AR037089A1 - Derivado de 1,2 benzotiazepina o 1,2,5-benzotiadiazepina,proceso para su preparacion, composicion farmaceutica que lo comprende, y su uso en la fabricacion de un medicamento para la produccion de un efecto inhibidor de transporte ileal de acidos biliares - Google Patents
Derivado de 1,2 benzotiazepina o 1,2,5-benzotiadiazepina,proceso para su preparacion, composicion farmaceutica que lo comprende, y su uso en la fabricacion de un medicamento para la produccion de un efecto inhibidor de transporte ileal de acidos biliaresInfo
- Publication number
- AR037089A1 AR037089A1 ARP020103379A ARP020103379A AR037089A1 AR 037089 A1 AR037089 A1 AR 037089A1 AR P020103379 A ARP020103379 A AR P020103379A AR P020103379 A ARP020103379 A AR P020103379A AR 037089 A1 AR037089 A1 AR 037089A1
- Authority
- AR
- Argentina
- Prior art keywords
- 4alkyl
- 6alkyl
- carbamoyl
- hydrogen
- amino
- Prior art date
Links
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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Oncology (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
Derivado de 1,2-benzotiazepina o 1,2,5-benzotiadiazepina que responde a la fórmula (1), donde Rv se selecciona entre hidrógeno o C1-6alquilo; uno de R1 y R2 se seleccionan entre hidrógeno, C1-6alquilo o C2-6alquenilo y el otro se selecciona entre C1-6alquilo o C2-6alquenilo; Rx y Ry se seleccionan independientemente entre hidrógeno, hidroxi, amino, mercapto, C1-6alquilo, C1-6alcoxi, N-(C1-6alquil)amino, N,N-(C1-6alquil)2amino, C1-6alquilS(O)a, donde a es entre 0 y 2; M se selecciona entre -N- o -CH-; Rz se selecciona entre halo, nitro, ciano, hidroxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C1-6alcoxi, C1-6alcanoilo, C1-6alcanoiloxi, N-(C1-6alquil)amino, N,N-(C1-6alquil)2amino, C1-6alcanoilamino, N-(C1-6alquil)carbamoilo, N,N-(C1-6alquil)2carbamoilo, C1-6alquilS(O)a, donde a es entre 0 y 2, C1-6alcoxicarbonilo, N-(C1-6alquil)sulfamoilo y N,N-(C1-6alquil)2sulfamoilo, v es 0-5; uno de R4 y R5 es un grupo de fórmula (2); R3 y R6 y el otro de R4 y R5 se seleccionan independientemente entre hidrógeno, halo, nitro, ciano, hidroxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-4alquilo, C2-4alquenilo, C2-4alquinilo, C1-4alcoxi, C1-4alcanoilo, C1-4alcanoiloxi, N-(C1-4alquil)amino, N,N-(C1-4alquil)2amino, C1-4alcanoilamino, N-(C1-4alquil)carbamoilo, N,N-(C1-4alquil)2carbamoilo, C1-4alquilS(O)a, donde a es entre 0 y 2, C1-4alcoxicarbonilo, N-(C1-4alquil)sulfamoilo y N,N-(C1-4alquil)2sulfamoilo, donde R3 y R6 y el otro de R4 y R5 pueden estar opcionalmente sustituidos en un carbono por uno o más R16; X es -O-, -N(Ra)-,-S(O)b- ó -CH(Ra)-; donde Ra es hidrógeno o C1-6alquilo y b es 0-2; el anillo A es arilo o heteroarilo; donde el anillo A está sustituido en un carbono por uno o más sustituyentes seleccionados entre R17; R7 es hidrógeno, C1-4alquilo, carbociclilo o heterociclilo; donde R7 está opcionalmente sustituido por uno o más sustituyentes seleccionados entre R18; R8 es hidrógeno o C1-4alquilo; R9 es hidrógeno o C1-4alquilo; R10 es hidrógeno, C1-4alquilo, carbociclilo o heterociclilo; donde R10 está opcionalmente sustituido por uno o más sustituyentes seleccionados entre R19; R11 es carboxi, sulfo, sulfino, fosfono, -P(O)(ORc)(ORd), -P(O)(OH)(ORc), -P(O)(OH)(Rd) o -P(O)(ORc)(Rd) donde Rc y Rd se seleccionan independientemente entre C1-6alquilo; o R11 es un grupo de fórmula (3) o (4) donde: Y es -N(Rn)-, -N(Rn)C(O)-, -N(Rn)C(O)(CRsRt)v, N(Rn)C(O)-, -O-, y -S(O)a-; donde a es 0-2, v es 1-2, Rs y Rt se seleccionan independientemente entre hidrógeno o C1-4alquilo opcionalmente sustituido por R26 y Rn es hidrógeno o C1-4alquilo; R12 es hidrógeno o C1-4alquilo; R13 y R14 se