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1. 发明授权

US5264455A Sulfur-substituted mevinic acid derivatives 失效
标题翻译：硫取代的维甲酸衍生物
公开(公告)号：US5264455A
公开(公告)日：1993-11-23
申请号：US724272
申请日：1991-07-01
申请人： Ravi K. Varma , Jeffrey O. Saunders , Sam T. Chao , Eric M. Gordon , Dinos P. Santafianos
发明人： Ravi K. Varma , Jeffrey O. Saunders , Sam T. Chao , Eric M. Gordon , Dinos P. Santafianos
IPC分类号： C07C317/46 , C07C323/61 , C07C323/65 , A61K31/35 , A61K31/215 , C07D339/00
CPC分类号： C07C317/46 , C07C323/61 , C07C323/65 , C07C2101/08 , C07C2101/14 , C07C2102/10
摘要： X is hydrogen or --S(O).sub.m --R.sup.1 and Y is hydrogen or S(O).sub.n --R.sup.2, except that X and Y are not both hydrogen, or one of X and Y is --S--alkyl--SH and the other is hydrogen; ##STR2## and the remaining symbols are as defined in the specification.
摘要翻译：其作为细胞选择性HMG-CoA还原酶抑制剂具有活性，因此可用作抗高胆固醇血症药。在上式中，X是氢或-S（O）m -R 1，Y是氢或S（O）n -R 2，不同之处在于X和Y不同时为氢，X和Y之一为-S- 烷基-SH，另一个是氢; ＆lt; IMAGE＆gt;其余符号如说明书中所定义。

2. 发明授权

US5173487A Mevinic acid derivatives 失效
标题翻译：油酸衍生物
公开(公告)号：US5173487A
公开(公告)日：1992-12-22
申请号：US435843
申请日：1989-11-13
申请人： Jeffrey O. Saunders , Eric M. Gordon
发明人： Jeffrey O. Saunders , Eric M. Gordon
IPC分类号： A61K31/21 , A01N37/02 , A01N43/16 , A61K31/215 , A61K31/27 , A61K31/365 , A61K31/435 , A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07C69/013 , C07C69/675 , C07C69/732 , C07C317/44 , C07C323/52 , C07C323/61 , C07D211/62 , C07D213/79 , C07D233/36 , C07D295/20 , C07D309/30 , C07D405/12 , C07D471/04 , C07F7/18
CPC分类号： C07D309/30 , C07C69/732
摘要： Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, is exhibited by a compound of the formula ##STR1## m is 0 to 3; R is selected from:(1) alkyl;(2) substituted alkyl;(3) alkoxy;(4) alkenyl;(5) cycloalkyl;(6) phenyl; and(7) substituted aryl; andR.sup.1 and R.sup.2 are as defined in the specification.

3. 发明授权

US5166364A Mevinic acid derivatives useful as antihypercholesterolemic agents and method for preparing same 失效
标题翻译：可用作抗高胆固醇血症药的米维酸衍生物及其制备方法
公开(公告)号：US5166364A
公开(公告)日：1992-11-24
申请号：US765806
申请日：1991-09-26
申请人： Jeffrey O. Saunders , Eric M. Gordon
发明人： Jeffrey O. Saunders , Eric M. Gordon
IPC分类号： C07C59/11 , C07D309/30 , C07F7/18
CPC分类号： C07F7/1856 , C07C59/11 , C07D309/30
摘要： Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy- 2-methyl)-substituted-decahydronaphthalene esters and have the structure ##STR1## wherein Z is ##STR2## wherein R is alkali metal such as Na, or H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, a method for preparing the above-mevinic acid derivatives is also provided.
摘要翻译：提供了6-羟基-8-（2,2-二甲基-1-氧丁氧基-2-甲基） - 取代十氢萘酯的维甲酸衍生物，其结构为：其中R为碱金属如Na或H或低级烷基，并且是HMG CoA还原酶抑制剂，因此可用作抗高胆固醇血症药物和治疗动脉粥样硬化，并且还可用作抗真菌剂。此外，还提供了制备上述维甲酸衍生物的方法。

