PE20071100A1 - Derivados de azepinoindol como agentes farmaceuticos - Google Patents

Derivados de azepinoindol como agentes farmaceuticos

Info

Publication number
PE20071100A1
PE20071100A1 PE2006001614A PE2006001614A PE20071100A1 PE 20071100 A1 PE20071100 A1 PE 20071100A1 PE 2006001614 A PE2006001614 A PE 2006001614A PE 2006001614 A PE2006001614 A PE 2006001614A PE 20071100 A1 PE20071100 A1 PE 20071100A1
Authority
PE
Peru
Prior art keywords
substituted
alkyl
tetrahidroazepino
indol
rental
Prior art date
Application number
PE2006001614A
Other languages
English (en)
Inventor
Taegon Baik
Chris A Buhr
Brett B Busch
Diva Sze-Ming Chan
Brenton T Flatt
Xiao Hui Gu
Vasu Jammalamadaka
Richard George Khoury
Katherine Lara
Sunghoon Ma
Richard Martin
Raju Mohan
John M Nuss
Jason Jevious Park
Longcheng Wang
Tie Ling Wang
Wei Xu
Bryan K S Yeung
Original Assignee
Exelixis 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 Exelixis Inc filed Critical Exelixis Inc
Publication of PE20071100A1 publication Critical patent/PE20071100A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DODNE R1 ES -C(J)R11, -C(J)OR11, -C(J)N(R10)(R11); J ES UN ENLACE DIRECTO, NR10; n ES 0-4; R3 ES H, C(O)R9, CON(R11)(R12); R6 Y R7 SON CADA UNO ALQUILO SUSTITUIDO O NO, CICLOALQUILO SUSTITUIDO O NO, CICLOALQUILALQUILO SUSTITUIDO O NO; R8 ES OH, ALQUILO SUSTITUIDO O NO, HALO, HALOALCOXI, HALOALQUILO, ENTRE OTROS; R9 ES ALQUILO SUSTITUIDO O NO, ARALQUILO SUSTITUIDO O NO, ALQUINILO SUSTITUIDO O NO, ENTRE OTROS; R10 ES H, ALQUILO SUSTITUIDO O NO, HETEROCICLILO SUSTITUIDO O NO, ENTRE OTROS; R11 ES H, ALQUILO SUSTITUIDO O NO, ALQUINILO SUSITUIDO O NO, ENTRE OTROS; R12 ES H, ALQUILO SUSTITUIDO O NO, ALQUENILO SUSTITUIDO O NO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 1-METILETIL 1,1-DIMETIL-3-{[(1S,4S)-5-METIL-2,5-DIAZABICICLO[2.2.1]HEPT-2-IL]CARBONIL}-1,2,3,6-TETRAHIDROAZEPINO[4,5-b]INDOL-5-CARBOXILATO; 1-METILETIL 1,1-DIMETIL-3-({4-[(1-METILPIPERIDIN-4-IL)METIL]PIPERAZIN-1-IL}CARBONIL)-1,2,3,6-TETRAHIDROAZEPINO[4,5-b]INDOL-5-CARBOXILATO; ENTRE OTROS. DICHOS COMPUESTOS SON MODULADORES DE LOS RECEPTORES NUCLEARES ESPECIALMENTE FARNESOIDE X UTILES EN EL TRATAMIENTO ATEROSCLEROSIS Y RELACIONADOS
PE2006001614A 2005-12-15 2006-12-15 Derivados de azepinoindol como agentes farmaceuticos PE20071100A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US75063405P 2005-12-15 2005-12-15
US75067905P 2005-12-15 2005-12-15

Publications (1)

Publication Number Publication Date
PE20071100A1 true PE20071100A1 (es) 2007-12-21

Family

ID=37946206

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006001614A PE20071100A1 (es) 2005-12-15 2006-12-15 Derivados de azepinoindol como agentes farmaceuticos

Country Status (13)