seleccionan independientemente entre hidrógeno, C1-6alquilo, carbociclilo o heterociclilo; y cuando q es 0, R14 puede adicionalmente ser seleccionado entre hidroxi; donde R13 y R14 pueden ser opcionalmente sustituidos en forma independiente por uno o más sustituyentes seleccionados entre R20; R15 es carboxi, sulfo, sulfino, fosfono, -P(O)(ORe)(ORf)-, -P(O)(OH)(Re), -P(O)(OH)(Re) o -P(O)(ORe)(Rf) donde Re y Rf se seleccionan independientemente entre C1-6alquilo; p es 1-3; donde los valores de R13 pueden ser iguales o diferentes; q es 0-1; r es 0-3; donde los valores de R14 pueden ser iguales o diferentes; m es 0-2; donde los valores de R10 pueden ser iguales o diferentes; n es 1-3; donde los valores de R' pueden ser iguales o diferentes; el anillo B es un heterociclilo unido a nitrógeno sustituido en un carbono por un grupo seleccionado entre R23, y opcionalmente adicionalmente sustituido en un carbono por uno o más R24; y donde si dicho heterociclilo unido a nitrógeno contiene una porción -NH-, ese nitrógeno puede ser opcionalmente sustituido por un grupo seleccionado entre R25; R16, R17 y R18 se seleccionan independientemente entre halo, nitro, ciano, hidroxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-4alquilo, C2-4alquenilo, C2-4alquinilo, C1-4alcoxi, C1-4alcanoilo, C1-4alcanoiloxi, N-(C1-4alquil)amino, N,N-(C1-4alquil)2amino, C1-4alcanoilamino, N-(C1-4alquil)carbamoilo, N,N-(C1-4alquil)2carbamoilo, C1-4alquilS(O)a, donde a es entre 0 y 2, C1-4alcoxicarbonilo, N-(C1-4alquil)sulfamoilo y N,N-(C1-4alquil)2sulfamoilo; donde R16, R17, y R18 pueden ser opcionalmente sustituidos en forma independiente en un carbono por uno o más R21; R19, R20, R24 y R26 se seleccionan independientemente entre halo, nitro, ciano, hidroxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-4alquilo, C2-4alquenilo, C2-4alquinilo, C1-4alcoxi, C1-4alcanoilo, C1-4alcanoiloxi, N-(C1-4alquil)amino, N,N-(C1-4alquil)2amino, C1-4alcanoilamino, N-(C1-4alquil)carbamoilo, N,N-(C1-4alquil)2carbamoilo, C1-4alquilS(O)a, donde a es entre 0 y 2, C1-4alcoxicarbonilo, N-(C1-4alquil)sulfamoilo, N,N-(C1-4alquil)2sulfamoilo, carbociclilo, heterociclilo, benciloxicarbonilamino, (C1-4alquil)3sililo, sulfo, sulfino, amidino, fosfono, -P(O)(ORa)(ORb), -P(O)(OH)(ORa)-, -P(O)(OH)(Ra) o -P(O)(ORa)(Rb), donde Ra y Rb se seleccionan independientemente entre C1-6alquilo; donde R19, R20, R24, y R26 pueden ser opcionalmente sustituidos en forma independiente en un carbono por uno o más R22; R21 y R22 se seleccionan independientemente entre halo, hidroxi, ciano, carbamoilo, ureido, amino, nitro, carboxi, carbamoilo, mercapto, sulfamoilo, trifluorometilo, trifluorometoxi, metilo, etilo, metoxi, etoxi, vinilo, alilo, etinilo, metoxicarbonilo, formilo, acetilo, formamido, acetilamino, acetoxi, metilamino, dimetilamino, N-metilcarbamoilo, N,N-dimetilcarbamoilo, metiltio, metilsulfinilo, mesilo, N-metilsulfamoilo y N,N-dimetilsulfamoilo; R23 es carboxi, sulfo, sulfino, fosfono, -P(O)(ORg)(ORh), -P(O)(OH)(ORg), -P(O)(OH)(Rg) o -P(O)(ORg)(Rh) donde Rg y Rh se seleccionan independientemente entre C1-6alquilo; R25 se selecciona entre C1-6alquilo, C1-6alcanoilo, C1-6alquilsulfonilo, C1-6alcoxicarbonilo, carbamoilo, N-(C1-6alquil)carbamoilo, N,N-(C1-6alquil)carbamoilo, bencilo, benciloxicarbonilo, benzoilo y fenilsulfonilo; o una sal aceptable para uso farmacéutico, solvato, solvato de dicha sal o un profármaco del mismo. También se describe el uso de estos derivados en la fabricación de medicamentos útiles como inhibidores del transporte ileal de ácidos biliares (IBAT) para el tratamiento de la hiperlipidemia, los procesos para su fabricación y combinaciones y composiciones farmacéuticas que los contienen.
