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41. 发明申请

WO2003016292A1 ULTRAVIOLET LIGHT ABSORBERS 审中-公开
标题翻译： ULTRAVIOLET光吸收器
公开(公告)号：WO2003016292A1
公开(公告)日：2003-02-27
申请号：PCT/EP2002/008709
申请日：2002-08-05
申请人： CIBA SPECIALTY CHEMICALS HOLDING INC. , RAVICHANDRAN, Ramanathan , PASTOR, Stephen, Daniel , JUDD, Deborah , BABIARZ, Joseph, Edmund , NAUGHTON, Andrew, Brian , WOOD, Mervin, Gale , DEBELLIS, Anthony, David , XIONG, Rong , DETLEFSEN, Robert, Edward , SUHADOLNIK, Joseph
发明人： RAVICHANDRAN, Ramanathan , PASTOR, Stephen, Daniel , JUDD, Deborah , BABIARZ, Joseph, Edmund , NAUGHTON, Andrew, Brian , WOOD, Mervin, Gale , DEBELLIS, Anthony, David , XIONG, Rong , DETLEFSEN, Robert, Edward , SUHADOLNIK, Joseph
IPC分类号： C07D265/22
CPC分类号： C07D239/91 , C07D239/74 , C07D239/86 , C07D249/20 , C07D265/22 , C07D405/04
摘要： The present invention relates to novel ultraviolet light absorbers of the benzoxazinone, oxanilide, benzylidene malonate, quinazoline and benzotriazole classes. The invention also relates to polymer and photographic compositions stabilized against the deleterious effects of light induced degradation which comprise the novel ultraviolet light absorbers.
摘要翻译：本发明涉及苯并恶嗪酮，草酰苯胺，丙二酸亚苄酯，喹唑啉和苯并三唑类的新型紫外光吸收剂。本发明还涉及针对包含新型紫外光吸收剂的光诱导降解的有害影响而稳定的聚合物和照相组合物。

42. 发明申请

WO0228841A3 REAGENTS FOR LABELING BIOMOLECULES HAVING ALDEHYDE OR KETONE MOIETIES 审中-公开
标题翻译：用于标记具有醛或酮的生物分子的试剂
公开(公告)号：WO0228841A3
公开(公告)日：2002-08-01
申请号：PCT/US0130851
申请日：2001-10-02
申请人： MOLECULAR PROBES INC
发明人： HAUGLAND RICHARD P , STEINBERG THOMAS H , PATTON WAYNE P , ZHENJUN DIWU
IPC分类号： G01N33/532 , C07D239/91 , C07D239/94 , C07D249/08 , C07D263/60 , C07D265/22 , C07D277/66 , C07D401/04 , G01N33/58
CPC分类号： C07D265/22 , C07D239/91 , Y10T436/143333 , Y10T436/200833
摘要： Novel fluorescent derivitization reagents are described that are suitable for coupling to biomolecules that contain aldehyde or ketone functional groups. The method of treating a sample with the derivativization reagents is described. The reagents are particularly useful for labeling glycoproteins or glycopeptides, nucleic acids, and lipopolysaccharides in electrophoresis gels.
摘要翻译：描述了适用于与含有醛或酮官能团的生物分子偶联的新的荧光衍生试剂。描述了用衍生化试剂处理样品的方法。这些试剂特别适用于标记电泳凝胶中的糖蛋白或糖肽，核酸和脂多糖。

43. 发明申请

WO99048878A1 HETEROCYCLIC COMPOUNDS REGULATING CLOTTING 审中-公开
标题翻译：杂环化合物调节包装
公开(公告)号：WO99048878A1
公开(公告)日：1999-09-30
申请号：PCT/DK1999/000138
申请日：1999-03-17
IPC分类号： A61K31/536 , A61K31/5415 , C07D265/22 , C07D413/04 , C07D265/20 , A61K31/535 , A61K31/54 , C07D279/08
CPC分类号： C07D265/22 , A61K31/536 , A61K31/5415 , C07D413/04
摘要： The use of compounds of general formula (I) as factor VII-tissue factor inhibitors as well as novel benzoaxin derivatives are disclosed. The compounds of general formula (I) and pharmaceutical acceptable salts thereof have been shown to be inhibitors of factor VIIa-tissue factor activity. The compounds show anticoagulant properties. The compounds are useful for the treatment of deficiencies of blood clotting factors or the effects of inhibitors to blood clotting factors. Methods for inhibiting clotting activity are disclosed.
摘要翻译：公开了使用通式（I）的化合物作为因子VII-组织因子抑制剂以及新的苯并三嗪衍生物。通式（I）的化合物及其药学上可接受的盐已被证明是因子VIIa组织因子活性的抑制剂。化合物显示抗凝血性。该化合物可用于治疗凝血因子的缺陷或抑制剂对凝血因子的作用。公开了抑制凝血活性的方法。