4. 发明授权

US5099035A Mevinic acid derivatives useful as antihypercholesterolemic agents and method for preparing same 失效
标题翻译：可用作抗高胆固醇血症药的米维酸衍生物及其制备方法
公开(公告)号：US5099035A
公开(公告)日：1992-03-24
申请号：US662597
申请日：1991-03-01
申请人： Jeffrey O. Saunders , Eric M. Gordon
发明人： Jeffrey O. Saunders , Eric M. Gordon
IPC分类号： C07C59/11 , C07D309/30 , C07F7/18
CPC分类号： C07D309/30 , C07C59/11 , C07F7/1856
摘要： Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-decahydronaphthalene esters and have the structure ##STR1## wherein Z is ##STR2## wherein R is alkali metal such as Na, or H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, a method for preparing the above-mevinic acid derivatives is also provided.
摘要翻译：提供了6-羟基-8-（2,2-二甲基-1-氧丁氧基-2-甲基） - 取代十氢邻苯二甲酸酯的维甲酸衍生物，并且具有其中Z为的结构，其中R为碱金属如Na或H或低级烷基，并且是HMG CoA还原酶抑制剂，因此可用作抗高胆固醇血症药物和治疗动脉粥样硬化，并且还可用作抗真菌剂。此外，还提供了制备上述维甲酸衍生物的方法。

5. 发明授权

US5001148A Mevinic acid derivatives 失效
标题翻译：乙酸衍生物
公开(公告)号：US5001148A
公开(公告)日：1991-03-19
申请号：US362899
申请日：1989-06-07
申请人： Jeffrey O. Saunders , Eric M. Gordon
发明人： Jeffrey O. Saunders , Eric M. Gordon
IPC分类号： A61K31/215 , A01N37/18 , A61K31/235 , A61P3/06 , A61P9/10 , A61P43/00 , C07C235/04 , C07C235/06 , C07C235/08 , C07C235/16 , C07C239/06 , C07D295/18 , C07D295/185 , C07D309/30 , C07F7/18
CPC分类号： C07D295/185 , C07C235/06 , C07C235/08 , C07C235/16 , C07D309/30 , C07F7/1856 , C07C2102/28
摘要： Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.n,(x) phenyl-S(O).sub.n,(xi) substituted phenyl-S(O).sub.n in which one or more substituents are X and Y, and(xii) oxo,(c) alkyl-S(O).sub.n,(d) cycloalkyl-S(O).sub.n,(e) phenyl-S(O).sub.n,(f) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y,(g) halogen,(h) hydroxy,(i) alkoxy,(j) alkoxycarbonyl,(k) acyloxy,(l) phenyl, and(m) substituted phenyl in which one or more substituents are X and Y,(7) phenyl,(8) substituted phenyl in which one or more substituents are X or Y,(9) amino,(10) alkylamino,(11) dialkylamino,(12) phenylamino,(13) substituted phenylamino in which one or more substituents are X or Y,(14) alkyl(substituted phenyl)amino in which one or more substituents are X and Y,(15) phenylalkylamino,(16) di(phenylalkyl)amino,(17) substituted phenylalkylamino in which one or more substituents are X or Y,(18) a member selected from(a) piperidinyl,(b) pyrrolidinyl,(c) piperazinyl,(d) morpholinyl,(e) thiomorpholino,(f) histaminyl,(g) 3-aminomethyl pyridinyl, and(19) hydroxy substituted alkylamino;X and Y are independently hydrogen, halogen, trifluoromethyl, alkyl, nitro, alkoxy, or cyano;n is 0, 1, or 2;R.sup.4 is ##STR2## M+ is hydrogen, ammonium, or an alkali metal.

6. 发明授权

US09328077B2 Bicyclic PKM2 activators 有权
标题翻译：双环PKM2激活剂
公开(公告)号：US09328077B2
公开(公告)日：2016-05-03
申请号：US13996286
申请日：2011-12-21
申请人： Francesco G. Salituro , Jeffrey O. Saunders
发明人： Francesco G. Salituro , Jeffrey O. Saunders
IPC分类号： C07D265/36 , C07D265/18 , C07D413/12
CPC分类号： C07D413/12 , C07D265/18 , C07D265/36
摘要： Compounds and compositions comprising compounds that activate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that activate PKM2 in the treatment of cancer.
摘要翻译：包含激活丙酮酸激酶M2（PKM2）的化合物的化合物和组合物在本文中描述。本文还描述了使用激活PKM2的化合物治疗癌症的方法。

