HUP0401196A2 - Csípőbélbeni epesav-transzportot gátló hatású benzotiazepin- és benzotiadiazepin-származékok, előállításuk és az ezeket tartalmazó gyógyászati készítmények hiperlipidémia kezelésére - Google Patents
Csípőbélbeni epesav-transzportot gátló hatású benzotiazepin- és benzotiadiazepin-származékok, előállításuk és az ezeket tartalmazó gyógyászati készítmények hiperlipidémia kezeléséreInfo
- Publication number
- HUP0401196A2 HUP0401196A2 HU0401196A HUP0401196A HUP0401196A2 HU P0401196 A2 HUP0401196 A2 HU P0401196A2 HU 0401196 A HU0401196 A HU 0401196A HU P0401196 A HUP0401196 A HU P0401196A HU P0401196 A2 HUP0401196 A2 HU P0401196A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- amino
- group
- sulfamoyl
- carbamoyl
- Prior art date
Links
- 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 title 1
- KAOYLRLQZXRRBD-UHFFFAOYSA-N 1,2,3-benzothiadiazepine Chemical class S1N=NC=CC2=CC=CC=C12 KAOYLRLQZXRRBD-UHFFFAOYSA-N 0.000 title 1
- FHGWEHGZBUBQKL-UHFFFAOYSA-N 1,2-benzothiazepine Chemical compound S1N=CC=CC2=CC=CC=C12 FHGWEHGZBUBQKL-UHFFFAOYSA-N 0.000 title 1
- 208000031226 Hyperlipidaemia Diseases 0.000 title 1
- 239000003613 bile acid Substances 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- -1 hydroxyl- Chemical group 0.000 abstract 20
- 229910052799 carbon Inorganic materials 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000004423 acyloxy group Chemical group 0.000 abstract 2
- 125000005236 alkanoylamino group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000001589 carboacyl group Chemical group 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
Classifications
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/36—Seven-membered rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Steroid Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A találmány az (I) általános képletű vegyületekre, valamint azokgyógyászatilag alkalmazható sóira, szolvátjaira, a sók szolvátjaira éselőgyógyszer-származékaikra vonatkozik - a képletben Rv hidrogénatomotvagy 1-6 szénatomos alkilcsoportot jelent; R1 és R2 közül az egyikhidrogénatomot vagy 1-6 szénatomos alkil- vagy 2-6 szénatomosalkenilcsoportot, a másik pedig 1-6 szénatomos alkil- vagy 2-6szénatomos alkenilcsoportot jelent; Rx és Ry egymástól függetlenülhidrogénatomot vagy hidroxil-, amino-, merkapto-, 1-6 szénatomosalkil-, 1-6 szénatomos alkoxi-, N-(1-6 szénatomos alkil-amino-; N,N-di-(1-6 szénatomos alkil)-amino- vagy (1-6 szénatomos alkil)-S(O)a-csoportot jelent, ahol az utóbbiban a értéke 0-2; M -N- vagy -CH-csoportot jelent; Rz halogénatomot vagy nitro-, ciano-, hidroxil-,amino-, karboxil-, karbamoil-, merkapto-, szulfamoil-, 1-6 szénatomosalkil-, 2-6 szénatomos alkenil-, 2-6 szénatomos alkinil-, 1-6szénatomos alkoxi-, 1-6 szénatomos alkanoil-, 1-6 szénatomos alkanoil-oxi-, N-(1-6 szénatomos alkil)-amino-, N,N-di-(1-6 szénatomos alkil)-amino-, 1-6 szénatomos alkanoil-amino-, N-(1-6 szénatomos alkil)-karbamoil-, N,N-di-(1-6 szénatomos alkil)-karbamoil-, (1-6 szénatomosalkoxi)-karbonil-, N-(1-6 szénatomos alkil)-szulfamoil-, N,N-di-(1-6szénatomos alkil)-szulfamoil- vagy (1-6 szénatomos alkil)-S(O)a-csoportot jelent, ahol az utóbbiban a értéke 0-2; v értéke 0-5; R3 ésR6; továbbá R4 és R5 közül az egyik csoport egymástól függetlenülhidrogénatomot, halogénatomot vagy nitro-, ciano-, hidroxil-, amino-,karboxil-, karbamoil-, merkapto-, szulfamoil-, 1-4 szénatomos alkil-,2-4 szénatomos afkenil-, 2-4 szénatomos alkinil-, 1-4 szénatomosalkoxi-, 1-4 szénatomos alkanoil-, 1-4 szénatomos alkanoil-oxi-, N-(1-4 szénatomos alkil)-amino-, N,N-di-(1-4 szénatomos alkil)-amino-, 1-4szénatomos alkanoil-amino-, N-(1-4 szénatomos alkil)-karbamoil-, N,N-di-(1-4 szénatomos alkil)-karbamoil-, (1-4 