AR058068A1 - 2-azetidinonas sustituidas,composiciones farmaceuticas que las contienen y usos como agentes anti-hipercolesterolemicos. - Google Patents
2-azetidinonas sustituidas,composiciones farmaceuticas que las contienen y usos como agentes anti-hipercolesterolemicos.Info
- Publication number
- AR058068A1 AR058068A1 ARP060104231A ARP060104231A AR058068A1 AR 058068 A1 AR058068 A1 AR 058068A1 AR P060104231 A ARP060104231 A AR P060104231A AR P060104231 A ARP060104231 A AR P060104231A AR 058068 A1 AR058068 A1 AR 058068A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- aryl
- integer
- substituted
- Prior art date
Links
- 239000003529 anticholesteremic agent Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 238000008214 LDL Cholesterol Methods 0.000 abstract 1
- 230000003143 atherosclerotic effect Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
-
- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Los compuestos son utiles para disminuir los niveles de colesterol en plasma, particularmente colesterol LDL, y para tratar y prevenir la aterosclerosis y sucesos de enfermedad aterosclerotica. Reivindicacion 1: Un compuesto de la formula estructural (1) y sales y ésteres farmacéuticamente aceptables del mismo, donde Ar1 se selecciona entre el grupo constituido por arilo y arilo R4-sustituido; X, Y y Z se seleccionan independientemente entre el grupo constituido por -CH2-, - CH(alquilo C1-6)- y -C(alquilo C1-6)2; R se selecciona entre el grupo constituido por -OR6, -O(CO)R6, -O(CO)O R6, -O(CO)NR6R7, un resto de azucar, un resto de diazucar, un resto de triazucar y un resto de tetraazucar; R1 se selecciona entre el grupo constituido por -H, alquilo C1-6 y arilo, o R y R1 juntos son oxo; R2 se selecciona entre el grupo constituido por -OR6, -O(CO)R6, -O(CO)OR8 y -O(CO)NR6R7; R3 se selecciona entre el grupo constituido por -H, -alquilo C1-6 y arilo, o R2 y R3 juntos son oxo; cada uno de q y r es un numero entero seleccionado independientemente entre 0 y 1 con la condicion de que al menos uno de q y r es 1; cada uno de m, n y p es un numero entero seleccionado independientemente entre 0, 1, 2, 3 y 4; con la condicion de que la suma de m, n, p, q y r es 1, 2, 3, 4, 5 o 6; y con la condicion de que cuando p es 0 y r es 1, entonces la suma de m, q y n es 1, 2, 3, 4 o 5; t es un numero entero seleccionado entre 0, 1 y 2; R4 son 1-5 sustituyentes seleccionados independientemente en cada caso entre el grupo constituido por:-OR5, -O(CO)R5, -O(CO)OR8, -O-alquil C1-5OR5, -O(CO)NR5R6, -NR5R6, -NR5(CO)R6, -NR5(CO)OR8, -NR5(CO)NR6R7, -NR5SO2R8, -COOR5, -CONR5R6, -COR5, -SO2NR5R6, -S(O)tR8, O-alquil C1-10-COOR5, O-alquil C1-10-CONR5R6, y fluoro; R5, R6 y R7 se seleccionan independientemente en cada caso entre el grupo constituido por -H, -alquilo C1-6, arilo y -alquilo C1-6 aril-sustituido; R8 se selecciona entre el grupo constituido por - alquilo C1-6, arilo y -alquil C1-6 aril-sustituido; R9 se selecciona entre el grupo constituido por -CsC-(CH2)y-NR10R11, -C=C-(CH2)y-NR10R11 y -(CH2)w-NR10R11; w es un numero entero seleccionado entre 1, 2, 3, 4, 5, 6, 7 y 8; e y es un numero entero seleccionado