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1. 发明授权

US07754747B2 Oxazolo-naphthyl acids 失效
标题翻译：恶唑烷酸
公开(公告)号：US07754747B2
公开(公告)日：2010-07-13
申请号：US11208777
申请日：2005-08-22
申请人： Thomas J. Commons , Richard P. Woodworth, Jr.
发明人： Thomas J. Commons , Richard P. Woodworth, Jr.
IPC分类号： C07D263/30 , A01N43/76
CPC分类号： C07D263/14 , C07D263/32 , C07D413/04 , C07D413/12 , C07D413/14
摘要： The present invention relates to oxazolo-naphthyl acids of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
摘要翻译：本发明涉及下式的恶唑并萘酸及其用于调节PAI-1表达和治疗PAI-1相关疾病的方法。

2. 发明授权

US07605172B2 Thiazolo-naphthyl acids 失效
标题翻译：噻唑并 - 萘酸
公开(公告)号：US07605172B2
公开(公告)日：2009-10-20
申请号：US11208772
申请日：2005-08-22
申请人： Thomas J. Commons
发明人： Thomas J. Commons
IPC分类号： A61K31/44 , C07D277/20 , A01N43/78
CPC分类号： C07D277/24 , C07D417/12
摘要： The present invention relates to thiazolo-naphthyl acids of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
摘要翻译：本发明涉及下式的噻唑并 - 萘酸及其用于调节PAI-1表达和治疗PAI-1相关疾病的方法。

3. 发明授权

US5527804A 4-carbamoyloxy-piperidine-1-carboxylic acid esters: inhibitors or cholesterol absorption 失效
标题翻译： 4-氨基甲酰氧基 - 哌啶-1-甲酸酯：抑制剂或胆固醇吸收
公开(公告)号：US5527804A
公开(公告)日：1996-06-18
申请号：US259229
申请日：1994-06-13
申请人： Thomas J. Commons , Christa M. LaClair
发明人： Thomas J. Commons , Christa M. LaClair
IPC分类号： A61K31/445 , A61P3/06 , A61P9/10 , C07D211/46 , C07D221/20 , C07D401/10 , C07D401/12
CPC分类号： C07D211/46
摘要： Compounds which inhibit the enzyme cholesterol ester hydrolase (CEH) thus inhibit the formation of esterified cholesterol. Esterified cholesterol is absorbed through the intestine and inhibition of the enzyme therefore results in inhibition of cholesterol absorption. The compounds of this invention inhibit cholesterol ester hydrolase and have the formula: ##STR1## wherein Z is --Ar.sup.1, --Ar.sup.1 --Ar.sup.2, --Ar.sup.1 --O--Ar.sup.2, --Ar.sup.1 --S--Ar.sup.2, ##STR2## --Ar.sup.1 --(CH.sub.2).sub.1-20 --Ar.sup.2, --Ar.sup.1 --(CH.sub.2).sub.1-20 --O--Ar.sup.2, --Ar.sup.1 --O--(CH.sub.2).sub.1-20 --Ar.sup.2, --Ar.sup.1 --(CR.sup.6 .dbd.CR.sup.6).sub.1-3 --Ar.sup.2 or --Ar.sup.1 --NR.sup.7 --Ar.sup.2 ; andA is a hydrocarbon linking group which may be interrupted by a heteroatom or a cycloalkyl, aryl, heterocycloalkyl, or an azacycloalkyl group;and R.sup.4 and R.sup.5 are independently alkyl, alkenyl, acyl, alkoxycarbonyl or H or R.sup.4 and R.sup.5 together with the interposed nitrogen form a saturated heterocyclic ring.
摘要翻译：抑制酶胆固醇酯水解酶（CEH）因此抑制酯化胆固醇形成的化合物。酯化的胆固醇通过肠被吸收，因此酶的抑制导致胆固醇吸收的抑制。本发明的化合物抑制胆固醇酯水解酶并具有下式：其中Z是-Ar1，-Ar1-Ar2，-Ar1-O-Ar2，-Ar1-S-Ar2，-I1-S-Ar2， Ar1-（CH2）1-20-Ar2 -Ar1-（CH2）1-20-O-Ar2，-Ar1-O-（CH2）1-20-Ar2，-Ar1-（CR6 = CR6）1-3 -Ar 2或-Ar 1 -NR 7 -Ar 2; 并且A是可被杂原子或环烷基，芳基，杂环烷基或氮杂环烷基间隔的烃连接基团; 并且R 4和R 5独立地是烷基，烯基，酰基，烷氧基羰基或H或R 4和R 5与所述插入的氮一起形成饱和杂环。

