OA10597A - Hypolipidemic 1,4-benzothiazepine-1, 1-dioxides - Google Patents
Hypolipidemic 1,4-benzothiazepine-1, 1-dioxides Download PDFInfo
- Publication number
- OA10597A OA10597A OA60961A OA60961A OA10597A OA 10597 A OA10597 A OA 10597A OA 60961 A OA60961 A OA 60961A OA 60961 A OA60961 A OA 60961A OA 10597 A OA10597 A OA 10597A
- Authority
- OA
- OAPI
- Prior art keywords
- phenyl
- tetrahydro
- dioxide
- hydrogen
- butyl
- Prior art date
Links
- 230000000055 hyoplipidemic effect Effects 0.000 title abstract description 3
- IVGHNDNOFMTFMK-UHFFFAOYSA-N 1$l^{6},4-benzothiazepine 1,1-dioxide Chemical class O=S1(=O)C=CN=CC2=CC=CC=C12 IVGHNDNOFMTFMK-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 133
- 238000000034 method Methods 0.000 claims abstract description 34
- 150000003839 salts Chemical class 0.000 claims abstract description 26
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 15
- 238000011282 treatment Methods 0.000 claims abstract description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 78
- 239000001257 hydrogen Substances 0.000 claims description 78
- 239000000203 mixture Substances 0.000 claims description 75
- 125000000217 alkyl group Chemical group 0.000 claims description 52
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 37
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 27
- -1 benzothiazepin-8-yl hydrogen sulfate Chemical compound 0.000 claims description 24
- 239000003613 bile acid Substances 0.000 claims description 24
- 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 description 20
- 229910052736 halogen Inorganic materials 0.000 claims description 19
- 150000002367 halogens Chemical class 0.000 claims description 19
- 241000124008 Mammalia Species 0.000 claims description 16
- 150000002431 hydrogen Chemical class 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 12
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 12
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 9
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 7
- 230000005764 inhibitory process Effects 0.000 claims description 7
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 5
- 229940009098 aspartate Drugs 0.000 claims description 5
- 230000003647 oxidation Effects 0.000 claims description 5
- 238000007254 oxidation reaction Methods 0.000 claims description 5
- 239000003112 inhibitor Substances 0.000 claims description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 4
- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
- 229910019142 PO4 Inorganic materials 0.000 claims description 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 3
- 239000013543 active substance Substances 0.000 claims description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 claims description 3
- 239000010452 phosphate Substances 0.000 claims description 3
- FHGWEHGZBUBQKL-UHFFFAOYSA-N 1,2-benzothiazepine Chemical compound S1N=CC=CC2=CC=CC=C12 FHGWEHGZBUBQKL-UHFFFAOYSA-N 0.000 claims description 2
- 210000000941 bile Anatomy 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- BYXNIXWNXSNWOH-WZONZLPQSA-N (3r,5r)-3-butyl-7,8-diethoxy-5-phenyl-2,3,4,5-tetrahydro-1$l^{6},4-benzothiazepine 1,1-dioxide Chemical compound C1([C@@H]2C3=CC(OCC)=C(OCC)C=C3S(=O)(=O)C[C@H](N2)CCCC)=CC=CC=C1 BYXNIXWNXSNWOH-WZONZLPQSA-N 0.000 claims 1
- VMJNTFXCTXAXTC-UHFFFAOYSA-N 2,2-difluoro-1,3-benzodioxole-5-carbonitrile Chemical group C1=C(C#N)C=C2OC(F)(F)OC2=C1 VMJNTFXCTXAXTC-UHFFFAOYSA-N 0.000 claims 1
- QBWKPGNFQQJGFY-QLFBSQMISA-N 3-[(1r)-1-[(2r,6s)-2,6-dimethylmorpholin-4-yl]ethyl]-n-[6-methyl-3-(1h-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine Chemical compound N1([C@H](C)C2=NSC(NC=3C4=NC=C(N4C=C(C)N=3)C3=CNN=C3)=C2)C[C@H](C)O[C@H](C)C1 QBWKPGNFQQJGFY-QLFBSQMISA-N 0.000 claims 1
