ZA200401551B - Benzothiazepine derivatives. - Google Patents

Benzothiazepine derivatives. Download PDF

Info

Publication number: ZA200401551B
Authority: ZA; South Africa
Prior art keywords: solvate; formula; carbamoyl; hydrogen; pharmaceutically acceptable
Prior art date: 2001-09-04

Application number

ZA200401551A

Other languages

English (en)

Inventor

Ingemar Starke

David Blomberg

Peter Nordberg

Stig Jonas Bostrom

Mikael Ulf Johan Dahlstrom

Suzanne Alenfalk

Andreas Christer Wallberg

Original Assignee

Astrazeneca Ab

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.)

2001-09-04

Filing date

2004-02-25

Publication date

2004-11-24

2004-02-25 Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab

2004-11-24 Publication of ZA200401551B publication Critical patent/ZA200401551B/en

Links

150000007657 benzothiazepines Chemical class 0.000 title description 5
229940085242 benzothiazepine derivative selective calcium channel blockers with direct cardiac effects Drugs 0.000 title description 4
150000003839 salts Chemical class 0.000 claims abstract description 74
239000012453 solvate Substances 0.000 claims abstract description 66
150000001875 compounds Chemical class 0.000 claims abstract description 62
229940002612 prodrug Drugs 0.000 claims abstract description 35
239000000651 prodrug Substances 0.000 claims abstract description 35
238000000034 method Methods 0.000 claims abstract description 18
239000003613 bile acid Substances 0.000 claims abstract description 11
238000004519 manufacturing process Methods 0.000 claims abstract description 10
230000008569 process Effects 0.000 claims abstract description 9
HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims abstract description 7
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 7
-1 nitro, cyano, hydroxy, amino, carboxy, carbamoyl Chemical group 0.000 claims description 142
239000001257 hydrogen Substances 0.000 claims description 74
229910052739 hydrogen Inorganic materials 0.000 claims description 74
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 67
125000000217 alkyl group Chemical group 0.000 claims description 51
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 44
229910052757 nitrogen Inorganic materials 0.000 claims description 44
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 42
229910052799 carbon Inorganic materials 0.000 claims description 42
125000000623 heterocyclic group Chemical group 0.000 claims description 42
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 38
IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 34
125000001424 substituent group Chemical group 0.000 claims description 27
125000004452 carbocyclyl group Chemical group 0.000 claims description 23
150000002431 hydrogen Chemical class 0.000 claims description 21
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 19
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 14
241001465754 Metazoa Species 0.000 claims description 12
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 11
230000002401 inhibitory effect Effects 0.000 claims description 11
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239000000126 substance Substances 0.000 claims description 9
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108010080180 poststatin Proteins 0.000 description 1
XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
125000005344 pyridylmethyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 description 1
125000000719 pyrrolidinyl group Chemical group 0.000 description 1
125000001422 pyrrolinyl group Chemical group 0.000 description 1
150000003254 radicals Chemical class 0.000 description 1
229920005989 resin Polymers 0.000 description 1
239000011347 resin Substances 0.000 description 1
208000037803 restenosis Diseases 0.000 description 1
229960002855 simvastatin Drugs 0.000 description 1
RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
239000011734 sodium Substances 0.000 description 1
230000036262 stenosis Effects 0.000 description 1
208000037804 stenosis Diseases 0.000 description 1
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
125000005329 tetralinyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
125000001984 thiazolidinyl group Chemical group 0.000 description 1
125000000335 thiazolyl group Chemical group 0.000 description 1
125000005505 thiomorpholino group Chemical group 0.000 description 1
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
230000008733 trauma Effects 0.000 description 1
125000001425 triazolyl group Chemical group 0.000 description 1
125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
230000006492 vascular dysfunction Effects 0.000 description 1
210000005166 vasculature Anatomy 0.000 description 1
210000003462 vein Anatomy 0.000 description 1
125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
229920002554 vinyl polymer Polymers 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
- 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
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- 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
- A61P9/06—Antiarrhythmics
- 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
- C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D281/02—Seven-membered rings
- C07D281/04—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D281/08—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D281/10—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring

