AU2012328453B2 - Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease - Google Patents

Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease Download PDF

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AU2012328453B2
AU2012328453B2 AU2012328453A AU2012328453A AU2012328453B2 AU 2012328453 B2 AU2012328453 B2 AU 2012328453B2 AU 2012328453 A AU2012328453 A AU 2012328453A AU 2012328453 A AU2012328453 A AU 2012328453A AU 2012328453 B2 AU2012328453 B2 AU 2012328453B2
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asbti
bile
bile acid
substituted
alkyl
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AU2012328453A1 (en
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Bronislava Gedulin
Michael GREY
Niall O'donnell
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Shire Human Genetics Therapies Inc
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Shire Human Genetics Therapies Inc
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Priority to AU2017210623A priority Critical patent/AU2017210623B2/en
Priority to AU2019226227A priority patent/AU2019226227B2/en
Assigned to SHIRE HUMAN GENETIC THERAPIES, INC. reassignment SHIRE HUMAN GENETIC THERAPIES, INC. Request for Assignment Assignors: LUMENA PHARMACEUTICALS LLC
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    • C07H13/00Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/12Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by acids having the group -X-C(=X)-X-, or halides thereof, in which each X means nitrogen, oxygen, sulfur, selenium or tellurium, e.g. carbonic acid, carbamic acid
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    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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    • A61K31/554Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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AU2012328453A 2011-10-28 2012-10-26 Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease Active AU2012328453B2 (en)

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AU2017210623A AU2017210623B2 (en) 2011-10-28 2017-08-04 Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease
AU2019226227A AU2019226227B2 (en) 2011-10-28 2019-09-06 Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease

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US201161553094P 2011-10-28 2011-10-28
US61/553,094 2011-10-28
US201261607487P 2012-03-06 2012-03-06
US61/607,487 2012-03-06
PCT/US2012/062303 WO2013063526A1 (en) 2011-10-28 2012-10-26 Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease

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AU2012328453B2 true AU2012328453B2 (en) 2017-05-04

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Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS57778B1 (sr) * 2010-11-04 2018-12-31 Albireo Ab Inhibitori crevnog transportera žučne kiseline (ibat) za lečenje bolesti jetre
EP2771003B1 (en) 2011-10-28 2017-04-19 Lumena Pharmaceuticals LLC Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
KR102051031B1 (ko) * 2011-10-28 2019-12-02 루메나 파마수티컬즈, 인코포레이티드 고담혈증 및 담즙 정체성 간 질환 치료용 담즙산 재순환 억제제
MX2015013193A (es) * 2013-03-15 2016-04-15 Lumena Pharmaceuticals Inc Inhibidores del reciclaje de acidos biliares para el tratamiento de colangitis esclerosante primaria y enfermedad inflamatoria intestinal.
JO3301B1 (ar) 2013-04-26 2018-09-16 Albireo Ab تعديلات بلورية على إيلوبيكسيبات
WO2015065983A1 (en) * 2013-10-29 2015-05-07 Lumena Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of gastrointestinal infections
WO2015175381A1 (en) 2014-05-12 2015-11-19 Conatus Pharmaceuticals, Inc. Treatment of the complications of chronic liver disease with caspase inhibitors
BR112016029129A2 (pt) 2014-06-13 2018-01-30 Inventiva compostos ppar para serem utilizados no tratamento de doenças fibróticas.
CA2952406A1 (en) 2014-06-25 2015-12-30 Ea Pharma Co., Ltd. Solid formulation and method for preventing or reducing coloration thereof
EP3012252A1 (en) 2014-10-24 2016-04-27 Ferring BV Crystal modifications of elobixibat
JP6356364B1 (ja) 2015-05-20 2018-07-11 アムジエン・インコーポレーテツド Apj受容体のトリアゾールアゴニスト
KR20180101418A (ko) 2015-12-31 2018-09-12 코나터스 파마슈티칼스, 인크. 간 질환의 치료에서의 카스파제 억제제의 사용 방법
US10786529B2 (en) 2016-02-09 2020-09-29 Albireo Ab Oral cholestyramine formulation and use thereof
US10441604B2 (en) 2016-02-09 2019-10-15 Albireo Ab Cholestyramine pellets and methods for preparation thereof
US10441605B2 (en) 2016-02-09 2019-10-15 Albireo Ab Oral cholestyramine formulation and use thereof
EP3452466B1 (en) 2016-05-03 2020-08-12 Amgen Inc. Heterocyclic triazole compounds as agonists of the apj receptor
CN108990420B (zh) 2016-05-29 2022-06-24 深圳市绘云生物科技有限公司 肝病相关生物标志物和其使用方法
US10736883B2 (en) 2016-11-16 2020-08-11 Amgen Inc. Triazole furan compounds as agonists of the APJ receptor
US10689367B2 (en) 2016-11-16 2020-06-23 Amgen Inc. Triazole pyridyl compounds as agonists of the APJ receptor
US11046680B1 (en) 2016-11-16 2021-06-29 Amgen Inc. Heteroaryl-substituted triazoles as APJ receptor agonists
US11191762B2 (en) 2016-11-16 2021-12-07 Amgen Inc. Alkyl substituted triazole compounds as agonists of the APJ Receptor
WO2018093579A1 (en) 2016-11-16 2018-05-24 Amgen Inc. Triazole phenyl compounds as agonists of the apj receptor
US11020395B2 (en) 2016-11-16 2021-06-01 Amgen Inc. Cycloalkyl substituted triazole compounds as agonists of the APJ receptor
EP3664781A1 (en) 2017-08-09 2020-06-17 Albireo AB Cholestyramine granules, oral cholestyramine formulations and use thereof
EP3704122B1 (en) 2017-11-03 2021-09-01 Amgen Inc. Fused triazole agonists of the apj receptor
US20210077413A1 (en) * 2018-01-30 2021-03-18 Pharmascience Inc. Cholestyramine formulations and methods of use
US11807624B2 (en) 2018-05-01 2023-11-07 Amgen Inc. Substituted pyrimidinones as agonists of the APJ receptor
JP7391048B2 (ja) * 2018-06-05 2023-12-04 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
US10793534B2 (en) 2018-06-05 2020-10-06 Albireo Ab Benzothia(di)azepine compounds and their use as bile acid modulators
US11801226B2 (en) 2018-06-20 2023-10-31 Albireo Ab Pharmaceutical formulation of odevixibat
MX2020013774A (es) * 2018-06-20 2021-03-02 Albireo Ab Modificaciones de cristales de odevixibat.