- 229940125846 compound 25 Drugs 0.000 claims 1
- 238000013160 medical therapy Methods 0.000 claims 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 abstract description 4
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- 239000012453 solvate Substances 0.000 abstract 1
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- OISVCGZHLKNMSJ-UHFFFAOYSA-N 2,6-dimethylpyridine Chemical compound CC1=CC=CC(C)=N1 OISVCGZHLKNMSJ-UHFFFAOYSA-N 0.000 description 18
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 16
- 229960004132 diethyl ether Drugs 0.000 description 16
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 15
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- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- HYHCSLBZRBJJCH-UHFFFAOYSA-M sodium hydrosulfide Chemical compound [Na+].[SH-] HYHCSLBZRBJJCH-UHFFFAOYSA-M 0.000 description 1
- 229940001584 sodium metabisulfite Drugs 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 229940032147 starch Drugs 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 229910021653 sulphate ion Inorganic materials 0.000 description 1
- 235000011149 sulphuric acid Nutrition 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- WBWWGRHZICKQGZ-GIHLXUJPSA-N taurocholic acid Chemical compound C([C@@H]1C[C@H]2O)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@@H]([C@@H](CCC(=O)NCCS(O)(=O)=O)C)[C@@]2(C)[C@H](O)C1 WBWWGRHZICKQGZ-GIHLXUJPSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- DGQOCLATAPFASR-UHFFFAOYSA-N tetrahydroxy-1,4-benzoquinone Chemical compound OC1=C(O)C(=O)C(O)=C(O)C1=O DGQOCLATAPFASR-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- NYERMPLPURRVGM-UHFFFAOYSA-N thiazepine Chemical group S1C=CC=CC=N1 NYERMPLPURRVGM-UHFFFAOYSA-N 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- UORVGPXVDQYIDP-UHFFFAOYSA-N trihydridoboron Substances B UORVGPXVDQYIDP-UHFFFAOYSA-N 0.000 description 1
- 229940030010 trimethoxybenzene Drugs 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic 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
-
- 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
- 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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28852794A | 1994-08-10 | 1994-08-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| OA10597A true OA10597A (en) | 2002-08-22 |
Family
ID=23107516
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| OA60961A OA10597A (en) | 1994-08-10 | 1997-02-06 | Hypolipidemic 1,4-benzothiazepine-1, 1-dioxides |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US5910494A (de) |
| EP (2) | EP1203769A1 (de) |
| JP (1) | JP2935756B2 (de) |
| KR (1) | KR100354288B1 (de) |
| CN (1) | CN1059673C (de) |
| AP (1) | AP720A (de) |
| AT (1) | ATE226946T1 (de) |
| AU (1) | AU696073B2 (de) |
| BG (1) | BG62048B1 (de) |
| BR (1) | BR9508586A (de) |
| CA (1) | CA2197099A1 (de) |
| CZ (1) | CZ37397A3 (de) |
| DE (1) | DE69528704T2 (de) |
| DK (1) | DK0775126T3 (de) |
| EE (1) | EE9700028A (de) |
| ES (1) | ES2185711T3 (de) |
| FI (1) | FI970531A (de) |
| HK (1) | HK1003936A1 (de) |
| HU (1) | HUT77129A (de) |
| IL (1) | IL114877A (de) |
| IS (1) | IS4418A (de) |
| MX (1) | MX9700890A (de) |
| NO (1) | NO308131B1 (de) |
| NZ (1) | NZ290911A (de) |
| OA (1) | OA10597A (de) |
| PL (1) | PL184512B1 (de) |
| PT (1) | PT775126E (de) |
| RU (1) | RU2156245C2 (de) |
| SK (1) | SK17797A3 (de) |
| WO (1) | WO1996005188A1 (de) |
| ZA (1) | ZA956647B (de) |
Families Citing this family (99)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| GB9423172D0 (en) * | 1994-11-17 | 1995-01-04 | Wellcom Foundation The Limited | Hypolipidemic benzothiazepines |
