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1. 发明申请

WO0179180A3 5-SUBSTITUTED TETRALONES AS INHIBITORS OF RAS FARNESYL TRANSFERASE 审中-公开
标题翻译：作为RAS FARNESYL转移的抑制剂的5-取代的四氢呋喃
公开(公告)号：WO0179180A3
公开(公告)日：2002-05-23
申请号：PCT/US0112490
申请日：2001-04-16
申请人： WARNER LAMBERT CO , DENNY WILLIAM ALEXANDER , HUTCHINGS RICHARD H , JOHNSON DOUGLAS S , KALTENBRONN JAMES STANLEY , LEE HO HUAT , LEONARD DANIELE MARIE , MILBANK JARED BRUCE JOHN , REPINE JOSEPH THOMAS , REWCASTLE GORDON WILLIAM , WHITE ANDREW DAVID
发明人： DENNY WILLIAM ALEXANDER , HUTCHINGS RICHARD H , JOHNSON DOUGLAS S , KALTENBRONN JAMES STANLEY , LEE HO HUAT , LEONARD DANIELE MARIE , MILBANK JARED BRUCE JOHN , REPINE JOSEPH THOMAS , REWCASTLE GORDON WILLIAM , WHITE ANDREW DAVID
IPC分类号： C07D233/60 , A61K31/4164 , A61K31/4178 , A61K31/422 , A61K31/4439 , A61K31/4725 , A61K31/496 , A61K31/497 , A61P9/10 , A61P13/00 , A61P13/08 , A61P17/06 , A61P27/02 , A61P31/12 , A61P35/00 , A61P43/00 , C07D233/54 , C07D233/91 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14 , C07D521/00 , C07D403/12 , C07D409/06 , C07D417/06
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D233/91 , C07D249/08 , C07D401/12
摘要： The present invention provides novel 5-substituted tetralones of Formulas (I), (II), (III) and (IV) and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis. Specifically, the present invention relates to compounds that inhibit the farnesyl transferase enzyme.
摘要翻译：本发明提供式（I），（II），（III）和（IV）的新的5-取代四氢萘酮及其药学上可接受的盐，酯，酰胺和前药，其可用于治疗和预防不受控制或异常增殖的组织，如癌症，动脉粥样硬化，再狭窄和牛皮癣。具体地，本发明涉及抑制法呢基转移酶的化合物。

2. 发明专利

CA2590533C 7-(2H-PYRAZOL-3-YL)-3,5-DIHYDROXY-HEPTANOIC ACID DERIVATIVES AS HMG CO-A REDUCTASE INHIBITORS FOR THE TREATMENT OF LIPIDEMIA 未知
公开(公告)号：CA2590533C
公开(公告)日：2010-09-07
申请号：CA2590533
申请日：2005-11-14
申请人： WARNER LAMBERT CO
发明人： CHOI CHULHO , HUTCHINGS RICHARD H , PFEFFERKORN JEFFREY A , BOWLES DANIEL MERRITT , PARK WILLIAM KEUN CHAN
IPC分类号： C07D231/14 , A61P3/06 , A61P3/10 , C07D405/06
摘要： The present invention provides compounds of the formula (I), (IV) and (V) and intermediates of the formuale (VI) and (VII): (I), (IV), (V), (VI), (VII). wherein: R1 is hydrogen, halogen, C1-C7 alkyl, C3-C8 cycloalkyl, aryl, aralkyl, heteroaryt, or heteroaralkyl; more specifically, R1 is C1-C7 alkyl or C3-C8 cycloalkyl; even more specifically, R1 is isopropyl; where alkyl, cycloalkyt, aryl, aralkyt, heteroaryl, or heteroaralkyl of R1 is optionally substituted, R2 is hydrogen, halogen, C1-C7 alkyl, C3-C8 cycloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, NC-, R2bR2aNCO(CH2)n -, R2bR2a NS(O)n-, R2cS(O)n-, R2bR2a N(CH2)n-, R2b-J-C(O)NR2a(CH2)n-, R2b-J-~SO2NR2a(CH2)n-, R2b-J-SONR2a(CH2)n, R7OOC(CH2)n-, or R7CO(CH2)n-; more specifically, R2 is R2bR2aNCO(CH2)n-; even more specifically, R2 is R2bR2a NCO-; where alkyl, cycloalkyl, aryl , aralkyl, heteroaryl, or heteroaralkyl of R2 is optionally substituted, R3 is hydrogen, C1-6 aikyl, C3-6necycloafkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; more specifically, R3 is aryl; even more specifically, R3 is phenyl or p-fluorophenyl; where alkyl, cycloalkyl, aryl, aralkyl, heteroaryt, or beteroaralkyd of A3 is opltianally substituted and is a bond or is absent. The other substituents are defined in the claims. The present invention relates to compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents. Moree specifically, the present invention concerns certain potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase ("HMG CoA reciuctase"). The compounds are useful for the treatement of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis.

