als substanz p antagonisten
EP0650476B1 (en) * 1993-04-07 2002-06-26 Otsuka Pharmaceutical Co., Ltd. Peripheral vasodilating agent containing n-acylated 4-amino piperidine derivatives as active ingredients
US5496833A (en) 1993-04-13 1996-03-05 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
DK0696280T3 (da) 1993-05-06 1998-01-12 Merrell Pharma Inc Substituerede pyrrolidin-3-yl-alkyl-piperidiner anvendelige som tachykinin-antagonister
IL109646A0 (en) 1993-05-19 1994-08-26 Pfizer Heteroatom substituted alkyl benzylamino-quinuclidines
EP0702681A1 (en) 1993-06-07 1996-03-27 Merck & Co. Inc. Spiro-substituted azacycles as neurokinin antagonists
EP0634402A1 (en) 1993-07-14 1995-01-18 Takeda Chemical Industries, Ltd. Isochinolinone derivatives, their production and use
US5869499A (en) 1993-07-15 1999-02-09 Pfizer Inc Benzyloxyquinuclidines as substance P antagonists
GB9315808D0 (en) 1993-07-30 1993-09-15 Merck Sharp & Dohme Therapeutic agents
TW365603B (en) 1993-07-30 1999-08-01 Rhone Poulenc Rorer Sa Novel perhydroisoindole derivatives, their preparation and pharmaceutical compositions which contain them
GB9317987D0 (en) 1993-08-26 1993-10-13 Glaxo Group Ltd Chemical compounds
EP1209157A1 (en) 1993-09-17 2002-05-29 Pfizer Inc. Heteroarylamino and heteroarylsulfonamido substituted 3-benzylaminomethyl piperidines and related compounds
WO1995007886A1 (en) 1993-09-17 1995-03-23 Pfizer Inc. 3-amino-5-carboxy-substituted piperidines and 3-amino-4-carboxy-substituted pyrrolidines as tachykinin antagonists
IL111002A (en) 1993-09-22 1998-09-24 Glaxo Group Ltd Piperidine derivatives their preparation and pharmaceutical compositions containing them
WO1995011880A1 (en) 1993-10-27 1995-05-04 Merck Sharp & Dohme Limited Substituted amides as tachykinin antagonists
US6403577B1 (en) 1993-11-17 2002-06-11 Eli Lilly And Company Hexamethyleneiminyl tachykinin receptor antagonists
IT1271462B (it) 1993-12-03 1997-05-28 Menarini Farma Ind Antagonisti delle tachichinine,procedimento per la loro preparazione e loro impiego in formulazioni farmaceutiche.
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
JPH09506898A (ja) 1993-12-21 1997-07-08 イーライ・リリー・アンド・カンパニー 非ペプチドタキキニン受容体アンタゴニスト
AU699465B2 (en) 1993-12-29 1998-12-03 Pfizer Inc. Diazabicyclic neurokinin antagonists
CN1067683C (zh) 1993-12-29 2001-06-27 默克·夏普-道姆公司 取代的吗啉衍生物及其作为治疗剂的用途
DE69504300T2 (de) 1994-01-13 1999-04-29 Merck Sharp & Dohme Ltd., Hoddesdon, Hertfordshire Gem-bissubstituierte azazyclische tachykinin-antagonisten
US5728716A (en) 1994-01-28 1998-03-17 Merck Sharp & Dohme Limited Aralkylamino substituted azacyclic therapeutic agents
GB9402688D0 (en) 1994-02-11 1994-04-06 Merck Sharp & Dohme 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
FR2718136B1 (fr) 1994-03-29 1996-06-21 Sanofi Sa Composés aromatiques aminés, procédé pour leur obtention et compositions pharmaceutiques les contenant.