| GB9704208D0 (en) * | 1997-02-28 | 1997-04-16 | Glaxo Group Ltd | Chemical compounds |
| PT864582E (pt) * | 1997-03-14 | 2003-10-31 | Aventis Pharma Gmbh | 1,4-benzotiazepina-1,1-dioxidos hipolipidemicos |
| GB9800428D0 (en) | 1998-01-10 | 1998-03-04 | Glaxo Group Ltd | Chemical compounds |
| ATE228012T1 (de) | 1998-12-23 | 2002-12-15 | Searle Llc | Kombinationen von ileumgallensäuretransports inhibitoren und gallensäure sequestriermitteln für kardiovaskuläre indikationen |
| EP1140185B1 (de) | 1998-12-23 | 2003-06-04 | G.D. Searle LLC. | Kombnationen von cholesteryl ester transfer protein inhibitoren und gallensäure sequestriermitteln für kardiovaskuläre indikationen |
| AU2157400A (en) | 1998-12-23 | 2000-07-31 | G.D. Searle & Co. | Combinations of cholesteryl ester transfer protein inhibitors and hmg coa reductase inhibitors for cardiovascular indications |
| DK1140184T3 (da) | 1998-12-23 | 2003-09-29 | Searle Llc | Kombinationer af cholesterylestertransferproteinhæmmere og nikotinsyrederivater til hjertekar indikationer |
| ATE241386T1 (de) | 1998-12-23 | 2003-06-15 | Searle Llc | Kombinationen von ileumgallensäuretransports inhibitoren und cholesteryl ester transfer protein inhibitoren |
| PL348503A1 (en) | 1998-12-23 | 2002-05-20 | Searle Llc | Combinations of cholesteryl ester transfer protein inhibitors and fibric acid derivatives for cardiovascular indications |
| PL348580A1 (en) | 1998-12-23 | 2002-06-03 | Searle Llc | Combinations of ileal bile acid transport inhibitors and fibric acid derivatives for cardiovascular indications |
| CN1195748C (zh) * | 1999-02-12 | 2005-04-06 | G.D.瑟尔有限公司 | 具有作为回肠胆汁酸转运和牛磺胆酸摄取抑制剂活性的新的1,2－苯并硫氮杂 |
| 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 |
| GB9914745D0 (en) * | 1999-06-24 | 1999-08-25 | Knoll Ag | Therapeutic agents |
| FR2796070B1 (fr) * | 1999-07-06 | 2003-02-21 | Lipha | Derives de benzodiazepines utilisables dans le traitement de dyslipidemies, de l'atherosclerose et du diabete, compositions pharmaceutiques les contenant et procedes de preparation |
| SE0000772D0 (sv) | 2000-03-08 | 2000-03-08 | Astrazeneca Ab | Chemical compounds |
| AU2001240115A1 (en) | 2000-03-10 | 2001-09-24 | Pharmacia Corporation | Method for the preparation of tetrahydrobenzothiepines |
| US7879840B2 (en) | 2005-08-25 | 2011-02-01 | The Trustees Of Columbia University In The City Of New York | Agents for preventing and treating disorders involving modulation of the RyR receptors |
| US7312044B2 (en) | 2003-03-07 | 2007-12-25 | The Trustees Of Columbia University In The City Of New York | Type 1 ryanodine receptor-based methods |
| US7718644B2 (en) | 2004-01-22 | 2010-05-18 | The Trustees Of Columbia University In The City Of New York | Anti-arrhythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) and uses thereof |
| US8022058B2 (en) | 2000-05-10 | 2011-09-20 | The Trustees Of Columbia University In The City Of New York | Agents for preventing and treating disorders involving modulation of the RyR receptors |
| US7393652B2 (en) | 2000-05-10 | 2008-07-01 | The Trustees Of Columbia University In The City Of New York | Methods for identifying a chemical compound that directly enhances binding of FKBP12.6 to PKA-phosphorylated type 2 ryanodine receptor (RyR2) |
| 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 |
| EG26979A (en) | 2000-12-21 | 2015-03-01 | Astrazeneca Ab | Chemical compounds |
| WO2002053548A1 (en) * | 2000-12-27 | 2002-07-11 | Banyu Pharmaceutical Co.,Ltd. | Benzothiazepine derivatives |
| GB0121337D0 (en) * | 2001-09-04 | 2001-10-24 | 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 |
| MXPA04002179A (es) | 2001-09-08 | 2004-06-29 | Astrazeneca Ab | Derivados de benzotiazepina y benzotiadiazepina con actividad inhibidora de transporte del acido ileal biliar (ibat) para tratar hiperlipidemia. |