44. 发明申请

WO98054135A1 NITROGENOUS HETEROCYCLIC COMPOUNDS AND HYPERLIPEMIA REMEDY CONTAINING THE SAME 审中-公开
标题翻译：含氮杂环化合物和含有它们的高效液
公开(公告)号：WO98054135A1
公开(公告)日：1998-12-03
申请号：PCT/JP1998/002411
申请日：1998-06-01
IPC分类号： C07D209/46 , C07D217/24 , C07D265/22 , C07D279/08 , C07D409/12 , G03F7/20 , A61K31/495 , A61K31/535 , A61K31/54 , C07D401/06 , C07D401/12 , C07D405/06 , C07D417/06
CPC分类号： C07D409/12 , C07D209/46 , C07D217/24 , C07D265/22 , C07D279/08 , G03F7/2049 , Y10S977/915
摘要： Compounds represented by general formula (I) and pharmacologically acceptable salts and solvates thereof. The compounds inhibit the biosynthesis of triglycerides in the liver and also inhibit the secretion of lipoproteins containing apolipoprotein B from the liver. They are hence useful for the prevention/treatment of hyperlipemia (especially hyper-VLDL-emia) and diseases caused thereby, such as arteriosclerotic diseases, e.g., myocardial infarct, and pancreatitis. Wherein A represents -CR R -(CH2)i- (wherein R and R each represents hydrogen or alkyl), -CH=CH-, -O-CH2-, or -S(O)j-CH2-; B represents hydrogen or halogen; X represents -CR R R , -NR R , -(CH2-CH=C(CH3)-CH2)p-CH2CH=C(CH3)2, alkyl, cycloalkyl, phenyl, cinnamyl, or heteroaryl; Y represents -(CH2)q-, -CH=CH-, -NR -, oxygen, or a bond; Z represents carbonyl or a bond; K represents alkylene or a bond; L represents -CH=CH- or a bond; and M represents hydrogen, alkyl, cycloalkyl, phenyl, heterocycle, biphenyl, or diphenymethyl.
摘要翻译：由通式（I）表示的化合物及其药理学上可接受的盐和溶剂化物。该化合物抑制肝脏中甘油三酯的生物合成，并且还抑制从肝脏分泌含有载脂蛋白B的脂蛋白。因此，它们可用于预防/治疗高脂血症（特别是超VLDL-emia）和由此引起的疾病，例如动脉硬化疾病，例如心肌梗死和胰腺炎。其中A表示-CR 1 R 2 - （CH 2）i - （其中R 1和R 2各自表示氢或烷基）， - CH = CH-， - O-CH 2 - 或 - S（O）J-CH2-; B表示氢或卤素; X表示-CR 3 R 4 R 5，-NR 6 R 7， - （CH 2 -CH = C（CH 3）-CH 2）p-CH 2 CH = C（CH 3）2，烷基，环烷基，苯基，肉桂基或杂芳基; Y表示 - （CH 2）q - ， - CH = CH - ， - NR 8 - ，氧或键; Z表示羰基或键; K表示亚烷基或键; L表示-CH = CH-或键; M代表氢，烷基，环烷基，苯基，杂环，联苯或二苯甲基。

