EP1423113A4 - Nr1h4 nuclear receptor binding compounds - Google Patents

Nr1h4 nuclear receptor binding compounds

Info

Publication number: EP1423113A4
Authority: EP; European Patent Office
Prior art keywords: receptor binding; nuclear receptor; binding compounds; nr1h4; nr1h4 nuclear
Prior art date: 2001-08-13
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.): Ceased

Application number

EP02750474A

Other languages

German (de)

French (fr)

Other versions

EP1423113A1 (en

Inventor

Ulrike Bauer

Zach Cheruvallath

Ulrich Deuschle

Elena Dneprovskaia

Tim Gahman

Kristina Giegrich

Ronnie Hanecak

Normand Hebert

John Kiely

Ingo Kober

Manfred Kogl

Harald Kranz

Claus Kremoser

Matthew Lee

Kerstin Otte

Carlton Sage

Manish Sud

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.)

Phenex Pharmaceuticals AG

Original Assignee

Phenex Pharmaceuticals AG

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.)

2001-08-13

Filing date

2002-08-13

Publication date

2007-04-18

2001-08-13 Priority claimed from EP01119473A external-priority patent/EP1285914B1/en

2002-08-13 Application filed by Phenex Pharmaceuticals AG filed Critical Phenex Pharmaceuticals AG

2002-08-13 Priority to EP02750474A priority Critical patent/EP1423113A4/en

2004-06-02 Publication of EP1423113A1 publication Critical patent/EP1423113A1/en

2007-04-18 Publication of EP1423113A4 publication Critical patent/EP1423113A4/en

Status Ceased legal-status Critical Current

Links

101150027485 NR1H4 gene Proteins 0.000 title 1
150000001875 compounds Chemical class 0.000 title 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/50—Nitrogen atoms bound to hetero atoms
- C07D277/52—Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
- 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
- C07B2200/11—Compounds covalently bound to a solid support

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

EP02750474A 2001-08-13 2002-08-13 Nr1h4 nuclear receptor binding compounds Ceased EP1423113A4 (en)

Priority Applications (1)

Application Number	Priority Date	Filing Date	Title
EP02750474A EP1423113A4 (en)	2001-08-13	2002-08-13	Nr1h4 nuclear receptor binding compounds

Applications Claiming Priority (6)

Application Number	Priority Date	Filing Date	Title
EP01119473		2001-08-13
EP01119473A EP1285914B1 (en)	2001-08-13	2001-08-13	Nr1h4 nuclear receptor binding compounds
US185731		2002-07-01
US10/185,731 US6974830B2 (en)	2001-08-13	2002-07-01	NR1H4 nuclear receptor binding compounds
PCT/US2002/025438 WO2003015777A1 (en)	2001-08-13	2002-08-13	Nr1h4 nuclear receptor binding compounds
EP02750474A EP1423113A4 (en)	2001-08-13	2002-08-13	Nr1h4 nuclear receptor binding compounds

Publications (2)

Publication Number	Publication Date
EP1423113A1 EP1423113A1 (en)	2004-06-02
EP1423113A4 true EP1423113A4 (en)	2007-04-18

Family

ID=26076685

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
EP02750474A Ceased EP1423113A4 (en)	2001-08-13	2002-08-13	Nr1h4 nuclear receptor binding compounds

Country Status (2)