4. 发明授权

US5527794A Pyrido[3,4-b]indole derivatives as serotonergic agents 失效
标题翻译：吡啶并[3,4-b]吲哚衍生物作为血清素能药
公开(公告)号：US5527794A
公开(公告)日：1996-06-18
申请号：US448282
申请日：1995-05-23
申请人： Thomas J. Commons , Christa M. LaClair , Susan Christman
发明人： Thomas J. Commons , Christa M. LaClair , Susan Christman
IPC分类号： C07D471/04 , A61K31/445 , A61K31/55
CPC分类号： C07D471/04
摘要： The compound of the formula: ##STR1## where R.sub.1 and R.sub.5 are independently hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, CO.sub.2 H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl, C.sub.3 -C.sub.8 cycloalkyloxy, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkylcarbonyloxy, C.sub.2 -C.sub.7 alkoxycarbonyl, mono- or di-alkylaminocarbonyl, tetrazolyl, --OH, --(CH.sub.2).sub.1-6 OH, --SH, --NH.sub.2 or --(CH.sub.2).sub.1-6 NR.sub.8 R.sub.9 where R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkoxycarbonyl and R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 and R.sub.4 are hydrogen or taken together with the carbon atoms to which they are attached form a double bond; R.sub.6 and R.sub.7 are independently H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl or R.sub.6 and R.sub.7 taken together are polymethylene, which, with the nitrogen atom to which they are attached, form a ring of 3 to 8 atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：下式的化合物：其中R 1和R 5独立地是氢，氟，氯，溴，碘，三氟甲基，氰基，硝基，CO 2 H，C 1 -C 6烷基，C 2 -C 10烯基，C 1 -C 6烷氧基，C 3 -C 8环烷基，环烷基烷基，C 3 -C 8环烷氧基，C 2 -C 7烷基羰基，C 2 -C 7烷基羰基氧基，C 2 -C 7烷氧基羰基，单 - 或二 - 烷基氨基羰基，四唑基，-OH， - （CH 2）1-6 OH， NH 2或 - （CH 2）1-6 NR 8 R 9，其中R 8是氢，C 1 -C 6烷基，C 2 -C 7烷基羰基，C 2 -C 7烷氧基羰基和R 9是氢或C 1 -C 6烷基; R2是氢或C1-C6烷基; R3和R4是氢或与它们所连接的碳原子一起形成双键; R6和R7独立地为H，C1-C10烷基，C2-C10烯基，C3-C8环烷基，环烷基烷基或R6和R7一起是聚亚甲基，它们与它们所连接的氮原子形成3〜 8个原子; 或其药学上可接受的盐。

5. 发明授权

US5373009A Dibenzofuranyl esters of N-heterocyclic carboxylic acids 失效
标题翻译： N-杂环羧酸的二苯并呋喃基酯
公开(公告)号：US5373009A
公开(公告)日：1994-12-13
申请号：US190416
申请日：1994-02-02
申请人： Thomas J. Commons , Donald P. Strike
发明人： Thomas J. Commons , Donald P. Strike
IPC分类号： C07D307/91 , C07D405/12 , A61K31/54 , A61K31/535 , C07D211/06 , C07D295/205
CPC分类号： C07D307/91 , C07D405/12
摘要： A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, halo, trifluoromethyl, cyano, nitro, alkyl, alkoxy, --CO.sub.2 H, alkylcarbonyl, alkylcarbonyloxy, alkoxycarbonyl, mono- or di-alkylaminocarbonyl, or mono- or di-alkylaminocarbonyloxy;m is 0, 1 or 2 andR.sup.3 is alkyl;n and p are, independently, 0, 1 or 2;X is O, S or CR.sup.4 R.sup.5,where R.sup.4 and R.sup.5 are, independently, H or alkyl or R.sup.4 and R.sup.5 together with the interposed carbon atom form a 3 to 8 membered carbocyclic ring, are anti-cholesterolemic agents.
摘要翻译：下式的化合物：其中R 1和R 2独立地是卤素，三氟甲基，氰基，硝基，烷基，烷氧基，-CO 2 H，烷基羰基，烷基羰基氧基，烷氧基羰基，单或二烷基氨基羰基，或单或二烷基氨基羰基氧基; m为0,1或2，R 3为烷基; n和p独立地是0,1或2; X是O，S或CR 4 R 5，其中R 4和R 5独立地是H或烷基或R 4和R 5与插入的碳原子一起形成3至8元碳环，是抗胆固醇血症药。