3. 发明专利

ES2328384T3 DERIVADOS DEL ACIDO 7-(2H-PIRAZOL-3-IL)-3,5-DIHIDROXI-HEPTANOICO COMO INHIBIDORES DE HMG CO-A REDUCTASA PARA EL TRATAMIENTO DE LA LIPIDEMIA. 未知
公开(公告)号：ES2328384T3
公开(公告)日：2009-11-12
申请号：ES05801166
申请日：2005-11-14
申请人： WARNER LAMBERT CO
发明人： CHOI CHULHO , HUTCHINGS RICHARD H , PFEFFERKORN JEFFREY A , BOWLES DANIEL MERRITT , PARK WILLIAM KEUN CHAN
IPC分类号： C07D231/14 , A61P3/06 , A61P3/10 , C07D405/06
摘要： Un compuesto de la fórmula (I): ** ver fórmula** o una de sus sales farmacéuticamente aceptables, en la que: R 1 es hidrógeno, halógeno, alquilo C 1-C 7, cicloalquilo C 3-C 8, arilo, aralquilo, heteroarilo o heteroaralquilo; estando el alquilo, cicloalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo de R 1 opcionalmente sustituido; R2 es R2bR2aNCO(CH2)n- o R2b-J-C(O)NR2a(CH2)n-; J es un enlace directo, O o N; cada uno de R2a y R2b es independientemente hidrógeno, alquilo C1-C10, cicloalquilo C3-C8, arilo, aralquilo, heteroarilo o heteroaralquilo; estando el alquilo, cicloalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo de R2a y R2b opcionalmente sustituido; o R2a y R2b tomados junto con el nitrógeno al que están unidos forman un anillo de 4-11 miembros que opcionalmente contiene al menos un heteroátomo adicional seleccionado de O, N y S, estando dicho anillo opcionalmente sustituido con al menos uno de arilo, aralquilo, heteroarilo, heteroaralquilo, alquilo C1-C10, haloalquilo C1-C10, cicloalquilo C 3-C 8, halógeno, R 7 O-, R 7 OOC(CH 2) n-, R 7 R 8 NCO(CH 2) n-, R 7 O 2S(CH 2) n-, R 8 R 7 NSO 2- o CN-; cada uno de R 7 y R 8 es independientemente hidrógeno, alquilo C1-C12, arilo o aralquilo; estando el alquilo, arilo o aralquilo de R 7 y R 8 opcionalmente sustituido; n es 0, 1 ó 2; R3 es hidrógeno, alquilo C1-C6, cicloalquilo C3-C8, arilo, aralquilo, heteroarilo o heteroaralquilo; estando el alquilo, cicloalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo de R3 opcionalmente sustituido; y --- es un enlace o está ausente.

4. 发明专利

DOP2005000228A NUEVOS INHIBIDORES DE HMG CO-A REDUCTASA BASADOS EN PIRAZOL 未知
公开(公告)号：DOP2005000228A
公开(公告)日：2006-05-31
申请号：DO2005000228
申请日：2005-11-10
申请人： WARNER LAMBERT CO
发明人： CHOI CHULHO , HUTCHINGS RICHARD H , PFEFFERKORN JEFFREY A , BOWLES DANIEL MERRITT , PARK WILLIAM KEUN CHAN
摘要： Se describen nuevos compuestos y composiciones farmaceuticas utiles como agentes hipocolesterolemicos e hipolipidemicos. Mas especificamente, se describen potentes inhibidores de la enzima 3-hidroxi-3-metilglutaril coenzima A reductasa ("HMG CoA reductasa"). Se describen tambien procedimientos de use de tales compuestos y composiciones para tratar sujetos, incluyendo seres humanos, que sufren hiperlipidemia, hipercolesterolemia, hipertrigliceridemia, aterosclerosis, enfermedad de Alzheimer, hipertrofia prostatica benigna (HPB), diabetes y osteoporosis.

