AR045828A1 - Inhibidores de 3- hidroxi-3-metilglutaril -coenzima a reductasa - Google Patents
Inhibidores de 3- hidroxi-3-metilglutaril -coenzima a reductasaInfo
- Publication number
- AR045828A1 AR045828A1 ARP040103478A ARP040103478A AR045828A1 AR 045828 A1 AR045828 A1 AR 045828A1 AR P040103478 A ARP040103478 A AR P040103478A AR P040103478 A ARP040103478 A AR P040103478A AR 045828 A1 AR045828 A1 AR 045828A1
- Authority
- AR
- Argentina
- Prior art keywords
- cycloalkyl
- lower alkyl
- alkyl
- inhibitors
- cycloheteroalkyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000005515 coenzyme Substances 0.000 title 1
- 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 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 235000012000 cholesterol Nutrition 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000032928 Dyslipidaemia Diseases 0.000 abstract 1
- 102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 abstract 1
- 108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 abstract 1
- 208000035150 Hypercholesterolemia Diseases 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- 208000017170 Lipid metabolism disease Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 1
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000006350 alkyl thio alkyl group Chemical group 0.000 abstract 1
- 125000004691 alkyl thio carbonyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000005100 aryl amino carbonyl group Chemical group 0.000 abstract 1
- 125000005129 aryl carbonyl group Chemical group 0.000 abstract 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 abstract 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000005222 heteroarylaminocarbonyl group Chemical group 0.000 abstract 1
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 abstract 1
- 125000005226 heteroaryloxycarbonyl group Chemical group 0.000 abstract 1
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 abstract 1
- 238000002657 hormone replacement therapy Methods 0.000 abstract 1
- 208000006575 hypertriglyceridemia Diseases 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 239000002184 metal Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 210000002966 serum Anatomy 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
- C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
- C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
- C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
- C04B35/632—Organic additives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Abstract
La presente proporciona compuestos que tienen la estructura, los cuales son inhibidores de HMG CoA reductasa y por consiguiente son activos en la inhibición de la biosíntesis del colesterol, la modulación de los lípidos en el suero de la sangre, por ejemplo, para reducir el colesterol de LDL y/o para incrementar el colesterol de HDL, y para tratar la hiperlipidemia, dislipidemia, terapia de reemplaza de hormonas, hipercolesterolemia, hipertrigliceridemia y ateroesclerosis así como la enfermedad de Alzheimer y la osteoporosis. Reivindicación 1: Un compuesto de la fórmula (1), caracterizado porque X es N o CR5; R1 y R2 son los mismos o diferentes y son seleccionados independientemente de H, alquilo, alcoxialquilo, arilalquilo, cicloalquilo, alquenilo, cicloalquenilo, arilo, heteroarilo o cicloheteroalquilo; R3 es arilo, heteroarilo, cicloalquilo, o cicloheteroalquilo; R4 es H, alquilo, cicloalquilo, haloalquilo, alcoxialquilo, alquiltioalquilo, alquilsulfonilo, arilsulfonilo, alcoxicarbonilo, ariloxicarbonilo, heteroariloxicarbonilo, alquilaminocarbonilo, arilaminocarbonilo, alquiltiocarbonilo, heteroarilaminocarbonilo, alquilaminosulfonilo, alquilcarbonilo, arilcarbonilo, heteroarilcarbonilo, o heteroarilsulfonilo; R5 es H o alquilo inferior; Z es un grupo de fórmulas (2); R6 es H, o alquilo inferior o un metal; R7 es H o alquilo inferior; y "líneas y puntos" representan un enlace sencillo o un doble enlace (el cual puede ser cis o trans); o una sal del mismo aceptable farmacéuticamente en donde R6 es H, o un éster del mismo, un éster de profármaco del mismo, y todos los estereoisómeros del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US50589303P | 2003-09-25 | 2003-09-25 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR045828A1 true AR045828A1 (es) | 2005-11-16 |
Family
ID=34393081