US5610145A (en) 1994-04-15 1997-03-11 Warner-Lambert Company Tachykinin antagonists
US5607939A (en) * 1994-04-28 1997-03-04 Takeda Chemical Industries, Ltd. Condensed heterocyclic compounds, their production and use
PE27997A1 (es) 1994-04-29 1997-09-20 Lilly Co Eli Antagonistas de receptores de taquicininas
US5747491A (en) 1994-05-05 1998-05-05 Merck Sharp & Dohme Ltd. Morpholine derivatives and their use as antagonists of tachikinins
PL317127A1 (en) 1994-05-07 1997-03-17 Boehringer Ingelheim Kg Novel derivatives of amino acids, method of obtaining them and pharmaceutic agents containing such derivatives
WO1995033744A1 (en) 1994-06-06 1995-12-14 Warner-Lambert Company Tachykinin (nk1) receptor antagonists
CA2150992A1 (en) 1994-06-10 1995-12-11 Philip Arthur Hipskind Cyclohexyl tachykinin receptor antagonists
CA2134038C (en) * 1994-06-16 1997-06-03 David Taiwai Wong Potentiation of drug response
RU2151769C1 (ru) 1994-07-12 2000-06-27 Эли Лилли Энд Компани Тригидрат дигидрохлорида (r)-3-(1н-индол-3-ил)-1-[n-(2-метоксибензил)ацетиламино]-2-[n-(2-(4-(пиперидин-1-ил)пиперидин-1-ил)ацетил)амино]пропана и фармацевтический состав
PL318298A1 (en) * 1994-07-20 1997-06-09 Byk Gulden Lomberg Chem Fab Thiopyridil compounds for fighting against heliobacter
CA2154116A1 (en) 1994-07-22 1996-01-23 Philip Arthur Hipskind 1-aryl-2-acetamidopentanone derivatives for use as tachykinin receptor antagonists
GB9415997D0 (en) 1994-08-08 1994-09-28 Merck Sharp & Dohme Therapeutic agents
GB9415996D0 (en) 1994-08-08 1994-09-28 Merck Sharp & Dohme Therapeutic agents
TW432061B (en) 1994-08-09 2001-05-01 Pfizer Res & Dev Lactams
ES2157337T3 (es) 1994-08-15 2001-08-16 Merck Sharp & Dohme Derivados de morfolina y su uso como agentes terapeuticos.
ES2132709T3 (es) 1994-08-25 1999-08-16 Merrell Pharma Inc Nuevas piperidinas substituidas utiles para el tratamiento de las enfermedades alergicas.
EP0699655B1 (en) 1994-08-29 1997-09-24 Akzo Nobel N.V. Process for the preparation of quaternary diesters
GB9417956D0 (en) 1994-09-02 1994-10-26 Merck Sharp & Dohme Therapeutic agents
GB9418545D0 (en) 1994-09-15 1994-11-02 Merck Sharp & Dohme Therapeutic agents
US5457107A (en) 1994-09-16 1995-10-10 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
ATE212981T1 (de) 1994-09-30 2002-02-15 Novartis Erfind Verwalt Gmbh 1-acyl-4-aliphatische aminopiperidin verbindungen
TW397825B (en) 1994-10-14 2000-07-11 Novartis Ag Aroyl-piperidine derivatives
FR2725986B1 (fr) 1994-10-21 1996-11-29 Adir Nouveaux derives de piperidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP0709375B1 (en) 1994-10-25 2005-05-18 AstraZeneca AB Therapeutic heterocycles
GB9421709D0 (en) 1994-10-27 1994-12-14 Zeneca Ltd Therapeutic compounds
CA2162786A1 (en) 1994-11-22 1996-05-23 Philip Arthur Hipskind Heterocyclic tachykinin receptor antagonists
FR2727411B1 (fr) 1994-11-30 1997-01-03 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent
PE38997A1 (es) 1994-12-13 1997-10-02 Novartis Ag Antagonista de taquicinina
GB9426103D0 (en) 1994-12-23 1995-02-22 Merck Sharp & Dohme Therapeutic agents
ATE279406T1 (de) 1995-01-12 2004-10-15 Glaxo Group Ltd Piperidinderivate mit tachykinin-antagonistischer wirkung
FR2729951B1 (fr) 1995-01-30 1997-04-18 Sanofi Sa Nouveaux composes heterocycliques, procede pour leur preparation et compositions pharmaceutiques en contenant
GB9505491D0 (en) 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
GB9505492D0 (en) 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
