SG11201807784SA - 3-desoxy derivative and pharmaceutical compositions thereof - Google Patents
3-desoxy derivative and pharmaceutical compositions thereofInfo
- Publication number
- SG11201807784SA SG11201807784SA SG11201807784SA SG11201807784SA SG11201807784SA SG 11201807784S A SG11201807784S A SG 11201807784SA SG 11201807784S A SG11201807784S A SG 11201807784SA SG 11201807784S A SG11201807784S A SG 11201807784SA SG 11201807784S A SG11201807784S A SG 11201807784SA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- pct
- perugia
- cpd
- suite
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J11/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
-
- 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
- A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- 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
- 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
- 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
- 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
- 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
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Cephalosporin Compounds (AREA)
- Steroid Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 111111110111101110101011111010111110111011111011001101010IMIMINIOEMI International Bureau .. .... ..Yejd ..... .....1 (10) International Publication Number (43) International Publication Date WO 2017/156024 Al 14 September 2017 (14.09.2017) WIP0 I PCT (51) International Patent Classification: (71) Applicant: INTERCEPT PHARMACEUTICALS, INC. A61P 3/04 (2006.01) CO7J 9/00 (2006.01) [US/US]; 450 W. 15th Street, Suite 505, New York, NY A61P 9/02 (2006.01) 10011 (US). (21) International Application Number: (72) Inventors: PELLICCIARI, Roberto; Via Ulisse Rocchi PCT/US2017/021194 60, 06100 Perugia (IT). GIOIELLO, Antimo; Via A. Pesenti 51, 06125 Perugia (IT). (22) International Filing Date: 7 March 2017 (07.03.2017) (74) Agent: IWAMOTO-FAN, Michelle; Intercept Pharma- ceuticals, Inc., 450 W. 15th Street, Suite 505, New York, (25) Filing Language: English NY 10011 (US). (26) Publication Language: English (81) Designated States (unless otherwise indicated, for every (30) Priority Data: kind of national protection available): AE, AG, AL, AM, 62/306,914 11 March 2016 (11.03.2016) US 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, [Continued on next page] (54) Title: a E 3-DESOXY DERIVATIVE AND PHARMACEUTICAL COMPOSITIONS THEREOF - F --. - (57) : The present application provides Compound 1 : or a pharmaceutically acceptable salt or amino acid conjugate o thereof. The present invention relates to an FXR activator and to - methods of making and using said compound. E 0 4 E 1.11 2 to -i 4 E o . 0 I - T - --t-1 Ctrl ._ I P S I HO 71' ei © `O H , ir) 11 IN 11 0 ei Cpd 1 -'• OH 1pM Cpd 110pM Figure 1 CO2H (1), O WO 2017/156024 Al 1#11101MOMMIHMEMOMIIHINIMMIMMEHOIS HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, 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. DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). LT, SE, GA, Published: (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, with international search report (Art. 21(3)) GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ,
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662306914P | 2016-03-11 | 2016-03-11 | |
| PCT/US2017/021194 WO2017156024A1 (en) | 2016-03-11 | 2017-03-07 | 3-desoxy derivative and pharmaceutical compositions thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201807784SA true SG11201807784SA (en) | 2018-10-30 |
Family
ID=59787771
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201807784SA SG11201807784SA (en) | 2016-03-11 | 2017-03-07 | 3-desoxy derivative and pharmaceutical compositions thereof |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US10815267B2 (en) |
| EP (1) | EP3426348B1 (en) |
| JP (1) | JP6892457B2 (en) |
| KR (1) | KR102359191B1 (en) |
| CN (1) | CN108883305B (en) |
| AR (1) | AR107864A1 (en) |
| AU (1) | AU2017229481B2 (en) |
| BR (1) | BR112018068278B1 (en) |
| CA (1) | CA3016875C (en) |
| EA (1) | EA038632B1 (en) |
| ES (1) | ES2874682T3 (en) |
| HK (1) | HK1259145A1 (en) |
| IL (1) | IL261548B (en) |
| MX (1) | MX2018010983A (en) |
| PH (1) | PH12018501956A1 (en) |
| PL (1) | PL3426348T3 (en) |
| PT (1) | PT3426348T (en) |
| SG (1) | SG11201807784SA (en) |
| SI (1) | SI3426348T1 (en) |
| TW (1) | TWI772289B (en) |
| WO (1) | WO2017156024A1 (en) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017533923A (en) | 2014-11-06 | 2017-11-16 | エナンタ ファーマシューティカルズ インコーポレイテッド | Bile acid analogs as FXR / TGR5 agonists and methods of use thereof |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| US11578097B2 (en) | 2014-11-26 | 2023-02-14 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof |