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Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Diabetes (AREA)
Obesity (AREA)
Hematology (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Hospice & Palliative Care (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Thiazole And Isothizaole Compounds (AREA)
Steroid Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

ZA200401551A 2001-09-04 2004-02-25 Benzothiazepine derivatives. ZA200401551B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
GBGB0121337.0A GB0121337D0 (en)	2001-09-04	2001-09-04	Chemical compounds

Publications (1)

Publication Number	Publication Date
ZA200401551B true ZA200401551B (en)	2004-11-24

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ID=9921450

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200401551A ZA200401551B (en)	2001-09-04	2004-02-25	Benzothiazepine derivatives.

Country Status (18)

Country	Link
US (1)	US7192946B2 (de)
EP (1)	EP1430040B1 (de)
JP (1)	JP4441261B2 (de)
KR (1)	KR20040029147A (de)
CN (1)	CN1599731A (de)
AT (1)	ATE438634T1 (de)
BR (1)	BR0212277A (de)
CA (1)	CA2459346A1 (de)
DE (1)	DE60233239D1 (de)
ES (1)	ES2329226T3 (de)
GB (1)	GB0121337D0 (de)
IL (1)	IL160503A0 (de)
MX (1)	MXPA04002032A (de)
NO (1)	NO20040924L (de)
NZ (1)	NZ531512A (de)
UY (1)	UY27431A1 (de)
WO (1)	WO2003020710A1 (de)
ZA (1)	ZA200401551B (de)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
SE0000772D0 (sv)	2000-03-08	2000-03-08	Astrazeneca Ab	Chemical compounds
EG26979A (en)	2000-12-21	2015-03-01	Astrazeneca Ab	Chemical compounds
GB0121622D0 (en)	2001-09-07	2001-10-31	Astrazeneca Ab	Chemical compounds
GB0121621D0 (en)	2001-09-07	2001-10-31	Astrazeneca Ab	Chemical compounds
AU2002329387B2 (en)	2001-09-08	2007-06-07	Albireo Ab	Benzothiazepine and benzothiadiazepine derivatives with ileal bile acid transport (IBAT) inhibitory activity for the treatment hyperlipidaemia
SE0104333D0 (sv)	2001-12-19	2001-12-19	Astrazeneca Ab	Therapeutic agents
GB0209467D0 (en) *	2002-04-25	2002-06-05	Astrazeneca Ab	Chemical compounds
GB0213669D0 (en)	2002-06-14	2002-07-24	Astrazeneca Ab	Chemical compounds
BR0311932A (pt) *	2002-06-20	2005-03-22	Astrazeneca Ab	Composto, formulação farmacêutica, método para tratar ou prevenir resistência à insulina, uso de um composto, processo para preparar um composto, e, tratamento combinado
TW200410921A (en) *	2002-11-25	2004-07-01	Hoffmann La Roche	Mandelic acid derivatives
GB0304194D0 (en) *	2003-02-25	2003-03-26	Astrazeneca Ab	Chemical compounds
GB0307918D0 (en)	2003-04-05	2003-05-14	Astrazeneca Ab	Therapeutic use
US7262318B2 (en)	2004-03-10	2007-08-28	Pfizer, Inc.	Substituted heteroaryl- and phenylsulfamoyl compounds
AR057828A1 (es) *	2005-09-29	2007-12-19	Astrazeneca Ab	Compuestos derivados de azetidina, su preparacion y composicion farmaceuutica
RU2480453C2 (ru)	2007-03-08	2013-04-27	Альбирео Аб	Новые соединения