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
US10722457B2 (en) 2018-08-09 2020-07-28 Albireo Ab Oral cholestyramine formulation and use thereof
US10975045B2 (en) 2019-02-06 2021-04-13 Aibireo AB Benzothiazepine compounds and their use as bile acid modulators
JP7504109B2 (ja) 2019-02-06 2024-06-21 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
US10941127B2 (en) 2019-02-06 2021-03-09 Albireo Ab Benzothiadiazepine compounds and their use as bile acid modulators
WO2020167981A1 (en) 2019-02-12 2020-08-20 Mirum Pharmaceuticals, Inc. Methods for increasing growth in pediatric subjects having cholestatic liver disease
WO2020194531A1 (ja) * 2019-03-26 2020-10-01 国立大学法人東北大学 血中尿毒症物質の低減剤
CN114761080B (zh) 2019-12-04 2024-07-23 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
US11014898B1 (en) 2020-12-04 2021-05-25 Albireo Ab Benzothiazepine compounds and their use as bile acid modulators
CA3158184A1 (en) 2019-12-04 2021-08-10 Albireo Ab Benzothiadiazepine compounds and their use as bile acid modulators
DK4069360T3 (da) 2019-12-04 2024-02-26 Albireo Ab Benzothia(di)azepinforbindelser og anvendelse deraf som galdesyremodulatorer
CA3158276A1 (en) 2019-12-04 2021-06-10 Per-Goran Gillberg Benzothia(di)azepine compounds and their use as bile acid modulators
CA3186857A1 (en) 2020-08-03 2022-02-10 Per-Goran Gillberg Benzothia(di)azepine compounds and their use as bile acid modulators
CN116710100A (zh) * 2020-11-12 2023-09-05 阿尔比里奥公司 用于治疗进行性家族性肝内胆汁淤积(pfic)的奥德昔巴特
CA3196488A1 (en) 2020-11-12 2022-05-19 Albireo Ab Odevixibat for treating progressive familial intrahepatic cholestasis (pfic)
CN116583504A (zh) 2020-12-04 2023-08-11 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
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
TW202333723A (zh) * 2021-10-26 2023-09-01 美商米魯姆製藥公司 頂端鈉依賴型膽酸轉運蛋白抑制劑(asbti)之給藥方法
TW202333724A (zh) * 2021-11-05 2023-09-01 美商米魯姆製藥公司 以迴腸膽酸轉運蛋白(ibat)抑制劑治療以增加無事件存活期(efs)
JP2023160476A (ja) * 2022-04-22 2023-11-02 株式会社三共 遊技機
CN120091821A (zh) * 2022-10-23 2025-06-03 米鲁姆制药公司 治疗进行性家族性肝内胆汁淤积症的方法
AU2023390972A1 (en) * 2022-12-09 2025-06-05 Albireo Ab Cocrystals of odevixibat

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000062810A1 (en) * 1999-04-19 2000-10-26 Astrazeneca Ab An oral formulation for ileum administering comprising an inhibitor compound of the ileal bile acid transport
US6441022B1 (en) * 1998-06-10 2002-08-27 Aventis Pharma Deutschland Gmbh Benzothiepine 1,1-dioxide derivatives, a process for their preparation, pharmaceuticals comprising these compounds, and their use
US20040067872A1 (en) * 2001-11-02 2004-04-08 G.D. Searle, Llc Novel mono- and di-fluorinated benzothiepine compouds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake
US20050009805A1 (en) * 2002-08-28 2005-01-13 Takehiko Sasahara Novel quaternary ammonium compounds
US20070190041A1 (en) * 2004-02-27 2007-08-16 Ashai Kasei Pharama Corporation Novel benzothiazepine and bensothiepine compounds
US20100035961A1 (en) * 2006-11-14 2010-02-11 Sanofi-Aventis Deutschland Gmbh Novel 1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof
US20100130472A1 (en) * 2008-11-26 2010-05-27 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of obesity and diabetes
WO2012064266A1 (en) * 2010-11-04 2012-05-18 Albireo Ab Ibat inhibitors for the treatment of liver diseases

Family Cites Families (267)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE580490A (fr) 1958-07-15 1960-01-08 Merck & Co Inc Compositions et procédés pour abaisser la teneur en cholestérol du sang
US3383281A (en) 1961-09-22 1968-05-14 Merck & Co Inc Method for binding bile acids in vivo
US3308020A (en) 1961-09-22 1967-03-07 Merck & Co Inc Compositions and method for binding bile acids in vivo including hypocholesteremics
US3287370A (en) 1965-06-08 1966-11-22 Mcneilab Inc Tetrahydrobenzothiepins
US3389144A (en) 1965-06-08 1968-06-18 Mcneilab Inc 5-pyridyl-2, 3, 4, 5-tetrahydrobenzothiepin-5-ols
DE1593760A1 (de) 1967-02-01 1972-06-08 Boehringer Sohn Ingelheim Verfahren zur Herstellung neuer Benz-epinderivate
US3444176A (en) 1967-04-28 1969-05-13 Mcneilab Inc Certain 4-diloweralkylamino-lower alkyl - 5 - pyridyl (or phenyl)-2,3-dihydro - 1 - benzothiepins and derivatives thereof
GB1269551A (en) 1969-03-27 1972-04-06 Science Union & Cie New tricyclic derivatives and process for their manufacture
NL7017227A (enExample) 1969-12-27 1971-06-29
US3694446A (en) 1970-02-24 1972-09-26 William J Houlihan 5-(substituted-benzyl)-benzocycloheptenes and-1-benzthiepines
CH537404A (de) 1970-09-24 1973-05-31 Sandoz Ag Verfahren zur Herstellung neuer Thiophenderivate
CH531000A (de) 1970-03-11 1972-11-30 Sandoz Ag Verfahren zur Herstellung neuer Benzocycloheptathiophene
US3821249A (en) 1970-03-13 1974-06-28 En Nom Collectif Science Union Dibenzothiazefin derivatives
US3758528A (en) 1970-03-13 1973-09-11 Science Union & Cie Tricyclic compounds
GB1348642A (en) 1970-10-15 1974-03-20 Howard A N Hypocholesterolaemic compositions
US3769399A (en) 1971-03-05 1973-10-30 L Hagerman Intestinal bile acid binding process and compositions
JPS4711953U (enExample) 1971-03-08 1972-10-12
GB1428110A (en) 1972-05-30 1976-03-17 Reckitt & Colmann Prod Ltd Pharmaceutical antihypertensive and vasodilator compositions
US3974272A (en) 1972-09-01 1976-08-10 Merck & Co., Inc. Palatable cholestyramine coacervate compositions
CH582699A5 (enExample) 1973-03-26 1976-12-15 Sandoz Ag
US4044010A (en) 1973-03-30 1977-08-23 Hoffmann-La Roche Inc. Dibenzo[b,f] thiepins bearing piperazinyl substitution
US3954764A (en) 1973-03-30 1976-05-04 Hoffmann-La Roche Inc. Dibenzo [b,f]thiepins bearing piperazinyl substitution
CH593970A5 (en) 1973-03-30 1977-12-30 Hoffmann La Roche 10-(4-Substd. piperazino) dibenzo (b,f) thiepins - CNS depressants without cataleptic side-effects
US3928383A (en) 1973-06-08 1975-12-23 Hoffmann La Roche Propynylamine-substituted dibenzo{8 b,f{9 thiepins and dibenz{8 b,f{9 oxepins
SE7504508L (sv) 1974-05-10 1975-11-11 Ciba Geigy Ag Nya heterocykliska s-imino-s-oxider.
