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1. 发明授权

US5332716A Pollen suppressant comprising a 5-oxy- or amino-substituted cinnoline 失效
标题翻译：含有5-氧基或氨基取代的噌啉的花粉抑制剂
公开(公告)号：US5332716A
公开(公告)日：1994-07-26
申请号：US243895
申请日：1988-09-13
申请人： Jeffrey Labovitz , William J. Guilford , Yi Liang , Lawrence Fang , Thomas G. Patterson
发明人： Jeffrey Labovitz , William J. Guilford , Yi Liang , Lawrence Fang , Thomas G. Patterson
IPC分类号： A01H1/02 , A01N43/58 , C07D237/28
CPC分类号： A01H1/02 , A01N43/58 , C07D237/28
摘要： Pollen suppressants of the formula ##STR1## wherein X represents a group of the formula OR.sup.1 or NR.sup.1 R.sup.2 wherein R.sup.1 represents a C.sub.1 -C.sub.4 alkyl (optionally substituted with a C.sub.1 -C.sub.4 alkoxy group, 1 to 3 halogen atoms, or a carboxy or C.sub.1 -C.sub.4 alkylcarbonyl group), alkenyl (optionally substituted with 1 to 3 halogen atoms), or alkynyl group and R.sup.2 represents H or CH.sub.3, with the proviso that when R.sup.1 is CH.sub.3 , R.sup.2 is CH.sub.3 ; Y is hydrogen, C.sub.1 -C.sub.22 linear alkyl or alkenyl containing up to four C.dbd.C double bonds C.sub.3 -C.sub.6 branched alkyl or alkenyl, C.sub.2 -C.sub.4 alkoxyalkyl, cyclohexylmethyl, halogenated C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, --(CH.sub.2 CH.sub.2 O).sub.m CH.sub.2 CH.sub.3 in which m is an integer from 1 to 5, or --CH(CH.sub.2 OR.sup.4)CH.sub.2 OR.sup.5 or --CH.sub.2 CHOR.sup.4 CH.sub.2 OR.sup.5 in which either R.sup. 4 or R.sup.5 but not both represent a C.sub.1 -C.sub.22 linear alkyl- or alkenyl-carbonyl group containing up to four C-C double bonds; and R represents C.sub.1 -C.sub.4 alkyl, phenyl, naphthyl, or phenyl or naphthyl substituted with one to three substituents selected from the group consisting of halogen, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, and cyano; and salts thereof are disclosed along with methods of producing these compounds and of using them to produce hybrid seed in self-fertilizing plants.
摘要翻译：其中X表示式OR1或NR1R2的基团，其中R1表示C1-C4烷基（任选被C 1 -C 4烷氧基，1至3个卤素原子或羧基或C 1 -C 4烷氧基取代）的花粉抑制剂， C4烷基羰基），烯基（任选被1至3个卤素原子取代）或炔基，R 2表示H或CH 3，条件是当R 1为CH 3时，R 2为CH 3; Y是氢，含有至多四个C = C双键的C-C22直链烷基或烯基C 3 -C 6支链烷基或烯基，C 2 -C 4烷氧基烷基，环己基甲基，卤代C 1 -C 4烷基，苯基，苄基， - （CH 2 CH 2 O）m CH 2 CH 3 其中m是1至5的整数，或-CH（CH 2 OR 4）CH 2 OR 5或-CH 2 CHOR 4 CH 2 OR 5，其中R 4或R 5不是均表示包含至多四个CC双重的C 1 -C 22直链烷基或链烯基 - 羰基债券苯基，萘基或被一至三个选自卤素，三卤代甲基，C 1 -C 4烷氧基，C 1 -C 4烷基和氰基的取代基取代的苯基或萘基; 以及它们的盐以及这些化合物的制备方法以及使用它们在自体施肥植物中产生杂交种子。