Country	Link
EP (1)	EP1423113A4 (en)
WO (1)	WO2003015777A1 (en)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
ES2248581T3 (en)	2001-03-12	2006-03-16	Intercept Pharmaceuticals, Inc.	STEROIDS AS FXR AGONISTS.
US6987121B2 (en)	2002-04-25	2006-01-17	Smithkline Beecham Corporation	Compositions and methods for hepatoprotection and treatment of cholestasis
GB0315111D0 (en)	2003-06-27	2003-07-30	Cancer Rec Tech Ltd	Substituted 5-membered ring compounds and their use
CA2551611C (en)	2003-12-26	2013-06-25	Kyowa Kirin Co., Ltd.	Thiazole derivatives for treating or preventing parkinson's disease
US10987362B2 (en)	2004-03-12	2021-04-27	Intercept Pharmaceuticals, Inc.	Treatment of fibrosis using FXR ligands
PL1734970T3 (en)	2004-03-12	2015-05-29	Intercept Pharmaceuticals Inc	Treatment of fibrosis using fxr ligands
SG155188A1 (en)	2004-07-30	2009-09-30	Exelixis Inc	Pyrrole derivatives as pharmaceutical agents
EP1841749A1 (en)	2004-09-02	2007-10-10	Metabasis Therapeutics, Inc.	Derivatives of thiazole and thiadiazole inhibitors of tyrosine phosphatases
WO2006029719A2 (en) *	2004-09-14	2006-03-23	Bayer Healthcare Ag	Diagnostics and therapeutics for diseases associated with nuclear receptor subfamily 1, group h, member 4 (nr1h4)
ITMI20050912A1 (en)	2005-05-19	2006-11-20	Erregierre Spa	PROCESS OF PREPARATION OF ACIDS 3-A-YA (B) -DIDROSSI-6-A (B) -ALCHIL-5B-COLANICI
KR101555716B1 (en)	2007-01-19	2015-09-25	인터셉트 파마슈티컬즈, 인크.	5 23- 23-substituted bile acids as tgr5 modulators and methods of use thereof
WO2010014836A2 (en)	2008-07-30	2010-02-04	Intercept Pharmaceuticals, Inc.	Tgr5 modulators and methods of use thereof
DK2698375T3 (en)	2008-11-19	2018-05-28	Intercept Pharmaceuticals Inc	TGR5 modulators and methods for using them
EP2379081B1 (en)	2008-12-19	2013-03-20	Royal College of Surgeons in Ireland	Treatment of diarrhoea
EP2545964A1 (en)	2011-07-13	2013-01-16	Phenex Pharmaceuticals AG	Novel FXR (NR1H4) binding and activity modulating compounds
US9982008B2 (en)	2012-06-19	2018-05-29	Intercept Pharmaceuticals, Inc.	Preparation and uses of obeticholic acid
SI3336097T1 (en)	2012-06-19	2021-07-30	Intercept Pharmaceuticals, Inc.	Preparation of the non-crystalline form of obeticholic acid
MX385718B (en)	2016-06-13	2025-03-18	Gilead Sciences Inc	FXR MODULATING COMPOUNDS (NR1H4).
CA3252823A1 (en)	2016-06-13	2025-02-25	Gilead Sciences, Inc.	Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds
PT3600309T (en)	2017-03-28	2022-10-03	Gilead Sciences Inc	THERAPEUTIC COMBINATIONS FOR THE TREATMENT OF LIVER DISEASES
EP3911647B1 (en)	2019-01-15	2023-12-13	Gilead Sciences, Inc.	Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same
CA3233305A1 (en)	2019-02-19	2020-08-27	Gilead Sciences, Inc.	Solid forms of fxr agonists
CN114008040B (en) *	2019-06-14	2024-09-10	南京瑞捷医药科技有限公司	Compounds for modulating FXR
KR20220035365A (en)	2019-07-18	2022-03-22	엔요 파마	How to reduce the side effects of interferon
IL293892A (en)	2020-01-15	2022-08-01	Inserm Institut National De La Sant? Et De La Rech M?Dicale	Use of fxr agonists to treat hepatitis d virus infection
US11478533B2 (en)	2020-04-27	2022-10-25	Novo Nordisk A/S	Semaglutide for use in medicine
JP2024502673A (en)	2021-01-14	2024-01-22	ウエヌイグレックオ・ファーマ	Synergistic effect of FXR agonist and IFN for treatment of HBV infection
JP2024517181A (en)	2021-04-28	2024-04-19	ウエヌイグレックオ・ファーマ	Strong enhancement of the effects of TLR3 agonists using FXR agonists as combination therapy

