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1. 发明授权

US4870199A Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters 失效
标题翻译：合成二保护R [R *，S *] - 3,5-二羟基-6-氧代己酸酯的方法
公开(公告)号：US4870199A
公开(公告)日：1989-09-26
申请号：US166594
申请日：1988-03-10
申请人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
发明人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
IPC分类号： C07D209/18 , C07D233/54 , C07F7/18
CPC分类号： C07D233/64 , C07D209/18 , C07F7/1852 , Y02P20/55
摘要： Process for the synthesis of compounds of the formula ##STR1## in R[R*,S*] enantiomeric form, wherein each P.sub.1 is independently an hydroxy group-protecting group, andR.sub.2z is C.sub.1-4 alkyl, benzyl or allyl,comprising, as a key step when R.sub.2z is R.sub.2x, the reaction of the compound of the formula ##STR2## in (S) enantiomeric form with a compound of the formulaMg.sup. .circle.+2 (.sup..crclbar. OOC--CH.sub.2 --COOR.sub.2x).sub.2to obtain a compound of the formula ##STR3## in (S) enantiomeric form, and, as a key step when R.sub.2z is R.sub.2y, the reaction of a compound of the formula ##STR4## in (S) enantioimeric form with a compound of the formulaLi.sup..sym..crclbar. CH.sub.2 --COOR.sub.2yto obtain a compound of the formula ##STR5## in (S) enantiomeric form, wherein R.sub.2x is primary or secondary C.sub.1-4 alkyl, benzyl or allyl,R.sub.2y is C.sub.1-4 alkyl not containing an asymmetric carbon atom, andR.sub.3 ' is methyl or ethyl,processes for the synthesis of compounds of the formula ##STR6## comprising reacting a compound of the formula ##STR7## with the reaction product of a strong base and a compound of the formula ##STR8## optionally followed by, when R.sub.2z is allyl, cleavage of the allyl and P.sub.1 groups to obtain the corresponding compound of the formula ##STR9## wherein each R.sub.7 is methyl or ethyl,R is as defined in the specification, and eachP.sub.1 independently and R.sub.2z are as defined above, andthe compounds of the formula ##STR10## wherein R and each R.sub.7 are as defined above.
摘要翻译：用于合成R [R *，S *]对映体形式的式“IMAGE”的化合物的方法，其中每个P1独立地是羟基保护基，R2z是C1-4烷基，苄基或烯丙基，包括作为 R2z为R2x时的关键步骤，式（S）对映异构形式的式（IMA）化合物与式Mg＆cir＆+2（（ - ）OOC-CH2-COOR2x）2的化合物的反应，得到化合物式（S）对映体形式的式（IMAGE）式中，作为R2z为R2y的关键步骤，式（S）对映异构体形式的式“IMAGE”的化合物与式Li ）（ - ）CH2-COOR2y，得到（S）对映异构体形式的下式的化合物，其中R2x是伯或仲C 1-4烷基，苄基或烯丙基，R2y是不含不对称碳原子的C 1-4烷基，并且R 3'是甲基或乙基，用于合成式IMA化合物的方法包括使式IMA的化合物与强碱的反应产物 da化合物，其中当R 2z是烯丙基时，烯丙基和P1基团裂解，得到相应的式“IMAGE”化合物，其中每个R 7是甲基或乙基，R如说明书中所定义，每个P1独立地和R2z如上所定义，并且式“IMAGE”的化合物其中R和每个R 7如上所定义。

2. 发明申请

US20090203694A1 INHIBITORS OF UNDECAPRENYL PYROPHOSPHATE SYNTHASE 审中-公开
公开(公告)号：US20090203694A1
公开(公告)日：2009-08-13
申请号：US12375129
申请日：2007-07-25
申请人： Timothy Brian Hurley , Stefan Peukert , Sompong Wattanasin
发明人： Timothy Brian Hurley , Stefan Peukert , Sompong Wattanasin
IPC分类号： A61K31/5377 , C07D401/12 , A61K31/454 , C07D413/12 , C07D471/10 , A61K31/438 , A61K31/4439 , A61P31/04
CPC分类号： C07D207/416 , C07D209/54 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/10 , C07D487/10
摘要： The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions comprising these compounds and methods of using these compounds for treating bacterial disease, such as bacterial infection.