45. 发明申请

WO98045291A1 SUBSTITUTED THIAZOLIDINEDIONE AND OXAZOLIDINEDIONE HAVING ANTIDIABETIC, HYPOLIPIDEMIA AND ANTIHYPERTENSIVE PROPERTIES 审中-公开
标题翻译：具有抗高血压，抗高血压药物和抗高血压药物的替代噻唑烷二酮和氧杂环丁二烯
公开(公告)号：WO98045291A1
公开(公告)日：1998-10-15
申请号：PCT/US1998/007284
申请日：1998-04-10
IPC分类号： C07D239/88 , A61K31/517 , A61K31/536 , A61K31/5415 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/10 , C07D263/44 , C07D265/22 , C07D277/20 , C07D277/34 , C07D413/12 , C07D417/12 , A61K31/425 , C07D239/90
CPC分类号： C07D277/20 , C07D265/22 , C07D277/34 , C07D413/12 , C07D417/12
摘要： The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinediones of general formula (I), their analogues, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
摘要翻译：本发明涉及新的抗糖尿病化合物，其互变异构形式，其衍生物，其类似物，其立体异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂合物和含有它们的药学上可接受的组合物。本发明特别涉及通式（I）的新型唑烷二酮类，其类似物，其衍生物，其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐，药学上可接受的溶剂合物和含有它们的药物组合物。

46. 发明申请

WO1995020581A1 NOVEL HUMAN LEUKOCYTE ELASTASE (HLE) INHIBITORS, AND RELATED PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：新型人类LEUKOCYTE ELASTASE（HLE）抑制剂及相关药物组合物及其使用方法
公开(公告)号：WO1995020581A1
公开(公告)日：1995-08-03
申请号：PCT/US1995000885
申请日：1995-01-20
申请人： SRI INTERNATIONAL
发明人： SRI INTERNATIONAL , HIEBERT, Charles, K. , LAIBELMAN, Alan , RYAN, Kenneth, J.
IPC分类号： C07D265/22
CPC分类号： C07D265/22 , C07D265/24 , C07D265/26 , C07D413/04
摘要： Novel therapeutic agents useful as inhibitors of HLE are provided. The compounds have structural formula (I) wherein R through R , m, n and p are as defined herein. Methods of using the compounds of formula (I) to inhibit serine proteases and to treat physiological conditions and disease states associated with elevated HLE levels are also provided, as are pharmaceutical compositions containing the compounds.
摘要翻译：提供了可用作HLE抑制剂的新型治疗剂。化合物具有其中R 1至R 9，m，n和p如本文所定义的结构式（I）。还提供了使用式（I）化合物抑制丝氨酸蛋白酶和治疗与升高的HLE水平相关的生理状态和疾病状态的方法，以及含有这些化合物的药物组合物。

47. 发明申请

WO9119707A3 ANTIATHEROSCLEROTIC AND ANTITHROMBOTIC 1-BENZOPYRAN-4-ONES AND 2-AMINO-1,3-BENZOXAZINE-4-ONES 审中-公开
标题翻译：抗真菌剂和抗坏血酸的1-苯并噻吩-4-酮和2-氨基-1,3-苯并恶唑-4-酮
公开(公告)号：WO9119707A3
公开(公告)日：1992-03-05
申请号：PCT/US9104140
申请日：1991-06-18
申请人： UPJOHN CO
发明人： GAMMILL RONALD B , JUDGE THOMAS M , MORRIS JOEL
IPC分类号： A61K31/35 , A61K31/352 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/443 , A61K31/535 , A61K31/536 , A61K31/54 , A61P1/16 , A61P3/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P17/00 , A61P29/00 , A61P35/00 , C07D265/22 , C07D265/24 , C07D311/22 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D265/22 , C07D311/22 , C07D405/12 , C07D405/14 , C07D413/10 , C07D417/12
摘要： This invention relates to compounds of formula (I) which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of formula (I) are useful inhibitors of cell proliferation.

48. 发明申请

WO2021067335A1 BENZOXAZINONE COMPOUNDS AS KLK5/7 DUAL INHIBITORS 审中-公开
公开(公告)号：WO2021067335A1
公开(公告)日：2021-04-08
申请号：PCT/US2020/053369
申请日：2020-09-30
申请人： MOLECULAR SKIN THERAPEUTICS, INC.
发明人： BETZ, Andreas , ZAMBONI, Robert
IPC分类号： A61K31/536 , C07D265/22 , C07D498/04 , A61P17/00
摘要： The present invention provides compounds and pharmaceutical compositions including the compounds for the treatment of a skin disease associated with proteolytic activity of one or more KLK proteases, wherein the compounds are according to formula (I): wherein R is as described herein.