5. 发明专利

AT439347T 未知
公开(公告)号：AT439347T
公开(公告)日：2009-08-15
申请号：AT05801166
申请日：2005-11-14
申请人： WARNER LAMBERT CO
发明人： CHOI CHULHO , HUTCHINGS RICHARD H , PFEFFERKORN JEFFREY A , BOWLES DANIEL , PARK WILLIAM
IPC分类号： C07D231/14 , A61P3/06 , A61P3/10 , C07D405/06
摘要： Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase ("HMG CoA reductase") are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described.

6. 发明专利

DE602005016009D1 未知
公开(公告)号：DE602005016009D1
公开(公告)日：2009-09-24
申请号：DE602005016009
申请日：2005-11-14
申请人： WARNER LAMBERT CO
发明人： CHOI CHULHO , HUTCHINGS RICHARD H , PFEFFERKORN JEFFREY A , BOWLES DANIEL MERRITT , PARK WILLIAM KEUN CHAN
IPC分类号： C07D231/14 , A61P3/06 , A61P3/10 , C07D405/06
摘要： Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase ("HMG CoA reductase") are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described.

7. 发明专利

TNSN07202A1 DERIVES D'ACIDE 7-(2H-PYRAZOLE-3-YL)-3, 5-DIHYROXY HEPTANOIQUE SERVANT D'INHIBITEURS DE HMG-CO A REDUCTASE POUR LE TRAITEMENT DE LA LIPIDEMIE 未知
公开(公告)号：TNSN07202A1
公开(公告)日：2008-11-21
申请号：TNSN07202
申请日：2007-05-22
申请人： WARNER LAMBERT CO
发明人： CHOI CHULHO , HUTCHINGS RICHARD H , PFEFFERKORN JEFFREY A , BOWLES DANIEL MERITT , PARK WILLIAM KEUN CHAN
IPC分类号： A61P3/06 , A61P3/10 , C07D231/14 , C07D405/06
摘要： La présente invention propose des composés de formules (I), (IV) et (V) et des intermédiaires de formules (VI) et (VII) : (I), (IV), (V), (VI), (VII), formules dans lesquelles : R1 représente un atome d'hydrogène, un atome d'halogène, un groupe alkyle en C1 à C7, cycloalkyle en C3 à C8, aryle, aralkyle, hétéroaryle ou hétéroaralkyle ; plus spécifiquement, R1 représente un groupe alkyle en C1 à C7 ou cycloalkyle en C3 à C8 ; encore plus spécifiquement, R1 représente un groupe isopropyle ; le groupe alkyle cycloalkyle, aryle aralkyle, hétéroaryle ou hétéroaralkyle de R1 étant facultativement substitué ; R2 représente un atome d'hydrogène, un atome d'halogène, un groupe alkyle en C1 à C7, cycloalkyle en C3 à C8, aryle aralkyle, hétéroaryle, hétéroaralkyle, NC-, R2bR2aNCO(CH2)n -, R2bR2aNS(O)n -, R2cS(O)n-, R2bR2aN(CH2)n -, R2b-J-C(O)NR2a(CH2)n -, R2b-J-SO2NR2a(CH2)n -, R2b-J-SONR2a(CH2)n, R7OOC(CH2)n – ou R7CO(CH2)n - ; plus spécifiquement, R2 représente un groupe R2bR2a NCO(CH2)n - ; encore plus spécifiquement, R2 représente un groupe R2bR2aNCO- ; le groupe alkyle, cycloalkyle, hétéroaryle ou hétéroaralkyle de R2 étant facultativement substitué ; R3 représente un atome d'hydrogène, un groupe alkyle en C1 à C6, cycloalkyle en C3 à C6, aryle, aralkyle, hétéroaryle ou hétéroaralkyle ; plus spécifiquement R3 représente un groupe aryle ; encore plus spécifiquement, R3 représente un groupe phényle ou p-fluorophényle ; le groupe alkyle, cycloalkyle, aryle aralkyle, hétéroaryle ou hétéroaralkyle de R3 étant facultativement substitué et représentant une liaison ou étant absent. Les autres substituants sont définis dans les revendications. La présente invention concerne des composés et compositions pharmaceutiques utiles comme agents hypocholestérolémiques et hypolipidémiques. Plus spécifiquement, la présente invention concerne certains puissants inhibiteurs de l'enzyme 3-hydroxy-3-méthylglutaryl-coenzyme-A-réductase (« HMG-CoA-réductase »). Les composés sont utiles pour le traitement de l'hyperlipidémie, l'hypercholestérolémie, de l'hypertriglycéridémie, de l'athérosclérose, de la maladie d'Alzheimer, de l'hypertrophie prostatique bénigne (BPH) du diabète et de l'ostéoporose.