WO2010062861A2 (en) *	2008-11-26	2010-06-03	Satiogen Pharmaceuticals, Inc.	Bile acid recycling inhibitors for treatment of obesity and diabetes
ES2552657T3 (es)	2010-05-26	2015-12-01	Satiogen Pharmaceuticals, Inc.	Inhibidores del reciclado de ácidos biliares y saciógenos para el tratamiento de diabetes, obesidad, y afecciones gastrointestinales inflamatorias
ES2687027T3 (es)	2010-11-04	2018-10-23	Albireo Ab	Inhibidores de ibat para el tratamiento de enfermedades hepáticas
DK2637646T3 (en)	2010-11-08	2016-08-29	Albireo Ab	PHARMACEUTICAL COMBINATION CONTAINING AN IBAT inhibitor and a bile acid binder
AU2012328526B2 (en)	2011-10-28	2017-05-25	Shire Human Genetic Therapies, Inc.	Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
US20130108573A1 (en)	2011-10-28	2013-05-02	Lumena Pharmaceuticals, Inc.	Bile Acid Recycling Inhibitors for Treatment of Hypercholemia and Cholestatic Liver Disease
CA2907230A1 (en)	2013-03-15	2014-09-18	Lumena Pharmaceuticals, Inc.	Bile acid recycling inhibitors for treatment of primary sclerosing cholangitis and inflammatory bowel disease
AU2014229050A1 (en)	2013-03-15	2015-10-22	Lumena Pharmaceuticals Llc	Bile acid recycling inhibitors for treatment of Barrett's esophagus and gastroesophageal reflux disease
JO3301B1 (ar)	2013-04-26	2018-09-16	Albireo Ab	تعديلات بلورية على إيلوبيكسيبات
CN106659726A (zh)	2014-06-25	2017-05-10	Ea制药株式会社	固体制剂及其着色防止或着色减少方法
KR101674806B1 (ko) *	2014-10-20	2016-11-10	씨제이헬스케어 주식회사	신규한 아미노알킬벤조티아제핀 유도체 및 이의 용도
EP3012252A1 (de)	2014-10-24	2016-04-27	Ferring BV	Kristalline Form von elobixibat
WO2017138878A1 (en)	2016-02-09	2017-08-17	Albireo Ab	Oral cholestyramine formulation and use thereof
CN108601739B (zh)	2016-02-09	2022-01-04	阿尔比里奥公司	考来烯胺丸剂及其制备方法
ES2874669T3 (es)	2016-02-09	2021-11-05	Albireo Ab	Formulación oral de colestiramina y uso de la misma
KR101844184B1 (ko)	2017-07-21	2018-04-02	씨제이헬스케어 주식회사	아미노알킬벤조티아제핀 유도체의 용도
CN111032019B (zh)	2017-08-09	2022-07-05	阿尔比里奥公司	考来烯胺颗粒、口服考来烯胺制剂及其用途
EP3664782B1 (de)	2017-08-09	2025-01-29	Albireo AB	Cholestyraminpellets, orale cholestyraminformulierungen und ihre medizinische verwendung
US10294265B1 (en)	2017-11-17	2019-05-21	International Business Machines Corporation	Functionalized bile acids for therapeutic and material applications
CA3091338A1 (en)	2018-03-09	2019-09-12	Elobix Ab	Process for the preparation of elobixibat
CN112449637B (zh)	2018-06-05	2024-03-19	阿尔比里奥公司	苯并硫杂(二)氮杂环庚三烯化合物及其作为胆汁酸调节剂的用途
US11801226B2 (en)	2018-06-20	2023-10-31	Albireo Ab	Pharmaceutical formulation of odevixibat
PL3810581T3 (pl)	2018-06-20	2025-04-28	Albireo Ab	Modyfikacje kryształu odewiksibatu
US10722457B2 (en)	2018-08-09	2020-07-28	Albireo Ab	Oral cholestyramine formulation and use thereof
US11007142B2 (en)	2018-08-09	2021-05-18	Albireo Ab	Oral cholestyramine formulation and use thereof
US11549878B2 (en)	2018-08-09	2023-01-10	Albireo Ab	In vitro method for determining the adsorbing capacity of an insoluble adsorbant