US5554641A (en) 1995-03-20 1996-09-10 Horwell; David C. Nonpeptides as tachykinin antagonists
GB9505692D0 (en) 1995-03-21 1995-05-10 Glaxo Group Ltd Chemical compounds
DE69628484T2 (de) 1995-03-24 2004-05-19 Takeda Chemical Industries, Ltd. Zyklische Verbindungen, ihre Herstellung und ihre Verwendung als Tachykininrezeptorantagonisten
US5565568A (en) 1995-04-06 1996-10-15 Eli Lilly And Company 2-acylaminopropanamides as tachykinin receptor antagonists
CA2217006C (en) 1995-04-13 2001-05-22 Hoechst Marion Roussel, Inc. Novel substituted piperazine derivatives having tachykinin receptor antagonists activity
EP0846116A1 (en) 1995-05-25 1998-06-10 Fujisawa Pharmaceutical Co., Ltd. 1-benzoyl-2-(indolyl-3-alkyl)-piperazine derivatives as neurokinin receptor antagonists
US5654316A (en) * 1995-06-06 1997-08-05 Schering Corporation Piperidine derivatives as neurokinin antagonists
DE19520964A1 (de) 1995-06-08 1996-12-12 Inst Neue Mat Gemein Gmbh Beschichtete anorganische Pigmente, Verfahren zu deren Herstellung und deren Verwendung
US5817832A (en) * 1995-06-22 1998-10-06 Ciba Specialty Chemicals Corporation Blue diketopyrrolopyrrole pigments
GB9513117D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513118D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513121D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
MX9800187A (es) 1995-07-07 1998-05-31 Pfizer Compuestos de benzolactama substituidos como antagonistas de la substancia p.
TW340842B (en) 1995-08-24 1998-09-21 Pfizer Substituted benzylaminopiperidine compounds
WO1997014671A1 (en) 1995-10-18 1997-04-24 Merck & Co., Inc. Cyclopentyl tachykinin receptor antagonists
DE19541283A1 (de) 1995-11-06 1997-05-07 Boehringer Ingelheim Kg Neue Aminosäurederivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
GB9523244D0 (en) 1995-11-14 1996-01-17 Merck Sharp & Dohme Therapeutic agents
JP2000500760A (ja) 1995-11-23 2000-01-25 メルク シヤープ エンド ドーム リミテツド スピロピペリジン誘導体およびタキキニン拮抗薬としてのその使用
GB9524157D0 (en) 1995-11-25 1996-01-24 Pfizer Ltd Therapeutic agents
HU224225B1 (hu) 1995-12-01 2005-06-28 Sankyo Co. Ltd. Tachikinin receptor antagonista hatású heterociklusos vegyületek, ezek előállítási eljárása és alkalmazásuk gyógyszerkészítmények előállítására
GB9525296D0 (en) 1995-12-11 1996-02-07 Merck Sharp & Dohme Therapeutic agents
ZA9610738B (en) 1995-12-22 1997-06-24 Warner Lambert Co Subtype selective nmda receptor ligands and the use thereof
US6025355A (en) * 1997-05-19 2000-02-15 Cambridge Neuroscience, Inc. Pharmaceutically active compounds and methods of use
UA49872C2 (uk) 1996-02-22 2002-10-15 Н'Юросерч А/С Похідні тропану, спосіб їх одержання, фармацевтична композиція та спосіб лікування
JP2000507955A (ja) 1996-04-03 2000-06-27 メルク エンド カンパニー インコーポレーテッド ファルネシル―タンパク質転移酵素の阻害剤
US5827875A (en) * 1996-05-10 1998-10-27 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
US5885983A (en) 1996-05-10 1999-03-23 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
AU722541B2 (en) 1996-06-21 2000-08-03 Merck Sharp & Dohme Limited Spiro-piperidine derivatives and their use as therapeutic agents
DE19638484A1 (de) * 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
DE19638486A1 (de) * 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
WO1998035939A1 (en) 1997-02-18 1998-08-20 Sanwa Kagaku Kenkyusho Co., Ltd. Malonic diamide derivatives and use thereof
US5907041A (en) 1997-03-12 1999-05-25 Rhone-Poulenc Inc. Process for preparing pyrazole derivatives
JPH10292008A (ja) 1997-04-21 1998-11-04 Grand Polymer:Kk α−オレフィンの重合方法
