EA202190663A1 - Кристаллические формы агониста фарнезоидного х-рецептора - Google Patents
Кристаллические формы агониста фарнезоидного х-рецептораInfo
- Publication number
- EA202190663A1 EA202190663A1 EA202190663A EA202190663A EA202190663A1 EA 202190663 A1 EA202190663 A1 EA 202190663A1 EA 202190663 A EA202190663 A EA 202190663A EA 202190663 A EA202190663 A EA 202190663A EA 202190663 A1 EA202190663 A1 EA 202190663A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- receptor agonist
- crystalline forms
- pharnesoid
- trans
- farnesoid
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Inorganic Chemistry (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Biotechnology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
В изобретении описан агонист фарнезоидного Х-рецептора, транс-N-(3-(1-циклопропил-1H-пиразол-4-ил)фенил)-4-гидрокси-N-((транс-4-(4-метокси-3-метилфенил)циклогексил)метил)циклогексанкарбоксамид, включая кристаллические формы и его фармацевтически приемлемые соли, сольваты и составы.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862733007P | 2018-09-18 | 2018-09-18 | |
PCT/US2019/051605 WO2020061115A1 (en) | 2018-09-18 | 2019-09-17 | Crystalline forms of a farnesoid x receptor agonist |
Publications (1)
Publication Number | Publication Date |
---|---|
EA202190663A1 true EA202190663A1 (ru) | 2021-08-13 |
Family
ID=69887984
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA202190663A EA202190663A1 (ru) | 2018-09-18 | 2019-09-17 | Кристаллические формы агониста фарнезоидного х-рецептора |
Country Status (15)
Country | Link |
---|---|
US (1) | US20210347736A1 (ru) |
EP (1) | EP3852749A4 (ru) |
JP (1) | JP2022500395A (ru) |
KR (1) | KR20210064261A (ru) |
CN (1) | CN113056270A (ru) |
AU (1) | AU2019344905A1 (ru) |
BR (1) | BR112021004931A2 (ru) |
CA (1) | CA3112485A1 (ru) |
CL (1) | CL2021000631A1 (ru) |
EA (1) | EA202190663A1 (ru) |
IL (1) | IL281464A (ru) |
MA (1) | MA53671A (ru) |
MX (1) | MX2021003083A (ru) |
SG (1) | SG11202102586RA (ru) |
WO (1) | WO2020061115A1 (ru) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SG10202110242YA (en) | 2015-09-16 | 2021-10-28 | Metacrine Inc | Farnesoid x receptor agonists and uses thereof |
CN113056271A (zh) | 2018-09-18 | 2021-06-29 | 梅塔科林公司 | 法尼醇x受体激动剂及其用途 |
KR20220155596A (ko) * | 2020-03-18 | 2022-11-23 | 메타크린, 인크. | 파르네소이드 x 수용체 효능제의 제제 |
WO2022094816A1 (en) * | 2020-11-04 | 2022-05-12 | Janssen Pharmaceuticals, Inc. | Solid formulation |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1914205A (zh) * | 2003-12-19 | 2007-02-14 | 葛兰素集团有限公司 | 吡唑并[3,4-b]吡啶化合物及其作为磷酸二酯酶抑制剂的用途 |
PT1734970E (pt) * | 2004-03-12 | 2015-03-11 | Intercept Pharmaceuticals Inc | Tratamento de fibrose utilizando ligandos de rfx |
CA2642220A1 (en) * | 2006-02-14 | 2007-08-23 | Intercept Pharmaceuticals, Inc. | Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions |
US20090270418A1 (en) * | 2008-01-09 | 2009-10-29 | Marianne Sloss | Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith |
EP2393811A1 (en) * | 2009-02-04 | 2011-12-14 | Pfizer Inc. | 4-amino-7,8-dihydropyrido[4,3-d]pyrimidin-5(6h)-one derivatives |
CN103391937A (zh) * | 2010-12-20 | 2013-11-13 | Irm责任有限公司 | 用于调控法尼醇x受体的组合物和方法 |
EP3350164A4 (en) * | 2015-09-16 | 2019-03-27 | Metacrine, Inc. | X FARNESOID RECEPTOR AGONISTS AND USES THEREOF |
EP3350166A4 (en) * | 2015-09-16 | 2019-05-01 | Metacrine, Inc. | FARNESOID-X RECEPTOR AGONISTS AND USES THEREOF |
US10626081B2 (en) * | 2015-09-16 | 2020-04-21 | Metacrine, Inc. | Farnesoid X receptor agonists and uses thereof |
SG10202110242YA (en) * | 2015-09-16 | 2021-10-28 | Metacrine Inc | Farnesoid x receptor agonists and uses thereof |
JP6865743B2 (ja) * | 2015-10-01 | 2021-04-28 | フィルメニッヒ インコーポレイテッドFirmenich Incorporated | Trpm8の活性調節因子として有用な化合物 |
WO2017078928A1 (en) * | 2015-11-06 | 2017-05-11 | Salk Institute For Biological Studies | Fxr agonists and methods for making and using |
CA3056019A1 (en) * | 2017-03-15 | 2018-09-20 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
WO2018170173A1 (en) * | 2017-03-15 | 2018-09-20 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
-
2019
- 2019-09-17 EA EA202190663A patent/EA202190663A1/ru unknown
- 2019-09-17 KR KR1020217010822A patent/KR20210064261A/ko unknown
- 2019-09-17 BR BR112021004931-2A patent/BR112021004931A2/pt not_active Application Discontinuation
- 2019-09-17 SG SG11202102586RA patent/SG11202102586RA/en unknown
- 2019-09-17 US US17/276,763 patent/US20210347736A1/en active Pending
- 2019-09-17 AU AU2019344905A patent/AU2019344905A1/en not_active Abandoned
- 2019-09-17 CA CA3112485A patent/CA3112485A1/en active Pending
- 2019-09-17 MX MX2021003083A patent/MX2021003083A/es unknown
- 2019-09-17 MA MA053671A patent/MA53671A/fr unknown
- 2019-09-17 WO PCT/US2019/051605 patent/WO2020061115A1/en unknown
- 2019-09-17 CN CN201980075901.8A patent/CN113056270A/zh active Pending
- 2019-09-17 JP JP2021513445A patent/JP2022500395A/ja active Pending
- 2019-09-17 EP EP19863702.7A patent/EP3852749A4/en not_active Withdrawn
-
2021
- 2021-03-14 IL IL281464A patent/IL281464A/en unknown
- 2021-03-16 CL CL2021000631A patent/CL2021000631A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
KR20210064261A (ko) | 2021-06-02 |
WO2020061115A1 (en) | 2020-03-26 |
CA3112485A1 (en) | 2020-03-26 |
CN113056270A (zh) | 2021-06-29 |
EP3852749A4 (en) | 2022-08-24 |
BR112021004931A2 (pt) | 2021-06-01 |
MA53671A (fr) | 2021-07-28 |
EP3852749A1 (en) | 2021-07-28 |
CL2021000631A1 (es) | 2021-10-01 |
JP2022500395A (ja) | 2022-01-04 |
SG11202102586RA (en) | 2021-04-29 |
US20210347736A1 (en) | 2021-11-11 |
MX2021003083A (es) | 2021-05-27 |
AU2019344905A1 (en) | 2021-04-29 |
IL281464A (en) | 2021-04-29 |
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