SE420725B (sv) 1974-09-26 1981-10-26 Ciba Geigy Ag Sett att framstella 2,3-dihydro-1-benstiepin-4-karboxylsyraamider
US4252790A (en) 1974-10-23 1981-02-24 Interx Research Corporation Method for treating gastric ulcer-prone patients
GB1566609A (en) 1977-03-10 1980-05-08 Reckitt & Colmann Prod Ltd Pharmaceutical compositions containing cholestyramine and alginic acid
US4207239A (en) 1977-10-31 1980-06-10 The Upjohn Company Benzothiepins
US4153612A (en) 1977-10-31 1979-05-08 The Upjohn Company 2-Benzoxepins
US4251526A (en) 1977-10-31 1981-02-17 Mccall John M 2-Benzothiepins and compositions and methods of use therefore
US4247533A (en) 1978-05-01 1981-01-27 The Rockefeller University Hemoglobin A1c radioimmunoassay
IT1106718B (it) 1978-12-21 1985-11-18 Alfa Farmaceutici Spa Composizioni a base di resine anioniche salificate farmacologicamente attive
US5169857A (en) 1988-01-20 1992-12-08 Bayer Aktiengesellschaft 7-(polysubstituted pyridyl)-hept-6-endates useful for treating hyperproteinaemia, lipoproteinaemia or arteriosclerosis
AU548253B2 (en) 1981-05-11 1985-12-05 Pierre Fabre S.A. Benzoxepine derivatives and sulphur and nitrogen analogues thereof
US4647459A (en) 1983-07-20 1987-03-03 Warner-Lambert Company Confectionery compositions containing magnesium trisilicate adsorbates
US4771072A (en) 1985-01-10 1988-09-13 Tanabe Seiyaku Co., Ltd. Alkoxynaphthalene derivatives
AU597671B2 (en) 1986-06-20 1990-06-07 Suntory Limited 2-Phenylbenzoxepin derivative
JPS6310746A (ja) 1986-07-01 1988-01-18 Tanabe Seiyaku Co Ltd ナフタレン誘導体
US4895723A (en) 1986-09-08 1990-01-23 Amer And Company Cholestyramine compositions and method for preparation thereof
US4814354A (en) 1986-09-26 1989-03-21 Warner-Lambert Company Lipid regulating agents
ZA876930B (en) 1986-10-07 1988-05-25 Hoffmann La Roche Pharmaceutical compositions
AU626881B2 (en) 1988-07-14 1992-08-13 F. Hoffmann-La Roche Ag Benzofused heterocyclics used as pharmaceuticals
US5164387A (en) 1988-07-14 1992-11-17 Hoffmann-Laroche Inc. Condensed heterocyclic compounds
US5158943A (en) 1988-11-21 1992-10-27 Takeda Chemical Industries, Ltd. Sulfur-containing heterocyclic compounds
US4874744A (en) 1989-03-13 1989-10-17 University Of Cincinnati Method of using melanocyte stimulating hormone as dermatis treatment
US5275823A (en) 1989-04-27 1994-01-04 Smith Kline & French Laboratories Ltd. Pharmaceutical compositions
DE3930696A1 (de) 1989-09-14 1991-03-28 Hoechst Ag Gallensaeurederivate, verfahren zu ihrer herstellung, verwendung als arzneimittel
US4997665A (en) 1989-10-05 1991-03-05 Michigan Biotechnology Institute Dietary fibers and a process for their production
FR2661676A1 (fr) 1990-05-02 1991-11-08 Lipha Derives d'amino benzocycloalcanes, procedes de preparation et medicaments les contenant.
NZ240846A (en) 1990-12-06 1994-04-27 Hoechst Ag Dimeric bile acid derivatives; preparatory processes and pharmaceutical compositions
IT1245890B (it) 1991-04-12 1994-10-25 Alfa Wassermann Spa Formulazioni farmaceutiche per uso orale gastroresistenti contenenti acidi biliari.
AU1886892A (en) 1991-04-12 1992-11-17 Schering Corporation Bicyclic amides as inhibitors of acyl-coenzyme a: cholesterol acyl transferase
ATE175954T1 (de) 1991-10-17 1999-02-15 Shionogi & Co Verfahren zum herstellen von lignin-analoga und ausgangsprodukte dafür
AU653658B2 (en) 1991-12-20 1994-10-06 Hoechst Aktiengesellschaft Polymers and oligomers of bile acid derivatives, process for their preparation and their use as pharmaceuticals
GB9203347D0 (en) 1992-02-17 1992-04-01 Wellcome Found Hypolipidaemic compounds
DK0573848T3 (da) 1992-06-12 1998-08-10 Hoechst Ag Galdesyrederivater, fremgangsmåde til deres fremstilling og anvendelse af disse forbindelser som lægemidler
US5415872A (en) 1992-06-22 1995-05-16 Digestive Care Inc. Compositions of gastric acid-resistant microspheres containing salts of bile acids
FR2698873B1 (fr) 1992-12-07 1995-02-24 Lipha Benzocycloheptènes, benzoxépines et benzothiépines activateurs des canaux potassiques, procédé de préparation, composition pharmaceutique les contenant.
IL108634A0 (en) 1993-02-15 1994-05-30 Wellcome Found Hypolipidaemic heterocyclic compounds, their prepatation and pharmaceutical compositions containing them
IL108633A (en) 1993-02-15 1998-07-15 Wellcome Found History of Benzothiazepine Hypolipidemic Preparation and Pharmaceutical Preparations Containing Them
US5594001A (en) 1993-04-08 1997-01-14 The Dupont Merck Pharmaceutical Company Polycyclic systems, and derivatives thereof, as neurotransmitter release enhancers useful in the treatment of cognitive disorders
EP0646570B1 (en) 1993-04-16 1998-06-24 Shionogi & Co., Ltd. Process for producing lignan compound
DE4314583A1 (de) 1993-04-29 1994-11-03 Astra Chem Gmbh Colestyramin enthaltende Zusammensetzung und Verfahren zu deren Herstellung
TW289021B (enExample) 1993-05-08 1996-10-21 Hoechst Ag
TW289020B (enExample) 1993-05-08 1996-10-21 Hoechst Sktiengesellschaft
EP0624593A3 (de) 1993-05-08 1995-06-07 Hoechst Ag Gallensäurederivate, Verfahren zu ihrer Herstellung und Verwendung dieser Verbindungen als Arzneimittel.