DK1021404T3 (da) * 1997-10-07 2003-03-24 Boehringer Ingelheim Ca Ltd Azetidinonderivater til behandling af HCMV-infektioner
DE69810800T2 (de) * 1997-10-07 2003-09-18 Boehringer Ingelheim (Canada) Ltd., Laval Azetidinonderivate zur behandlung von hcmv entzündungen
US7041702B1 (en) * 1997-10-21 2006-05-09 Scion Pharmaceuticals, Inc. Pharmaceutically active compounds and methods of use
US6121261A (en) 1997-11-19 2000-09-19 Merck & Co., Inc. Method for treating attention deficit disorder
US6943159B1 (en) * 1998-02-18 2005-09-13 Neurosearch A/S Compounds and their use as positive AMPA receptor modulators
US6043253A (en) * 1998-03-03 2000-03-28 Merck & Co., Inc. Fused piperidine substituted arylsulfonamides as β3-agonists
AU756373B2 (en) 1998-04-09 2003-01-09 Pharmacia & Upjohn Company New treatments for nervous disorders
AU5907399A (en) 1998-09-04 2000-03-27 Ciba Specialty Chemicals Holding Inc. Process for making 2,4-dihydroxyphenyl and 2-hydroxy-4-alkoxyphenyl substituted triazine compounds
JP2000186110A (ja) 1998-12-21 2000-07-04 Ube Ind Ltd エチレン共重合体の製造方法
US6664293B2 (en) * 1999-02-26 2003-12-16 Fujiwawa Pharmaceutical Co., Ltd. Amide compounds for the potentiation of cholinergic activity
US6586447B1 (en) * 1999-04-01 2003-07-01 Pfizer Inc 3,3-disubstituted-oxindole derivatives useful as anticancer agents
JP2001026580A (ja) 1999-05-10 2001-01-30 Sumitomo Chem Co Ltd 光学活性１−アリール−１，２，３，４−テトラヒドロイソキノリン類の製造法
US6562836B1 (en) * 1999-05-24 2003-05-13 Queen's University Of Kingston Methods and compounds for inhibiting amyloid deposits
EP1106605A4 (en) * 1999-06-24 2005-12-07 Toray Industries ANTAGONISTS OF THE ADRENERGIC RECEPTOR-ALPHA1B
WO2001003680A2 (en) * 1999-07-09 2001-01-18 Isis Innovation Limited Compounds for inhibiting diseases and preparing cells for transplantation
US6340681B1 (en) * 1999-07-16 2002-01-22 Pfizer Inc 2-benzimidazolylamine compounds as ORL-1-receptor agonists
US6410736B1 (en) 1999-11-29 2002-06-25 Pfizer Inc. Biaryl ether derivatives useful as monoamine reuptake inhibitors
US7163949B1 (en) * 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
DK1246806T3 (da) * 1999-11-03 2008-06-16 Amr Technology Inc Aryl- og heteroarylsubstituerede tetrahydroisoquinoliner og anvendelse deraf til blokering af genoptagelse af norepinefrin, dopsmin og serotonin
AU784280B2 (en) 1999-11-03 2006-03-02 Albany Molecular Research, Inc. 4-phenyl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
WO2001070728A1 (en) 2000-03-23 2001-09-27 Sanofi-Synthelabo 2-[nitrogen-heterocyclic]pyrimidone derivatives
WO2001087844A1 (en) * 2000-05-15 2001-11-22 Darwin Discovery Limited Hydroxamic and carboxylic acid derivatives having mmp and tnf inhibitory activity
WO2002004455A2 (en) * 2000-07-11 2002-01-17 Albany Molecular Research, Inc 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
JP2004515494A (ja) * 2000-12-07 2004-05-27 アストラゼネカ・アクチエボラーグ 治療剤
US6506772B1 (en) * 2000-12-15 2003-01-14 Hoffmann-La Roche Inc. Substituted [1,2,4]triazolo[1,5a]pyridine derivatives with activity as adenosine receptor ligands
US6900220B2 (en) * 2001-01-02 2005-05-31 Syntex (U.S.A.) Llc Quinazolone derivatives as alpha 1A/B adrenergic receptor antagonists
JP2002281203A (ja) 2001-03-19 2002-09-27 Canon Inc 蓋付き電子機器
US6635675B2 (en) 2001-11-05 2003-10-21 Cypress Bioscience, Inc. Method of treating chronic fatigue syndrome
US6911453B2 (en) * 2001-12-05 2005-06-28 Aventis Pharma Deutschland Gmbh Substituted 4-phenyltetrahydroisoquinolinium, process for their preparation, their use as a medicament, and medicament containing them