| RU2017121457A (en) | 2014-11-26 | 2018-12-26 | Энанта Фармасьютикалс, Инк. | BILIC ACID ANALOGUES AS FXR / TGR5 AGONISTS AND WAYS OF THEIR APPLICATION |
| SG11201706089RA (en) | 2015-02-11 | 2017-09-28 | Enanta Pharm Inc | Bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
| SG10201910670RA (en) | 2015-03-31 | 2020-01-30 | Enanta Pharm Inc | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| EP3359160B1 (en) * | 2015-10-07 | 2021-08-25 | Intercept Pharmaceuticals, Inc. | Farnesoid x receptor modulators |
| US10323060B2 (en) | 2016-02-23 | 2019-06-18 | Enanta Pharmaceuticals, Inc. | Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof |
| US10364267B2 (en) | 2016-02-23 | 2019-07-30 | Enanta Pharmaceuticals, Inc. | Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| WO2017147174A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Heteroaryl containing bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
| AU2017229481B2 (en) | 2016-03-11 | 2022-06-16 | Intercept Pharmaceuticals, Inc. | 3-desoxy derivative and pharmaceutical compositions thereof |
| CN110121347A (en) | 2016-11-29 | 2019-08-13 | 英安塔制药有限公司 | The method for preparing sulfonylureas bile acid derivative |
| WO2018152171A1 (en) | 2017-02-14 | 2018-08-23 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as fxr agonists and methods of use thereof |
| WO2018187804A1 (en) | 2017-04-07 | 2018-10-11 | Enanta Pharmaceuticals, Inc. | Process for preparation of sulfonyl carbamate bile acid derivatives |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| WO2023288123A1 (en) | 2021-07-16 | 2023-01-19 | Interecept Pharmaceuticals, Inc. | Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid |
| WO2023205447A2 (en) * | 2022-04-21 | 2023-10-26 | Intercept Pharmaceuticals, Inc. | Uses of farnesoid x receptor agonists |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2712617B2 (en) * | 2004-03-12 | 2020-11-18 | Intercept Pharmaceuticals, Inc. | Treatment of fibrosis using Fxr ligands |
| US20130261317A1 (en) * | 2010-09-27 | 2013-10-03 | Kythera Biopharmaceuticals, Inc. | Methods for preparing synthetic bile acids and compositions comprising the same |
| CA2861000A1 (en) | 2011-12-29 | 2013-07-04 | Novo Nordisk A/S | Dipeptide comprising a non-proteogenic amino acid |
| DK3848038T3 (en) * | 2013-05-14 | 2023-02-06 | Intercept Pharmaceuticals Inc | 11-Hydroxyl-6-substituted derivatives of bile acids and their amino acid conjugates as farnesoid X receptor modulates. |
| DK3626725T3 (en) * | 2014-05-29 | 2023-02-27 | Bar Pharmaceuticals S R L | CHOLAN DERIVATIVES FOR USE IN THE TREATMENT AND/OR PREVENTION OF FXR AND TGR5/GPBAR1 MEDIATED DISEASES |
| EP3331896A4 (en) * | 2015-08-07 | 2019-08-14 | Intercept Pharmaceuticals, Inc. | Methods for preparation of bile acids and derivatives thereof |
| AU2017229481B2 (en) | 2016-03-11 | 2022-06-16 | Intercept Pharmaceuticals, Inc. | 3-desoxy derivative and pharmaceutical compositions thereof |
-
2017
- 2017-03-07 AU AU2017229481A patent/AU2017229481B2/en active Active
- 2017-03-07 PL PL17763922T patent/PL3426348T3/en unknown
- 2017-03-07 KR KR1020187028967A patent/KR102359191B1/en active IP Right Grant
- 2017-03-07 US US15/451,818 patent/US10815267B2/en active Active
- 2017-03-07 EA EA201892007A patent/EA038632B1/en unknown
- 2017-03-07 EP EP17763922.6A patent/EP3426348B1/en active Active
- 2017-03-07 CN CN201780018432.7A patent/CN108883305B/en active Active
- 2017-03-07 WO PCT/US2017/021194 patent/WO2017156024A1/en active Application Filing
- 2017-03-07 JP JP2018547355A patent/JP6892457B2/en active Active
- 2017-03-07 SG SG11201807784SA patent/SG11201807784SA/en unknown
- 2017-03-07 CA CA3016875A patent/CA3016875C/en active Active
- 2017-03-07 MX MX2018010983A patent/MX2018010983A/en unknown
- 2017-03-07 PT PT177639226T patent/PT3426348T/en unknown
- 2017-03-07 BR BR112018068278-0A patent/BR112018068278B1/en active IP Right Grant
- 2017-03-07 ES ES17763922T patent/ES2874682T3/en active Active
- 2017-03-07 SI SI201730776T patent/SI3426348T1/en unknown
- 2017-03-09 TW TW106107817A patent/TWI772289B/en active
- 2017-03-13 AR ARP170100619A patent/AR107864A1/en unknown
-
2018
- 2018-09-03 IL IL261548A patent/IL261548B/en active IP Right Grant
- 2018-09-06 US US16/124,122 patent/US20190002493A1/en not_active Abandoned
- 2018-09-11 PH PH12018501956A patent/PH12018501956A1/en unknown
-
2019
- 2019-01-23 HK HK19101169.2A patent/HK1259145A1/en unknown
-
2020
- 2020-09-18 US US17/025,475 patent/US11319337B2/en active Active
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