CA3067219A1 - Methods and intermediates for the preparation of bile acid derivatives - Google Patents

Methods and intermediates for the preparation of bile acid derivatives Download PDF

Info

Publication number
CA3067219A1
CA3067219A1 CA3067219A CA3067219A CA3067219A1 CA 3067219 A1 CA3067219 A1 CA 3067219A1 CA 3067219 A CA3067219 A CA 3067219A CA 3067219 A CA3067219 A CA 3067219A CA 3067219 A1 CA3067219 A1 CA 3067219A1
Authority
CA
Canada
Prior art keywords
compound
formula
reacting
halogen
disease
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3067219A
Other languages
English (en)
French (fr)
Inventor
Roberto Pellicciari
Antimo GIOIELLO
Gabriel GAVIN
Ronald D. Lewis
Matthew Yanik
Myoung Goo Kim
Fred Ronald LEUSINK
Bartjan KONING
Thomas HENSEL
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Intercept Pharmaceuticals Inc
Original Assignee
Intercept Pharmaceuticals 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 Intercept Pharmaceuticals Inc filed Critical Intercept Pharmaceuticals Inc
Publication of CA3067219A1 publication Critical patent/CA3067219A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CA3067219A 2017-06-23 2018-06-22 Methods and intermediates for the preparation of bile acid derivatives Pending CA3067219A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762523937P 2017-06-23 2017-06-23
US62/523,937 2017-06-23
PCT/US2018/039148 WO2018237350A1 (en) 2017-06-23 2018-06-22 METHODS AND INTERMEDIATES FOR PREPARING BILARY ACID DERIVATIVES

Publications (1)

Publication Number Publication Date
CA3067219A1 true CA3067219A1 (en) 2018-12-27

Family

ID=64691408

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3067219A Pending CA3067219A1 (en) 2017-06-23 2018-06-22 Methods and intermediates for the preparation of bile acid derivatives

Country Status (10)

Country Link
US (2) US11066437B2 (https=)
EP (1) EP3642217A4 (https=)
JP (1) JP7224307B2 (https=)
KR (2) KR20250109791A (https=)
CN (1) CN110945006A (https=)
AU (1) AU2018288883B2 (https=)
BR (1) BR112019027458A2 (https=)
CA (1) CA3067219A1 (https=)
IL (3) IL271343B2 (https=)
WO (1) WO2018237350A1 (https=)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20230747T1 (hr) 2011-09-08 2024-01-05 Sage Therapeutics, Inc. Neuroaktivni steroidi, pripravci i njihova uporaba
SMT201800657T1 (it) 2013-03-13 2019-01-11 Sage Therapeutics Inc Steroidi neuroattivi e loro metodi di utilizzo
WO2015195967A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
MX382122B (es) 2015-07-06 2025-03-13 Sage Therapeutics Inc Oxiesteroles y metodos de uso de los mismos.
PL3319611T3 (pl) 2015-07-06 2021-07-12 Sage Therapeutics, Inc. Oksysterole i sposoby ich stosowania
AU2016289965B2 (en) 2015-07-06 2021-09-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
MA42339A1 (fr) * 2015-10-07 2019-01-31 Intercept Pharmaceuticals Inc Modulateurs du récepteur farnésoïde x
EP3436022B1 (en) 2016-04-01 2022-03-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US10752653B2 (en) 2016-05-06 2020-08-25 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
WO2018009867A1 (en) 2016-07-07 2018-01-11 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
PT3519422T (pt) 2016-09-30 2022-12-05 Sage Therapeutics Inc Oxisteróis substituídos em c7 e métodos como moduladores nmda
DK4105223T3 (da) 2016-10-18 2025-07-07 Sage Therapeutics Inc Oxysteroler og fremgangsmåder til anvendelse deraf
CA3041088C (en) 2016-10-18 2024-05-21 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
JP2022552655A (ja) 2019-10-07 2022-12-19 キャリーオペ，インク． Ｇｐｒ１１９アゴニスト
WO2021155167A1 (en) * 2020-01-31 2021-08-05 The Johns Hopkins University Bile acid-gcpii inhibitor conjugates to treat inflammatory diseases
IL295825A (en) 2020-02-28 2022-10-01 Kallyope Inc gpr40 agonists
US12215127B2 (en) 2020-04-17 2025-02-04 Cornell University Compositions and methods for profiling of gut microbiota-associated bile salt hydrolase (BSH) activity
WO2021236617A1 (en) 2020-05-19 2021-11-25 Kallyope, Inc. Ampk activators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
CN112795615A (zh) * 2021-02-03 2021-05-14 湖南醇康医药科技有限公司 一种诱变菌种以及微生物发酵制备熊去氧胆酸的方法
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
CN114045239B (zh) * 2021-11-08 2023-09-29 浙江树人学院（浙江树人大学） 具有二甲基乙酰胺降解能力的泛养副球菌ybh-7及应用
WO2023205447A2 (en) * 2022-04-21 2023-10-26 Intercept Pharmaceuticals, Inc. Uses of farnesoid x receptor agonists
WO2024163640A2 (en) * 2023-02-01 2024-08-08 Intercept Pharmaceuticals, Inc. Methods and intermediates for the preparation of bile acid derivatives

