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21. 发明申请

US20170362165A1 MOISTURE-STABLE HOLOGRAPHIC MEDIA 审中-公开
公开(公告)号：US20170362165A1
公开(公告)日：2017-12-21
申请号：US15536841
申请日：2015-12-11
申请人： Covestro Deutschland AG
发明人： Thomas FÄCKE , Friedrich-Karl BRUDER , Thomas RÖLLE , Dennis HÖNEL
IPC分类号： C07C229/40 , G03F7/00 , G03H1/00 , C07C271/26 , G03F7/027 , G03F7/035 , G03F7/004 , G03H1/02
CPC分类号： C07C229/40 , C07C271/26 , C07C271/28 , C07C323/43 , G03F7/001 , G03F7/0046 , G03F7/027 , G03F7/035 , G03H1/0011 , G03H1/0248 , G03H2001/0264 , G03H2001/0415 , G03H2260/12 , G03H2260/31
摘要： The invention relates to novel compounds which are especially suitable for use as writing monomers in holographic media. The invention further provides a photopolymer and a holographic medium comprising the inventive compounds, and an optical display, a security document and a holographic optical element comprising an inventive holographic medium.

22. 发明申请

US20160207938A1 QUINAZOLINE DERIVATIVES 审中-公开
公开(公告)号：US20160207938A1
公开(公告)日：2016-07-21
申请号：US15003124
申请日：2016-01-21
申请人： Janssen Pharmaceutica NV
发明人： Eddy Jean Edgard FREYNE , Timothy Pietro Suren PERERA , Peter Jacobus Johannes Antonius BUIJNSTERS , Marc WILLEMS , Gaston Stanislas Marcella DIELS , Werner Constant Johan EMBRECHTS , Peter TEN HOLTE , Frederik Jan Rita ROMBOUTS , Carsten SCHULTZ-FADEMRECHT
IPC分类号： C07D498/06 , C07C229/40 , C07D239/94
CPC分类号： C07D498/06 , C07C229/16 , C07C229/40 , C07D239/88 , C07D239/93 , C07D239/94
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N═CH— or —C1-2alkyl-; R1 and R2 each independently represents hydrogen or halo; R3 represents hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 each independently represents hydrogen or C1-4alkyl; R14 and R15 represents hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 each independently represent hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 each independently represent hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 each independently represent a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.

23. 发明申请

US20150370164A1 Patterning Methods and Methods of Making a Photoresist Composition Using a Photoresist Additive 有权
标题翻译：使用光致抗蚀剂添加剂制备光刻胶组合物的图案化方法和方法
公开(公告)号：US20150370164A1
公开(公告)日：2015-12-24
申请号：US14310058
申请日：2014-06-20
申请人： Taiwan Semiconductor Manufacturing Company, Ltd.
发明人： Chien-Chih Chen
IPC分类号： G03F7/027 , G03F7/004 , G03F7/38
CPC分类号： C07C229/40 , G03F7/0045 , G03F7/0392 , G03F7/26 , G03F7/40
摘要： Methods of forming a semiconductor device using a photoresist additive and methods of making a photoresist composition using the photoresist additive are disclosed. The photosensitive additive includes a polymer; at least one photo-acid generator (PAG); and at least one additive compound comprising a base and an acid-labile group (ALG). The at least one additive compound undergoes intramolecular cyclization to from a cyclic amide compound in the presence of acid. The at least one additive compound also neutralizes acid generated by the PAG without consuming the acid and does not absorb much light in the exposure areas.
摘要翻译：公开了使用光致抗蚀剂添加剂形成半导体器件的方法和使用光致抗蚀剂添加剂制备光致抗蚀剂组合物的方法。光敏添加剂包括聚合物; 至少一种光酸产生剂（PAG）; 和至少一种包含碱和酸不稳定基团（ALG）的添加剂化合物。所述至少一种添加剂化合物在酸存在下进行分子内环化至环状酰胺化合物。所述至少一种添加剂化合物还中和PAG产生的酸，而不消耗酸，并且不会在曝光区域吸收太多的光。

24. 发明授权

US09040553B2 Phenoxyisobutyric acid compounds and method of synthesis 有权
标题翻译：苯氧基异丁酸化合物及其合成方法
公开(公告)号：US09040553B2
公开(公告)日：2015-05-26
申请号：US13940008
申请日：2013-07-11
申请人： Iraj Lalezari , Jill Fabricant
发明人： Iraj Lalezari , Jill Fabricant
IPC分类号： C07D307/87 , C07D215/14 , C07D215/52 , C07C235/72 , C07D215/50 , C07D219/04 , C07C275/42 , C07C229/40 , A61K8/41 , A61K8/42 , A61K8/49 , A61Q19/08 , C07C215/76 , C07C233/75 , C07C235/74 , C07C275/34 , C07D215/12
CPC分类号： C07D307/87 , A61K8/411 , A61K8/42 , A61K8/4926 , A61Q19/08 , C07C215/76 , C07C229/40 , C07C233/75 , C07C235/72 , C07C235/74 , C07C275/34 , C07C275/42 , C07D215/12 , C07D215/14 , C07D215/50 , C07D215/52 , C07D219/04
摘要： The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
摘要翻译：本发明提供了一种合成取代的苯氧基甲基丙酸和相关化合物的方法。该化合物可用于抑制AGEs（高级糖化终产物）的形成。