6. 发明授权

US4709025A Beta-lactams substituted at C-4 with substituted aminooxymethyl 失效
标题翻译：在C-4被取代的氨氧基甲基取代的β-内酰胺
公开(公告)号：US4709025A
公开(公告)日：1987-11-24
申请号：US4529
申请日：1987-01-20
申请人： Richard E. Mewshaw , Thomas J. Commons
发明人： Richard E. Mewshaw , Thomas J. Commons
IPC分类号： C07D417/12 , A61K31/425 , A61K31/55 , C07D417/14
CPC分类号： C07D417/12
摘要： This invention provides novel antibacterial beta-lactams of the formula: ##STR1## in which R is alkyl of 1 to 6 carbon atoms, carboxyalkyl of 2 to 6 carbon atoms or alkoxycarbonylalkyl wherein the alkyl and alkoxy moieties contain, independently, 1 to 6 carbon atoms;R.sup.1 is alkylideneamino of 2 to 6 carbon atoms, alkanoylamino of 2 to 6 carbon atoms, carboxyalkylideneamino of 2 to 6 carbon atoms, alkylsulfonylamino of 1 to 6 carbon atoms, alkoxycarbonylalkylsulfonylamino of 3 to 13 carbon atoms, or N,N-cyclodialkanoylamino of 4 to 6 carbon atoms;or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供新的抗菌β-内酰胺，其结构式为：其中R是1至6个碳原子的烷基，2至6个碳原子的羧基烷基或烷氧基羰基，其中烷基和烷氧基部分独立地包含1至6个碳原子 R 1是2至6个碳原子的亚烷基氨基，2至6个碳原子的烷酰基氨基，2至6个碳原子的羧基亚烷基氨基，1至6个碳原子的烷基磺酰基氨基，3至13个碳原子的烷氧基羰基烷基磺酰基氨基，或4个N，N-二环烷酰基氨基至6个碳原子; 或其药学上可接受的盐。

7. 发明授权

US07186749B2 Pyrrolo-naphthyl acids and methods for using them 失效
标题翻译：吡咯基萘酸及其使用方法
公开(公告)号：US07186749B2
公开(公告)日：2007-03-06
申请号：US11208775
申请日：2005-08-22
申请人： Thomas J. Commons , Douglas John Jenkins
发明人： Thomas J. Commons , Douglas John Jenkins
IPC分类号： A01N43/36 , C07D257/02 , C07D207/323
CPC分类号： C07D207/333 , C07D403/12
摘要： The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
摘要翻译：本发明涉及下式的吡咯基 - 萘基化合物及其用于调节PAI-1表达和治疗PAI-1相关病症的方法。

8. 发明授权

US5466688A Pyrido[3,4-B]indole derivatives as serotonergic agents 失效
标题翻译：吡啶并[3,4-B]吲哚衍生物作为血清素能药
公开(公告)号：US5466688A
公开(公告)日：1995-11-14
申请号：US326435
申请日：1994-10-20
申请人： Thomas J. Commons , Christa M. LaClair , Susan Christman
发明人： Thomas J. Commons , Christa M. LaClair , Susan Christman
IPC分类号： C07D471/04 , A61K31/445 , C07D401/14
CPC分类号： C07D471/04
摘要： The compound of the formula: ##STR1## where R.sub.1 and R.sub.5 are independently hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, CO.sub.2 H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl, C.sub.3 -C.sub.8 cycloalkyloxy, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkylcarbonyloxy, C.sub.2 -C.sub.7 alkoxycarbonyl, mono- or di-alkylaminocarbonyl, tetrazolyl, --OH, --(CH.sub.2).sub.1-6 OH, --SH, --NH.sub.2 or --(CH.sub.2).sub.1-6 NR.sub.8 R.sub.9 where R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkoxycarbonyl and R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 and R.sub.4 are hydrogen or taken together with the carbon atoms to which they are attached form a double bond; R.sub.6 and R.sub.7 are independently H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl or R.sub.6 and R.sub.7 taken together are polymethylene, which, with the nitrogen atom to which they are attached, form a ring of 3 to 8 atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：下式的化合物：其中R 1和R 5独立地是氢，氟，氯，溴，碘，三氟甲基，氰基，硝基，CO 2 H，C 1 -C 6烷基，C 2 -C 10烯基，C 1 -C 6烷氧基，C 3 -C 8环烷基，环烷基烷基，C 3 -C 8环烷氧基，C 2 -C 7烷基羰基，C 2 -C 7烷基羰基氧基，C 2 -C 7烷氧基羰基，单 - 或二 - 烷基氨基羰基，四唑基，-OH， - （CH 2）1-6 OH， NH 2或 - （CH 2）1-6 NR 8 R 9，其中R 8是氢，C 1 -C 6烷基，C 2 -C 7烷基羰基，C 2 -C 7烷氧基羰基和R 9是氢或C 1 -C 6烷基; R2是氢或C1-C6烷基; R3和R4是氢或与它们所连接的碳原子一起形成双键; R6和R7独立地为H，C1-C10烷基，C2-C10烯基，C3-C8环烷基，环烷基烷基或R6和R7一起是聚亚甲基，它们与它们所连接的氮原子形成3〜 8个原子; 或其药学上可接受的盐。