US5607669A (en) 1994-06-10 1997-03-04 Geltex Pharmaceuticals, Inc. Amine polymer sequestrant and method of cholesterol depletion
DK0640344T3 (da) 1993-08-30 1999-07-05 Medichemie Ag Ursodesoxycholsyreholdigt lægemiddel i flydende administreringsform
US5589358A (en) 1993-12-29 1996-12-31 Univ Wake Forest Ileal bile acid transporter compositions and methods
US5491152A (en) 1994-03-23 1996-02-13 The Du Pont Merck Pharmaceutical Company Derivatives of cyclic ethers and sulfides for the treatment of atherosclerosis
TW474813B (en) 1994-06-10 2002-02-01 Geltex Pharma Inc Alkylated composition for removing bile salts from a patient
KR970005178Y1 (ko) 1994-07-06 1997-05-24 김상수 개량형 노통연관 보일러
ZA956647B (en) 1994-08-10 1997-02-10 Wellcome Found Hypolipidaemic compounds.
WO1996008484A1 (en) 1994-09-13 1996-03-21 Monsanto Company Novel benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
US6262277B1 (en) 1994-09-13 2001-07-17 G.D. Searle And Company Intermediates and processes for the preparation of benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
US6268392B1 (en) 1994-09-13 2001-07-31 G. D. Searle & Co. Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors
US6107494A (en) 1994-09-13 2000-08-22 G.D. Searle And Company Substituted 5-aryl-benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
US6642268B2 (en) 1994-09-13 2003-11-04 G.D. Searle & Co. Combination therapy employing ileal bile acid transport inhibiting benzothipines and HMG Co-A reductase inhibitors
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
US5547975A (en) 1994-09-20 1996-08-20 Talley; John J. Benzopyranopyrazolyl derivatives for the treatment of inflammation
US6034118A (en) 1994-11-04 2000-03-07 Gilead Sciences, Inc. Thiepane compounds
GB9423172D0 (en) 1994-11-17 1995-01-04 Wellcom Foundation The Limited Hypolipidemic benzothiazepines
US5721103A (en) 1994-12-30 1998-02-24 Ligand Pharmaceuticals Incorporated Trienoic retinoid compounds and methods
US6861053B1 (en) 1999-08-11 2005-03-01 Cedars-Sinai Medical Center Methods of diagnosing or treating irritable bowel syndrome and other disorders caused by small intestinal bacterial overgrowth
TW438587B (en) 1995-06-20 2001-06-07 Takeda Chemical Industries Ltd A pharmaceutical composition for prophylaxis and treatment of diabetes
US5886016A (en) 1995-09-15 1999-03-23 G.D. Searle & Co. Benzopyranopyrazolyl derivatives for the treatment of inflammation
PL186714B1 (pl) 1995-11-02 2004-02-27 Warner Lambert Co Kompozycja farmaceutyczna do regulowania stężenialipidów do ssaka
US6069167A (en) 1996-01-16 2000-05-30 University Technology Corporation Use of antioxidant agents to treat cholestatic liver disease
GB9601697D0 (en) 1996-01-27 1996-03-27 Pfizer Ltd Therapeutic agents
JP2001526627A (ja) 1996-03-11 2001-12-18 ジー.ディー.サール アンド カンパニー 回腸胆汁酸輸送及びタウロコール酸塩吸収の阻害剤としての活性を有する新規ベンゾチエピン類
DE19616486C5 (de) 1996-04-25 2016-06-30 Royalty Pharma Collection Trust Verfahren zur Senkung des Blutglukosespiegels in Säugern
WO1998007749A1 (en) 1996-08-23 1998-02-26 Human Genome Sciences, Inc. Novel human growth factors
JPH1072371A (ja) 1996-08-28 1998-03-17 Sankyo Co Ltd 回腸型胆汁酸トランスポーター阻害剤
US6251852B1 (en) 1996-09-18 2001-06-26 Merck & Co., Inc. Combination therapy for reducing the risks associated with cardiovascular disease
US5908830A (en) 1996-10-31 1999-06-01 Merck & Co., Inc. Combination therapy for the treatment of diabetes and obesity
GB9704208D0 (en) 1997-02-28 1997-04-16 Glaxo Group Ltd Chemical compounds
BR9808013A (pt) 1997-03-11 2001-09-25 Searle & Co Terapia de combinação empregando benzotiepinas de inibição de transporte de ácido biliar ileal e inibidores de redutase de hmg co-a
DK0864582T3 (da) 1997-03-14 2003-09-29 Aventis Pharma Gmbh Hypolidemiske 1,4-benzothiazepin-1,1-dioxider
DE19845402B4 (de) 1998-10-02 2005-04-07 Aventis Pharma Deutschland Gmbh Mit Heterocyclen substituierte Propanolaminderivate, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
ES2223091T3 (es) 1997-04-04 2005-02-16 Aventis Pharma Deutschland Gmbh Derivados de propanolamina hipolipidemicos.