| BR0213501A (pt) | 2001-11-02 | 2004-08-24 | Searle Llc | Compostos de benzotiepina mono- e di-fluorada como inibidores de transporte de ácido biliar co-dependente de sódio apical (asbt) e captação de taurocolato |
| CA2471639A1 (en) | 2002-01-17 | 2003-07-31 | Pharmacia Corporation | Novel alkyl/aryl hydroxy or keto thiepines. |
| EP1490090A4 (de) | 2002-02-22 | 2006-09-20 | New River Pharmaceuticals Inc | Wirkstoff-abgabesystem und verfahren zum schutz und zur verabreichung von wirkstoffen |
| GB0209467D0 (en) | 2002-04-25 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
| GB0213669D0 (en) | 2002-06-14 | 2002-07-24 | Astrazeneca Ab | Chemical compounds |
| US7312208B2 (en) | 2002-08-28 | 2007-12-25 | Asahi Kasei Pharma Corporation | Quaternary ammonium compounds |
| US7544678B2 (en) | 2002-11-05 | 2009-06-09 | The Trustees Of Columbia University In The City Of New York | Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) |
| GB0304194D0 (en) | 2003-02-25 | 2003-03-26 | Astrazeneca Ab | Chemical compounds |
| GB0307918D0 (en) | 2003-04-05 | 2003-05-14 | Astrazeneca Ab | Therapeutic use |
| US8710045B2 (en) | 2004-01-22 | 2014-04-29 | The Trustees Of Columbia University In The City Of New York | Agents for preventing and treating disorders involving modulation of the ryanodine receptors |
| WO2005082874A1 (ja) * | 2004-02-27 | 2005-09-09 | Asahi Kasei Pharma Corporation | 新規なベンゾチアゼピン及びベンゾチエピン化合物 |
| US7704990B2 (en) | 2005-08-25 | 2010-04-27 | The Trustees Of Columbia University In The City Of New York | Agents for preventing and treating disorders involving modulation of the RyR receptors |
| CA2744817C (en) * | 2008-11-26 | 2020-07-07 | Satiogen Pharmaceuticals, Inc. | Bile acid recycling inhibitors for treatment of obesity and diabetes |
| JO3131B1 (ar) * | 2010-04-27 | 2017-09-20 | Glaxosmithkline Llc | مركبات كيميائية |
| EP2995317A1 (de) | 2010-05-26 | 2016-03-16 | Satiogen Pharmaceuticals, Inc. | Gallensäurerückflusshemmer zur behandlung von diabetes, adipositas und entzündlichen magen-darm-erkrankungen |
| SG190029A1 (en) | 2010-11-08 | 2013-06-28 | Albireo Ab | Ibat inhibitors for the treatment of liver diseases |
| DK2637646T3 (en) | 2010-11-08 | 2016-08-29 | Albireo Ab | PHARMACEUTICAL COMBINATION CONTAINING AN IBAT inhibitor and a bile acid binder |
| JP2015003861A (ja) * | 2011-10-18 | 2015-01-08 | 株式会社カネカ | （ｒ）−２−アミノ−２−エチルヘキサノールの製造法 |
| EP2771003B1 (de) | 2011-10-28 | 2017-04-19 | Lumena Pharmaceuticals LLC | Gallensäurerückflusshemmer zur behandlung von cholestase-erkrankungen im kindesalter |
| US20140323412A1 (en) | 2011-10-28 | 2014-10-30 | Lumena Pharmaceuticals, Inc. | Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease |
| MX2015013196A (es) | 2013-03-15 | 2016-04-15 | Lumena Pharmaceuticals Inc | Inhibidores de reciclaje de acidos biliares para el tratamiento de la enfermedad de reflujo gastroesofagico y esofago de barrett. |
| RU2015139731A (ru) | 2013-03-15 | 2017-04-20 | ЛУМЕНА ФАРМАСЬЮТИКАЛС ЭлЭлСи | Ингибиторы рециркуляции желчных кислот для лечения первичного склерозирующего холангита и воспалительного заболевания кишечника |
| JO3301B1 (ar) | 2013-04-26 | 2018-09-16 | Albireo Ab | تعديلات بلورية على إيلوبيكسيبات |
| WO2015199147A1 (ja) | 2014-06-25 | 2015-12-30 | 味の素株式会社 | 固形製剤及びその着色防止又は着色低減方法 |
| ES2682171T3 (es) | 2014-08-05 | 2018-09-19 | Glaxosmithkline Intellectual Property (No. 2) Limited | Síntesis de benzodiazepinas |
| EP3012252A1 (de) | 2014-10-24 | 2016-04-27 | Ferring BV | Kristalline Form von elobixibat |
| US10786529B2 (en) | 2016-02-09 | 2020-09-29 | Albireo Ab | Oral cholestyramine formulation and use thereof |