US6974803B2 (en) * 2001-12-06 2005-12-13 Pfizer Inc Pharmaceutical combination
AU2002360561A1 (en) 2001-12-11 2003-06-23 Sepracor, Inc. 4-substituted piperidines, and methods of use thereof
US6703405B2 (en) * 2001-12-22 2004-03-09 Aventis Pharma Deutschland Gmbh Substituted 4-phenyltetrahydroisoquinolinium salts, process for their preparation, their use as a medicament, and medicament containing them
US20050113283A1 (en) * 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 receptor
US20050261298A1 (en) * 2002-01-18 2005-11-24 David Solow-Cordero Methods of treating conditions associated with an Edg-7 receptor
EP1676844A1 (en) * 2004-12-28 2006-07-05 Laboratorios Del Dr. Esteve, S.A. 5-HT7 receptor antagonists
CA2478909A1 (en) * 2002-03-13 2003-09-25 Duane D. Miller Substituted tetrahydroisoquinoline compounds, methods of making, and their use
DK1513529T3 (da) 2002-05-30 2012-03-26 Neurosearch As Tredobbelte monoamin-genoptagelsesinhibitorer til behandling af kronisk smerte
MXPA05001784A (es) * 2002-08-13 2005-04-25 Warner Lambert Co Derivados de isoquinolina como inhibidores de metaloproteinasa de matriz.
WO2004014866A1 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Azaisoquinoline derivatives as matrix metalloproteinase inhibitors
US6919376B2 (en) * 2002-09-20 2005-07-19 Medisyn Technologies, Inc. Therapeutic agents and corresponding treatments
ES2337043T3 (es) * 2002-10-16 2010-04-20 Isis Innovation Limited Metodos de escrutinio empleando un modelo estructural de fih.
GB0224557D0 (en) * 2002-10-22 2002-11-27 Glaxo Group Ltd Novel compounds
WO2004050630A1 (en) * 2002-12-02 2004-06-17 Pharmacia & Upjohn Company Llc The use of aryl- and heteroaryl-substituted tetrahydroisoquinolines in the treatment of chronic and neuropathic pain, migraine headaches, and urge, stress and mixed urinary incontinence
CA2505783A1 (en) * 2002-12-02 2004-06-17 Pharmacia & Upjohn Company Llc The use of 4-phenyl-substituted tetrahydroisoquinolines in the treatment of pain, migraine headaches and urinary incontinence
DE10303254B3 (de) 2003-01-28 2004-09-23 Johannes-Gutenberg-Universität Mainz 3,3-Dimethyl-8-oxoisochinoline, Verfahren zu ihrer Herstellung, sie enthaltende pharmazeutische Zusammensetzungen und deren Verwendung
JP2006516573A (ja) * 2003-01-31 2006-07-06 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての３−アミノ−４−フェニルブタン酸誘導体
US7241775B2 (en) * 2003-03-24 2007-07-10 Sanofi-Aventis Deutschland Gmbh Composition, process of making, and medical use of substituted 4-phenyltetrahydroisoquinolines
WO2004096774A1 (en) 2003-05-01 2004-11-11 Glaxo Group Limited Acyl isoindoline derivatives and acyl isoquinoline derivatives as anti-viral agents
US7459460B2 (en) * 2003-05-28 2008-12-02 Bristol-Myers Squibb Company Trisubstituted heteroaromatic compounds as calcium sensing receptor modulators
WO2005002672A2 (en) 2003-07-01 2005-01-13 President And Fellows Of Harvard College Sirt1 modulators for manipulating cells/organism lifespan/stress response
US7501538B2 (en) * 2003-08-08 2009-03-10 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
CA2538864C (en) 2003-09-17 2013-05-07 The Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services Thalidomide analogs as tnf-alpha modulators
US7491794B2 (en) * 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
JP2007008816A (ja) 2003-10-15 2007-01-18 Ube Ind Ltd 新規イソキノリン誘導体
ES2299906T3 (es) * 2003-11-25 2008-06-01 Eli Lilly And Company Moduladores de receptores activados por proliferadores de peroxisomas.