TWI835997B (zh)	2019-02-06	2024-03-21	瑞典商艾爾比瑞歐公司	苯并噻氮呯化合物及其用作膽酸調節劑之用途
CN118852054A (zh)	2019-02-06	2024-10-29	阿尔比里奥公司	苯并硫杂二氮杂环庚三烯化合物及其用作胆汁酸调节剂的用途
EP3923943B1 (de)	2019-02-12	2024-07-31	Mirum Pharmaceuticals, Inc.	Genotyp und dosisabhängige reaktion auf einen asbti bei patienten mit gallensalzexportpumpenmangel
KR20220061110A (ko)	2019-09-09	2022-05-12	이에이 파마 가부시키가이샤	1,5-벤조티아제핀 화합물을 제조하기 위한 방법
US11014898B1 (en)	2020-12-04	2021-05-25	Albireo Ab	Benzothiazepine compounds and their use as bile acid modulators
WO2021110883A1 (en)	2019-12-04	2021-06-10	Albireo Ab	Benzothia(di)azepine compounds and their use as bile acid modulators
WO2021110887A1 (en)	2019-12-04	2021-06-10	Albireo Ab	Benzothiazepine compounds and their use as bile acid modulators
ES2973355T3 (es)	2019-12-04	2024-06-19	Albireo Ab	Compuestos de benzotia(di)azepina y su uso como moduladores del ácido biliar
CA3158175A1 (en) *	2019-12-04	2021-06-10	Per-Goran Gillberg	Benzothiazepine compounds and their use as bile acid modulators
IL293379B2 (en)	2019-12-04	2026-04-01	Albireo Ab	Benzothia(dia)azepine compounds and their use as bile acid modulators
JP7696898B2 (ja)	2019-12-04	2025-06-23	アルビレオ・アクチボラグ	ベンゾチア（ジ）アゼピン化合物及び胆汁酸モジュレータとしてのそれらの使用
TWI877263B (zh)	2019-12-04	2025-03-21	瑞典商艾爾比瑞歐公司	苯并噻二氮呯化合物及其作為膽酸調節劑之用途
AR120676A1 (es)	2019-12-04	2022-03-09	Albireo Ab	Compuestos de benzoti(di)azepina y su uso como ácido biliar
WO2021110884A1 (en)	2019-12-04	2021-06-10	Albireo Ab	Benzothia(di)azepine compounds and their use as bile acid modulators
EP4069247B1 (de)	2019-12-04	2025-03-26	Albireo AB	Benzothiadiazepinverbindungen und ihre verwendung als gallensäuremodulatoren
EP4188541B1 (de)	2020-08-03	2024-12-25	Albireo AB	Benzothia(di)azepin-verbindungen und ihre verwendung als gallensäuremodulatoren
WO2022029101A1 (en)	2020-08-03	2022-02-10	Albireo Ab	Benzothia(di)azepine compounds and their use as bile acid modulators
CA3196488A1 (en)	2020-11-12	2022-05-19	Albireo Ab	Odevixibat for treating progressive familial intrahepatic cholestasis (pfic)
BR112023010799A2 (pt)	2020-12-04	2023-10-03	Albireo Ab	Compostos de benzotia(di)azepina e seus usos como moduladores de ácidos biliares
TW202313579A (zh)	2021-06-03	2023-04-01	瑞典商艾爾比瑞歐公司	苯并噻(二)氮呯(benzothia(di)azepine)化合物及其作為膽酸調節劑之用途
WO2023039276A1 (en) *	2021-09-13	2023-03-16	Curtails Llc	Use of ibat inhibitors and antimicrobials for the treatment of diseases
EP4511038A1 (de)	2022-04-22	2025-02-26	Albireo AB	Subkutane verabreichung eines asbt-hemmers
KR20250022025A (ko)	2022-06-09	2025-02-14	알비레오 에이비	간염 치료
CN119487013A (zh)	2022-07-05	2025-02-18	阿尔比里奥公司	苯并硫杂(二)氮杂环庚三烯化合物及其作为胆汁酸调节剂的用途
AU2023390975A1 (en)	2022-12-09	2025-06-05	Albireo Ab	Asbt inhibitors in the treatment of renal diseases
WO2025146507A1 (en)	2024-01-05	2025-07-10	Albireo Ab	Benzothia(di)azepine compounds and their use as bile acid modulators
WO2025146508A1 (en)	2024-01-05	2025-07-10	Albireo Ab	Benzothia(di)azepine compounds and their use as bile acid modulators

