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1. 发明授权

US5318984A Imidazoles for the treatment of atherosclerosis 失效
公开(公告)号：US5318984A
公开(公告)日：1994-06-07
申请号：US940372
申请日：1992-09-03
申请人： Jeffrey T. Billheimer , Peter J. Gillies , C. Anne Higley , Thomas P. Maduskuie, Jr. , Ruth R. Wexler
发明人： Jeffrey T. Billheimer , Peter J. Gillies , C. Anne Higley , Thomas P. Maduskuie, Jr. , Ruth R. Wexler
IPC分类号： C07D233/54 , C07D233/70 , C07D233/84 , C07D233/88 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D491/04 , A61K31/415 , C07D233/66
CPC分类号： C07D233/64 , C07D233/70 , C07D233/84 , C07D233/88 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D491/04
摘要： Disclosed are compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are selected independently from H, C.sub.1 -C.sub.8 unbranched alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 araalkyl, 2-, 3- or 4-pyridinyl, 2-thienyl, 2-furanyl, phenyl optionally substituted with 1 to 3 groups selected from F, Cl, Br, OH, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, CH.sub.3 S(O).sub.r, NO.sub.2, CF.sub.3, or NR.sup.7 R.sup.8 ; or ##STR2## where L is O, O(CH.sub.2).sub.m+1 O, or (CH.sub.2).sub.m where m is 0-4; R.sup.3 is H, C.sub.1 -C.sub.6 alkyl, allyl, benzyl, or phenyl optionally substituted with F, Cl, CH.sub.3, CH.sub.3 O, or CF.sub.3 ;R.sup.4 is straight chain C.sub.1 -C.sub.8 alkyl optionally substituted with F; C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; C.sub.3 --C.sub.6 alkenyl or alkynyl, C.sub.1 -C.sub.3 perfluoroalkyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.1 -C.sub.4 alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8 or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, pyrimidinyl, or biphenyl;R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, or benzyl;R.sup.6 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.8 alkenyl or alkynyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ;R.sup.7 and R.sup.8 are selected independently from H or C.sub.1 -C.sub.4 alkyl;X is S(O).sub.r, O, NR.sup.5, CH.sub.2 ;A is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl, or C.sub.3 -C.sub.10 alkynyl;Y is O, S, H.sub.2, or NH;Z is NHR.sup.4, OR.sup.4, or R.sup.4 ;r is 0-2,or a pharmaceutically acceptable salt thereof and their use as antihypercholesterolemic agents or antiatherosclerotic agents.

2. 发明授权

US5166214A Use of imidazoles for the treatment of atherosclerosis 失效
公开(公告)号：US5166214A
公开(公告)日：1992-11-24
申请号：US533241
申请日：1990-06-04
申请人： Jeffrey T. Billheimer , Peter J. Gillies , C. Anne Higley , Thomas P. Maduskuie, Jr. , Ruth R. Wexler
发明人： Jeffrey T. Billheimer , Peter J. Gillies , C. Anne Higley , Thomas P. Maduskuie, Jr. , Ruth R. Wexler
IPC分类号： C07D233/54 , C07D233/70 , C07D233/84 , C07D233/88 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D491/04
CPC分类号： C07D233/64 , C07D233/70 , C07D233/84 , C07D233/88 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D491/04
摘要： This invention relates to imidazoles as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), processes for their preparation, and their use as antihypercholesterolemic agents or antiatherosclerotic.The compounds for use in the described method are compounds of Formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are selected independently from H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 araalkyl, phenyl optionally substituted with 1 to 3 groups selected from F, Cl, Br, OH, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, CH.sub.3 S(O).sub.r, NO.sub.2, CF.sub.3, or NR.sup.7 R.sup.8 ; R.sup.3 is H, C.sub.1 -C.sub.6 alkyl, allyl, benzyl, or phenyl optionally substituted with F, Cl, CH.sub.3, CH.sub.3 O, or CF.sub.3 ; R.sup.4 is straight chain C.sub.1 -C.sub.8 alkyl optionally substituted with F; C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 aralkyl where the aryl group is optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; C.sub.3 -C.sub.6 alkenyl or alkynyl, C.sub.1 -C.sub.3 perfluoroalkyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.1 -C.sub.4, alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8 or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; 2-, 3-, or 4- or pyrindinyl, pyrimidinyl, or biphenyl; R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, or benzyl; R.sup.6 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.8 alkenyl of alkynyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; R.sup.7 and R.sup.8 are selected independently from H or C.sub.1 -C.sub.4 alkyl; A is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl, or C.sub.3 -C.sub.10 alkynyl; Y is O; Z is NHR.sup.4, OR.sup.4, or R.sup.4 ; r is 0-2, or a pharmaceutically acceptable salt thereof.