Applications Claiming Priority (2)
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR037089A1 true AR037089A1 (es) | 2004-10-20 |
Family
ID=26246524
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020103379A AR037089A1 (es) | 2001-09-08 | 2002-09-06 | Derivado de 1,2 benzotiazepina o 1,2,5-benzotiadiazepina,proceso para su preparacion, composicion farmaceutica que lo comprende, y su uso en la fabricacion de un medicamento para la produccion de un efecto inhibidor de transporte ileal de acidos biliares |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US7132416B2 (es) |
| EP (1) | EP1427423B9 (es) |
| JP (2) | JP3616635B2 (es) |
| KR (1) | KR100935623B1 (es) |
| CN (1) | CN1582151A (es) |
| AR (1) | AR037089A1 (es) |
| AT (1) | ATE349214T1 (es) |
| AU (1) | AU2002329387B2 (es) |
| BR (1) | BRPI0212346B1 (es) |
| CA (1) | CA2459449C (es) |
| CO (1) | CO5570671A2 (es) |
| CY (1) | CY1106348T1 (es) |
| DE (1) | DE60217136T2 (es) |
| DK (1) | DK1427423T5 (es) |
| ES (1) | ES2278045T3 (es) |
| HK (1) | HK1065258A1 (es) |
| HU (1) | HU227623B1 (es) |
| IL (2) | IL160691A0 (es) |
| IS (1) | IS7170A (es) |
| MX (1) | MXPA04002179A (es) |
| MY (1) | MY131995A (es) |
| NO (1) | NO327041B1 (es) |
| NZ (1) | NZ531796A (es) |
| PL (1) | PL216023B1 (es) |
| PT (1) | PT1427423E (es) |
| RU (1) | RU2305681C2 (es) |
| TW (1) | TWI331143B (es) |
| UY (1) | UY27436A1 (es) |
| WO (1) | WO2003022286A1 (es) |
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0000772D0 (sv) | 2000-03-08 | 2000-03-08 | Astrazeneca Ab | Chemical compounds |
| EG26979A (en) | 2000-12-21 | 2015-03-01 | Astrazeneca Ab | Chemical compounds |
| 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 |
| RU2004137094A (ru) | 2002-06-20 | 2005-08-10 | Астразенека Аб (Se) | Орто-замещенные производные бензойной кислоты для лечения инсулинорезистентности |
| GB0304194D0 (en) | 2003-02-25 | 2003-03-26 | Astrazeneca Ab | Chemical compounds |
| AU2008202120B2 (en) * | 2003-04-05 | 2009-12-17 | Albireo Ab | Use of an IBAT inhibitor for the treatment of prophylaxis of constipation |
| GB0307918D0 (en) * | 2003-04-05 | 2003-05-14 | Astrazeneca Ab | Therapeutic use |
| GB0314131D0 (en) * | 2003-06-18 | 2003-07-23 | Astrazeneca Ab | Therapeutic agents |
| AR057828A1 (es) * | 2005-09-29 | 2007-12-19 | Astrazeneca Ab | Compuestos derivados de azetidina, su preparacion y composicion farmaceuutica |
| US8062824B2 (en) | 2006-07-17 | 2011-11-22 | E. I. Du Pont De Nemours And Company | Thermally imageable dielectric layers, thermal transfer donors and receivers |
| US7528448B2 (en) * | 2006-07-17 | 2009-05-05 | E.I. Du Pont De Nemours And Company | Thin film transistor comprising novel conductor and dielectric compositions |
| PL2125711T3 (pl) | 2007-03-08 | 2014-05-30 | Albireo Ab | Pochodne kwasy 3-fenylopropionowego oraz ich zastosowanie w leczeniu nieswoistego zapalenia jelit |
| US7666568B2 (en) * | 2007-10-23 | 2010-02-23 | E. I. Du Pont De Nemours And Company | Composition and method for providing a patterned metal layer having high conductivity |
| US7666567B2 (en) | 2007-10-23 | 2010-02-23 | E. I. Du Pont De Nemours And Company | Negative imaging method for providing a patterned metal layer having high conductivity |
| CN102316872B (zh) | 2008-11-26 | 2016-12-21 | 萨蒂奥根制药公司 | 治疗肥胖症和糖尿病的胆汁酸再循环抑制剂 |
| US20110294767A1 (en) | 2010-05-26 | 2011-12-01 | Satiogen Pharmaceuticals, Inc. | Bile acid recycling inhibitors and satiogens for treatment of diabetes, obesity, and inflammatory gastrointestinal conditions |
| BR112013010705B1 (pt) * | 2010-11-08 | 2020-11-17 | Albireo Ab | uso de um inibidor de ibat e um coagulante de ácido biliar, e formulação farmacêutica |
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| KR101890959B1 (ko) * | 2010-11-08 | 2018-08-22 | 알비레오 에이비 | 간질환 치료를 위한 ｉｂａｔ 억제제 |
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| US20130108573A1 (en) | 2011-10-28 | 2013-05-02 | Lumena Pharmaceuticals, Inc. | Bile Acid Recycling Inhibitors for Treatment of Hypercholemia and Cholestatic Liver Disease |
| CN104023727B (zh) | 2011-10-28 | 2017-04-05 | 鲁美纳医药公司 | 用于治疗小儿胆汁淤积性肝病的胆汁酸再循环抑制剂 |
| KR20230152818A (ko) | 2013-03-15 | 2023-11-03 | 샤이어 휴먼 지네틱 테라피즈 인크. | 원발성 담관염 및 염증성 장 질환 치료용 담즙산 재순환 억제제 |
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