8. 发明专利

MX2007005137A DERIVADOS DEL ACIDO 7-(2H-PYRAZOL-3-IL)-3, 5-DIHIDROXI-HEPTANOICO COMO INHIBIDORES DE HMG CO-A REDUCTASA PARA EL TRATAMIENTO DE LIPIDEMIA. 未知
公开(公告)号：MX2007005137A
公开(公告)日：2007-06-22
申请号：MX2007005137
申请日：2005-11-14
申请人： WARNER LAMBERT CO
发明人： CHOI CHULHO , HUTCHINGS RICHARD H , PFEFFERKORN JEFFREY A , BOWLES DANIEL MERRIT , PARK WILLIAM KEUN CHAN
IPC分类号： A61P3/10 , A61P3/06 , C07D231/14 , C07D405/06
摘要： Se describen nuevos compuestos y composiciones farmaceuticas utiles como agentes hipocolesterolemicos e hipolipidemicos. Mas especificamente, se describen potentes inhibidores de la enzima 3-hidroxi-3-metilglutaril-coenzima A reductasa ("HMG CoA reductasa"); se describen tambien procedimientos de uso de tales compuestos y composiciones para tratar sujetos, incluyendo seres humanos, que sufren hiperlipidemia, hipercolesterolemia, hipertrigliceridemia, aterosclerosis, enfermedad de Alzheimer, hipertrofia prostatica benigna (HPB), diabetes y osteoporosis.

9. 发明专利

CA2590533A1 7-(2H-PYRAZOL-3-YL)-3, 5-DIHYROXY-HEPTANOIC ACID DERIVATIVESAS HMG CO-A REDUCTASE INHIBITORS FOR THE TREATMENT OF LIPIDEMIA 未知
公开(公告)号：CA2590533A1
公开(公告)日：2006-06-01
申请号：CA2590533
申请日：2005-11-14
申请人： WARNER LAMBERT CO
发明人： BOWLES DANIEL MERRITT , HUTCHINGS RICHARD H , PFEFFERKORN JEFFREY A , CHOI CHULHO , PARK WILLIAM KEUN CHAN
IPC分类号： C07D231/14 , A61P3/06 , A61P3/10 , C07D405/06
摘要： Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase ("HMG CoA reductase") are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described.

10. 发明专利

DOP2005000063A NUEVOS IMIDAZOLES 未知
公开(公告)号：DOP2005000063A
公开(公告)日：2005-11-15
申请号：DO2005000063
申请日：2005-04-15
申请人： WARNER LAMBERT CO
发明人： TRIVEDI BHARAT KALIDAS , BOLTON GARY LOUIS , SONG YUNTAO , POEL TONI-JO , HUTCHINGS RICHARD H , BOWLES DANIEL MERRITT , PARK WILLIAM KEUN CHAN , BOYLES DAVID CHRISTOPHER
摘要： Nuevos imidazoles que son utiles como inhibidores de HMG Co-A reductasa. Tambien se proporcionan composiciones farmaceuticas de los compuestos. Tambien se proporcionan metodos para prepararlos y metodos para usar los compuestos.

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