9. 发明授权

US5391571A Cholesterol ester hydrolase inhibitors 失效
标题翻译：胆固醇酯水解酶抑制剂
公开(公告)号：US5391571A
公开(公告)日：1995-02-21
申请号：US62026
申请日：1993-05-13
申请人： Richard E. Mewshaw , Thomas J. Commons , Donald P. Strike
发明人： Richard E. Mewshaw , Thomas J. Commons , Donald P. Strike
IPC分类号： C07C271/40 , C07D295/205 , A61K31/325 , C07C271/02
CPC分类号： C07D295/205 , C07C271/40 , C07C2101/14 , C07C2103/93
摘要： The compounds of the formula: ##STR1## in which R.sup.1 is alkyl of 4 or more carbon atoms, cycloalkyl, 1-adamantyl, 2-adamantyl, 3-noradamantyl, 3-methyl-1-adamantyl, 1-fluorenyl, 9-fluorenyl, cycloalkylalkyl, phenyl, substituted phenyl, alkyl, alkoxy, halo, nitro, cyano or trifluoromethyl, phenylalkyl or substituted phenylalkyl, where the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R.sup.2 is hydrogen, alkyl or R.sup.1 taken with R.sup.2 and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula: ##STR2## wherein ##STR3## in which R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; useful as inhibitors of cholesterol ester hydrolase.
摘要翻译：下式的化合物：其中R1是4个或更多个碳原子的烷基，环烷基，1-金刚烷基，2-金刚烷基，3-降金刚烷基，3-甲基-1-金刚烷基，1-芴基，9-芴基烷基，烷氧基，卤素，硝基，氰基或三氟甲基，苯基烷基或取代的苯基烷基，其中苯环上的取代基是烷基，烷氧基，卤素，硝基，氰基，三氟甲基或苯基; R 2是氢，烷基或R 1与R 2取代，并且与它们相连的氮原子形成下式的杂环部分：其中R7是氢，烷基，羟基，烷酰氧基，羟基烷基，羟基羰基，烷氧基羰基，苯基或取代的苯基，其中取代基是烷基，烷氧基，卤素，硝基，氰基，卤代烷基，全卤代烷基或二烷基氨基烷基; R8是氢或烷基或R7和R8一起是聚亚甲基; R9是氢，烷基，苯基或取代的苯基，其中取代基是烷基，烷氧基，卤素，硝基，氰基或全卤代烷基; R10为氢，烷基或偕二烷基; n是整数0,1或2之一; 并且R 3，R 4，R 5和R 6独立地为氢，烷基，烷氧基，卤素，硝基，氰基或全卤代烷基，烷氧基羰基或羟基羰基。当X是-NR9-或R7是氨基烷基时，其药学上可接受的盐; 可用作胆固醇酯水解酶的抑制剂。

10. 发明授权

US5602151A Cholesterol ester hydrolase inhibitors 失效
标题翻译：胆固醇酯水解酶抑制剂
公开(公告)号：US5602151A
公开(公告)日：1997-02-11
申请号：US572993
申请日：1995-12-15
申请人： Richard E. Mewshaw , Thomas J. Commons , Donald P. Strike
发明人： Richard E. Mewshaw , Thomas J. Commons , Donald P. Strike
IPC分类号： C07C271/40 , C07D295/205 , A61K31/445 , C07D211/06
CPC分类号： C07D295/205 , C07C271/40 , C07C2101/14 , C07C2103/93
摘要： The compounds of the formula: ##STR1## in which X is ##STR2## where R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; are useful as inhibitors of cholesterol ester hydrolase.
摘要翻译：其中X为的化合物，其中R 7为氢，烷基，羟基，烷酰氧基，羟基烷基，羟基羰基，烷氧基羰基，苯基或取代的苯基，其中取代基为烷基，烷氧基，卤素，硝基，氰基，卤代烷基，全卤代烷基或二烷基氨基烷基; R8是氢或烷基或R7和R8一起是聚亚甲基; R9是氢，烷基，苯基或取代的苯基，其中取代基是烷基，烷氧基，卤素，硝基，氰基或全卤代烷基; R10为氢，烷基或偕二烷基; n是整数0,1或2之一; 并且R 3，R 4，R 5和R 6独立地为氢，烷基，烷氧基，卤素，硝基，氰基或全卤代烷基，烷氧基羰基或羟基羰基。当X是-NR9-或R7是氨基烷基时，其药学上可接受的盐; 可用作胆固醇酯水解酶的抑制剂。

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