IT1292092B1 (it) 1997-06-05 1999-01-25 Geange Ltd Impiego di derivati eterociclici aromatici azotati nel trattamento topico di affezioni di tessuti epiteliali
WO1998056757A1 (fr) 1997-06-11 1998-12-17 Sankyo Company, Limited Derives de benzylamine
GB9714274D0 (en) 1997-07-08 1997-09-10 Zeneca Ltd Pharmaceutical composition
US6180660B1 (en) 1997-08-26 2001-01-30 Merck & Co., Inc. Cholesterol-lowering therapy
US6066336A (en) 1997-09-29 2000-05-23 Bristol-Myers Squibb Company Cholesterol-lowering tablets
US5900233A (en) 1997-10-16 1999-05-04 Day; Charles E. Epichlorohydrin and 1-(3-aminopropyl) imidazole copolymer and its use in treating irritable bowel syndrome
US6245797B1 (en) 1997-10-22 2001-06-12 Merck & Co., Inc. Combination therapy for reducing the risks associated with cardio-and-cerebrovascular disease
US6083497A (en) 1997-11-05 2000-07-04 Geltex Pharmaceuticals, Inc. Method for treating hypercholesterolemia with unsubstituted polydiallylamine polymers
DE19755480A1 (de) 1997-12-13 1999-06-24 Gruenenthal Gmbh Substituierte heterocyclische Benzocycloalkene und ihre Verwendung als analgetisch wirksame Substanzen
PT1042314E (pt) 1997-12-19 2003-07-31 Searle & Co Metodo de preparacao de oxidos de tetra-hidrobenzotiepina enantiomericamente enriquecidos
GB9800428D0 (en) 1998-01-10 1998-03-04 Glaxo Group Ltd Chemical compounds
EP2433623A1 (en) 1998-02-02 2012-03-28 Trustees Of Tufts College Use of dipeptidylpeptidase inhibitors to regulate glucose metabolism
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
JP2000026300A (ja) 1998-07-02 2000-01-25 Pola Chem Ind Inc 血管内皮細胞保護医薬組成物
EP1103552A4 (en) 1998-08-07 2003-01-15 Takeda Chemical Industries Ltd BENZOTHIEPINE DERIVATIVES, METHOD FOR THEIR PRODUCTION AND THEIR USE
US6096780A (en) 1998-08-20 2000-08-01 Takeda Chemical Industries, Ltd. Quaternary ammonium salts and their use
DE19845405C2 (de) 1998-10-02 2000-07-13 Aventis Pharma Gmbh Arylsubstituierte Propanolaminderivate und deren Verwendung
DE19845406C2 (de) 1998-10-02 2001-10-18 Aventis Pharma Gmbh Substituierte 1,3-Diaryl-2-pyridin-2-yl-3-(pyridin-2-ylamino)- propanolderivate, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
DE19845403B4 (de) 1998-10-02 2005-02-10 Aventis Pharma Deutschland Gmbh Mit Gallensäuren verknüpfte Propanolaminderivate, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
WO2000035889A1 (en) 1998-12-11 2000-06-22 Sankyo Company, Limited Substituted benzylamines
AU1690100A (en) 1998-12-21 2000-07-12 Takeda Chemical Industries Ltd. Benzothiepin-anilide derivatives, their production and their use for antagonizing ccr-5
CA2356156A1 (en) 1998-12-23 2000-07-06 G.D. Searle Llc Combinations of ileal bile acid transport inhibitors and bile acid sequestring agents for cardiovascular indications
CA2356607A1 (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
ATE241386T1 (de) 1998-12-23 2003-06-15 Searle Llc Kombinationen von ileumgallensäuretransports inhibitoren und cholesteryl ester transfer protein inhibitoren
EP1354604A1 (en) 1998-12-23 2003-10-22 G.D. Searle LLC. Combinations for cardiovascular indications
KR20020000139A (ko) 1999-02-12 2002-01-04 추후제출 회장 담즙산 수송 및 타우로콜산염 흡수의 억제제로서의활성을 보유하는 신규한 1,2-벤조티아제핀
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
US6309663B1 (en) 1999-08-17 2001-10-30 Lipocine Inc. Triglyceride-free compositions and methods for enhanced absorption of hydrophilic therapeutic agents
CZ290178B6 (cs) 1999-07-22 2002-06-12 Sankyo Company Limited Deriváty cyklobutenu
WO2001020331A1 (en) 1999-09-14 2001-03-22 Xenoport, Inc. Substrates and screening methods for transport proteins
WO2001034570A1 (en) 1999-11-08 2001-05-17 Sankyo Company, Limited Nitrogenous heterocycle derivatives
WO2001052823A2 (en) * 2000-01-20 2001-07-26 Noven Pharmaceuticals, Inc. Compositions to effect the release profile in the transdermal administration of drugs
EP1741445B1 (en) 2000-01-21 2013-08-14 Novartis AG Combinations comprising dipeptidylpeptidase-IV inhibitors and antidiabetic agents
SE0000772D0 (sv) 2000-03-08 2000-03-08 Astrazeneca Ab Chemical compounds
AU2001247331A1 (en) 2000-03-10 2001-09-24 Pharmacia Corporation Combination therapy for the prophylaxis and treatment of hyperlipidemic conditions and disorders
HK1052183A1 (zh) 2000-03-10 2003-09-05 Pharmacia Corporation 制造tetrahydrobenzothiepines的方法
WO2001077325A1 (fr) 2000-04-12 2001-10-18 Takeda Chemical Industries, Ltd. Nouvelle proteine de recepteur couple aux proteines g et adn de celle-ci
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
NZ523684A (en) 2000-07-28 2005-04-29 F New pharmaceutical composition
SE0003766D0 (sv) 2000-10-18 2000-10-18 Astrazeneca Ab Novel formulation
DE60142079D1 (de) 2000-11-17 2010-06-17 Banyu Pharma Co Ltd Verfahren zur suche nach komponenten, in dem das guanosintriphosphat- (gtp-) bindungsprotein gekoppeltes rezeptorprotein bg37 verwendet wird
WO2002050027A1 (de) 2000-12-21 2002-06-27 Aventis Pharma Deutschland Gmbh Neue diphenzylazetidinone, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung zur behandlung von lipidstoffwechselstörungen
EG26979A (en) 2000-12-21 2015-03-01 Astrazeneca Ab Chemical compounds
JP2004517920A (ja) 2001-01-26 2004-06-17 シェーリング コーポレイション 血管状態を治療するためのステロール吸収阻害剤と血液調整剤との組合せ
WO2002078625A2 (en) 2001-03-28 2002-10-10 Pharmacia Corporation Therapeutic combinations for cardiovascular and inflammatory indications
EA200400029A1 (ru) 2001-07-19 2004-08-26 Фармация Корпорейшн КОМБИНАЦИЯ АНТАГОНИСТА РЕЦЕПТОРА АЛЬДОСТЕРОНА И ИНГИБИТОРА ГМГ-КоА-РЕДУКТАЗЫ
NZ531293A (en) 2001-08-22 2005-08-26 Aventis Pharma Gmbh Pharamceuticals containing 1,4-benzothiepine-1,1-dioxide derivatives and another active substances such as ezetimibe, pamaqueside or tiqueside for treating lipid metabolism and atherosclerotic disorders
GB0121337D0 (en) 2001-09-04 2001-10-24 Astrazeneca Ab Chemical compounds
GB0121621D0 (en) 2001-09-07 2001-10-31 Astrazeneca Ab Chemical compounds
GB0121622D0 (en) 2001-09-07 2001-10-31 Astrazeneca Ab Chemical compounds
RU2305681C2 (ru) 2001-09-08 2007-09-10 Астразенека Аб Производные бензотиадиазепина, способ их получения (варианты)
WO2003022861A1 (en) 2001-09-13 2003-03-20 Bristol-Myers Squibb Company Process for the preparation of rebeccamycin and analogs thereof
AU2002336609B2 (en) 2001-09-21 2006-08-24 Merck Sharp & Dohme Corp. Treatment of xanthoma with azetidinone derivatives as sterol absorption inhibitors
WO2003028632A2 (en) 2001-10-01 2003-04-10 Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services, The Development of a preventive vaccine for filovirus infection in primates
AU2003207431A1 (en) 2002-01-17 2003-09-02 Pharmacia Corporation Novel alkyl/aryl hydroxy or keto thiepines.