Citations (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
GB2022085A (en) *	1978-06-02	1979-12-12	Pfizer	Novel Aminothiazoles
JPH04173782A (en) *	1990-11-08	1992-06-22	Taisho Pharmaceut Co Ltd	2-sulfonamido-4,5-diphenylthiazole derivative
EP0592664A1 (en) *	1991-03-07	1994-04-20	Hisamitsu Pharmaceutical Co., Inc.	Novel diphenylthyazole derivative
JPH07149745A (en) *	1993-11-30	1995-06-13	Hisamitsu Pharmaceut Co Inc	Novel 2-aminothiazole derivative
FR2735777A1 (en) *	1995-06-21	1996-12-27	Sanofi Sa	4-PHENYLAMINOTHIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
FR2796380A1 (en) *	1999-07-15	2001-01-19	Sanofi Synthelabo	NOVEL AMINOTHIAZOLE DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
FR2692893B1 (en) *	1992-06-24	1994-09-02	Sanofi Elf	Branched alkylamino thiazole derivatives, processes for their preparation and pharmaceutical compositions containing them.
FR2714059B1 (en) *	1993-12-21	1996-03-08	Sanofi Elf	Branched amino derivatives of thiazole, processes for their preparation and pharmaceutical compositions containing them.
AU689972B2 (en) *	1994-11-29	1998-04-09	Hisamitsu Pharmaceutical Co., Inc.	Antibacterial preparation or bactericide comprising 2-aminothiazole derivative and/or salt thereof
JP4136024B2 (en) *	1995-12-29	2008-08-20	富山化学工業株式会社	2-aminothiazol derivative or salt thereof

2002
- 2002-08-13 WO PCT/US2002/025438 patent/WO2003015777A1/en not_active Ceased
- 2002-08-13 EP EP02750474A patent/EP1423113A4/en not_active Ceased

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
GB2022085A (en) *	1978-06-02	1979-12-12	Pfizer	Novel Aminothiazoles
JPH04173782A (en) *	1990-11-08	1992-06-22	Taisho Pharmaceut Co Ltd	2-sulfonamido-4,5-diphenylthiazole derivative
EP0592664A1 (en) *	1991-03-07	1994-04-20	Hisamitsu Pharmaceutical Co., Inc.	Novel diphenylthyazole derivative
JPH07149745A (en) *	1993-11-30	1995-06-13	Hisamitsu Pharmaceut Co Inc	Novel 2-aminothiazole derivative
FR2735777A1 (en) *	1995-06-21	1996-12-27	Sanofi Sa	4-PHENYLAMINOTHIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
FR2796380A1 (en) *	1999-07-15	2001-01-19	Sanofi Synthelabo	NOVEL AMINOTHIAZOLE DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
MALONEY P R ET AL: "Identification of a Chemical Tool for the rphan Nuclear Receptor FXR", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 43, no. 16, 10 August 2000 (2000-08-10), pages 2971 - 2974, XP002992679, ISSN: 0022-2623 *
See also references of WO03015777A1 *

Also Published As

Publication number	Publication date
EP1423113A1 (en)	2004-06-02
WO2003015777A1 (en)	2003-02-27