szénatomos alkoxi)-karbonil-, N-(1-4 szénatomos alkil)-szulfamoil-, N,N-di-(1-4szénatomos alkil)-szulfamoil- vagy (1-4 szénatomos alkil)-S(O)a-csoportot jelent, ahol az utóbbiban a értéke 0-2; mimellett R3-hoz,R6-hoz, továbbá R4 és R5 közül az egyik csoporthoz adott esetbenszénatomon keresztül egy vagy több R16 szubsztituens kapcsolódhat; ésR4 és R5 közül a másik csoport (IA) általános képletű csoportotjelent. A találmány tárgya továbbá az (I) általános képletű vegyületekelőállítása és az (I) általános képletű vegyületeket tartalmazógyógyszerek. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0121768A GB0121768D0 (en) | 2001-09-08 | 2001-09-08 | Chemical compounds |
GB0209463A GB0209463D0 (en) | 2002-04-25 | 2002-04-25 | Chemical compounds |
PCT/GB2002/004033 WO2003022286A1 (en) | 2001-09-08 | 2002-09-05 | Benzothiazepine and benzothiadiazepine derivatives with ileal bile acid transport (ibat) inhibitory activity for the treatment hyperlipidaemia |
Publications (3)
Publication Number | Publication Date |
---|---|
HUP0401196A2 true HUP0401196A2 (hu) | 2004-10-28 |
HUP0401196A3 HUP0401196A3 (en) | 2008-01-28 |
HU227623B1 HU227623B1 (en) | 2011-09-28 |
Family
ID=26246524
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0401196A HU227623B1 (en) | 2001-09-08 | 2002-09-05 | Benzothiazepine and benzothiadiazepine derivatives with ileal bile acid transport (ibat) inhibitory activity for the treatment of hyperlipidaemia, process for their preparation and pharmaceutical compositions containing them |
Country Status (29)
Country | Link |
---|---|
US (1) | US7132416B2 (hu) |
EP (1) | EP1427423B9 (hu) |
JP (2) | JP3616635B2 (hu) |
KR (1) | KR100935623B1 (hu) |
CN (1) | CN1582151A (hu) |
AR (1) | AR037089A1 (hu) |
AT (1) | ATE349214T1 (hu) |
AU (1) | AU2002329387B2 (hu) |
BR (1) | BRPI0212346B1 (hu) |
CA (1) | CA2459449C (hu) |
CO (1) | CO5570671A2 (hu) |
CY (1) | CY1106348T1 (hu) |
DE (1) | DE60217136T2 (hu) |
DK (1) | DK1427423T5 (hu) |
ES (1) | ES2278045T3 (hu) |
HK (1) | HK1065258A1 (hu) |
HU (1) | HU227623B1 (hu) |
IL (2) | IL160691A0 (hu) |
IS (1) | IS7170A (hu) |
MX (1) | MXPA04002179A (hu) |
MY (1) | MY131995A (hu) |
NO (1) | NO327041B1 (hu) |
NZ (1) | NZ531796A (hu) |
PL (1) | PL216023B1 (hu) |
PT (1) | PT1427423E (hu) |
RU (1) | RU2305681C2 (hu) |
TW (1) | TWI331143B (hu) |
UY (1) | UY27436A1 (hu) |
WO (1) | WO2003022286A1 (hu) |
Families Citing this family (79)
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SE0000772D0 (sv) | 2000-03-08 | 2000-03-08 | Astrazeneca Ab | Chemical compounds |
EG26979A (en) | 2000-12-21 | 2015-03-01 | Astrazeneca Ab | Chemical compounds |
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 |
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 |
DK1517883T3 (da) | 2002-06-20 | 2008-05-26 | Astrazeneca Ab | Ortho-substituerede benzoesyrederivater til behandling af insulinresistens |
GB0304194D0 (en) * | 2003-02-25 | 2003-03-26 | Astrazeneca Ab | Chemical compounds |
GB0307918D0 (en) * | 2003-04-05 | 2003-05-14 | Astrazeneca Ab | Therapeutic use |
AU2008202120B2 (en) * | 2003-04-05 | 2009-12-17 | Albireo Ab | Use of an IBAT inhibitor for the treatment of prophylaxis of constipation |
GB0314131D0 (en) * | 2003-06-18 | 2003-07-23 | Astrazeneca Ab | Therapeutic agents |
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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. |
KR20160002773A (ko) | 2013-03-15 | 2016-01-08 | 루메나 파마수티컬즈, 인코포레이티드 | 원발성 담관염 및 염증성 장 질환 치료용 담즙산 재순환 억제제 |
JO3301B1 (ar) | 2013-04-26 | 2018-09-16 | Albireo Ab | تعديلات بلورية على إيلوبيكسيبات |
JP6751020B2 (ja) | 2014-06-25 | 2020-09-02 | Eaファーマ株式会社 | 固形製剤及びその着色防止又は着色低減方法 |
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