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4900757A (en)	1988-12-08	1990-02-13	Merrell Dow Pharmaceuticals Inc.	Hypocholesterolemic and antiatherosclerotic uses of bix(3,5-di-tertiary-butyl-4-hydroxyphenylthio)methane
JPH05186357A (ja)	1991-12-31	1993-07-27	Shigeo Ochi	飲食物消化分解産物吸収抑制手段
GB9203347D0 (en)	1992-02-17	1992-04-01	Wellcome Found	Hypolipidaemic compounds
JP2658783B2 (ja) *	1992-12-10	1997-09-30	田辺製薬株式会社	抗動脈硬化剤
IL108634A0 (en)	1993-02-15	1994-05-30	Wellcome Found	Hypolipidaemic heterocyclic compounds, their prepatation and pharmaceutical compositions containing them
ZA941003B (en)	1993-02-15	1995-08-14	Wellcome Found	Hypolipidaemic compounds
ZA956647B (en)	1994-08-10	1997-02-10	Wellcome Found	Hypolipidaemic compounds.
US5994391A (en)	1994-09-13	1999-11-30	G.D. Searle And Company	Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
CN1084741C (zh)	1994-09-13	2002-05-15	孟山都公司	具有回肠胆汁酸转运和牛磺胆酸盐摄入抑制剂作用的新的苯并硫杂䓬
GB9423172D0 (en) *	1994-11-17	1995-01-04	Wellcom Foundation The Limited	Hypolipidemic benzothiazepines
HUP9903047A3 (en)	1996-03-11	2002-12-28	G D Searle & Co Chicago	Novel benzothiazepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
GB9704208D0 (en)	1997-02-28	1997-04-16	Glaxo Group Ltd	Chemical compounds
PL336415A1 (en)	1997-03-11	2000-06-19	Searle & Co	Combined therapy employing ileic bile acid transport inhibiting benzothiepins as well as a hmg co-enzyme reductase inhibitors
DK0864582T3 (da) *	1997-03-14	2003-09-29	Aventis Pharma Gmbh	Hypolidemiske 1,4-benzothiazepin-1,1-dioxider
AUPO763197A0 (en)	1997-06-30	1997-07-24	Sigma Pharmaceuticals Pty Ltd	Health supplement
ATE234829T1 (de)	1997-12-19	2003-04-15	Searle & Co	Verfahren zu herstellung von enantiomerisch- anreicherte tetrahydrobenzothiepin oxyden
GB9800428D0 (en) *	1998-01-10	1998-03-04	Glaxo Group Ltd	Chemical compounds
DE19825804C2 (de)	1998-06-10	2000-08-24	Aventis Pharma Gmbh	1,4-Benzothiepin-1,1-dioxidderivate, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel
PT1140190E (pt)	1998-12-23	2003-02-28	Searle Llc	Combinacoes de inibidores do transporte ileal dos acidos biliares e agentes sequestrantes dos acidos biliares usadas para problemas cardiovasculares
KR20020002367A (ko)	1998-12-23	2002-01-09	윌리암스 로저 에이	심혈관 징후를 위한 조합물
JP2002533415A (ja)	1998-12-23	2002-10-08	ジー．ディー．サールエルエルシー	心臓血管に適用するための回腸胆汁酸輸送阻害剤およびニコチン酸誘導体の組み合わせ
WO2000038727A1 (en)	1998-12-23	2000-07-06	G.D. Searle Llc	Combinations of ileal bile acid transport inhibitors and fibric acid derivatives for cardiovascular indications
JP2002533412A (ja)	1998-12-23	2002-10-08	ジー．ディー．サールエルエルシー	心臓血管に適用するための回腸胆汁酸輸送阻害剤およびコレステリルエステル転送タンパク質阻害剤の組み合わせ
JP2002536440A (ja)	1999-02-12	2002-10-29	ジー．ディー．サールエルエルシー	回腸胆汁酸輸送およびタウロコール酸塩取り込みの阻害剤としての活性を有する新規１，２−ベンゾチアゼピン
DE19916108C1 (de)	1999-04-09	2001-01-11	Aventis Pharma Gmbh	Mit Zuckerresten substituierte 1,4-Benzothiazepin-1,1-dioxidderivate, Verfahren zu deren Herstellung und deren Verwendung
SE9901387D0 (sv)	1999-04-19	1999-04-19	Astra Ab	New pharmaceutical foromaulations
US6287609B1 (en)	1999-06-09	2001-09-11	Wisconsin Alumni Research Foundation	Unfermented gel fraction from psyllium seed husks
JP2003523336A (ja)	2000-02-18	2003-08-05	メルクエンドカムパニーインコーポレーテッド	糖尿病及び脂質障害のためのアリールオキシ酢酸
SE0000772D0 (sv)	2000-03-08	2000-03-08	Astrazeneca Ab	Chemical compounds
WO2001068096A2 (en)	2000-03-10	2001-09-20	Pharmacia Corporation	Combination therapy for the prophylaxis and treatment of hyperlipidemic conditions and disorders
US6586434B2 (en)	2000-03-10	2003-07-01	G.D. Searle, Llc	Method for the preparation of tetrahydrobenzothiepines
US20020183307A1 (en)	2000-07-26	2002-12-05	Tremont Samuel J.	Novel 1,4-benzothiazephine and 1,5-benzothiazepine compounds as inhibitors of apical sodium co-dependent bile acid transport and taurocholate uptake
SE0003766D0 (sv)	2000-10-18	2000-10-18	Astrazeneca Ab	Novel formulation
EG26979A (en) *	2000-12-21	2015-03-01	Astrazeneca Ab	Chemical compounds
WO2002053548A1 (fr)	2000-12-27	2002-07-11	Banyu Pharmaceutical Co.,Ltd.	Derives de la benzothiazepine
GB0121622D0 (en)	2001-09-07	2001-10-31	Astrazeneca Ab	Chemical compounds
GB0121621D0 (en)	2001-09-07	2001-10-31	Astrazeneca Ab	Chemical compounds
AU2002329387B2 (en)	2001-09-08	2007-06-07	Albireo Ab	Benzothiazepine and benzothiadiazepine derivatives with ileal bile acid transport (IBAT) inhibitory activity for the treatment hyperlipidaemia
GB0201850D0 (en)	2002-01-26	2002-03-13	Astrazeneca Ab	Therapeutic treatment
GB0209467D0 (en)	2002-04-25	2002-06-05	Astrazeneca Ab	Chemical compounds
GB0213669D0 (en)	2002-06-14	2002-07-24	Astrazeneca Ab	Chemical compounds
GB0216321D0 (en)	2002-07-13	2002-08-21	Astrazeneca Ab	Therapeutic treatment
GB0304194D0 (en)	2003-02-25	2003-03-26	Astrazeneca Ab	Chemical compounds
GB0307918D0 (en)	2003-04-05	2003-05-14	Astrazeneca Ab	Therapeutic use