GB0201850D0 (en) 2002-01-26 2002-03-13 Astrazeneca Ab Therapeutic treatment
US20040014806A1 (en) 2002-03-08 2004-01-22 Pharmacia Corporation Methods and compositions for lowering levels of blood lipids
US6987121B2 (en) * 2002-04-25 2006-01-17 Smithkline Beecham Corporation Compositions and methods for hepatoprotection and treatment of cholestasis
GB0209467D0 (en) 2002-04-25 2002-06-05 Astrazeneca Ab Chemical compounds
WO2003099264A1 (en) 2002-05-23 2003-12-04 Umd, Inc. Compositions and method for transmucosal drug delivery and cryoprotection
GB0213669D0 (en) 2002-06-14 2002-07-24 Astrazeneca Ab Chemical compounds
GB0215579D0 (en) 2002-07-05 2002-08-14 Astrazeneca Ab Chemical compounds
GB0216321D0 (en) 2002-07-13 2002-08-21 Astrazeneca Ab Therapeutic treatment
CN100494185C (zh) * 2002-08-28 2009-06-03 旭化成制药株式会社 新型季铵化合物
JP2006508188A (ja) 2002-11-06 2006-03-09 シェーリング コーポレイション 脱髄の処置のためのコレステロール吸収インヒビター
US20040122033A1 (en) 2002-12-10 2004-06-24 Nargund Ravi P. Combination therapy for the treatment of obesity
FR2848452B1 (fr) * 2002-12-12 2007-04-06 Aventis Pharma Sa Application des inhibiteurs de recapture intestinale des acides biliaires pour la prevention et le traitement de la maladie d'alzheimer
US20040138145A1 (en) 2002-12-12 2004-07-15 Aventis Pharma S.A. Application of intestinal biliary acid reuptake inhibitors for the prevention and treatment of alzheimer's disease
US20040147774A1 (en) 2002-12-20 2004-07-29 Aventis Pharma S.A. Novel chiral compounds derived from hexanoic acid esters, preparation process and intermediates, use in the synthesis of chiral 2-(bromomethyl)-2-ethylhexanoic acid
US20050031651A1 (en) 2002-12-24 2005-02-10 Francine Gervais Therapeutic formulations for the treatment of beta-amyloid related diseases
GB0304194D0 (en) 2003-02-25 2003-03-26 Astrazeneca Ab Chemical compounds
US7192944B2 (en) 2003-03-07 2007-03-20 Schering Corp. Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
US7208486B2 (en) 2003-03-07 2007-04-24 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
GB0307918D0 (en) 2003-04-05 2003-05-14 Astrazeneca Ab Therapeutic use
JP2005044778A (ja) 2003-07-19 2005-02-17 Samsung Sdi Co Ltd 電界発光素子
JP2005097216A (ja) 2003-09-26 2005-04-14 Kaneka Corp PPARγリガンド剤
CA2544309A1 (en) 2003-11-05 2005-05-26 Schering Corporation Combinations of lipid modulating agents and substituted azetidinones and treatments for vascular conditions
EP1564554A1 (en) 2004-02-12 2005-08-17 Pepscan Systems B.V. Method for the detection of early B cell populations in vaccine development
DE102004016845A1 (de) 2004-04-07 2005-10-27 Bayer Healthcare Ag Phenylthioessigsäure-Derivate und ihre Verwendung
WO2006017257A2 (en) 2004-07-12 2006-02-16 Phenomix Corporation Azetidinone derivatives
JP2008513465A (ja) 2004-09-15 2008-05-01 ザ プレジデント アンド フェロウズ オブ ハーバード カレッジ 肥満及び糖尿病の治療におけるerストレス低減
DE102004046623A1 (de) 2004-09-25 2006-03-30 Bayer Healthcare Ag Neue Pyrimidin-Derivate und ihre Verwendung
WO2006039334A1 (en) 2004-09-29 2006-04-13 Schering Corporation Combinations of substituted azetidonones and cb1 antagonists
EP1810689A4 (en) 2004-10-15 2009-07-22 Mitsubishi Tanabe Pharma Corp MEANS FOR THE PREVENTION AND / OR TREATMENT OF DIABETES
MX2007004934A (es) 2004-10-25 2007-06-12 Novartis Ag Combinacion de inhibidor de dpp-iv, anti-diabetico de ppar, y metformina.
