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91. 发明申请

US20070269368A1 HYDROPHILIC LIGHT ABSORBING COMPOSITIONS FOR DETERMINATION OF PHYSIOLOGICAL FUNCTION IN CRITICALLY ILL PATIENTS 失效
标题翻译：用于确定临床病人生理功能的亲水性吸收组合物
公开(公告)号：US20070269368A1
公开(公告)日：2007-11-22
申请号：US11778447
申请日：2007-07-16
申请人： Samuel Achilefu , Raghavan Rajagopalan , Richard Dorshow , Joseph Bugaj , Muthunadar Periasamy
发明人： Samuel Achilefu , Raghavan Rajagopalan , Richard Dorshow , Joseph Bugaj , Muthunadar Periasamy
IPC分类号： A61K49/20 , A61K31/19 , C07D235/04 , C07D277/84 , C07D293/10 , C07D263/60 , A61K31/4184
CPC分类号： C07D209/58 , A61K31/403 , A61K49/0021 , A61K49/0032 , C07D209/08 , C07D209/12 , C07D209/60
摘要： Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
摘要翻译：公开了在可见光区域吸收和发出荧光的高度亲水的吲哚和苯并吲哚衍生物。这些化合物可用于生理和器官功能监测。特别地，本发明的分子可用于肾脏和心脏疾病的光学诊断以及体内血液体积估计。

92. 发明申请

US20070208055A1 ALTERNATIVE SYNTHESIS OF RENIN INHIBITORS AND INTERMEDIATES THEREOF 失效
标题翻译：瑞宁抑制剂及其中间体的替代合成
公开(公告)号：US20070208055A1
公开(公告)日：2007-09-06
申请号：US11573790
申请日：2005-08-30
申请人： Gottfried Sedelmeier , Stuart Mickel , Heinrich Rueeger
发明人： Gottfried Sedelmeier , Stuart Mickel , Heinrich Rueeger
IPC分类号： A61K31/45 , A61K31/165 , C07D263/60 , C07D211/40
CPC分类号： C07D207/26 , C07C271/16 , C07C271/22 , C07D211/76 , C07D307/33
摘要： The present invention relates to synthetic routes to prepare a compound of the formula wherein R1 is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-4alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C—C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.
摘要翻译：本发明涉及制备下式化合物的合成路线：其中R 1是卤素，C 1-6卤代烷基，C 1-6 烷氧基-C 1-6烷氧基或C 1-6烷氧基-C 1-6烷基; R 2是卤素，C 1-4烷基或C 1-4烷氧基; R 3和R 4分别独立地为支链C 3-6烷基; 和R 5是环烷基，C 1-6烷基，C 1-6 1-6羟基烷基，C 1-6烷基，烷氧基-C 1-6烷基，C 1-4烷酰氧基-C 1-6烷基，C 1-6烷基，亚氨基烷基，C 1-6烷基氨基-C 1-6烷基，C 1-6二烷基氨基-C 1-6 C 1 -C 6烷基，C 1-6烷酰基氨基-C 1-6烷基，HO（O）C 1-6亚烷基，C C 1 -C 6烷基-O-（O）C 1-6烷基，H 2 NC（O）-C 1 - C 1 -C 6烷基，C 1-6烷基-NH-C（O）-C 1-6烷基或（C 1-6）烷基，（O）-C 1-6烷基;（C 1 -C 6）烷基; 或其药学上可接受的盐以及按照这些途径获得的关键中间体及其制备方法。

93. 发明申请

US20070135633A1 Process for producing N-(hetero)aryl-substituted nitrogen-containing heteroaryl compound 有权
标题翻译：制备N-（杂）芳基取代的含氮杂芳基化合物的方法
公开(公告)号：US20070135633A1
公开(公告)日：2007-06-14
申请号：US11635664
申请日：2006-12-08
申请人： Yuji Ishikawa , Susumu Harada , Ken Umihara
发明人： Yuji Ishikawa , Susumu Harada , Ken Umihara
IPC分类号： C07D215/38 , C07D263/60 , C07D263/52 , C07D241/02
CPC分类号： C07D207/325 , C07D233/54 , C07D401/04 , C07D403/04 , C07D405/04
摘要： A process for producing an N-(hetero)aryl-substituted nitrogen-containing heteroaryl compound, the process comprising: reacting a heteroaryl compound having an NH group as a ring-constituting component with a (hetero)aryl compound having a leaving group in the presence of a heterogeneous-system platinum group metal catalyst, a ligand and a base.
摘要翻译：一种制备N-（杂）芳基取代的含氮杂芳基化合物的方法，该方法包括：将具有作为构成环的组分的NH基的杂芳基化合物与具有离去基团的（杂）芳基化合物反应在存在异质系铂族金属催化剂，配体和碱。