2001
- 2001-09-04 GB GBGB0121337.0A patent/GB0121337D0/en not_active Ceased
2002
- 2002-08-30 US US10/488,540 patent/US7192946B2/en not_active Expired - Fee Related
- 2002-08-30 IL IL16050302A patent/IL160503A0/xx unknown
- 2002-08-30 MX MXPA04002032A patent/MXPA04002032A/es active IP Right Grant
- 2002-08-30 BR BR0212277-4A patent/BR0212277A/pt not_active IP Right Cessation
- 2002-08-30 CN CNA028221575A patent/CN1599731A/zh active Pending
- 2002-08-30 KR KR10-2004-7003185A patent/KR20040029147A/ko not_active Ceased
- 2002-08-30 WO PCT/GB2002/003983 patent/WO2003020710A1/en not_active Ceased
- 2002-08-30 JP JP2003524981A patent/JP4441261B2/ja not_active Expired - Fee Related
- 2002-08-30 AT AT02755285T patent/ATE438634T1/de not_active IP Right Cessation
- 2002-08-30 CA CA002459346A patent/CA2459346A1/en not_active Abandoned
- 2002-08-30 ES ES02755285T patent/ES2329226T3/es not_active Expired - Lifetime
- 2002-08-30 DE DE60233239T patent/DE60233239D1/de not_active Expired - Lifetime
- 2002-08-30 EP EP02755285A patent/EP1430040B1/de not_active Expired - Lifetime
- 2002-08-30 NZ NZ531512A patent/NZ531512A/en unknown
- 2002-09-04 UY UY27431A patent/UY27431A1/es unknown
2004
- 2004-02-25 ZA ZA200401551A patent/ZA200401551B/en unknown
- 2004-03-03 NO NO20040924A patent/NO20040924L/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
KR20040029147A (ko)	2004-04-03
ES2329226T3 (es)	2009-11-24
WO2003020710A1 (en)	2003-03-13
CA2459346A1 (en)	2003-03-13
ATE438634T1 (de)	2009-08-15
UY27431A1 (es)	2003-03-31
JP4441261B2 (ja)	2010-03-31
MXPA04002032A (es)	2004-06-07
NO20040924L (no)	2004-04-21
GB0121337D0 (en)	2001-10-24
CN1599731A (zh)	2005-03-23
JP2005505554A (ja)	2005-02-24
DE60233239D1 (de)	2009-09-17
BR0212277A (pt)	2004-10-19
US20040254160A1 (en)	2004-12-16
IL160503A0 (en)	2004-07-25
EP1430040B1 (de)	2009-08-05
NZ531512A (en)	2005-10-28
EP1430040A1 (de)	2004-06-23
US7192946B2 (en)	2007-03-20