25. 发明申请

US20150133407A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF RESPIRATORY DISORDERS 有权
标题翻译：用于治疗呼吸道疾病的组合物和方法
公开(公告)号：US20150133407A1
公开(公告)日：2015-05-14
申请号：US14399181
申请日：2013-05-14
申请人： Mahesh Kandula
发明人： Mahesh Kandula
IPC分类号： C07D473/04 , C07D213/66 , C07C237/40 , C07C237/20 , C07D339/04 , C07C229/40
CPC分类号： C07D473/04 , A61K47/48038 , A61K47/481 , A61K47/48107 , A61K47/542 , A61K47/55 , A61K47/551 , C07C229/40 , C07C237/20 , C07C237/40 , C07C239/20 , C07C275/40 , C07C2601/14 , C07D213/66 , C07D339/04
摘要： The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of viscid or excessive mucus, cough, inflammation, redness in sore throat, infection in the throat, sore throat, abnormal mucus secretion, impaired mucus transport, allergic rhinitis, asthma, COPD, respiratory muscular disorders and pain in acute sore throat.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，以及其多晶型物，溶剂合物，对映体，立体异构体和水合物。包含有效量的式I化合物和用于治疗呼吸系统疾病的方法的药物组合物可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。这些组合物可用于治疗粘稠或过度粘液，咳嗽，炎症，喉咙发红，咽喉感染，喉咙痛，粘液分泌异常，粘液运输受损，过敏性鼻炎，哮喘，COPD，呼吸肌肉疾病和疼痛在喉咙痛。

26. 发明申请

US20140228325A1 ALKENE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS 审中-公开
标题翻译：亚磷酸酯衍生物作为磷脂酸1-磷酸（S1P）受体调节剂
公开(公告)号：US20140228325A1
公开(公告)日：2014-08-14
申请号：US14174032
申请日：2014-02-06
申请人： Allergan, Inc.
发明人： Wenkui K. Fang , Ken Chow , Evelyn G. Corpuz
IPC分类号： C07F9/38 , C07C229/40
CPC分类号： C07C229/40 , C07C229/14 , C07C317/32 , C07C323/32 , C07F9/3808
摘要： The present invention relates to alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
摘要翻译：本发明涉及烯烃衍生物，其制备方法，含有它们的药物组合物及其作为药物作为鞘氨醇-1-磷酸受体调节剂的用途。

27. 发明申请

US20130178624A1 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：US20130178624A1
公开(公告)日：2013-07-11
申请号：US13744878
申请日：2013-01-18
申请人： Janssen Pharmaceutica N.V.
发明人： Eddy Jean Edgard FREYNE , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts , Peter Ten Holte , Frederik Jan Rita Rombouts , Carsten Schultz-Fademrecht
IPC分类号： C07D239/94 , C07C229/40 , C07C229/16
CPC分类号： C07D498/06 , C07C229/16 , C07C229/40 , C07D239/88 , C07D239/93 , C07D239/94
摘要： The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl, —O—N═CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 are hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 are a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.
摘要翻译：本发明涉及下式的化合物其中Z代表NH; Y代表任选被氨基，一或二（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - ， - C 3-7烯基-CO-的氨基取代的-C 3-9烷基 - ， - C 2-9烯基 - ， - 氨基，一或二（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基-NR 13 -C 1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - C 1-6烷基-CO-NH - ， - C 1-5烷基-CO NR 15 -C 1-5烷基 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het 21 -CO-， - C 1-2烷基 -NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-或-NR22-CO-C1-3烷基 - NH-; X1表示直接键，O或-O-C 1-2烷基 - ; X 2代表直接键，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基，-O-N = CH-或-C 1-2烷基 - ; R1和R2是氢或卤素; R3是氢; R4表示氢或C1-4烷氧基; R 12和R 13是氢或C 1-4烷基; R14和R15是氢; R 16和R 17各自独立地表示氢或C 1-4烷基; R 18和R 19是氢或任选被苯基或羟基取代的C 1-4烷基; R 20和R 21是氢或任选被C 1-4烷氧基取代的C 1-4烷基; Het20，Het21和Het22是选自吡咯烷基，2-吡咯烷基或任选被羟基取代的哌啶基的杂环。