Legal Events

Date	Code	Title	Description
2004-04-16	PUAI	Public reference made under article 153(3) epc to a published international application that has entered the european phase	Free format text: ORIGINAL CODE: 0009012
2004-06-02	17P	Request for examination filed	Effective date: 20040225
2004-06-02	AK	Designated contracting states	Kind code of ref document: A1 Designated state(s): AT BE BG CH CY CZ DE DK EE ES FI FR GB GR IE IT LI LU MC NL PT SE SK TR
2004-06-02	AX	Request for extension of the european patent	Extension state: AL LT LV MK RO SI
2004-06-16	RIN1	Information on inventor provided before grant (corrected)	Inventor name: SUD, MANISH Inventor name: SAGE, CARLTON Inventor name: OTTE, KERSTIN Inventor name: LEE, MATTHEW Inventor name: KREMOSER, CLAUS Inventor name: KRANZ, HARALD Inventor name: KOGL, MANFRED Inventor name: KOBER, INGO Inventor name: KIELY, JOHN Inventor name: HEBERT, NORMAND Inventor name: HANECAK, RONNIE Inventor name: GIEGRICH, KRISTINA Inventor name: GAHMAN, TIM Inventor name: DNEPROVSKAIA, ELENA Inventor name: DEUSCHLE, ULRICH Inventor name: CHERUVALLATH, ZACH Inventor name: BAUER, ULRIKE
2004-06-30	RIN1	Information on inventor provided before grant (corrected)	Inventor name: SUD, MANISH Inventor name: SAGE, CARLTON Inventor name: OTTE, KERSTIN Inventor name: LEE, MATTHEW Inventor name: KREMOSER, CLAUS Inventor name: KRANZ, HARALD Inventor name: KOGL, MANFRED Inventor name: KOBER, INGO Inventor name: KIELY, JOHN Inventor name: HEBERT, NORMAND Inventor name: HANECAK, RONNIE Inventor name: GIEGRICH, KRISTINA Inventor name: GAHMAN, TIM Inventor name: DNEPROVSKAIA, ELENA Inventor name: DEUSCHLE, ULRICH Inventor name: CHERUVALLATH, ZACH Inventor name: BAUER, ULRIKE
2004-12-01	RAP1	Party data changed (applicant data changed or rights of an application transferred)	Owner name: PHENEX PHARMACEUTICALS AG
2006-04-05	RAP1	Party data changed (applicant data changed or rights of an application transferred)	Owner name: PHENEX PHARMACEUTICALS AG
2007-04-18	A4	Supplementary search report drawn up and despatched	Effective date: 20070315
2007-04-18	RIC1	Information provided on ipc code assigned before grant	Ipc: C07D 277/52 20060101ALI20070309BHEP Ipc: C07D 277/46 20060101ALI20070309BHEP Ipc: C07D 277/44 20060101ALI20070309BHEP Ipc: C07D 277/42 20060101ALI20070309BHEP Ipc: C07D 277/40 20060101ALI20070309BHEP Ipc: A61K 31/426 20060101AFI20030306BHEP
2008-07-02	17Q	First examination report despatched	Effective date: 20080602
2008-11-05	RIN1	Information on inventor provided before grant (corrected)	Inventor name: SUD, MANISH Inventor name: DNEPROVSKAIA, ELENAC Inventor name: DEUSCHLE, ULRICH Inventor name: CHERUVALLATH, ZACH Inventor name: SAGE, CARLTON Inventor name: OTTE, KERSTIN Inventor name: LEE, MATTHEW Inventor name: KREMOSER, CLAUS Inventor name: KRANZ, HARALD Inventor name: KOGL, MANFRED Inventor name: KOBER, INGO Inventor name: KIELY, JOHN Inventor name: HEBERT, NORMANDC Inventor name: HANECAK, RONNIE Inventor name: GIEGRICH, KRISTINA Inventor name: GAHMAN, TIM Inventor name: BAUER, ULRIKE
2011-03-31	REG	Reference to a national code	Ref country code: DE Ref legal event code: R003
2011-07-08	STAA	Information on the status of an ep patent application or granted ep patent	Free format text: STATUS: THE APPLICATION HAS BEEN REFUSED
2011-08-10	18R	Application refused	Effective date: 20110331

Publication	Publication Date	Title
EP1423113A4 (en)	2007-04-18	Nr1h4 nuclear receptor binding compounds
GB0205954D0 (en)	2002-04-24	Binder mechanism
AU7476301A (en)	2002-01-02	Novel compounds
EP1276755A4 (en)	2004-03-31	Novel compounds
AU9261901A (en)	2002-03-26	Novel compounds
EP1292617A4 (en)	2005-04-06	Novel compounds
AU149010S (en)	2002-08-26	Binder
EP1472352A4 (en)	2005-10-12	Novel compounds
EP1343813A4 (en)	2004-11-17	Novel compounds
AU7476401A (en)	2002-01-02	Novel compounds
EP1276866A4 (en)	2005-03-16	Novel compounds
GB0028964D0 (en)	2001-01-10	Novel compounds
AU1252102A (en)	2002-05-21	Receptor
EP1299530A4 (en)	2005-03-09	Novel compounds
AU2002234786A1 (en)	2002-09-19	Nuclear hormone receptor ligand binding domain
AU2002319806A1 (en)	2003-03-03	Nr1h4 nuclear receptor binding compounds
AU2002329243A1 (en)	2003-03-03	Nr1h4 nuclear receptor binding compounds
AU2002319805A1 (en)	2003-03-03	Fxr nr1h4 nuclear receptor binding compounds
AU2002319804A1 (en)	2003-03-03	Fxr nr1h4 nuclear receptor binding compounds
GB0110129D0 (en)	2001-06-20	Novel compounds
AU2002234782A1 (en)	2002-09-19	Nuclear hormone receptor ligand binding domain
AU9462801A (en)	2002-05-06	Chemokine receptor binding heterocyclic compounds
PL359523A1 (en)	2004-08-23	Chemokine receptor binding heterocyclic compounds
CA91927S (en)	2001-03-30	Binder
TW487148U (en)	2002-05-11	Structure improvement for binding device