Publication	Publication Date	Title
ZA200401551B (en)	2004-11-24	Benzothiazepine derivatives.
US7238684B2 (en)	2007-07-03	Benzothiadiazepine derivatives, processes for their preparation and pharmaceutical compositions containing them
CA2431461C (en)	2011-02-08	1,5 benzothiazepines and their use as antihyperlipidemics
US7125864B2 (en)	2006-10-24	Benzothiazepine derivatives for the treatment of hyperlipidemia
US8067584B2 (en)	2011-11-29	Benzothiazepine derivatives
ZA200401797B (en)	2005-04-19	Benzothiepine ileal bile acid transport inhibitors.
ZA200410340B (en)	2005-10-20	Diphenylazetidinone derivatives for treating disorders of the lipid metabolism.
ZA200409860B (en)	2005-10-19	Peptides derivatives comprising thiazepine group for the treatment of hyperlipidemic conditions.
ZA200401798B (en)	2005-04-26	Benzothiazepine and benzothiadiazepine derivatives with ileal bile acid transport (IBAT) inhibitory activity for the treatment of hyperlipidaemia.
ZA200304266B (en)	2004-08-30	Chemical compounds.
AU2002321579A1 (en)	2003-03-18	Benzothiazepine derivatives
AU2002329386A1 (en)	2003-03-24	Benzothiepine ileal bile acid transport inhibitors
HK1056732B (en)	2007-09-21	1,5 benzothiazepines and their use as antihyperlipidemics