| EP3413878B1 (de) | 2016-02-09 | 2021-04-14 | Albireo AB | Orale cholestyraminformulierungen und verwendung davon |
| 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 |
| CA3011565C (en) | 2016-02-09 | 2024-01-02 | Albireo Ab | Oral cholestyramine formulation and use thereof |
| EP3664782A1 (de) | 2017-08-09 | 2020-06-17 | Albireo AB | Cholestyraminpellets, orale cholestyraminformulierungen und ihre verwendung |
| CA3071285A1 (en) | 2017-08-09 | 2019-02-14 | Albireo Ab | Cholestyramine granules, oral cholestyramine formulations and use thereof |
| TW202015699A (zh) | 2018-06-05 | 2020-05-01 | 瑞典商艾爾比瑞歐公司 | 苯并噻(二)氮呯(benzothia(di)azepine)化合物及其作為膽汁酸調節劑之用途 |
| US10793534B2 (en) | 2018-06-05 | 2020-10-06 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| BR112020024461A2 (pt) | 2018-06-20 | 2021-03-23 | Albireo Ab | formulação farmacêutica de odevixibat, processo para a preparação da formulação farmacêutica, e, formulação. |
| US11801226B2 (en) | 2018-06-20 | 2023-10-31 | Albireo Ab | Pharmaceutical formulation of odevixibat |
| US11007142B2 (en) | 2018-08-09 | 2021-05-18 | Albireo Ab | Oral cholestyramine formulation and use thereof |
| US10722457B2 (en) | 2018-08-09 | 2020-07-28 | 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 |
| JP7504110B2 (ja) | 2019-02-06 | 2024-06-21 | アルビレオ・アクチボラグ | ベンゾチ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 |
| US10975045B2 (en) | 2019-02-06 | 2021-04-13 | Aibireo AB | Benzothiazepine compounds and their use as bile acid modulators |
| US10941127B2 (en) | 2019-02-06 | 2021-03-09 | Albireo Ab | Benzothiadiazepine compounds and their use as bile acid modulators |
| EP3921028B1 (de) | 2019-02-06 | 2022-11-09 | Albireo AB | Benzothiadiazepinverbindungen und ihre verwendung als gallensäuremodulatoren |
| EP3923943B1 (de) | 2019-02-12 | 2024-07-31 | Mirum Pharmaceuticals, Inc. | Genotyp und dosisabhängige reaktion auf einen asbti bei patienten mit gallensalzexportpumpenmangel |
| US11014898B1 (en) | 2020-12-04 | 2021-05-25 | Albireo Ab | Benzothiazepine compounds and their use as bile acid modulators |
| EP4069361B1 (de) | 2019-12-04 | 2024-01-03 | Albireo AB | Benzothia(di)azepinverbindungen und ihre verwendung als gallensäuremodulatoren |
| EP4069247A1 (de) | 2019-12-04 | 2022-10-12 | Albireo AB | Benzothiadiazepinverbindungen und ihre verwendung als gallensäuremodulatoren |
| TW202134222A (zh) | 2019-12-04 | 2021-09-16 | 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 |
| WO2021110883A1 (en) | 2019-12-04 | 2021-06-10 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| EP4069360B1 (de) | 2019-12-04 | 2024-01-03 | Albireo AB | Benzothia(di)azepinverbindungen und ihre verwendung als gallensäuremodulatoren |
| WO2021110886A1 (en) | 2019-12-04 | 2021-06-10 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| WO2021110885A1 (en) | 2019-12-04 | 2021-06-10 | Albireo Ab | Benzothiadiazepine compounds and their use as bile acid modulators |
| ES2972045T3 (es) | 2019-12-04 | 2024-06-10 | Albireo Ab | Compuestos de benzotia(di)azepina y su uso como moduladores del ácido biliar |
| TW202134218A (zh) | 2019-12-04 | 2021-09-16 | 瑞典商艾爾比瑞歐公司 | 苯并噻氮呯化合物及其作為膽酸調節劑之用途 |
| EP4188541A1 (de) | 2020-08-03 | 2023-06-07 | 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 |
| JP2023549226A (ja) | 2020-11-12 | 2023-11-22 | アルビレオ エービー | 進行性家族性肝内胆汁うっ滞症（ｐｆｉｃ）を処置するためのオデビキシバット |
| WO2022101379A1 (en) | 2020-11-12 | 2022-05-19 | Albireo Ab | Odevixibat for treating progressive familial intrahepatic cholestasis (pfic) |
| WO2022117778A1 (en) | 2020-12-04 | 2022-06-09 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| 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 |
| US20230398125A1 (en) | 2022-06-09 | 2023-12-14 | Albireo Ab | Treating hepatitis |