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2403683A (en) * 1942-04-25 1946-07-09 Relchstein Tadeus Compounds of the cyclopentanopolyhydrophenanthrene series and process of making same
US2554882A (en) * 1943-02-04 1951-05-29 Reichstein Tadeus 3-hydroxy-11-ketoetiocholanic acid and its esters
US3277121A (en) * 1964-05-04 1966-10-04 Canada Packers Ltd Conversion of delta11-steroids to 11-oxygenated steroids
DE3040634A1 (de) * 1980-10-29 1982-05-27 Hoechst Ag, 6000 Frankfurt Verfahren zur herstellung von 3 (alpha) -hydroxy-5- (beta) -pregnan-11,20-dion
JPS58155098A (ja) * 1982-03-09 1983-09-14 Yakult Honsha Co Ltd 微生物によるウルソデオキシコ−ル酸の製造法
DK0464153T3 (da) * 1989-02-07 1995-04-24 Upjohn Co Dehalogenering af organiske forbindelser under anvendelse af tin eller bly
DE10113257C1 (de) 2001-03-19 2002-11-14 Inst Mikrotechnik Mainz Gmbh Elektrophoresevorrichtung und ihre Verwendung
ITMI20050912A1 (it) * 2005-05-19 2006-11-20 Erregierre Spa Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici
US20080318870A1 (en) * 2007-06-19 2008-12-25 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
SI3336097T1 (sl) * 2012-06-19 2021-07-30 Intercept Pharmaceuticals, Inc. Priprava nekristalinične oblike obetiholne kisline
TN2015000497A1 (en) * 2013-05-14 2017-04-06 Intercept Pharmaceuticals Inc 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators
SG11201703717SA (en) 2014-11-06 2017-06-29 Enanta Pharm Inc Bile acid analogs an 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
EP3223823A4 (en) 2014-11-26 2018-10-17 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
EP3256134A4 (en) 2015-02-11 2018-10-03 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
WO2016161003A1 (en) 2015-03-31 2016-10-06 Enanta Phamraceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
US10604544B2 (en) 2015-08-07 2020-03-31 Intercept Pharmaceuticals, Inc. Methods for preparation of bile acids and derivatives thereof
MA42339A1 (fr) * 2015-10-07 2019-01-31 Intercept Pharmaceuticals Inc Modulateurs du récepteur farnésoïde x
CN107973834A (zh) 2016-10-22 2018-05-01 合帕吉恩治疗公司 作为fxr/tgr5调节剂的胆酸衍生物
WO2018081285A1 (en) 2016-10-26 2018-05-03 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as fxr agonists and methods of use thereof

Also Published As

Publication number Publication date
US20220127302A1 (en) 2022-04-28
BR112019027458A2 (pt) 2020-07-07
JP7224307B2 (ja) 2023-02-17
US20180371009A1 (en) 2018-12-27
JP2020525426A (ja) 2020-08-27
CN110945006A (zh) 2020-03-31
KR102831293B1 (ko) 2025-07-08
IL304455A (en) 2023-09-01
IL271343B1 (en) 2023-08-01
KR20250109791A (ko) 2025-07-17
IL271343B2 (en) 2023-12-01
AU2018288883B2 (en) 2022-06-02
KR20200020877A (ko) 2020-02-26
WO2018237350A1 (en) 2018-12-27
EP3642217A1 (en) 2020-04-29
EP3642217A4 (en) 2021-06-16
IL304455B1 (en) 2026-03-01
US11066437B2 (en) 2021-07-20
IL326587A (en) 2026-04-01
AU2018288883A1 (en) 2020-01-16
IL271343A (en) 2020-01-30

Similar Documents

Publication Publication Date Title
US11066437B2 (en) Methods and intermediates for the preparation of bile acid derivatives
US12291549B2 (en) Farnesoid X receptor modulators
CN110003301B (zh) 用于治疗和/或预防fxr和tgr5/gpbar1介导的疾病的胆烷衍生物
AU2016297821B2 (en) Methods for preparation of bile acids and derivatives thereof
Sepe et al. Modification on ursodeoxycholic acid (UDCA) scaffold. Discovery of bile acid derivatives as selective agonists of cell-surface G-protein coupled bile acid receptor 1 (GP-BAR1)
CA2994687A1 (en) Methods for preparation of bile acids and derivatives thereof
JP2018528230A (ja) 胆汁酸誘導体の調製のための方法および中間体
JP6937893B2 (ja) 胆汁酸類を製造するための方法
WO2017184598A1 (en) Methods for the preparation of obeticholic acid and derivatives thereof
US20130102580A1 (en) Compositions and methods related to deoxycholic acid and its polymorphs
WO2024163640A2 (en) Methods and intermediates for the preparation of bile acid derivatives
CN101508717B (zh) 抗结核化合物帕格甾醇的合成方法
WO2023288123A1 (en) Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid
HK1251216A1 (en) Methods for preparation of bile acids and derivatives thereof
Bunyathaworn et al. Synthesis and Cytotoxicity Studies of Polyhydroxysterols and Their Sulfate Analogs
HK1260503A1 (zh) 制备奥贝胆酸及其衍生物的方法

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20230621

D15 Examination report completed

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT

Effective date: 20240822

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION

Effective date: 20241220

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20250210

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 7TH ANNIV.) - STANDARD

Year of fee payment: 7

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250613

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20250613

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20250627

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20250627

D22 Grant of ip right intended

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D22-D128 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: ALLOWANCE REQUIREMENTS DETERMINED COMPLIANT

Effective date: 20251118

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20251118

R11 Change to the name of applicant or owner or transfer of ownership requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-R10-R11-R127 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: TRANSFER RECORDAL REQUEST OR RESPONSE

Effective date: 20260313

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20260313