2. 发明授权

US5696055A Pollen suppressant comprising a 5-oxy- or amino substituted cinnoline 失效
标题翻译：含有5-氧基或氨基取代的噌啉的花粉抑制剂
公开(公告)号：US5696055A
公开(公告)日：1997-12-09
申请号：US818732
申请日：1992-01-06
申请人： Jeffrey Labovitz , William J. Guilford , Yi Liang , Lawrence Fang , Thomas G. Patterson
发明人： Jeffrey Labovitz , William J. Guilford , Yi Liang , Lawrence Fang , Thomas G. Patterson
IPC分类号： A01H1/02 , A01N43/58 , C07D237/28
CPC分类号： A01H1/02 , A01N43/58 , C07D237/28
摘要： Pollen suppressants of the formula ##STR1## wherein X represents a group of the formula OR.sup.1 or NR.sup.1 R.sup.2 wherein R.sup.1 represents a C.sub.1 -C.sub.4 alkyl (optionally substituted with a C.sub.1 -C.sub.4 alkoxy group, 1 to 3 halogen atoms, or a carboxy or C.sub.1 -C.sub.4 alkylcarbonyl group), alkenyl (optionally substituted with 1 to 3 halogen atoms), or alkynyl group and R.sup.2 represents H or CH.sub.3, with the proviso that when R.sup.1 is C.sub.3, R.sup.2 is CH.sub.3 ; Y is hydrogen, C.sub.1 -C.sub.22 linear alkyl or alkenyl containing up to four C.dbd.C double bonds, C.sub.3 -C.sub.6 branched alkyl or alkenyl, C.sub.2 -C.sub.4 alkoxyalkyl, cyclohexylmethyl, halogenated C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, --(CH.sub.2 CH.sub.2 O).sub.m CH.sub.2 CH.sub.3 in which m is an integer from 1 to 5, or --CH(CH.sub.2 OR.sup.4)CH.sub.2 OR.sup.5 or --CH.sub.2 CHOR.sup.4 CH OR.sup.5 in which either R.sup.4 or R.sup.5 but not both represent a C.sub.1 -C.sub.22 linear alkyl- or alkenyl-carbonyl group containing up to four C--C double bonds; and R represents C.sub.1 -C.sub.4 alkyl, phenyl, naphthyl, or phenyl or naphthyl substituted with one to three substituents selected from the group consisting of halogen, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, and cyano; and salts thereof are disclosed along with methods of producing these compounds and of using them to produce hybrid seed in self-fertilizing plants.
摘要翻译：其中X表示式OR1或NR1R2的基团，其中R1表示C1-C4烷基（任选被C 1 -C 4烷氧基，1至3个卤素原子或羧基或C 1 -C 4烷氧基取代）的花粉抑制剂， C4烷基羰基），烯基（任选被1至3个卤素原子取代）或炔基，R 2表示H或CH 3，条件是当R 1为C 3时，R 2为CH 3; Y是氢，含有最多四个C = C双键的C1-C22直链烷基或烯基，C3-C6支链烷基或烯基，C2-C4烷氧基烷基，环己基甲基，卤代C1-C4烷基，苯基，苄基， - （CH2CH2O） mCH2CH3，其中m是1至5的整数，或-CH（CH 2 OR 4）CH 2 OR 5或-CH 2 CHOR 4 CH OR 5，其中R 4或R 5不是均表示含有至多4个CC的C 1 -C 22直链烷基或链烯基 - 羰基双重债券苯基，萘基或被一至三个选自卤素，三卤代甲基，C 1 -C 4烷氧基，C 1 -C 4烷基和氰基的取代基取代的苯基或萘基; 以及它们的盐以及这些化合物的制备方法以及使用它们在自体施肥植物中产生杂交种子。