| WO2024008766A1 (en) | 2022-07-05 | 2024-01-11 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| WO2024094841A1 (en) | 2022-11-03 | 2024-05-10 | Albireo Ab | Treating alagille syndrome (algs) |
| WO2024121434A1 (en) | 2022-12-09 | 2024-06-13 | Albireo Ab | Asbt inhibitors in the treatment of renal diseases |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3362962A (en) * | 1964-01-24 | 1968-01-09 | Hoffmann La Roche | Certain benzothiazepine derivatives |
| US4564612A (en) * | 1983-04-22 | 1986-01-14 | Takeda Chemical Industries, Ltd. | Condensed, seven-membered ring compounds and their use |
| GB9111376D0 (en) * | 1991-05-25 | 1991-07-17 | Boots Co Plc | Therapeutic agents |
| GB9203347D0 (en) * | 1992-02-17 | 1992-04-01 | Wellcome Found | Hypolipidaemic compounds |
| US5276025A (en) * | 1992-09-09 | 1994-01-04 | Merck & Co., Inc. | Heterobicyclic sulfonamides |
| ZA941003B (en) * | 1993-02-15 | 1995-08-14 | Wellcome Found | Hypolipidaemic compounds |
| IL108634A0 (en) * | 1993-02-15 | 1994-05-30 | Wellcome Found | Hypolipidaemic heterocyclic compounds, their prepatation and pharmaceutical compositions containing them |
| DE69520364T2 (de) * | 1994-09-13 | 2001-09-13 | Monsanto Company, St. Louis | Benzothepines mit wirkung als inhibitoren des gallensäuretransports und der taurocholate-aufnahme |
| GB9423172D0 (en) * | 1994-11-17 | 1995-01-04 | Wellcom Foundation The Limited | Hypolipidemic benzothiazepines |
-
1995
- 1995-08-08 ZA ZA9506647A patent/ZA956647B/xx unknown
- 1995-08-09 DE DE69528704T patent/DE69528704T2/de not_active Expired - Fee Related
- 1995-08-09 MX MX9700890A patent/MX9700890A/es unknown
- 1995-08-09 CN CN95195419A patent/CN1059673C/zh not_active Expired - Fee Related
- 1995-08-09 KR KR1019970700845A patent/KR100354288B1/ko not_active IP Right Cessation
- 1995-08-09 EP EP02003711A patent/EP1203769A1/de not_active Withdrawn
- 1995-08-09 AT AT95927877T patent/ATE226946T1/de not_active IP Right Cessation
- 1995-08-09 US US08/793,040 patent/US5910494A/en not_active Expired - Fee Related
- 1995-08-09 BR BR9508586A patent/BR9508586A/pt not_active Application Discontinuation
- 1995-08-09 AU AU44260/96A patent/AU696073B2/en not_active Ceased
- 1995-08-09 CZ CZ97373A patent/CZ37397A3/cs unknown
- 1995-08-09 NZ NZ290911A patent/NZ290911A/en unknown
- 1995-08-09 EP EP95927877A patent/EP0775126B1/de not_active Expired - Lifetime
- 1995-08-09 CA CA002197099A patent/CA2197099A1/en not_active Abandoned
- 1995-08-09 RU RU97104002/04A patent/RU2156245C2/ru active
- 1995-08-09 SK SK177-97A patent/SK17797A3/sk unknown
- 1995-08-09 AP APAP/P/1997/000920A patent/AP720A/en active
- 1995-08-09 IL IL11487795A patent/IL114877A/xx active IP Right Grant
- 1995-08-09 EE EE9700028A patent/EE9700028A/xx unknown
- 1995-08-09 JP JP8507116A patent/JP2935756B2/ja not_active Expired - Lifetime
- 1995-08-09 PT PT95927877T patent/PT775126E/pt unknown
- 1995-08-09 DK DK95927877T patent/DK0775126T3/da active
- 1995-08-09 ES ES95927877T patent/ES2185711T3/es not_active Expired - Lifetime
- 1995-08-09 PL PL95318496A patent/PL184512B1/pl unknown
- 1995-08-09 WO PCT/GB1995/001884 patent/WO1996005188A1/en active IP Right Grant
- 1995-08-09 HU HU9700408A patent/HUT77129A/hu active IP Right Revival
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1997
- 1997-01-24 IS IS4418A patent/IS4418A/is unknown
- 1997-02-06 OA OA60961A patent/OA10597A/en unknown
- 1997-02-07 FI FI970531A patent/FI970531A/fi unknown
- 1997-02-07 NO NO970585A patent/NO308131B1/no not_active IP Right Cessation
- 1997-02-07 BG BG101209A patent/BG62048B1/bg unknown
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1998
- 1998-04-15 HK HK98103105A patent/HK1003936A1/xx not_active IP Right Cessation
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