49. 发明申请

WO2014097188A1 COMPOUNDS OF 2,3-DIHYDRO-4H-1,3-BENZOXAZINE-4-ONE, METHOD FOR PREPARING THEM AND PHARMACEUTICAL FORM COMPRISING THEM 审中-公开
标题翻译： 2,3-二氢-4H-1,3-苯并噻嗪-4-酮的化合物，其制备方法和包含它们的药物形式
公开(公告)号：WO2014097188A1
公开(公告)日：2014-06-26
申请号：PCT/IB2013/061106
申请日：2013-12-18
申请人： C4T S.C. A.R.L.
发明人： TOPAI, Alessandra , MISCIOSCIA, Teresa Fabiola , BARILE, Fabio , GUZZO, Tatiana , MINISSI, Franco , SABLONE, Manolo , MACCARRONE, Mauro
IPC分类号： C07D413/12 , A61K31/535 , A61K31/537 , C07D265/22 , C07D498/10
CPC分类号： C07D265/22 , C07D413/12 , C07D498/10
摘要： The present invention concerns new compounds of 2,3-dihydro-4H-1,3- benzoxazine-4-one, a method for preparing the said compounds, a pharmaceutical form that contains the said compounds, and their use. In particular, the present invention concerns new compounds of 2,3-dihydro-4H-1,3-benzoxazine-4-one having a selective agonist action for the type 2 cannabinoid receptor (CB2), and their use in the treatment of pathologies associated with non-activation of this receptor, particularly chronic pain.
摘要翻译：本发明涉及2,3-二氢-4H-1,3-苯并恶嗪-4-酮的新化合物，制备所述化合物的方法，含有所述化合物的药物形式及其用途。特别地，本发明涉及对2型大麻素受体（CB2）具有选择性激动作用的2,3-二氢-4H-1,3-苯并恶嗪-4-酮的新化合物及其在治疗病理学中的用途与该受体的非活化相关，特别是慢性疼痛。

50. 发明申请

WO2012154760A1 FUSED HETEROCYCLIC COMPOUNDS AS SODIUM CHANNEL MODULATORS 审中-公开
标题翻译：熔融杂环化合物作为钠通道调节剂
公开(公告)号：WO2012154760A1
公开(公告)日：2012-11-15
申请号：PCT/US2012/036976
申请日：2012-05-08
申请人： GILEAD SCIENCES, INC. , CORKEY, Britton Kenneth , ELZEIN, Elfatih , JIANG, Robert H. , KALLA, Rao V. , KOBAYASHI, Tetsuya , KOLTUN, Dmitry , LI, Xiaofen , MARTINEZ, Ruben , NOTTE, Gregory , PARKHILL, Eric Q. , PERRY, Thao , ZABLOCKI, Jeff , VENKATARAMANI, Chandrasekar , GRAUPE, Michael , GUERRERO, Juan
发明人： CORKEY, Britton Kenneth , ELZEIN, Elfatih , JIANG, Robert H. , KALLA, Rao V. , KOBAYASHI, Tetsuya , KOLTUN, Dmitry , LI, Xiaofen , MARTINEZ, Ruben , NOTTE, Gregory , PARKHILL, Eric Q. , PERRY, Thao , ZABLOCKI, Jeff , VENKATARAMANI, Chandrasekar , GRAUPE, Michael , GUERRERO, Juan
IPC分类号： C07D237/32 , C07D253/08 , C07D265/22 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06
CPC分类号： C07D498/10 , C07D217/26 , C07D237/32 , C07D239/88 , C07D239/90 , C07D253/08 , C07D263/58 , C07D265/22 , C07D279/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I), wherein Q, R 1 , X 1 , X 2 , Y and R 2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
摘要翻译：本公开涉及作为钠通道抑制剂的化合物及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的用途。在具体实施方案中，化合物的结构由式（I）给出，其中Q，R 1，X 1，X 2，Y和R 2如本文所述，用于制备和使用化合物的方法以及含有相同。

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