3. 发明授权

US5129939A Pollen suppressant comprising a 5-oxy- or amino-substituted cinnoline 失效
标题翻译：含有5-氧基或氨基取代的噌啉的花粉抑制剂
公开(公告)号：US5129939A
公开(公告)日：1992-07-14
申请号：US614380
申请日：1990-11-16
申请人： Jeffrey Labovitz , William J. Guilford , Yi Liang , Lawrence Fang , Thomas G. Patterson
发明人： Jeffrey Labovitz , William J. Guilford , Yi Liang , Lawrence Fang , Thomas G. Patterson
IPC分类号： A01H1/02 , A01N43/58 , C07D237/28
CPC分类号： C07D237/28 , A01H1/02 , A01N43/58
摘要： Pollen suppressants of the formula ##STR1## wherein X represents a group of the formula OR.sup.1 or NR.sup.1 R.sup.2 wherein R.sup.1 represents a C.sub.1 -C.sub.4 alkyl (optionally substituted with a C.sub.1 -C.sub.4 alkoxy group, 1 to 3 halogen atoms, or a carboxy or C.sub.1 -C.sub.4 alkylcarbonyl group), alkenyl (optionally substituted with 1 to 3 halogen atoms), or alkynyl group and R.sup.2 represents H or CH.sub.3, with the proviso that when R.sup.1 is CH.sub.3, R.sup.2 is CH.sub.3 ; Y is hydrogen, C.sub.1 -C.sub.22 linear alkyl or alkenyl containing up to four C.dbd.C double bonds, C.sub.3 -C.sub.6 branched alkyl or alkenyl, C.sub.2 -C.sub.4 alkoxyalkyl, cyclohexylmethyl, halogenated C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, --(CH.sub.2 CH.sub.2 O).sub.m CH.sub.2 CH.sub.3 in which m is an integer from 1 to 5, or --CH(CH.sub.2 OR.sup.4)CH.sub.2 OR.sup.5 or --CH.sub.2 CHOR.sup.4 CH.sub.2 OR.sup.5 in which either R.sup.4 or R.sup.5 but not both represent a C.sub.1 -C.sub.22 linear alkyl- or alkenyl-carbonyl group containing up to four C--C double bonds; and R represents C.sub.1 -C.sub.4 alkyl, phenyl, naphthyl, or phenyl or naphthyl substituted with one to three substituents selected from the group consisting of halogen, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, and cyano; and salts thereof are disclosed along with methods of producing these compounds and of using them to produce hybrid seed in self-fertilizing plants.
摘要翻译：其中X表示式OR1或NR1R2的基团，其中R1表示C1-C4烷基（任选被C 1 -C 4烷氧基，1至3个卤素原子或羧基或C 1 -C 4烷氧基取代）的花粉抑制剂， C4烷基羰基），烯基（任选被1至3个卤素原子取代）或炔基，R 2表示H或CH 3，条件是当R 1为CH 3时，R 2为CH 3; Y是氢，含有最多四个C = C双键的C1-C22直链烷基或烯基，C3-C6支链烷基或烯基，C2-C4烷氧基烷基，环己基甲基，卤代C1-C4烷基，苯基，苄基， - （CH2CH2O） mCH2CH3，其中m是1至5的整数，或-CH（CH 2 OR 4）CH 2 OR 5或-CH 2 CHOR 4 CH 2 OR 5，其中R 4或R 5不是均表示包含至多四个CC双重的C 1 -C 22直链烷基或链烯基 - 羰基债券苯基，萘基或被一至三个选自卤素，三卤代甲基，C 1 -C 4烷氧基，C 1 -C 4烷基和氰基的取代基取代的苯基或萘基; 以及它们的盐以及这些化合物的制备方法以及使用它们在自体施肥植物中产生杂交种子。

4. 发明授权

US5304672A Method for the preparation of substituted 1,4-dihydro-4-oxo-cinnoline-3-carboxylic acid, esters and salts thereof, and intermediates used in their preparation 失效
标题翻译：制备取代的1,4-二氢-4-氧代 - 噌啉-3-羧酸的方法，其酯和盐及其制备中使用的方法
公开(公告)号：US5304672A
公开(公告)日：1994-04-19
申请号：US973629
申请日：1992-11-09
申请人： Jeffrey Labovitz , William J. Guilford , Lawrence Fang , Yi Liang
发明人： Jeffrey Labovitz , William J. Guilford , Lawrence Fang , Yi Liang
IPC分类号： C07D237/28 , C07C69/76
CPC分类号： C07D237/28
摘要： A method for the preparation of compounds of the formula ##STR1## wherein X represents a group of the formula OR.sub.1 or NR.sub.1 R.sub.2, wherein R.sub.1 and R.sub.2 independently represent H or an organic group that forms a stable covalent bond with the N or 0 of said X; Y is H or an organic group that forms a stable ester with the adjacent COO group; R is an alkyl or aryl group optionally substituted with one or more stable organic substituents; each R.sub.3 independently represents a stable organic group; and n is an integer from 0 to 3;the method using new intermediates of the formula ##STR2## wherein R.sub.3 and Y have the foregoing meanings;W is either F or Cl; andR.sub.9 is a hydrocarbon such as a C.sub.1 -C.sub.4 alkyl or alkenyl group.
摘要翻译：一种制备式（I）化合物的方法，其中X代表式OR1或NR1R2的基团，其中R1和R2独立地表示H或与N或O形成稳定的共价键的有机基团的X Y是H或与相邻COO基形成稳定酯的有机基团; R是任选被一个或多个稳定的有机取代基取代的烷基或芳基; 每个R 3独立地表示稳定的有机基团; n为0〜3的整数，使用式（VI）的新中间体的方法，其中R3和Y具有上述含义; W是F或Cl; 并且R 9是烃，例如C 1 -C 4烷基或烯基。