AU2004312072B2 (en) * 2003-12-29 2011-06-23 President And Fellows Of Harvard College Compositions for treating or preventing obesity and insulin resistance disorders
BRPI0507839A (pt) * 2004-02-18 2007-05-08 Pfizer Prod Inc derivados tetraidroisoquinolinil de quinazolina e isoquinolina
CA2559611C (en) 2004-03-09 2012-01-17 National Health Research Institutes Pyrrolidine compounds
EP1749007A2 (en) 2004-03-30 2007-02-07 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
JP4991527B2 (ja) 2004-06-01 2012-08-01 ユニバーシティ オブ バージニア パテント ファンデーション 二つの部分からなる低分子量の癌および血管新生の抑制剤
WO2006004722A2 (en) * 2004-06-30 2006-01-12 Biomol Research Laboratories, Inc. Compositions and methods for selectively activating human sirtuins
KR101389246B1 (ko) * 2004-07-15 2014-04-24 브리스톨-마이어스스퀴브컴파니 아릴- 및 헤테로아릴-치환된 테트라히드로이소퀴놀린, 및 이것의 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
CN103251953A (zh) 2004-07-19 2013-08-21 约翰·霍普金斯大学 供免疫抑制的flt3抑制剂
US7211585B2 (en) * 2004-08-18 2007-05-01 Laboratorios Del Dr. Esteve, S.A. 5-HT7 receptor antagonists
US7211584B2 (en) * 2004-08-18 2007-05-01 Laboratorios Del Dr. Esteve, S.A. 5-HT7 receptor ligands
DE102004046492A1 (de) 2004-09-23 2006-03-30 Sanofi-Aventis Deutschland Gmbh Substituierte 4-Phenyltetrahydroisochinoline, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, sowie sie enthaltendes Medikament
US20060111385A1 (en) 2004-11-22 2006-05-25 Molino Bruce F Novel 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
US20060111394A1 (en) * 2004-11-22 2006-05-25 Molino Bruce F Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
US20060111393A1 (en) * 2004-11-22 2006-05-25 Molino Bruce F 4-Phenyl substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
CA2592353A1 (en) * 2004-12-17 2006-06-22 Janssen Pharmaceutica, N.V. Tetrahydroisoquinoline compounds for treatment of cns disorders
US20070060589A1 (en) * 2004-12-21 2007-03-15 Purandare Ashok V Inhibitors of protein arginine methyl transferases
WO2006079021A2 (en) * 2005-01-20 2006-07-27 Sirtris Pharmaceuticals, Inc. Use of sirtuin-activating compounds for treating flushing and drug induced weight gain
MX2007009782A (es) 2005-02-15 2007-08-22 Novo Nordisk As 5-aminopiridin-2-ilesteres de acido 3,4-dihidro-1h-isoquinolin-2- carboxilico.
