SG11201810600WA - Fxr (nr1h4) modulating compounds - Google Patents

Fxr (nr1h4) modulating compounds

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Publication number
SG11201810600WA
SG11201810600WA SG11201810600WA SG11201810600WA SG11201810600WA SG 11201810600W A SG11201810600W A SG 11201810600WA SG 11201810600W A SG11201810600W A SG 11201810600WA SG 11201810600W A SG11201810600W A SG 11201810600WA SG 11201810600W A SG11201810600W A SG 11201810600WA
Authority
SG
Singapore
Prior art keywords
foster city
gilead sciences
international
lakeside drive
compounds
Prior art date
Application number
SG11201810600WA
Inventor
Peter A Blomgren
Kevin S Currie
Julie Farand
Christian Gege
Jeffrey E Kropf
Jianjun Xu
Original Assignee
Gilead Sciences 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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of SG11201810600WA publication Critical patent/SG11201810600WA/en

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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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P3/06—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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1111111011110111011111111010111110011111101111111101H1111111111111111111111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\"1 WO 2017/218337 Al 21 December 2017 (21.12.2017) WIP0 I PCT (51) International Patent Classification: MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, C07D 401/14 (2006.01) A61P 1/16 (2006.01) TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, CO7D 413/14 (2006.01) A61P 3/10 (2006.01) KM, ML, MR, NE, SN, TD, TG). A61K 31/42 (2006.01) A61P 35/00 (2006.01) A61K 31/415 (2006.01) Declarations under Rule 4.17: (21) International Application Number: — as to applicant's entitlement to apply for and be granted a PCT/US2017/036743 patent (Rule 4.17(H)) — as to the applicant's entitlement to claim the priority of the (22) International Filing Date: earlier application (Rule 4.17(iii)) 09 June 2017 (09.06.2017) Published: (25) Filing Language: English — with international search report (Art. 21(3)) (26) Publication Language: English — with sequence listing part of description (Rule 5.2(a)) (30) Priority Data: 62/349,479 13 June 2016 (13.06.2016) US (71) Applicant: GILEAD SCIENCES, INC. [US/US]; 333 Lakeside Drive, Foster City, CA 94404 (US). _ (72) Inventors: BLOMGREN, Peter A.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, 333 Lakeside Drive, Foster City, CA 94404 (US). CURRIE, Kevin S.; c/o Gilead Sciences, — Inc., 333 Lakeside Drive, 333 Lakeside Drive, Foster City, CA 94404 (US). FARAND, Julie; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404 (US). GEGE, Christian; c/o Phenex Pharmaceuticals AG, Donnersberg- = =_ weg 1, 67059 Ludwigshafen (DE). KROPF, Jeffrey E.; c/o _ Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA = 94404 (US). XU, Jianjun; c/o Gilead Sciences, Inc., 333 = Lakeside Drive, Foster City, CA 94404 (US). Agent: CAPPS, Kevin J. et al.; Gilead Sciences, Inc., 333 = (74) Lakeside Drive, Foster City, California 94404 (US). = Designated States (unless otherwise indicated, for every = (81) = kind of national protection available): AE, AG, AL, AM, = = AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, = CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, = DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, = = MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, = — OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, = SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, — TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. = Designated States (unless otherwise indicated, for every (84) kind of regional protection available): ARIPO (BW, GH, = 1-1 IN er) er) GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, GC 1-1 ! (54) Title: FXR (NR1H4) MODULATING COMPOUNDS IN ,-1 (57) : The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of 0 FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/ \" or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
SG11201810600WA 2016-06-13 2017-06-09 Fxr (nr1h4) modulating compounds SG11201810600WA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662349479P 2016-06-13 2016-06-13
PCT/US2017/036743 WO2017218337A1 (en) 2016-06-13 2017-06-09 Fxr (nr1h4) modulating compounds

Publications (1)

Publication Number Publication Date
SG11201810600WA true SG11201810600WA (en) 2018-12-28

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ID=59078248

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201810600WA SG11201810600WA (en) 2016-06-13 2017-06-09 Fxr (nr1h4) modulating compounds

Country Status (20)

Country Link
US (3) US10329286B2 (en)
EP (2) EP3468962A1 (en)
JP (1) JP6678779B2 (en)
KR (1) KR102269305B1 (en)
CN (1) CN109311849B (en)
AR (1) AR108710A1 (en)
AU (1) AU2017284160B2 (en)
BR (1) BR112018075734A2 (en)
CA (1) CA3026512A1 (en)
EA (1) EA037744B1 (en)
ES (1) ES2921432T3 (en)
IL (1) IL263495A (en)
MX (1) MX2018015443A (en)
NZ (1) NZ748641A (en)
PL (1) PL3730487T3 (en)
PT (1) PT3730487T (en)
SG (1) SG11201810600WA (en)
SI (1) SI3730487T1 (en)
TW (1) TWI643855B (en)
WO (1) WO2017218337A1 (en)

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