7. 发明授权

US08785450B2 Therapeutic compounds and compositions 有权
公开(公告)号：US08785450B2
公开(公告)日：2014-07-22
申请号：US12826630
申请日：2010-06-29
申请人： Francesco G. Salituro , Jeffrey O. Saunders , Shunqi Yan
发明人： Francesco G. Salituro , Jeffrey O. Saunders , Shunqi Yan
IPC分类号： A61K31/496 , A61K31/4709 , C07D215/36 , C07D401/12 , C07D401/14 , C07D405/06 , C07D471/00
CPC分类号： C07D215/36 , A61K31/497 , A61K31/5513 , C07D215/40 , C07D239/42 , C07D241/20 , C07D243/08 , C07D271/12 , C07D277/64 , C07D277/68 , C07D295/192 , C07D319/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D417/14 , Y02P20/582
摘要： Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

8. 发明申请

US20120122849A1 PKM2 MODULATORS FOR USE IN THE TREATMENT OF CANCER 有权
标题翻译：用于治疗癌症的PKM2调节剂
公开(公告)号：US20120122849A1
公开(公告)日：2012-05-17
申请号：US13289551
申请日：2011-11-04
申请人： Francesco G. Salituro , Jeffrey O. Saunders
发明人： Francesco G. Salituro , Jeffrey O. Saunders
IPC分类号： A61K31/551 , C07D417/12 , C07D413/12 , C07D339/06 , C07D409/12 , A61P35/00 , A61K31/428 , A61K31/385 , A61K31/4436 , A61K31/496 , A61K31/4709 , C07D263/58 , A61K31/423
CPC分类号： C07D263/58 , C07D277/68 , C07D339/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.
摘要翻译：本文描述了调节丙酮酸激酶M2（PKM2）的化合物。本文还描述了包含该化合物的药物组合物，以及使用该化合物治疗癌症的方法。

9. 发明申请

US20120088747A1 SULFONAMIDE CONTAINING COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：含有磺酰胺的化合物及其用途
公开(公告)号：US20120088747A1
公开(公告)日：2012-04-12
申请号：US13126613
申请日：2009-10-30
申请人： Jeffrey O. Saunders
发明人： Jeffrey O. Saunders
IPC分类号： A61K31/5377 , C07D403/04 , C07D413/04 , C07D405/04 , C07D403/06 , C07D405/06 , C07D409/06 , C07D411/06 , C07D403/12 , C07D403/14 , C07D417/12 , C07D401/12 , A61K31/4196 , A61K31/433 , A61K31/454 , A61K31/498 , A61K31/506 , A61P3/10 , A61P27/02 , A61P25/00 , A61P13/12 , A61P3/00 , A61P9/00 , C07D249/08
CPC分类号： C07D249/08 , A61K31/40 , A61K31/44 , C07D249/10 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/06 , C07D411/06 , C07D413/04
摘要： Compounds, compositions and methods for treating GHS-R mediated disorders are described herein.
摘要翻译：本文描述了用于治疗GHS-R介导的病症的化合物，组合物和方法。

10. 发明申请

US20100331307A1 THERAPEUTIC COMPOUNDS AND COMPOSITIONS 有权
标题翻译：治疗化合物和组合物
公开(公告)号：US20100331307A1
公开(公告)日：2010-12-30
申请号：US12826630
申请日：2010-06-29
申请人： Francesco G. Salituro , Jeffrey O. Saunders , Shunqi Yan
发明人： Francesco G. Salituro , Jeffrey O. Saunders , Shunqi Yan
IPC分类号： A61K31/5513 , A61P35/00 , A61K31/497 , C07D401/12 , C07D417/14 , C07D405/14 , C07D401/14
CPC分类号： C07D215/36 , A61K31/497 , A61K31/5513 , C07D215/40 , C07D239/42 , C07D241/20 , C07D243/08 , C07D271/12 , C07D277/64 , C07D277/68 , C07D295/192 , C07D319/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D417/14 , Y02P20/582
摘要： Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
摘要翻译：包含调节丙酮酸激酶M2（PKM2）的化合物的化合物和组合物在本文中描述。本文还描述了使用调节PKM2的化合物治疗癌症的方法。

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