3. 发明授权

US5310748A Imidazoles for the treatment of atherosclerosis 失效
标题翻译：咪唑用于治疗动脉粥样硬化
公开(公告)号：US5310748A
公开(公告)日：1994-05-10
申请号：US881034
申请日：1992-05-11
申请人： Richard G. Wilde , C. Anne Higley , Jeffrey T. Billheimer , Ruth R. Wexler
发明人： Richard G. Wilde , C. Anne Higley , Jeffrey T. Billheimer , Ruth R. Wexler
IPC分类号： C07D233/84 , C07D401/12 , C07D403/12 , A61K31/415
CPC分类号： C07D401/12 , C07D233/84
摘要： Disclosed are imidazoles as inhibitors of acylCoA:cholesterol acyltransferase (ACAT), processes for their preparation, pharmaceutical compositions, and their use as antihypercholesterolemics and/or antiatherosclerotics.
摘要翻译：公开了作为酰基CoA的抑制剂的咪唑：胆固醇酰基转移酶（ACAT），其制备方法，药物组合物及其作为抗高胆固醇血症和/或抗动脉粥样硬化的用途。

4. 发明授权

US5478830A Fused-ring heterocycles for the treatment of atherosclerosis 失效
标题翻译：用于治疗动脉粥样硬化的融合环杂环
公开(公告)号：US5478830A
公开(公告)日：1995-12-26
申请号：US889892
申请日：1992-05-29
申请人： C. Anne Higley , Ruth R. Wexler , Richard G. Wilde
发明人： C. Anne Higley , Ruth R. Wexler , Richard G. Wilde
IPC分类号： C07D487/04 , A61K31/44 , A61K31/505 , A61K31/52
CPC分类号： C07D487/04
摘要： This invention relates to pyrazolo pyrimidines for the treatment of atherosclerosis as inhibitors of acyl--CoA, cholesterol acyetransferase (ACAT), and their use as antihypercholesterolemic agents, pharmaceutical compositions and preparation, and having the formula (I): ##STR1## wherein: A and Q are selected independently from CH or N with no more than two nitrogens per ring:D, E, and G are selected independently from CR.sup.1 or N with no more than two nitrogens per ring;X is S(O).sub.r, O, NR.sup.4 or CH.sup.2 ;J is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl or C.sub.3 -C.sub.10 alkynyl;Y is O, S, H.sub.2 or NH:Z is NHR.sup.3, OR.sup.3 or R.sup.3 :R.sup.1 is selected independently from H, NO.sub.2, Br, Cl, F, CF.sub.3, CN, CH.sub.3 S(O).sub.r, C.sub.1 -C.sub.8 alkyl or alloxy, C.sub.3 -C.sub.8, branched alkyl, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.5 R.sup.6 or NR.sup.5 COR.sup.6 ;R.sup.2 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.8 alkenyl or alkynyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted; phenyl optionally substituted benzyl optionally substituted 2-, 3-, or 4- pyridinyl, pyrimidinyl: or biphenyl:R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloallylalkyl, C.sub.3 -C.sub.6 alkenyl or alkynyl, C.sub.1 -C.sub.3 perfluoroalkyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted phenyl optionally substituted benzyl optionally substituted 2-, 3-, or 4- pyridinyl, pyrimidinyl; or biphenyl:R.sup.4 is H, C.sub.1 -C.sub.6 alkyl or benzyl;R.sup.5 and R.sup.6 are selected independently from H or C.sub.1 -C.sub.4 alkyl;r is 0 to 2:or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及用于治疗动脉粥样硬化的吡唑并嘧啶作为酰基辅酶A，胆固醇转氨酶（ACAT）的抑制剂及其作为抗高胆固醇血症药物，药物组合物和制剂的用途，并具有式（I）：其中： A和Q独立地选自CH或N，每个环不多于两个氮：D，E和G独立地选自CR1或N，每个环不多于两个氮; X是S（O）r，O，NR 4或CH 2; J是C 2 -C 10烷基，C 3 -C 10支链烷基，C 3 -C 10链烯基或C 3 -C 10炔基; Y是O，S，H2或NH：Z是NHR3，OR3或R3：R1独立地选自H，NO2，Br，Cl，F，CF3，CN，CH3S（O）r，C1-C8烷基或烯氧基， C3-C8，支链烷基，C1-C4烷氧羰基，NR5R6或NR5COR6; R2是C1-C8烷基，C3-C8支链烷基，C3-C7环烷基，C3-C8链烯基或炔基，其中芳基任选被取代的C7-C14芳烷基; 苯基任选取代的苄基任选取代的2-，3-或4-吡啶基，嘧啶基或联苯基：R3是C1-C8烷基，C3-C8支链烷基，C3-C7环烷基，C4-C10环烯基烷基，C3-C6烯基或炔基，C1-C3全氟烷基，C7-C14芳烷基，其中芳基是任选取代的苯基任选取代的苄基任选取代的2-，3-或4-吡啶基，嘧啶基; 或联苯基：R 4是H，C 1 -C 6烷基或苄基; R 5和R 6独立地选自H或C 1 -C 4烷基; r为0〜2：或其药学上可接受的盐。