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP040103478A AR045828A1 (es) | 2003-09-25 | 2004-09-24 | Inhibidores de 3- hidroxi-3-metilglutaril -coenzima a reductasa |
Country Status (6)
Country | Link |
---|---|
US (1) | US7371759B2 (es) |
EP (1) | EP1667997A1 (es) |
AR (1) | AR045828A1 (es) |
PE (1) | PE20050958A1 (es) |
TW (1) | TW200522950A (es) |
WO (1) | WO2005030758A1 (es) |
Families Citing this family (27)
Publication number | Priority date | Publication date | Assignee | Title |
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GB0306615D0 (en) * | 2003-03-22 | 2003-04-30 | Astrazeneca Ab | New use |
FR2861303A1 (fr) * | 2003-10-24 | 2005-04-29 | Sanofi Synthelabo | Utilisation d'un derive de pyrazole pour la preparation de medicaments utiles dans la prevention et le traitement du syndrome metabolique |
GB0406757D0 (en) | 2004-03-26 | 2004-04-28 | Avecia Ltd | Process and compounds |
US20060058283A1 (en) * | 2004-09-15 | 2006-03-16 | Zymes, Inc. | Compositions comprising ubiquinones |
GB0427491D0 (en) | 2004-12-16 | 2005-01-19 | Avecia Ltd | Process and compounds |
MX2007011453A (es) * | 2005-04-22 | 2008-02-12 | Alantos Pharmaceuticals Holding Inc | Inhibidores de la dipeptidil peptidasa-iv. |
GB0524427D0 (en) * | 2005-11-30 | 2006-01-11 | 7Tm Pharma As | Use of receptor ligands in threapy |
EP1968941A1 (en) * | 2005-12-29 | 2008-09-17 | Novartis AG | Pyridinyl amine derivatives as inhibitors of cholesteryl ester transfer protein (cetp) |
US8232403B2 (en) * | 2006-05-10 | 2012-07-31 | Novartis Ag | Bicyclic derivatives as CETP inhibitors |
KR20090018946A (ko) * | 2006-05-11 | 2009-02-24 | 노파르티스 아게 | Cetp 억제제로서의 벤질아민 유도체 |
US20080033019A1 (en) * | 2006-08-07 | 2008-02-07 | Duke University | Cholesterol lowering drug combination |
AU2007321283A1 (en) * | 2006-11-15 | 2008-05-22 | Novartis Ag | Heterocyclic derivatives as CETP inhibitors |
US20080064701A1 (en) * | 2007-04-24 | 2008-03-13 | Ramesh Sesha | Anti-diabetic combinations |
US20070172525A1 (en) * | 2007-03-15 | 2007-07-26 | Ramesh Sesha | Anti-diabetic combinations |
US8551524B2 (en) * | 2008-03-14 | 2013-10-08 | Iycus, Llc | Anti-diabetic combinations |
EP2373344B1 (en) * | 2008-12-08 | 2016-03-30 | F. Hoffmann-La Roche AG | Combined drug administration |
JP5719835B2 (ja) * | 2009-04-27 | 2015-05-20 | ダウ アグロサイエンシィズ エルエルシー | 殺虫性ピリジン化合物 |
KR101157314B1 (ko) * | 2009-06-05 | 2012-06-15 | 주식회사종근당 | 로수바스타틴의 신규한 제조방법, 이 제조에 유용한 중간체 화합물 및 그의 제조방법 |
CN102219780B (zh) * | 2010-04-14 | 2014-08-06 | 上海京新生物医药有限公司 | 制备(3r,5s,e)-7-(2-(n-甲基甲磺酰胺基)-4-(4-氟苯基)-6-异丙基-嘧啶-5-基)-2,2-二甲基-3,5-二氧六环-6-庚烯酸酯的方法 |
CZ305457B6 (cs) | 2011-02-28 | 2015-09-30 | Ústav organické chemie a biochemie, Akademie věd ČR v. v. i. | Pyrimidinové sloučeniny inhibující tvorbu oxidu dusnatého a prostaglandinu E2, způsob výroby a použití |
CN102816152B (zh) * | 2011-06-09 | 2015-09-09 | 上海京新生物医药有限公司 | 一种瑞苏伐他汀中间体的制备方法 |
US8652527B1 (en) | 2013-03-13 | 2014-02-18 | Upsher-Smith Laboratories, Inc | Extended-release topiramate capsules |
US9101545B2 (en) | 2013-03-15 | 2015-08-11 | Upsher-Smith Laboratories, Inc. | Extended-release topiramate capsules |
WO2016065584A1 (en) | 2014-10-30 | 2016-05-06 | Merck Sharp & Dohme Corp. | Piperidine oxadiazole and thiadiazole orexin receptor antagonists |
WO2017218843A1 (en) * | 2016-06-16 | 2017-12-21 | Denali Therapeutics Inc. | Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders |
CN111518034A (zh) * | 2019-10-21 | 2020-08-11 | 山东理工职业学院 | 他汀类化合物及其中间体的制备方法 |
CN112679490A (zh) * | 2021-01-28 | 2021-04-20 | 安徽美诺华药物化学有限公司 | 瑞舒伐他汀钙含砜结构的手性侧链及其制备方法与用途 |
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-
2004
- 2004-09-21 US US10/946,055 patent/US7371759B2/en active Active
- 2004-09-22 EP EP04784885A patent/EP1667997A1/en not_active Withdrawn
- 2004-09-22 WO PCT/US2004/031212 patent/WO2005030758A1/en active Application Filing
- 2004-09-23 TW TW093128908A patent/TW200522950A/zh unknown
- 2004-09-24 AR ARP040103478A patent/AR045828A1/es unknown
- 2004-09-27 PE PE2004000935A patent/PE20050958A1/es not_active Application Discontinuation
Also Published As
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WO2005030758A1 (en) | 2005-04-07 |
PE20050958A1 (es) | 2005-11-17 |
US7371759B2 (en) | 2008-05-13 |
TW200522950A (en) | 2005-07-16 |
EP1667997A1 (en) | 2006-06-14 |
US20050085497A1 (en) | 2005-04-21 |
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