AU2004325203A1 (en) 2004-11-24 2006-06-01 Seo Hong Yoo Dried forms of aqueous solubilized bile acid dosage formulation: preparation and uses thereof
DE102004058062A1 (de) 2004-12-02 2006-06-08 Bayer Healthcare Ag Cyclische Iminocarbamate und ihre Verwendung
CN102633730A (zh) 2004-12-03 2012-08-15 先灵公司 作为cb1拮抗剂的取代哌嗪
US20070032420A1 (en) 2005-02-09 2007-02-08 Entelos, Inc. Treating diabetes with glucagon-like peptide-1 secretagogues
US20060193895A1 (en) 2005-02-25 2006-08-31 Use-Techno Corporation Additive for food and beverage, pharmaceutical composition, GLUT4 translocator, and method for translocating GLUT4
DE102005027150A1 (de) 2005-03-12 2006-09-28 Bayer Healthcare Ag Pyrimidincarbonsäure-Derivate und ihre Verwendung
FR2883284A1 (fr) 2005-03-15 2006-09-22 Commissariat Energie Atomique Nouveaux derives dihydropyrimidines et leur utilisation comme agents anti-cancereux
UY29445A1 (es) 2005-03-30 2006-10-02 Generex Pharm Inc Composiciones para la transmisión transmucosa oral de la metformina
US20080031968A1 (en) 2005-04-01 2008-02-07 The Brigham And Women's Hospital, Inc. Methods for increasing cellular energy expenditure
EP1874330A2 (en) 2005-04-04 2008-01-09 Julius-Maximilians-Universität Würzburg Peptides that down regulate the activity of plasma membrane transporters including sodium-d-glucose cotransporter sglt1
WO2006105913A1 (en) 2005-04-04 2006-10-12 Julius-Maximillians-Universität Würzburg Tripeptides that down regulate the activity of plasma membrane transporters including sodium-d-glucose cotransporter sglt1
EP1877067A1 (en) 2005-04-26 2008-01-16 Microbia, Inc. 4-biarylyl-1-phenylazetidin-2-one glucuronide derivatives for hypercholesterolemia
DE102005020229A1 (de) 2005-04-30 2006-11-09 Bayer Healthcare Ag Verwendung von Indolin-Phenylsulfonamid-Derivaten
US20090074895A1 (en) 2005-05-02 2009-03-19 Vanadis Bioscience Ltd Composition and uses thereof
US20090131395A1 (en) 2005-05-05 2009-05-21 Microbia, Inc. Biphenylazetidinone cholesterol absorption inhibitors
WO2006122186A2 (en) 2005-05-10 2006-11-16 Microbia, Inc. 1,4-diphenyl-3-hydroxyalkyl-2-azetidinone derivatives for treating hypercholestrolemia
WO2006124713A2 (en) 2005-05-13 2006-11-23 Microbia, Inc. 4-biarylyl-1-phenylazetidin-2-ones
SMAP200700061A (it) * 2005-05-31 2007-12-28 Novartis Ag Trattamento delle malattie epatiche in cui il ferro svolge un ruolo nella patogenesi
DE102005033099A1 (de) 2005-07-15 2007-01-18 Sanofi-Aventis Deutschland Gmbh Neues 1,4-Benzothiazepin-1,1-Dioxidderivat mit verbesserten Eigenschaften, Verfahren zu dessen Herstellung, diese Verbindung enthaltende Arzneimittel und dessen Verwendung
US20070025953A1 (en) 2005-07-27 2007-02-01 Jones Michael R Co-therapy for diabetic conditions
WO2007035703A1 (en) 2005-09-20 2007-03-29 Schering Corporation 1- [ [1- [ (2-amin0-6-methyl-4-pyridinyl) methyl] -4-flu0r0-4-piperidinyl,] carbonyl] -4- [2- (2-pyridinyl) -3h-imidaz0 [4 , 5-b] pyridin-3-yl] piperidine useful as histamine h3 antagonist
AU2006297130B2 (en) 2005-09-30 2009-12-24 Novartis Ag DPP IV inhibitor for use in the treatment of autoimmune diseases and graft rejection
EP1948280A4 (en) 2005-10-24 2011-07-06 Andrew Young BILARY / PANCREATIC DERIVATION DEVICE AND METHOD FOR THE TREATMENT OF METABOLIC DISEASES AND OTHER DISEASES
US7705028B2 (en) 2005-12-19 2010-04-27 Glaxosmithkline Llc Farnesoid X receptor agonists
CA2634940A1 (en) 2005-12-21 2007-07-05 Schering Corporation Treatment of nonalcoholic fatty liver disease using cholesterol lowering agents and h3 receptor antagonist/inverse agonist
JP2009525954A (ja) 2006-01-13 2009-07-16 シェーリング コーポレイション Cb1モジュレーターとしてのジアリールピペリジン
BRPI0706623A2 (pt) 2006-01-18 2011-04-12 Schering Corp moduladores de receptor canabinóide
AU2007243131A1 (en) 2006-01-20 2007-11-08 Smithkline Beecham Corporation Use of sulfonamide derivatives in the treatment of disorders of the metabolism and the nervous system
JP2010517931A (ja) 2006-02-14 2010-05-27 インターセプト ファーマシューティカルズ, インコーポレイテッド Fxr媒介性の疾患または状態の予防または治療用のfxrリガンドとしての胆汁酸誘導体
DE102006009813A1 (de) 2006-03-01 2007-09-06 Bayer Healthcare Ag Verwendung von A2b/A1 Rezeptor Agonisten zur Modulation der Lipidspiegel
WO2007123949A2 (en) 2006-04-21 2007-11-01 Schering Corporation Cannabinoid receptor modulators
DE102006024024A1 (de) 2006-05-23 2007-11-29 Bayer Healthcare Aktiengesellschaft Substituierte Arylimidazolone und -triazolone sowie ihre Verwendung
DE102006026585A1 (de) 2006-06-07 2007-12-13 Bayer Healthcare Aktiengesellschaft Substituierte 4-Aryl-1,4-dihydro-1,6-naphthyridine und ihre Verwendung
DE102006026583A1 (de) 2006-06-07 2007-12-13 Bayer Healthcare Aktiengesellschaft Aryl-substituierte hetero-bicyclische Verbindungen und ihre Verwendung
CA2656320C (en) 2006-06-27 2015-04-28 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions
WO2008028037A2 (en) 2006-08-30 2008-03-06 Andrew Young Distender device and method for treatment of obesity and metabolic and other diseases
DE102006042143A1 (de) 2006-09-08 2008-03-27 Bayer Healthcare Aktiengesellschaft Neue substituierte Bipyridin-Derivate und ihre Verwendung
DE102006043520A1 (de) 2006-09-12 2008-03-27 Bayer Healthcare Ag 2-Phenoxynikotinsäure-Derivate und ihre Verwendung
DE102006043519A1 (de) 2006-09-12 2008-03-27 Bayer Healthcare Ag 4-Phenoxynikotinsäure-Derivate und ihre Verwendung
WO2008033431A1 (en) 2006-09-15 2008-03-20 Schering Corporation Spirocyclic azetidinone derivatives for the treatment of disorders of lipid metabolism, pain, diabetes and other disorders
CA2663500A1 (en) 2006-09-15 2008-03-20 Schering Corporation Spiro-condensed azetidine derivatives useful in treating pain, diabetes and disorders of lipid metabolism
WO2008033468A2 (en) 2006-09-15 2008-03-20 Schering Corporation Azetidine and azetidone derivatives useful in treating pain and disorders of lipid metabolism
US20080070984A1 (en) 2006-09-15 2008-03-20 Tran Pierre V Compositions and Methods of Treating Schizophrenia
CN101528227A (zh) 2006-09-15 2009-09-09 先灵公司 氮杂环丁酮衍生物及其使用方法
CA2663947A1 (en) 2006-09-15 2008-03-20 Schering Corporation Azetidine and azetidone derivatives useful in treating pain and disorders of lipid metabolism