5. 发明授权

US5183891A Method for the preparation of substituted 1,4-dihydro-4-oxo-cinnoline-3-carboxylic acid, esters and salts thereof, and intermediates used in their preparation 失效
标题翻译：制备取代的1,4-二氢-4-氧代 - 噌啉-3-羧酸的方法，其酯和盐及其制备中使用的方法
公开(公告)号：US5183891A
公开(公告)日：1993-02-02
申请号：US434077
申请日：1989-11-09
申请人： Jeffrey Labovitz , William J. Guilford , Lawrence Fang , Yi Liang
发明人： Jeffrey Labovitz , William J. Guilford , Lawrence Fang , Yi Liang
IPC分类号： C07D237/28
CPC分类号： C07D237/28
摘要： A method for the preparation of compounds of the formula ##STR1## wherein X represents a group of the formula OR.sub.1 or NR.sub.1 R.sub.2, wherein R.sub.1 and R.sub.2 independently represent H or an organic group that forms a stable covalent bond with the N or O of said X; Y is H or an organic group that forms a stable ester with the adjacent COO group; R is an alkyl or aryl group optionally substituted with one or more stable organic substituents; each R.sub.3 independently represents a stable organic group; and n is an integer from 0 to 3;the method using new intermediates of the formula ##STR2## wherein R.sub.3 and Y have the foregoing meanings; W is either F or Cl;and R.sub.9 is a hydrocarbon such as a C.sub.1 -C.sub.4 alkyl or alkenyl group.
摘要翻译：制备式（I）的化合物的方法，其中X表示式OR1或NR1R2的基团，其中R1和R2独立地表示H或与N或O形成稳定的共价键的有机基团的X Y是H或与相邻COO基形成稳定酯的有机基团; R是任选被一个或多个稳定的有机取代基取代的烷基或芳基; 每个R 3独立地表示稳定的有机基团; n为0〜3的整数，使用式（VI）的新中间体的方法，其中R3和Y具有上述含义; W是F或Cl; 并且R 9是烃，例如C 1 -C 4烷基或烯基。

6. 发明申请

US20120190739A1 EP2 AND EP4 AGONISTS AS AGENTS FOR THE TREATMENT OF INFLUENZA A VIRAL INFECTION 审中-公开
标题翻译： EP2和EP4作为治疗流感病毒感染的代理人
公开(公告)号：US20120190739A1
公开(公告)日：2012-07-26
申请号：US13073889
申请日：2011-03-28
申请人： Daryl Faulds , William J. Guilford , Wolfgang Seifert
发明人： Daryl Faulds , William J. Guilford , Wolfgang Seifert
IPC分类号： A61K31/5585 , A61K31/5575 , A61P31/16 , A61K31/5578
CPC分类号： A61K31/5585 , A61K31/215 , A61K31/343 , A61K31/5575 , A61K31/5578 , A61K31/7012 , A61K47/6951 , A61K2300/00
摘要： The present invention is directed to the use of EP2 and/or EP4 agonists as therapeutics for the treatment of diseases associated with influenza A viruses, such as for example H5N1 and mutations thereof.
摘要翻译：本发明涉及EP2和/或EP4激动剂作为治疗剂用于治疗与甲型流感病毒（例如H5N1）及其突变相关的疾病的用途。

7. 发明申请

US20090036530A1 Crystalline acid of lipoxin A4 analogs and method of making 审中-公开
标题翻译：脂氧素A4类似物的结晶酸及其制备方法
公开(公告)号：US20090036530A1
公开(公告)日：2009-02-05
申请号：US12215928
申请日：2008-06-30
申请人： Klaus Bartel , Danja Grossbach , William J. Guilford , Michael Sander , Gabriele Winter
发明人： Klaus Bartel , Danja Grossbach , William J. Guilford , Michael Sander , Gabriele Winter
IPC分类号： A61K31/192 , C07C59/64 , A61P29/00
CPC分类号： C07C59/70 , C07C51/09
摘要： This invention is directed to a crystalline acid of a lipoxin A4 analog of Formula (II): wherein: R1 is —O—, —S(O)t— (where t is 0, 1 or 2), or a straight or branched alkylene chain; and R2 is aryl (optionally substituted by one or more substituents selected from alkyl, alkoxy, halo, haloalkyl and haloalkoxy) or aralkyl (optionally substituted by one or more substituents selected from f alkyl, alkoxy, halo, haloalkyl and haloalkoxy); and wherein the compound of Formula (II) is a single stereoisomer or any mixture of stereoisomers. This crystalline acid is useful in treating disease-states characterized by inflammation, such as inflammatory and autoimmune disorders or pulmonary or respiratory tract inflammations in humans. Methods of preparing the crystalline acid are also described.
摘要翻译：本发明涉及式（II）的脂氧素A4类似物的结晶酸：其中：R 1为-O - ， - S（O）t - （其中t为0,1或2），或直链或支链亚烷基链; 和R 2是芳基（任选被一个或多个选自烷基，烷氧基，卤素，卤代烷基和卤代烷氧基的取代基取代）或芳烷基（任选地被一个或多个选自f烷基，烷氧基，卤素，卤代烷基和卤代烷氧基的取代基取代）。并且其中式（II）的化合物是单一立体异构体或任何立体异构体的混合物。该结晶酸可用于治疗以炎症和自身免疫疾病为特征的疾病状态或人类肺或呼吸道炎症。还描述了制备结晶酸的方法。