entre 1, 2, 3, 4, 5 y 6; y R10 se selecciona entre el grupo constituido por -H y -alquilo C1-3; R11 se selecciona entre el grupo constituido por -H, -alquilo C1-3, -C(O)-alquilo C1-3, -C(O)-NR10R10, -SO2-alquilo C1-3 y -SO2-fenilo; R12 se selecciona entre el grupo constituido por -alquilo C1-15 mono- o polisustituido con -OH, -CH=CH-alquilo C1-13 mono- o poli-sustituido con -OH, -CsC-alquilo C1-13 mono- o poli-sustituido con -OH, y CH2-(CH2)v-C(=CH2)-CH2OH, v es un numero entero seleccionado entre 0 y 1; y R13 se selecciona entre el grupo constituido por -H y -OH.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72378105P | 2005-10-05 | 2005-10-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR058068A1 true AR058068A1 (es) | 2008-01-23 |
Family
ID=37845278
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104231A AR058068A1 (es) | 2005-10-05 | 2006-09-27 | 2-azetidinonas sustituidas,composiciones farmaceuticas que las contienen y usos como agentes anti-hipercolesterolemicos. |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US20090137546A1 (es) |
| EP (1) | EP1934175B1 (es) |
| JP (1) | JP4879991B2 (es) |
| KR (1) | KR20080050610A (es) |
| CN (1) | CN101277930A (es) |
| AR (1) | AR058068A1 (es) |
| AT (1) | ATE488495T1 (es) |
| AU (1) | AU2006302584B2 (es) |
| BR (1) | BRPI0616834A2 (es) |
| CA (1) | CA2624481C (es) |
| CR (1) | CR9903A (es) |
| DE (1) | DE602006018341D1 (es) |
| DO (1) | DOP2006000211A (es) |
| EA (1) | EA200801008A1 (es) |
| ES (1) | ES2354460T3 (es) |
| GT (1) | GT200600444A (es) |
| IL (1) | IL190434A0 (es) |
| MA (1) | MA30006B1 (es) |
| NO (1) | NO20082075L (es) |
| PE (1) | PE20070493A1 (es) |
| SV (1) | SV2009002863A (es) |
| TN (1) | TNSN08153A1 (es) |
| TW (1) | TW200806623A (es) |
| WO (1) | WO2007044318A2 (es) |
| ZA (1) | ZA200802587B (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7176193B2 (en) * | 2002-06-19 | 2007-02-13 | Sanofi-Aventis Deutschland Gmbh | Acid-group-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use |
| GB0215579D0 (en) * | 2002-07-05 | 2002-08-14 | Astrazeneca Ab | Chemical compounds |
| GB0329778D0 (en) * | 2003-12-23 | 2004-01-28 | Astrazeneca Ab | Chemical compounds |
| SA04250427A (ar) * | 2003-12-23 | 2005-12-03 | استرازينيكا ايه بي | مشتقات ثاني فينيل أزيتيدون |
| AU2004308332B2 (en) * | 2003-12-23 | 2008-04-10 | Merck Sharp & Dohme Corp. | Anti-hypercholesterolemic compounds |
| UY29607A1 (es) * | 2005-06-20 | 2007-01-31 | Astrazeneca Ab | Compuestos quimicos |
| AR057380A1 (es) * | 2005-06-22 | 2007-11-28 | Astrazeneca Ab | Compuestos quimicos derivados de 2-azetidinona y uso terapeutico de los mismos |
| AR054482A1 (es) * | 2005-06-22 | 2007-06-27 | Astrazeneca Ab | Derivados de azetidinona para el tratamiento de hiperlipidemias |
| AR057383A1 (es) * | 2005-06-22 | 2007-12-05 | Astrazeneca Ab | Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto |
| SA06270191B1 (ar) * | 2005-06-22 | 2010-03-29 | استرازينيكا ايه بي | مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم |
| AR057072A1 (es) * | 2005-06-22 | 2007-11-14 | Astrazeneca Ab | Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto |
| TW200806623A (en) * | 2005-10-05 | 2008-02-01 | Merck & Co Inc | Anti-hypercholesterolemic compounds |
| DE102005055726A1 (de) * | 2005-11-23 | 2007-08-30 | Sanofi-Aventis Deutschland Gmbh | Hydroxy-substituierte Diphenylazetidinone, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung |
| TW200811098A (en) * | 2006-04-27 | 2008-03-01 | Astrazeneca Ab | Chemical compounds |
| EP2124549A4 (en) * | 2006-12-20 | 2010-01-20 | Merck & Co Inc | ANTIHYPERCHOLESTERINAMIC COMPOUNDS |
| US8029405B2 (en) | 2008-05-30 | 2011-10-04 | Hyundai Motor Company | Gear train of automatic transmission for vehicles |
| WO2010056788A1 (en) * | 2008-11-17 | 2010-05-20 | Merck Sharp & Dohme Corp. | Anti-hypercholesterolemic compounds |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUT67341A (en) * | 1991-07-23 | 1995-03-28 | Schering Corp | Substituted beta-lactam compounds useful as hypocholesterolemic agents, pharmaceutical compositions containing the same and process for the production thereof |
| US5631365A (en) * | 1993-09-21 | 1997-05-20 | Schering Corporation | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
| EP0766667A1 (en) * | 1994-06-20 | 1997-04-09 | Schering Corporation | Substituted azetidinone compounds useful as hypocholesterolemic agents |
| US5624920A (en) * | 1994-11-18 | 1997-04-29 | Schering Corporation | Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents |
| HRP20030498A2 (en) * | 2000-12-21 | 2005-04-30 | Aventis Pharma Deutschland Gmbh | Novel 1,2-diphenzylazetidinones, method for producing the same, medicaments containing said compounds, and the use thereof for treating disorders of the lipid metabolism |
| TWI291957B (en) * | 2001-02-23 | 2008-01-01 | Kotobuki Pharmaceutical Co Ltd | Beta-lactam compounds, process for repoducing the same and serum cholesterol-lowering agents containing the same |
| US7176193B2 (en) * | 2002-06-19 | 2007-02-13 | Sanofi-Aventis Deutschland Gmbh | Acid-group-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use |
| US7176194B2 (en) * | 2002-06-19 | 2007-02-13 | Sanofi-Aventis Deutschland Gmbh | Ring-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use |
| ATE406364T1 (de) * | 2003-03-07 | 2008-09-15 | Schering Corp | Substituierte azetidinon-derivate, deren pharmazeutische formulierungen und deren verwendung zur behandlung von hypercholesterolemia |
| JP2005015434A (ja) * | 2003-06-27 | 2005-01-20 | Kotobuki Seiyaku Kk | 血清コレステロール低下剤或はアテローム性硬化症の予防又は治療剤 |
| AU2004308332B2 (en) * | 2003-12-23 | 2008-04-10 | Merck Sharp & Dohme Corp. | Anti-hypercholesterolemic compounds |
| WO2006086562A2 (en) * | 2005-02-09 | 2006-08-17 | Microbia, Inc. | Phenylazetidinone derivatives |
| JP2008543837A (ja) * | 2005-06-15 | 2008-12-04 | メルク エンド カムパニー インコーポレーテッド | 抗高コレステロール血症化合物 |
| TW200806623A (en) * | 2005-10-05 | 2008-02-01 | Merck & Co Inc | Anti-hypercholesterolemic compounds |
| DE102005055726A1 (de) * | 2005-11-23 | 2007-08-30 | Sanofi-Aventis Deutschland Gmbh | Hydroxy-substituierte Diphenylazetidinone, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung |
| JP2010508313A (ja) * | 2006-11-02 | 2010-03-18 | サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | ピペラジン−１−スルホン酸で置換され、そして改良された薬理学的性質を有する新規なジフェニルアゼチジノン |
-
2006
- 2006-09-26 TW TW095135631A patent/TW200806623A/zh unknown
- 2006-09-27 AR ARP060104231A patent/AR058068A1/es unknown
- 2006-09-29 KR KR1020087008305A patent/KR20080050610A/ko not_active Withdrawn
- 2006-09-29 BR BRPI0616834A patent/BRPI0616834A2/pt not_active IP Right Cessation
- 2006-09-29 CA CA2624481A patent/CA2624481C/en not_active Expired - Fee Related
- 2006-09-29 DE DE602006018341T patent/DE602006018341D1/de active Active
- 2006-09-29 WO PCT/US2006/038551 patent/WO2007044318A2/en not_active Ceased
- 2006-09-29 US US11/992,990 patent/US20090137546A1/en not_active Abandoned
- 2006-09-29 AT AT06816084T patent/ATE488495T1/de not_active IP Right Cessation
- 2006-09-29 JP JP2008534613A patent/JP4879991B2/ja not_active Expired - Fee Related
- 2006-09-29 AU AU2006302584A patent/AU2006302584B2/en not_active Ceased
- 2006-09-29 EA EA200801008A patent/EA200801008A1/ru unknown
- 2006-09-29 ES ES06816084T patent/ES2354460T3/es active Active
- 2006-09-29 EP EP06816084A patent/EP1934175B1/en active Active
- 2006-09-29 CN CNA2006800369359A patent/CN101277930A/zh active Pending
- 2006-10-03 GT GT200600444A patent/GT200600444A/es unknown
- 2006-10-03 PE PE2006001201A patent/PE20070493A1/es not_active Application Discontinuation
- 2006-10-04 US US11/542,966 patent/US7704988B2/en not_active Expired - Fee Related
- 2006-10-05 DO DO2006000211A patent/DOP2006000211A/es unknown
-
2008
- 2008-03-20 ZA ZA200802587A patent/ZA200802587B/xx unknown
- 2008-03-25 IL IL190434A patent/IL190434A0/en unknown
- 2008-04-04 TN TNP2008000153A patent/TNSN08153A1/en unknown
- 2008-04-04 SV SV2008002863A patent/SV2009002863A/es not_active Application Discontinuation
- 2008-04-18 CR CR9903A patent/CR9903A/es not_active Application Discontinuation
- 2008-05-02 MA MA30894A patent/MA30006B1/fr unknown
- 2008-05-02 NO NO20082075A patent/NO20082075L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US7704988B2 (en) | 2010-04-27 |
| EP1934175B1 (en) | 2010-11-17 |
| ATE488495T1 (de) | 2010-12-15 |
| DE602006018341D1 (de) | 2010-12-30 |
| PE20070493A1 (es) | 2007-06-13 |
| MA30006B1 (fr) | 2008-12-01 |
| AU2006302584A1 (en) | 2007-04-19 |
| US20090137546A1 (en) | 2009-05-28 |
| US20070078098A1 (en) | 2007-04-05 |
| TNSN08153A1 (en) | 2009-10-30 |
| EA200801008A1 (ru) | 2009-02-27 |
| CR9903A (es) | 2008-07-29 |
| GT200600444A (es) | 2007-05-04 |
| ZA200802587B (en) | 2009-06-24 |
| NO20082075L (no) | 2008-07-04 |
| KR20080050610A (ko) | 2008-06-09 |
| EP1934175A2 (en) | 2008-06-25 |
| WO2007044318A3 (en) | 2007-07-12 |
| CA2624481C (en) | 2012-04-03 |
| JP4879991B2 (ja) | 2012-02-22 |
| TW200806623A (en) | 2008-02-01 |
| SV2009002863A (es) | 2009-02-19 |
| ES2354460T3 (es) | 2011-03-15 |
| CA2624481A1 (en) | 2007-04-19 |
| JP2009511475A (ja) | 2009-03-19 |
| IL190434A0 (en) | 2008-11-03 |
| WO2007044318A2 (en) | 2007-04-19 |
| AU2006302584B2 (en) | 2011-10-13 |
| BRPI0616834A2 (pt) | 2016-08-23 |
| CN101277930A (zh) | 2008-10-01 |
| DOP2006000211A (es) | 2007-05-31 |
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