CA2663502A1 (en) 2006-09-15 2008-03-20 Schering Corporation Azetidinone derivatives and methods of use thereof
WO2008033460A2 (en) 2006-09-15 2008-03-20 Schering Corporation Treating pain, diabetes, and lipid metabolism disorders
DE102006044696A1 (de) 2006-09-22 2008-03-27 Bayer Healthcare Ag 3-Cyano-5-thiazaheteroaryl-dihydropyridine und ihre Verwendung
WO2008039829A2 (en) 2006-09-26 2008-04-03 Ironwood Pharmaceuticals, Inc. Diphenylheterocycle cholesterol absorption inhibitors
CL2007003035A1 (es) 2006-10-24 2008-05-16 Smithkline Beechman Corp Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos,
US20080161400A1 (en) 2006-10-26 2008-07-03 Xenoport, Inc. Use of forms of propofol for treating diseases associated with oxidative stress
DE102006053637B4 (de) * 2006-11-14 2011-06-30 Sanofi-Aventis Deutschland GmbH, 65929 Neue mit Fluor substituierte 1,4-Benzothiepin-1,1-Dioxidderivate, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
EP2083832B1 (de) 2006-11-14 2011-01-05 Sanofi-Aventis Deutschland GmbH Neue 1,4-benzothiepin-1,1-dioxidderivate mit verbesserten eigenschaften, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2008067219A2 (en) 2006-11-29 2008-06-05 Kalypsys, Inc. Quinazolinone modulators of tgr5
DE102006056740A1 (de) 2006-12-01 2008-06-05 Bayer Healthcare Ag Cyclisch substituierte 3,5-Dicyano-2-thiopyridine und ihre Verwendung
DE102006056739A1 (de) 2006-12-01 2008-06-05 Bayer Healthcare Ag Substituierte 4-Amino-3,5-dicyano-2-thiopyridine und ihre Verwendung
WO2008088836A2 (en) 2007-01-16 2008-07-24 The Burnham Institute For Medical Research Compositions and methods for treatment of colorectal cancer
US8410083B2 (en) 2007-01-19 2013-04-02 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as TGR5 modulators and methods of use thereof
WO2008097976A1 (en) 2007-02-09 2008-08-14 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
DE102007009494A1 (de) 2007-02-27 2008-08-28 Bayer Healthcare Ag Substituierte 4-Aryl-1, 4-dihydro-1,6-naphthyridinamide und ihre Verwendung
US20100144864A1 (en) 2007-04-05 2010-06-10 Ironwood Pharmaceuticals, Inc. Soluble guanylate cyclase (sgc) modulators for treatment of lipid related disorders
WO2008130616A2 (en) 2007-04-19 2008-10-30 Schering Corporation Diaryl morpholines as cb1 modulators
AU2008288770B2 (en) 2007-08-23 2014-06-12 Theracosbio, Llc Benzylbenzene derivatives and methods of use
WO2009115398A1 (en) * 2008-03-18 2009-09-24 INSERM (Institut National de la Santé et de la Recherche Médicale) Vitamin d compounds for the treatment of biliary diseases
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
AU2009276507B2 (en) 2008-07-30 2015-11-19 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CA2744189C (en) 2008-11-19 2016-10-11 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
CA2744697C (en) 2008-11-26 2016-06-21 Satiogen Pharmaceuticals, Inc. Use of compositions comprising bile acids, salts, and mimics thereof for the treatment of obesity or diabetes
US20110065676A1 (en) 2009-06-24 2011-03-17 Schering Corporation Combination therapies comprising par1 antagonists with nar agonists
BR112012004284B8 (pt) 2009-08-25 2021-05-25 Ahab Sheps Jonathan ácidos biliares poli-hidroxilados para tratamento de transtornos biliares
WO2011075539A2 (en) * 2009-12-18 2011-06-23 Satiogen Pharmaceuticals, Inc. Treatment of obesity or diabetes with bile acid sequestrants
EP2995317A1 (en) * 2010-05-26 2016-03-16 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors and satiogens for treatment of diabetes, obesity, and inflammatory gastrointestinal conditions
EP2637667A4 (en) 2010-11-08 2014-06-25 Albireo Ab IBAT HEMMER FOR THE TREATMENT OF METABOLISM DISEASES AND RELATED ACCIDENTS
US20120114588A1 (en) 2010-11-08 2012-05-10 Albireo Ab Ibat inhibitors for treatment of metabolic disorders and related conditions
KR101890960B1 (ko) 2010-11-08 2018-09-28 알비레오 에이비 Ⅰbat 억제제 및 담즙산 바인더를 포함하는 약학적 조합물
KR102051031B1 (ko) 2011-10-28 2019-12-02 루메나 파마수티컬즈, 인코포레이티드 고담혈증 및 담즙 정체성 간 질환 치료용 담즙산 재순환 억제제
EP2771003B1 (en) 2011-10-28 2017-04-19 Lumena Pharmaceuticals LLC Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
US9007272B2 (en) 2012-07-19 2015-04-14 Tensorcom, Inc. Method and apparatus for the alignment of a 60 GHz endfire antenna
MX2015013193A (es) 2013-03-15 2016-04-15 Lumena Pharmaceuticals Inc Inhibidores del reciclaje de acidos biliares para el tratamiento de colangitis esclerosante primaria y enfermedad inflamatoria intestinal.
DK3435996T3 (da) 2016-03-31 2025-07-21 Genfit Elafibranor til anvendelse i behandlingen af primær biliær cholangitis
SG11201909168VA (en) 2017-04-18 2019-11-28 Genfit Combination comprising a ppar agonist such as elafibranor and an acetyl-coa carboxylase (acc) inhibitor

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6441022B1 (en) * 1998-06-10 2002-08-27 Aventis Pharma Deutschland Gmbh Benzothiepine 1,1-dioxide derivatives, a process for their preparation, pharmaceuticals comprising these compounds, and their use
WO2000062810A1 (en) * 1999-04-19 2000-10-26 Astrazeneca Ab An oral formulation for ileum administering comprising an inhibitor compound of the ileal bile acid transport
US20040067872A1 (en) * 2001-11-02 2004-04-08 G.D. Searle, Llc Novel mono- and di-fluorinated benzothiepine compouds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake
US20050009805A1 (en) * 2002-08-28 2005-01-13 Takehiko Sasahara Novel quaternary ammonium compounds
US20070190041A1 (en) * 2004-02-27 2007-08-16 Ashai Kasei Pharama Corporation Novel benzothiazepine and bensothiepine compounds
US20100035961A1 (en) * 2006-11-14 2010-02-11 Sanofi-Aventis Deutschland Gmbh Novel 1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof
US20100130472A1 (en) * 2008-11-26 2010-05-27 Satiogen Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of obesity and diabetes
WO2012064266A1 (en) * 2010-11-04 2012-05-18 Albireo Ab Ibat inhibitors for the treatment of liver diseases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Huang, HC et al (2005) J Med Chem 48: 5853-5868 *

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