MA34767B1 - Compositions et procédés pour la modulation de fxr - Google Patents

Compositions et procédés pour la modulation de fxr

Info

Publication number
MA34767B1
MA34767B1 MA36062A MA36062A MA34767B1 MA 34767 B1 MA34767 B1 MA 34767B1 MA 36062 A MA36062 A MA 36062A MA 36062 A MA36062 A MA 36062A MA 34767 B1 MA34767 B1 MA 34767B1
Authority
MA
Morocco
Prior art keywords
compositions
methods
fxr modulation
fxr
present
Prior art date
Application number
MA36062A
Other languages
English (en)
Inventor
David C Tully
Paul Vincent Rucker
Phillip B Alper
Daniel Mutnick
Donatella Chianelli
Original Assignee
Irm Llc
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 Irm Llc filed Critical Irm Llc
Publication of MA34767B1 publication Critical patent/MA34767B1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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    • 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
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    • 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
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
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    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)

Abstract

La présente invention concerne des composés de Formule (I), un stéréoisomère, énantiomère, sel pharmaceutiquement acceptable ou son conjugué acide aminé ; les variables étant telles que définies présentement ; et leurs compositions pharmaceutiques qui sont utiles comme modulateurs de l'activité de récepteurs du Farnésoïde X (FXR).
MA36062A 2010-12-20 2013-06-28 Compositions et procédés pour la modulation de fxr MA34767B1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201061425189P 2010-12-20 2010-12-20
US201161554297P 2011-11-01 2011-11-01
PCT/US2011/062724 WO2012087519A1 (fr) 2010-12-20 2011-11-30 Compositions et procédés pour la modulation de fxr

Publications (1)

Publication Number Publication Date
MA34767B1 true MA34767B1 (fr) 2013-12-03

Family

ID=45349296

Family Applications (1)

Application Number Title Priority Date Filing Date
MA36062A MA34767B1 (fr) 2010-12-20 2013-06-28 Compositions et procédés pour la modulation de fxr

Country Status (39)

Country Link
US (2) US9150568B2 (fr)
EP (1) EP2655370B1 (fr)
JP (1) JP5740483B2 (fr)
KR (1) KR101626046B1 (fr)
CN (1) CN103443099B (fr)
AP (1) AP3414A (fr)
AR (1) AR084425A1 (fr)
AU (1) AU2011345233B2 (fr)
BR (1) BR112013015452B1 (fr)
CA (1) CA2819825C (fr)
CL (1) CL2013001677A1 (fr)
CO (1) CO6801729A2 (fr)
CR (1) CR20130307A (fr)
CU (1) CU24152B1 (fr)
CY (1) CY1119530T1 (fr)
DK (1) DK2655370T3 (fr)
EA (1) EA025569B1 (fr)
ES (1) ES2645728T3 (fr)
GT (1) GT201300159A (fr)
HR (1) HRP20171615T1 (fr)
HU (1) HUE034150T2 (fr)
IL (1) IL226853A (fr)
JO (1) JO3297B1 (fr)
LT (1) LT2655370T (fr)
MA (1) MA34767B1 (fr)
MX (1) MX338845B (fr)
MY (1) MY163216A (fr)
NZ (1) NZ613234A (fr)
PE (1) PE20140207A1 (fr)
PH (1) PH12013501256A1 (fr)
PL (1) PL2655370T3 (fr)
PT (1) PT2655370T (fr)
RS (1) RS56335B1 (fr)
SG (1) SG191046A1 (fr)
SI (1) SI2655370T1 (fr)
TW (1) TWI427078B (fr)
UY (1) UY33815A (fr)
WO (1) WO2012087519A1 (fr)
ZA (1) ZA201304044B (fr)

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EP2655368A1 (fr) * 2010-12-20 2013-10-30 Irm Llc Compositions et procédés de modulation des récepteurs farnésoïdes x
CU24152B1 (es) * 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
EP2545964A1 (fr) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Nouveaux composés se liant au fxr (nr1 h4) et modulant son activité
SG11201408284VA (en) 2012-05-22 2015-02-27 Xenon Pharmaceuticals Inc N-substituted benzamides and their use in the treatment of pain
CN103007081B (zh) * 2012-11-27 2013-12-04 鞠法红 一种治疗非酒精性脂肪肝的中药组合物
JP2016510764A (ja) 2013-03-07 2016-04-11 カリフィア バイオ, インク.Califia Bio, Inc. 混合系キナーゼ阻害剤および治療法
DK3065738T3 (en) * 2013-11-05 2018-06-06 Novartis Ag Compositions and Methods for Modulating Farnesoid X Receptors
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
EP3034499A1 (fr) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Nouveaux composés de modulation (FXR NR1H4)
EP3034501A1 (fr) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Hydroxy contenant des composés de modulation (FXR NR1H4)
BR112017011972A2 (pt) * 2014-12-18 2017-12-26 Novartis Ag derivados de azabicicloctano como agonistas de fxr para uso no tratamento de doenças hepáticas e gastrintestinais
TWI698430B (zh) 2015-02-13 2020-07-11 南北兄弟藥業投資有限公司 三環化合物及其在藥物中的應用
SI3277286T1 (sl) 2015-03-31 2021-09-30 Enanta Pharmaceuticals, Inc. Derivati žolčne kisline kot antagonisti FXR/TGR5 in metode za njihovo uporabo
CN106146483A (zh) * 2015-04-23 2016-11-23 上海迪诺医药科技有限公司 杂环类法尼酯衍生物x受体调节剂
CN106946867B (zh) * 2016-01-06 2019-11-12 广州市恒诺康医药科技有限公司 Fxr受体调节剂及其制备方法和用途
WO2017133521A1 (fr) * 2016-02-01 2017-08-10 山东轩竹医药科技有限公司 Agoniste du récepteur fxr
CA3012583A1 (fr) * 2016-02-08 2017-08-17 Redx Pharma Plc Composes heterocycliques, en particulier derives de 2-oxo -4,4,5,5,6,6,7,7-octahydrobenzoxazole, et leur utilisation en tant que composes antibacteriens
ES2902404T3 (es) * 2016-02-22 2022-03-28 Novartis Ag Métodos para utilizar agonistas de fxr.
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