94. 发明申请

US20060264483A1 Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors 审中-公开
公开(公告)号：US20060264483A1
公开(公告)日：2006-11-23
申请号：US11397055
申请日：2006-04-04
申请人： Daniel Getman , Gary DeCrescenzo , John Freskos , Michael Vazquez , James Sikorski , Balekudru Devadas , Srinivasan Nagarajan , Joseph McDonald
发明人： Daniel Getman , Gary DeCrescenzo , John Freskos , Michael Vazquez , James Sikorski , Balekudru Devadas , Srinivasan Nagarajan , Joseph McDonald
IPC分类号： A61K31/428 , A61K31/423 , A61K31/4184 , A61K31/343 , C07D417/02 , C07D277/62 , C07D263/60 , C07D235/04
CPC分类号： C07D263/56 , C07C317/44 , C07D215/36 , C07D217/02 , C07D217/04 , C07D235/30 , C07D235/32 , C07D249/20 , C07D277/62 , C07D277/82 , C07D307/79 , C07D307/82 , C07D311/58 , C07D317/62 , C07D319/18
摘要： Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

95. 发明申请

US20060199852A1 Process for the preparation of substituted benzoxazole compounds 审中-公开
标题翻译：取代苯并恶唑化合物的制备方法
公开(公告)号：US20060199852A1
公开(公告)日：2006-09-07
申请号：US11368719
申请日：2006-03-06
申请人： Silvio Iera
发明人： Silvio Iera
IPC分类号： C07D263/60 , A61K31/423
CPC分类号： C07D263/57 , C07D235/18 , C07D277/66
摘要： The present invention relates to processes for the preparation of substituted benzoxazole compounds, and in particular 2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl-benzoxazol-5-ol. The processes include the vinylation of a substituted benzoxazole compound having an appropriate substitutable moiety.
摘要翻译：本发明涉及制备取代的苯并恶唑化合物，特别是2-（3-氟-4-羟基 - 苯基）-7-乙烯基 - 苯并恶唑-5-醇的方法。所述方法包括具有适当的可取代部分的取代的苯并恶唑化合物的乙烯化。

96. 发明申请

US20060135782A1 Benzazole analogues and uses thereof 失效
标题翻译：苯并唑类似物及其用途
公开(公告)号：US20060135782A1
公开(公告)日：2006-06-22
申请号：US11303854
申请日：2005-12-15
申请人： Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
发明人： Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
IPC分类号： C07D277/62 , C07D263/60
CPC分类号： C07D417/12 , C07D473/34
摘要： The present invention relates to N2-heteroaryl-benzazole-2,(5 or 6)-diamine derivatives and compositions thereof as protein kinase inhibitors for the treatment of e.g. cancer.
摘要翻译：本发明涉及作为蛋白激酶抑制剂的N 2 - 杂芳基 - 苯并噻唑-2（5或6） - 二胺衍生物及其组合物。癌症。

97. 发明申请

US20050085503A1 Thiol-based NAALADase inhibitors 失效
标题翻译：基于硫醇的NAALADase抑制剂
公开(公告)号：US20050085503A1
公开(公告)日：2005-04-21
申请号：US10959199
申请日：2004-10-07
申请人： Takashi Tsukamoto , Pavel Majer , Doris Stoermer , Barbara Slusher
发明人： Takashi Tsukamoto , Pavel Majer , Doris Stoermer , Barbara Slusher
IPC分类号： A61P9/00 , A61K31/192 , A61K31/194 , A61K31/277 , A61P13/08 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/32 , A61P25/34 , A61P25/36 , A61P27/06 , A61P35/00 , A61P43/00 , C07C323/52 , C07C323/56 , C07C323/58 , C07C323/59 , C07C323/60 , C07C323/62 , C07C323/65 , C07D217/12 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/47 , C07D263/60 , C07D277/80
CPC分类号： C07C323/56 , C07C323/52 , C07C323/58 , C07C323/59 , C07C323/60 , C07C323/62 , C07C323/65
摘要： This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-β activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.
摘要翻译：本发明涉及包含这些化合物的新化合物，药物组合物和诊断试剂盒，以及使用这些化合物抑制NAALADase酶活性的方法，检测NAALADase水平改变，影响神经元活性，影响TGF-β活性，抑制血管生成的疾病，以及治疗谷氨酸异常，糖尿病性神经病，疼痛，强迫症，前列腺疾病，癌症和青光眼。