Country Link
US (1) US20090203577A1 (es)
EP (1) EP1963331A1 (es)
JP (2) JP5420908B2 (es)
AR (1) AR058781A1 (es)
AU (1) AU2006325815B2 (es)
BR (1) BRPI0620156A2 (es)
CA (1) CA2633243C (es)
EC (1) ECSP088623A (es)
IL (1) IL191907A0 (es)
PE (1) PE20071100A1 (es)
RU (1) RU2008128823A (es)
TW (1) TW200745124A (es)
WO (1) WO2007070796A1 (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0412262A (pt) * 2003-07-23 2006-09-19 X Ceptor Therapeutics Inc derivados de azepina como agentes farmacêuticos
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
EP2240481A1 (en) 2008-01-11 2010-10-20 Albany Molecular Research, Inc. (1-azinone) -substituted pyridoindoles as mch antagonists
EP2518052B1 (de) 2008-03-27 2017-12-20 Grünenthal GmbH Substituierte 4-Aminocyclohexan-Derivate
AU2009228645B2 (en) * 2008-03-27 2013-07-18 Grunenthal Gmbh Hydroxymethylcyclohexyl amines
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
WO2010036362A1 (en) * 2008-09-26 2010-04-01 Wyeth 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors
AR074760A1 (es) * 2008-12-18 2011-02-09 Metabolex Inc Agonistas del receptor gpr120 y usos de los mismos en medicamentos para el tratamiento de diabetes y el sindrome metabolico.
US8637501B2 (en) 2009-07-01 2014-01-28 Albany Molecular Research, Inc. Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine MCH-1 antagonists, methods of making, and use thereof
WO2011003012A1 (en) 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Azinone-substituted azapolycycle mch-1 antagonists, methods of making, and use thereof
US8629158B2 (en) 2009-07-01 2014-01-14 Albany Molecular Research, Inc. Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof
US9073925B2 (en) 2009-07-01 2015-07-07 Albany Molecular Research, Inc. Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof
TW201139370A (en) 2009-12-23 2011-11-16 Lundbeck & Co As H Processes for the manufacture of a pharmaceutically active agent
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
ITRM20100329A1 (it) * 2010-06-15 2011-12-16 Franco Baldelli Modulazione del recettore nucleare per i farnesoidi (fxr) con molecole agoniste per la prevenzione e trattamento di fenomeni aterosclerotici indotti da somministrazione di inibitori delle proteasi
WO2011157827A1 (de) 2010-06-18 2011-12-22 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
WO2012088038A2 (en) 2010-12-21 2012-06-28 Albany Molecular Research, Inc. Piperazinone-substituted tetrahydro-carboline mch-1 antagonists, methods of making, and uses thereof
US8993765B2 (en) 2010-12-21 2015-03-31 Albany Molecular Research, Inc. Tetrahydro-azacarboline MCH-1 antagonists, methods of making, and uses thereof
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
WO2012120055A1 (de) 2011-03-08 2012-09-13 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2683700B1 (de) 2011-03-08 2015-02-18 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2683705B1 (de) 2011-03-08 2015-04-22 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
WO2012120052A1 (de) 2011-03-08 2012-09-13 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
US10301268B2 (en) 2014-03-13 2019-05-28 The Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
AU2015229072A1 (en) * 2014-03-13 2016-09-29 Salk Institute For Biological Studies FXR agonists and methods for making and using
US10077268B2 (en) 2014-03-13 2018-09-18 Salk Institute For Biological Studies FXR agonists and methods for making and using
AU2015370588B2 (en) * 2014-12-22 2020-07-16 Akarna Therapeutics, Ltd. Fused bicyclic compounds for the treatment of disease
CA2980394A1 (en) * 2015-03-26 2016-09-29 Akarna Therapeutics, Ltd. Fused bicyclic compounds for the treatment of disease
WO2017078928A1 (en) * 2015-11-06 2017-05-11 Salk Institute For Biological Studies Fxr agonists and methods for making and using
WO2017143134A1 (en) * 2016-02-19 2017-08-24 Alios Biopharma, Inc. Fxr modulators and methods of their use
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
KR102269305B1 (ko) 2016-06-13 2021-06-25 길리애드 사이언시즈, 인코포레이티드 Fxr (nr1h4) 조정 화합물
CN110461328A (zh) 2017-03-28 2019-11-15 吉利德科学公司 治疗肝疾病的治疗组合
RS62711B1 (sr) 2017-04-12 2022-01-31 Il Dong Pharma Derivati izoksazola kao agonisti nuklearnih receptora i njihova upotreba
DK3911647T3 (da) 2019-01-15 2024-02-26 Gilead Sciences Inc Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan
JP2022519906A (ja) 2019-02-19 2022-03-25 ギリアード サイエンシーズ， インコーポレイテッド Ｆｘｒアゴニストの固体形態