CA2610854A1 (en) * 2005-03-30 2006-10-05 Sirtris Pharmaceuticals, Inc. Nicotinamide riboside and analogues thereof
DE102005025625A1 (de) 2005-06-01 2006-12-07 Friedrich-Schiller-Universität Jena Neue hochaffine Dopaminantagonisten zur Behandlung der Schizophrenie und Verfahren zu ihrer Herstellung
NZ565111A (en) * 2005-07-15 2011-10-28 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
US7425633B2 (en) * 2005-08-26 2008-09-16 National Health Research Institutes Pyrrolidine compounds
CA2621949A1 (en) 2005-09-14 2007-03-22 Amgen Inc. Conformationally constrained 3- (4-hydroxy-phenyl) - substituted-propanoic acids useful for treating metabolic disorders
CA2623034A1 (en) 2005-09-27 2007-04-05 Novartis Ag Carboxyamine compounds and their use in the treatment of hdac dependent diseases
PL1951674T3 (pl) 2005-10-26 2012-04-30 Merck Serono Sa Pochodne sulfonamidowe i ich zastosowania do modulowania metaloproteinaz
AU2006311101A1 (en) * 2005-11-11 2007-05-18 F. Hoffmann-La Roche Ag Carbocyclic fused cyclic amines as inhibitors of the coagulation factor Xa
WO2007098608A1 (en) 2006-03-02 2007-09-07 Chao-Jun Li Chiral ligands, their preparation and uses thereof in assymetric reactions
CN101410389A (zh) 2006-03-29 2009-04-15 诺瓦提斯公司 有机化合物
US7919598B2 (en) * 2006-06-28 2011-04-05 Bristol-Myers Squibb Company Crystal structures of SGLT2 inhibitors and processes for preparing same
JP5331690B2 (ja) 2006-08-07 2013-10-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 置換−１，２，３，４−テトラヒドロイソキノリン誘導体の製造方法
RU2009110172A (ru) 2006-08-23 2010-09-27 Валеант Фармасьютикалс Интернэшнл (Us) Производные 4-(n-азациклоалкил)анилидов в качестве модуляторов калиевых каналов
DE102006046922B3 (de) 2006-09-27 2007-11-15 Julius-Maximilians-Universität Würzburg Biofilm-hemmende Wirkung sowie anti-infektive Aktivität N,C-verknüpfter Arylisochinoline, deren pharmazeutischen Zusammensetzung und deren Verwendung
US20090099158A1 (en) * 2007-03-01 2009-04-16 Grice Cheryl A Tetrahydroisoquinoline compounds as modulators of the histamine h3 receptor
EA017249B8 (ru) 2007-05-10 2013-01-30 Олбани Молекьюлар Рисерч, Инк. Арил- и гетероарилзамещенные тетрагидробензо-1,4-диазепины и их применение для блокирования обратного захвата норэпинефрина, допамина и серотонина
NZ580802A (en) 2007-05-10 2012-09-28 Albany Molecular Res Inc Aryloxy-and heteroaryloxy-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
WO2008144305A1 (en) * 2007-05-18 2008-11-27 Janssen Pharmaceutica N.V. Diaryl-substituted tetrahydroisoquinolines as histamine h3 receptor and serotonin transporter modulators
EP2167083B1 (en) * 2007-06-06 2015-10-28 Euthymics Bioscience, Inc. 1- heteroaryl-3-azabicyclo[3.1.0]hexanes, methods for their preparation and their use as medicaments
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
WO2009155565A1 (en) 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine jak inhibitor compounds and methods
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶，其組合物及使用其之治療方法
TWI396689B (zh) 2008-11-14 2013-05-21 Amgen Inc 作為磷酸二酯酶１０抑制劑之吡衍生物
ES2528404T3 (es) 2009-05-12 2015-02-10 Bristol-Myers Squibb Company Formas cristalinas de (S)-7-([1,2,4]triazol[1,5-a]piridin-6-il)-4-(3,4-diclorofenil)-1,2,3,4-tetrahidroisoquinolina y sus usos
AU2010247763B2 (en) * 2009-05-12 2015-12-24 Albany Molecular Research, Inc. 7-([1,2,4,]triazolo[1,5,-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4- tetrahydroisoquinoline and use thereof
ES2446971T3 (es) * 2009-05-12 2014-03-11 Albany Molecular Research, Inc. Tetrahidroisoquinolinas sustituidas con arilo, heteroarilo, y heterociclo y su uso
EP2606049A4 (en) 2010-08-17 2014-01-08 Albany Molecular Res Inc 2,5-METHANO- AND 2,5-ETHANO-TETRAHYDROBENZAZEPINE DERIVATIVES AND USES THEREOF FOR BLOCKING NOREPINEPHRINE, DOPAMINE, AND SEROTONIN REUPTAKE

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