3. 发明授权

US06555533B2 Use of certain substituted caprolactams in treating tumors 失效
标题翻译：某些取代己内酰胺在治疗肿瘤中的应用
公开(公告)号：US06555533B2
公开(公告)日：2003-04-29
申请号：US09805010
申请日：2001-03-12
申请人： Frederick Ray Kinder, Jr. , Kenneth Walter Bair , Christopher Turchik Jagoe , Richard William Versace , Sompong Wattanasin
发明人： Frederick Ray Kinder, Jr. , Kenneth Walter Bair , Christopher Turchik Jagoe , Richard William Versace , Sompong Wattanasin
IPC分类号： A61K3155
CPC分类号： C07D401/12 , C07D223/10 , C07D403/12 , C07D409/12
摘要： The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.
摘要翻译：本发明涉及某些取代的己内酰胺化合物，含有所述化合物的药物组合物，所述化合物在治疗肿瘤中的用途以及制备所述化合物的方法。

4. 发明授权

US5753675A Quinoline analogs of mevalonolactone and derivatives thereof 失效
标题翻译：甲羟戊酸内酯的喹啉类似物及其衍生物
公开(公告)号：US5753675A
公开(公告)日：1998-05-19
申请号：US498301
申请日：1990-03-23
申请人： Sompong Wattanasin
发明人： Sompong Wattanasin
IPC分类号： C07D217/16 , C07D405/06 , A61K31/47 , C07D401/04 , C07D405/04
CPC分类号： C07D405/06 , C07D217/16
摘要： Quinoline analogs of mevalonolactone of the following formula are useful as anti-cholesterol synthesis agents: ##STR1## where the substituents are as defined in the specification.
摘要翻译：具有下式的甲羟戊酸内酯的喹啉类似物可用作抗胆固醇合成剂：其中取代基如说明书中所定义。

5. 发明授权

US07202364B2 Certain phenylacetic acids and derivatives 失效
标题翻译：某些苯乙酸及其衍生物
公开(公告)号：US07202364B2
公开(公告)日：2007-04-10
申请号：US10724457
申请日：2003-11-25
申请人： Roger A. Fujimoto , Leslie W. McQuire , Lauren G. Monovich , Benjamin B. Mugrage , David T. Parker , John H. VanDuzer , Sompong Wattanasin
发明人： Roger A. Fujimoto , Leslie W. McQuire , Lauren G. Monovich , Benjamin B. Mugrage , David T. Parker , John H. VanDuzer , Sompong Wattanasin
IPC分类号： C07D215/38 , C07D215/44 , C07C229/00
CPC分类号： C07D215/38 , C07C229/42 , C07D215/40 , C07D215/44 , C07D317/58 , C07D333/20 , C07D333/28
摘要： Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3–C6)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C3–C6)cycloalkyl-monocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof; and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.
摘要翻译：式（I）化合物

6. 发明授权

US5001255A Idene analogs of mevalonolactone and derivatives thereof 失效
标题翻译：甲羟戊酸内酯类似物及其衍生物
公开(公告)号：US5001255A
公开(公告)日：1991-03-19
申请号：US214560
申请日：1988-07-01
申请人： Faizulla G. Kathawala , Sompong Wattanasin
发明人： Faizulla G. Kathawala , Sompong Wattanasin
IPC分类号： C07C17/26 , C07C45/00 , C07C47/24 , C07C47/57 , C07D309/30
CPC分类号： C07D309/30 , C07C17/2632 , C07C45/00 , C07C47/24 , C07C47/57
摘要： Compounds of the formula ##STR1## the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
摘要翻译：下式的化合物其用于抑制胆固醇生物合成和降低血液胆固醇水平以及因此在治疗高脂蛋白血症和动脉粥样硬化中的用途，包含这些化合物的药物组合物及其合成方法和中间体。

7. 发明授权

US4939159A Azaindole derivatives useful as cholesterol biosynthesis inhibitors 失效
标题翻译：可用作胆固醇生物合成抑制剂的Azaindole衍生物
公开(公告)号：US4939159A
公开(公告)日：1990-07-03
申请号：US320664
申请日：1989-03-08
申请人： Paul L. Anderson , Faizulla G. Kathawala , Nicholas A. Paolella , Sompong Wattanasin
发明人： Paul L. Anderson , Faizulla G. Kathawala , Nicholas A. Paolella , Sompong Wattanasin
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of the formula I: ##STR1## wherein X is the residue of an unsubstituted 6-membered aromatic ring having 3 carbon atoms and one nitrogen atom;R.sup.1 is C.sub.1-6 primary alkyl (free of asymmetric carbon atoms), or isopropyl;R.sup.2 is substituted or unsubstituted phenyl, primary or secondary C.sub.1-6 alkyl (free of asymmetric carbons),C.sub.3-6 cycloalkyl or phenalkyl as defined in the Specification ##STR2## in which R.sup.8 is hydrogen, R.sup.9 or M, whereinR.sup.9 is a physiologically acceptable and hydrolyzable ester group, andM is a pharmaceutically acceptable cation;are obtained by multi-step processes and are useful as cholesterol biosynthesis inhibitors. 3
摘要翻译：式I的化合物：其中X是具有3个碳原子和一个氮原子的未取代的6元芳环的残基; R1是C1-6的伯烷基（不含不对称碳原子）或异丙基; R2是取代或未取代的苯基，主要或仲C 1-6烷基（不含不对称碳），如说明书中所定义的C 3-6环烷基或苯烷基，其中R 8是氢，R 9或M 其中R9是生理上可接受和可水解的酯基，M是药学上可接受的阳离子; 通过多步法获得并且可用作胆固醇生物合成抑制剂。