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2663935A1 (fr) * 1990-06-27 1992-01-03 Adir Nouveaux 1,2,3,4,5,6-hexahydroazepino [4,5-b] indoles et 1,2,3,4-tetrahydrobethacarbolines, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent.
MY122278A (en) * 1999-07-19 2006-04-29 Upjohn Co 1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles containing arylsulfones at the 9-position
US7595311B2 (en) * 2002-05-24 2009-09-29 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
TWI329111B (en) * 2002-05-24 2010-08-21 X Ceptor Therapeutics Inc Azepinoindole and pyridoindole derivatives as pharmaceutical agents
BRPI0412262A (pt) * 2003-07-23 2006-09-19 X Ceptor Therapeutics Inc derivados de azepina como agentes farmacêuticos

Also Published As

Publication number Publication date
JP2014028829A (ja) 2014-02-13
CA2633243C (en) 2014-05-27
EP1963331A1 (en) 2008-09-03
US20090203577A1 (en) 2009-08-13
RU2008128823A (ru) 2010-01-20
AU2006325815A1 (en) 2007-06-21
CA2633243A1 (en) 2007-06-21
TW200745124A (en) 2007-12-16
IL191907A0 (en) 2008-12-29
AU2006325815B2 (en) 2012-07-05
AR058781A1 (es) 2008-02-20
JP5420908B2 (ja) 2014-02-19
JP2009519964A (ja) 2009-05-21
ECSP088623A (es) 2008-08-29
BRPI0620156A2 (pt) 2011-12-20
WO2007070796A1 (en) 2007-06-21

Similar Documents

Publication Publication Date Title
PE20071100A1 (es) Derivados de azepinoindol como agentes farmaceuticos
PE20211911A1 (es) Compuestos heterociclicos como inmunomoduladores
CO6270320A2 (es) Derivados de piperidina utiles como antagonistas del receptor orexina
CO5590957A2 (es) Amino-1,3,5-triazinas sustituidas en n con radicales biciclicos quirales, procedimiento para su preparacion, composiciones de las mismas y su uso como herbicidas y reguladores del crecimiento de las plantas
PE20060555A1 (es) Derivados de pirrol-oxindol como moduladores del receptor de progesterona
PE20080677A1 (es) Inhibidores de pirrolotriazina cinaza
AR065985A1 (es) Derivados de arilisoxazolina,composiciones que los contienen y usos de los mismos como agentes insecticidas y acaricidas.
AR066144A1 (es) Derivados de aril pirrolidinas utiles como insecticidas y/o acaricidas y composiciones insecticidas que los contienen.
PE20060383A1 (es) Nuevos derivados amino de urea ciclicos como inhibidores de quinasa
PE20010544A1 (es) Derivados de mutilina utiles como agentes antibacterianos
AR056317A1 (es) Compuestos de oxindol y composicion farmaceutica
PE20090816A1 (es) Derivados de pirrolopirimidinona como agentes ligandos de los receptores p2x3
PE20090276A1 (es) Compuestos derivados de imidazoquinolina como moduladores de tlr7
PE20080839A1 (es) Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
PE20051141A1 (es) Inhibidores de la polimerasa viral
AR051461A1 (es) Compuesto de pirazolo[1,5-a]pirimidin-7-il-amina forma poliformica 1 de [3-(4-metoxi-2-metil-fenil)-2,5-dimetil-pirazolo[1,5-a]pirimidin-7-il]-[(s)-1-(3-metil-[1,2,4]oxadiazol-5-il)-propil]-amina, composicion farmaceutica que lo comprende y su uso para prepararla
PE20060691A1 (es) Serinamidas sustituidas por benzoilo
AR044795A1 (es) Derivados de pirido [2,1-a] isoquinolina como inhibidores de la dpp-iv
AR047076A1 (es) Compuestos de pirrolotriazina como inhibidores de tirosina quinasas, composiciones farmaceuticas
PE20091381A1 (es) Inhibidores del virus de la hepatitis c
AR072576A1 (es) Metodo para la represion de malezas en un cesped
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
AR076838A1 (es) Sulfonamidas nematocidas
PE20120693A1 (es) Compuestos heterociclos como moduladores de la piruvato cinasa m2 (pkm2)
PE20141228A1 (es) Derivados de pirrolopirimidina y purina

Legal Events

Date Code Title Description
FX Voluntary withdrawal