8. 发明申请

US20080182901A1 Crystalline acid of lipoxin A4 analogs and method of making 审中-公开
标题翻译：脂氧素A4类似物的结晶酸及其制备方法
公开(公告)号：US20080182901A1
公开(公告)日：2008-07-31
申请号：US11999003
申请日：2007-12-03
申请人： Klaus Bartel , Danja Grossbach , William J. Guilford , Michael Sander , Gabriele Winter
发明人： Klaus Bartel , Danja Grossbach , William J. Guilford , Michael Sander , Gabriele Winter
IPC分类号： A61K31/192 , C07C59/64 , C07C51/367 , A61P11/00 , A61P29/00
CPC分类号： C07C59/70 , C07C51/09
摘要： This invention is directed to a crystalline acid of a lipoxin A4 analog of Formula (II): wherein: R1 is —O—, —S(O)t— (where t is 0, 1 or 2), or a straight or branched alkylene chain; and R2 is aryl (optionally substituted by one or more substituents selected from alkyl, alkoxy, halo, haloalkyl and haloalkoxy) or aralkyl (optionally substituted by one or more substituents selected from f alkyl, alkoxy, halo, haloalkyl and haloalkoxy); and wherein the compound of Formula (II) is a single stereoisomer or any mixture of stereoisomers. This crystalline acid is useful in treating disease-states characterized by inflammation, such as inflammatory and autoimmune disorders or pulmonary or respiratory tract inflammations in humans. Methods of preparing the crystalline acid are also described.
摘要翻译：本发明涉及式（II）的脂氧素A 4 H 4类似物的结晶酸：其中：R 1是-O - ， - S（O）（其中t为0,1或2）或直链或支链亚烷基链; 和R 2是芳基（任选被一个或多个选自烷基，烷氧基，卤素，卤代烷基和卤代烷氧基的取代基取代）或芳烷基（任选地被一个或多个选自F，烷基，烷氧基，卤素，卤代烷基和卤代烷氧基）; 并且其中式（II）的化合物是单一立体异构体或任何立体异构体的混合物。该结晶酸可用于治疗以炎症和自身免疫疾病为特征的疾病状态或人类肺或呼吸道炎症。还描述了制备结晶酸的方法。

9. 发明授权

US06686364B2 Benzamidine derivatives and their use as anti-coagulants 失效
标题翻译：苄脒衍生物及其作为抗凝剂的用途
公开(公告)号：US06686364B2
公开(公告)日：2004-02-03
申请号：US09924893
申请日：2001-08-07
申请人： Brad O. Buckman , David D. Davey , William J. Guilford , Michael M. Morrissey , Howard P. Ng , Gary B. Phillips , Shung C. Wu , Wei Xu
发明人： Brad O. Buckman , David D. Davey , William J. Guilford , Michael M. Morrissey , Howard P. Ng , Gary B. Phillips , Shung C. Wu , Wei Xu
IPC分类号： A61K314965
CPC分类号： C07D213/69
摘要： This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
摘要翻译：本发明涉及可用作抗凝剂的苯甲脒衍生物。本发明还涉及含有本发明化合物的药物组合物，以及使用该化合物治疗以血栓形成活性为特征的疾病状态的方法。

10. 发明授权

US06479485B2 Benzamidine derivatives and their use as anti-coagulants 失效
公开(公告)号：US06479485B2
公开(公告)日：2002-11-12
申请号：US09924413
申请日：2001-08-07
申请人： Brad O. Buckman , David D. Davey , William J. Guilford , Michael M. Morrissey , Howard P. Ng , Gary B. Phillips , Shung C. Wu , Wei Xu
发明人： Brad O. Buckman , David D. Davey , William J. Guilford , Michael M. Morrissey , Howard P. Ng , Gary B. Phillips , Shung C. Wu , Wei Xu
IPC分类号： A61K31534
CPC分类号： C07D213/69 , C07C257/18 , C07C275/42 , C07D213/74 , C07D213/79 , C07D213/81 , C07D213/82 , C07D231/12 , C07D233/56 , C07D239/52 , C07D241/18 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14
摘要： This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

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