8. 发明授权

US08372885B2 Organic compounds and their uses 有权
标题翻译：有机化合物及其用途
公开(公告)号：US08372885B2
公开(公告)日：2013-02-12
申请号：US12557654
申请日：2009-09-11
申请人： Markus Rolf Dobler , Francois Lenoir , David Thomas Parker , Yunshan Peng , Grazia Piizzi , Sompong Wattanasin
发明人： Markus Rolf Dobler , Francois Lenoir , David Thomas Parker , Yunshan Peng , Grazia Piizzi , Sompong Wattanasin
IPC分类号： A61K31/19 , C07C229/00 , C07C259/04
CPC分类号： C07D309/22 , C07B2200/05 , C07C259/06 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07D211/70 , C07D213/30 , C07D307/42 , C07D307/80
摘要： The present application describes organic compounds of a general formula: and salts, and isomers thereof, wherein R, R2 and R3 are defined in the specification. The compounds are useful for treating a gram-negative bacterial infection.
摘要翻译：本申请描述了通式为的有机化合物及其盐及其异构体，其中R 1，R 2和R 3在本说明书中定义。该化合物可用于治疗革兰氏阴性细菌感染。

9. 发明授权

US06407065B1 VLA-4 antagonists 失效
公开(公告)号：US06407065B1
公开(公告)日：2002-06-18
申请号：US09233517
申请日：1999-01-19
申请人： Sompong Wattanasin , Peter Josef Von Matt
发明人： Sompong Wattanasin , Peter Josef Von Matt
IPC分类号： C07K5062
CPC分类号： C07C275/42 , A61K31/167 , C07B2200/07 , C07C237/22
摘要： Compounds of the formula I as defined, and their pharmaceutically acceptable salts are VLA-4 antagonists which are useful in inhibiting cell adhesion and in the therapeutic or prophylactic treatment of inflammatory and autoimmune diseases, particularly inflammatory airways diseases. They are particularly useful in reducing post-surgical inflammation, especially that resulting from transplant surgery.

10. 发明授权

US06239127B1 Certain substituted caprolactams, pharmaceutical compositions containing them and a process for their preparation 有权
标题翻译：某些取代的己内酰胺，含有它们的药物组合物及其制备方法
公开(公告)号：US06239127B1
公开(公告)日：2001-05-29
申请号：US09441739
申请日：1999-11-17
申请人： Frederick Ray Kinder, Jr. , Kenneth Walter Bair , Christopher Turchik Jagoe , Richard William Versace , Sompong Wattanasin
发明人： Frederick Ray Kinder, Jr. , Kenneth Walter Bair , Christopher Turchik Jagoe , Richard William Versace , Sompong Wattanasin
IPC分类号： C07D22310
CPC分类号： C07D401/12 , C07D223/10 , C07D403/12 , C07D409/12
摘要： The present invention relates to certain substituted caprolactam compounds of formula (I), where R1 is (C1-6)alkyl or (C3-6)cycloalkyl; R2 hydrogen or (C1-6)alkyl; X is (C1-12)alkynylene; (C2-12)alkynylene; m is 0 or 1; and R3 is (C3-8)cycloalkyl; or an aromatic ring system selected from (II, III, IV and V), where R4 is hydrogen, chloro, or methoxy; R5 is hydrogen, chloro, (C1-18)alkyl or (C1-18)alkoxy, and Z is oxygen, sulfur, N—H, or N—CH3; or a pharmaceutically acceptable acid addition salt thereof, where possible, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.
摘要翻译：本发明涉及式（I）的某些取代的己内酰胺化合物，其中R 1是（C 1-6）烷基或（C 3-6）环烷基; R2氢或（C1-6）烷基; X为（C1-12）亚炔基; （C2-12）亚炔基; m为0或1; 并且R 3是（C 3-8）环烷基; 或选自（II，III，IV和V）的芳族环系统，其中R 4是氢，氯或甲氧基; R5是氢，氯，（C1-18）烷基或（C1-18）烷氧基，Z是氧，硫，N-H或N-CH3; 或其药学上可接受的酸加成盐，在可能的情况下，含有所述化合物的药物组合物，所述化合物在治疗肿瘤中的用途以及制备所述化合物的方法。

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