5. 发明授权

US5290801A Benzimidazoles for the treatment of atherosclerosis 失效
标题翻译：苯并咪唑用于治疗动脉粥样硬化
公开(公告)号：US5290801A
公开(公告)日：1994-03-01
申请号：US889909
申请日：1992-05-29
申请人： C. Anne Higley , Thomas P. Muduskuie, Jr. , Ruth R. Wexler , Richard G. Wilde
发明人： C. Anne Higley , Thomas P. Muduskuie, Jr. , Ruth R. Wexler , Richard G. Wilde
IPC分类号： A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/52 , C07D235/28 , C07D263/58 , C07D277/74 , C07D471/04 , C07D473/04
CPC分类号： C07D263/58 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/52 , C07D235/28 , C07D277/74 , C07D471/04 , C07D473/04
摘要： This invention relates to imidazoles, namely, fused-ring heterocycles as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), pharmaceutical compositions containing them, processes for their preparation, and their use as antihypercholesterolemic and/or antiatherosclerotic agents for the treatment of atherosclerosis.
摘要翻译：本发明涉及咪唑，即作为酰基辅酶A的抑制剂的稠环杂环：胆固醇酰基转移酶（ACAT），含有它们的药物组合物，其制备方法及其作为抗高胆固醇血和/或抗动脉粥样硬化剂用于治疗动脉粥样硬化的用途。

6. 发明授权

US06844318B2 Peptidase-cleavable, targeted antineoplastic drugs and their therapeutic use 有权
标题翻译：肽酶切割，靶向抗肿瘤药物及其治疗用途
公开(公告)号：US06844318B2
公开(公告)日：2005-01-18
申请号：US09808832
申请日：2001-03-15
申请人： Robert A. Copeland , Charles F. Albright , Andrew P. Combs , Randine L. Dowling , Nilsa R. Graciani , Wei Han , C. Anne Higley , Pearl S. Huang , Eddy W. Yue , Susan V. DiMeo
发明人： Robert A. Copeland , Charles F. Albright , Andrew P. Combs , Randine L. Dowling , Nilsa R. Graciani , Wei Han , C. Anne Higley , Pearl S. Huang , Eddy W. Yue , Susan V. DiMeo
IPC分类号： A61K31/704 , A61K38/00 , A61K47/48 , A61P35/00 , A61P35/02 , C07K5/02 , C07K5/04 , C07K5/117 , C07K7/06 , A61K38/07 , A61K38/08 , A61K38/14
CPC分类号： C07K7/06 , A61K38/00 , A61K47/65
摘要： This invention is directed to antineoplastic agents conjugated to enzyme-cleavable peptides comprising the amino acid recognition sequence of a membrane-bound and/or cell-secreted peptidase, and to the use of such conjugated compounds as chemotherapeutic agents in the targeted treatment of cancers.
摘要翻译：本发明涉及与包含膜结合和/或细胞分泌的肽酶的氨基酸识别序列的酶切割肽缀合的抗肿瘤剂，以及在靶向治疗癌症中使用这些缀合化合物作为化学治疗剂。

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