28. 发明申请

US20100105668A1 Quinazoline derivatives 有权
标题翻译：喹唑啉衍生物
公开(公告)号：US20100105668A1
公开(公告)日：2010-04-29
申请号：US12624637
申请日：2009-11-24
申请人： Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts , Peter ten Holte , Frederik Jan Rita Rombouts , Carsten Schultz-Fademrecht
发明人： Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts , Peter ten Holte , Frederik Jan Rita Rombouts , Carsten Schultz-Fademrecht
IPC分类号： A61K31/541 , C07D239/70 , A61K31/517 , C07D413/02 , A61K31/5377 , C07D417/02 , C07C211/00 , C07D239/72
CPC分类号： C07D498/06 , C07C229/16 , C07C229/40 , C07D239/88 , C07D239/93 , C07D239/94
摘要： The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N═CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 are hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 are a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.
摘要翻译：本发明涉及下式的化合物其中Z代表NH; Y代表任选被氨基，一或二（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - ， - C 3-7烯基-CO-的氨基取代的-C 3-9烷基 - ， - C 2-9烯基 - ， - 氨基，一或二（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基-NR 13 -C 1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - C 1-6烷基-CO-NH - ， - C 1-5烷基-CO NR 15 -C 1-5烷基 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het 21 -CO-， - C 1-2烷基 -NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-或-NR22-CO-C1-3烷基 - NH-; X1表示直接键，O或-O-C 1-2烷基 - ; -X 2表示直接键，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基 - ， - O-N = CH-或-C 1-2烷基 - ; R1和R2是氢或卤素; R3是氢; R4代表氢或C1-4烷氧基; R 12和R 13是氢或C 1-4烷基; R14和R15是氢; R 16和R 17各自独立地表示氢或C 1-4烷基; R 18和R 19是氢或任选被苯基或羟基取代的C 1-4烷基; R 20和R 21是氢或任选被C 1-4烷氧基取代的C 1-4烷基; Het20，Het21和Het22是选自吡咯烷基，2-吡咯烷基或任选被羟基取代的哌啶基的杂环。

29. 发明授权

US5886024A Thiophene-containing butonic acid derivatives as matrix metalloprotease inhibitors 失效
标题翻译：含噻吩的丁酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5886024A
公开(公告)日：1999-03-23
申请号：US865325
申请日：1997-05-28
申请人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , William Harrison Bullock
发明人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , William Harrison Bullock
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , A61K31/38 , A61K31/40 , C07D409/00
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
摘要翻译：基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。本发明的化合物具有通用化合物“IMAGE”，其中每个T是取代基; x为0,1或2; 基团D表示基团R6表示D和G之间的碳链上的各种可能的取代基，基团G表示M，其中M表示-CO 2 H，-CON（R 11）2，或-CO 2 R 12; R13表示19个非环状天然氨基酸的任一侧链。

30. 发明授权

US5789434A Derivatives of substituted 4-biarylbutyric acid as matrix metalloprotease inhibitors 失效
标题翻译：取代的4-联芳基丁酸的衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5789434A
公开(公告)日：1998-08-04
申请号：US539409
申请日：1995-11-06
申请人： Harold Clinton Eugene Kluender , Guenter Hans Heinz Herbert Benz , David Ross Brittelli , William Harrison Bullock , Kerry Jeanne Combs , Brian Richard Dixon , Stephan Schneider , Jill Elizabeth Wood , Michael Christopher VanZandt , Donald John Wolanin , Scott M. Wilhelm
发明人： Harold Clinton Eugene Kluender , Guenter Hans Heinz Herbert Benz , David Ross Brittelli , William Harrison Bullock , Kerry Jeanne Combs , Brian Richard Dixon , Stephan Schneider , Jill Elizabeth Wood , Michael Christopher VanZandt , Donald John Wolanin , Scott M. Wilhelm
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , A61K31/405 , A61K31/40
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The presently claimed compounds have the generalized formula ##STR1## in which each T represents a substituent group; x is 0, 1, or 2; D represents ##STR2## .delta. is 0 or 1; U' represents O, S, or N, with the proviso that when U' is N, then .delta.=0, and when U' is O or S, then .delta.=1; R.sup.14 is any of a variety of substituent groups; and G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, R.sup.11 represents H or an alkyl group, R.sup.12 represents an alkyl group, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids; and pharmaceutically acceptable salts thereof.
摘要翻译：基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。目前要求保护的化合物具有其中每个T表示取代基的广义化学式“IMAGE”; x为0,1或2; D表示 delta为0或1; U'表示O，S或N，条件是当U'为N时，则δ= 0，当U'为O或S时，则δ= 1; R14是各种取代基中的任意一种; 和G表示M，其中M表示-CO 2 H，-CON（R 11）2或-CO 2 R 12，R 11表示H或烷基，R 12表示烷基，R 13表示任何侧链的M， 19个非环状天然存在的氨基酸; 及其药学上可接受的盐。

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