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1. 发明申请

US20090326021A1 THIAZOLO NAPHTHYL ACIDS 审中-公开
标题翻译：三唑酚酸
公开(公告)号：US20090326021A1
公开(公告)日：2009-12-31
申请号：US12554131
申请日：2009-09-04
申请人： Thomas J. COMMONS
发明人： Thomas J. COMMONS
IPC分类号： A61K31/426 , C07D277/24 , C07D417/02 , A61K31/427 , A61P1/00
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。

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

US06316467B1 Elevation of HDL cholesterol by 4-[(Aminothioxomethyl)-hydrazono]-N-(substituted)-4-arylbutanamides 失效
标题翻译： 4 - [（氨基硫代甲基） - 肼基] -N-（取代的）-4-芳基丁酰胺升高HDL胆固醇
公开(公告)号：US06316467B1
公开(公告)日：2001-11-13
申请号：US09193026
申请日：1998-11-16
申请人： Thomas J. Commons
发明人： Thomas J. Commons
IPC分类号： A61K31445
CPC分类号： A61K31/4453 , A61K31/175
摘要： Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis. These compounds are represented by the formula wherein: R1, R2, and R3 are independently hydrogen, C1-C6 alkyl, phenyl or —(CH2)1-6 phenyl where phenyl is optionally substituted by halogen, cyano, nitro, C1-C6 alkyl, C1-C6alkoxy, trifluoromethyl, C1-C6 alkoxycarbonyl, —CO2H or OH; R4 and R5 are independently hydrogen, C1-C10 alkyl, C3-C8 cycloalkyl, —(CH2)0-6Ar1 where Ar1 is phenyl, naphthyl, furanyl, pyridinyl or thenyl and Ar1 can be optionally substituted by halogen, cyano, nitro, C1-C6 alkyl, phenyl, C1-C6 alkoxy, phenoxy, trifluoromethyl, C1-C6 alkoxycarbonyl, —CO2H or OH, or R4 and R5 together with the nitrogen to which R4 and R5 are attached form a ring containing 4-7 carbon atoms; and Ar is phenyl, naphthyl, furanyl, pyridinyl or thienyl which may be optionally substituted by halogen, cyano, nitro, C1-C6 alkyl, C3-C6 cycloalkyl, phenyl, C1-C6 alkoxy, phenoxy, trifluoromethyl, C1-C6 alkoxycarbonyl, —CO2H or OH.
摘要翻译：本发明的化合物增加高密度脂蛋白或HDL的血浆水平，“良好”胆固醇，因此可用于治疗疾病如动脉粥样硬化。这些化合物可以由下式表示：R1，R2和R3独立地为氢，C1-C6烷基，苯基或 - （CH2）1-6苯基，其中苯基任选被卤素，氰基，硝基，C 1 -C 6烷基， C 1 -C 6烷氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH; R 4和R 5独立地是氢，C 1 -C 10烷基，C 3 -C 8环烷基， - （CH 2）0-6Ar1，其中Ar 1是苯基，萘基，呋喃基，或芳基，Ar 1可以任选被卤素，氰基，硝基，C 1 -C 6烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH，或R 4和R 5与氮一起取代 R 4和R 5连接形成含有4-7个碳原子的环; Ar是苯基，萘基，呋喃基，吡啶基或噻吩基，其可任选被卤素，氰基，硝基，C 1 -C 6烷基，C 3 -C 6环烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH。

8. 发明授权

US5512565A 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：US5512565A
公开(公告)日：1996-04-30
申请号：US413559
申请日：1995-03-30
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 , A61K31/54 , C07D279/12
CPC分类号： C07D295/205 , C07C271/40 , C07C2101/14 , C07C2103/93
摘要： The compounds of the formula: ##STR1## in which ##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。

9. 发明授权

US5190940A 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：US5190940A
公开(公告)日：1993-03-02
申请号：US796500
申请日：1991-11-22
申请人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
发明人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
IPC分类号： C07C271/44 , C07C271/56 , C07D211/16 , C07D295/205
CPC分类号： C07D295/205 , C07C271/44 , C07C271/56 , C07D211/16
摘要： The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## where R.sup.3,R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl or gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.
摘要翻译：下式的化合物：其中R 1是氢或烷基; R2是烷基，环烷基，环烷基烷基，苯基烷基或烷基苯基烷基; 或者R 1和R 2一起形成下式的杂环部分：其中X是，其中R 3，R 4和R 5独立地是氢，烷基，苯基或取代的苯基，其中取代基是卤代，烷氧基或三氟甲基; R6是氢，烷基或偕二烷基，n是整数0,1或2之一，是用于治疗哺乳动物高血清胆固醇水平和相关疾病状态的胆固醇酯水解酶抑制剂，例如冠心病，动脉粥样硬化，家族性高胆固醇血症，高脂血症等。

10. 发明授权

US5169844A 4-substituted piperidinecarboxylic acid esters: inhibition of cholesterol absorption 失效
标题翻译： 4-取代哌啶羧酸酯：抑制胆固醇吸收
公开(公告)号：US5169844A
公开(公告)日：1992-12-08
申请号：US812512
申请日：1991-12-20
申请人： Thomas J. Commons , Donald P. Strike
发明人： Thomas J. Commons , Donald P. Strike
IPC分类号： C07D211/46
CPC分类号： C07D211/46
摘要： Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in inhibition of absorption of cholesterol and thus lowers serum cholesterol levels. Compounds of the formula below: ##STR1## where R.sup.1 is selected from alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or arylalkyl and R.sup.2 is hydrogen or alkyl or --NR.sup.1 R.sup.2 is morpholine, thiomorpholine or 4-substituted or unsubstituted piperidine and R.sup.3, R.sup.4, R.sup.5, R.sup.6 are hydrogen, alkyl, alkoxy, halogen, nitro, cyano, perhaloalkyl, alkanoyloxy, alkoxycarbonyl or hydroxycarbonyl have been shown to inhibit the enzymes CEH and/or ACAT in in vitro tests to inhibit absorption of radio-labeled cholesterol in rats.
摘要翻译：酶胆固醇酯水解酶（CEH）和/或酰基辅酶A：胆固醇酰基转移酶（ACAT）的抑制导致胆固醇吸收的抑制，从而降低血清胆固醇水平。下式的化合物：其中R 1选自烷基，烯基，环烷基，环烷基烷基或芳烷基，R 2是氢或烷基或-NR 1 R 2是吗啉，硫代吗啉或4-取代或未取代的哌啶，R 3，R 4，R 5， R6是氢，烷基，烷氧基，卤素，硝基，氰基，全卤烷基，烷酰氧基，烷氧基羰基或羟基羰基，在体外试验中抑制酶CEH和/或ACAT以抑制大鼠放射性标记胆固醇的吸收。

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