98. 发明申请

US20040087626A1 Substituted benz-azoles and methods of their use as inhibitors of Raf kinase 失效
标题翻译：取代的苯并唑及其用作Raf激酶抑制剂的方法
公开(公告)号：US20040087626A1
公开(公告)日：2004-05-06
申请号：US10405945
申请日：2003-03-31
发明人： Paul A. Renhowe , Savithri Ramurthy , Payman Amiri , Barry Haskell Levine , Daniel J. Poon , Skaradha Subramanian , Leonard Sung , Wendy Fantl
IPC分类号： A61K031/4439 , A61K031/428 , A61K031/423 , C07D277/82 , C07D263/60 , C07D417/02 , C07D413/02
CPC分类号： C07D401/14 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D453/02
摘要： New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译：提供了新的取代的苯并唑化合物，抑制人或动物受试者中Raf激酶活性的组合物和方法。新化合物组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。

99. 发明申请

US20020037910A1 Novel anilide compounds and pharmaceutical compositions comprising them 失效
标题翻译：新型酰苯胺化合物和包含它们的药物组合物
公开(公告)号：US20020037910A1
公开(公告)日：2002-03-28
申请号：US09789967
申请日：2001-02-21
发明人： Kimiyuki Shibuya , Katsumi Kawamine , Yukihiro Sato , Toshiyuki Edano , Souhei Tanabe , Masami Shiratsuchi
IPC分类号： A61K031/428 , A61K031/423 , A61K031/4184 , C07D277/68 , C07D263/60 , C07D235/24
CPC分类号： C07D263/58 , C07D235/28 , C07D277/70
摘要： The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: 1 wherein Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is nullNHnull, or an oxygen or sulfur atom; Y is nullNHnull, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or nullNR6null; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.
摘要翻译：本发明提供了新的酰苯胺化合物和包含它们的药物组合物。本发明涉及下式的化合物：其中Ar是任选取代的芳基; R4和R5相同或不同，各自为氢原子，低级烷基或低级烷氧基; 并且R 4和R 5可以一起形成其中一个或多个亚甲基部分可以任选被氧和/或硫原子取代的低级亚烷基; X是-NH-，或氧或硫原子; Y是-NH-，氧或硫原子，或亚砜或砜基; Z是单键，或-NR 6 - ; R6表示氢原子或低级亚烷基; n为0〜15的整数。及其盐和溶剂合物。本发明的化合物可用作药物组合物，特别是作为酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。

100. 发明授权

US5470858A Derivatives of (hetero)aromatic ethers and thioethers having antihyperlipidemic activity, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：具有抗高脂血症活性的（杂）芳香醚和硫醚的衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5470858A
公开(公告)日：1995-11-28
申请号：US901628
申请日：1992-06-19
申请人： Cristina Fraire , Massimo Bani , Ermes Vanotti , Vincenzo Olgiati
发明人： Cristina Fraire , Massimo Bani , Ermes Vanotti , Vincenzo Olgiati
IPC分类号： A61K31/19 , A61K31/235 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/496 , A61K31/52 , A61K31/522 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P3/06 , C07C69/24 , C07C323/19 , C07C323/20 , C07C323/22 , C07C323/62 , C07D207/36 , C07D213/70 , C07D233/84 , C07D235/24 , C07D235/26 , C07D235/28 , C07D239/38 , C07D249/12 , C07D263/38 , C07D263/46 , C07D263/58 , C07D263/60 , C07D277/62 , C07D277/74 , C07D413/12 , C07D473/00 , C07D473/08 , C07D473/12 , C07D473/34 , C07H19/16 , C07H19/167 , C07H19/20
CPC分类号： C07D213/70 , C07C323/20 , C07D233/84 , C07D235/26 , C07D235/28 , C07D239/38 , C07D249/12 , C07D263/46 , C07D263/58 , C07D263/60 , C07D277/74 , C07D413/10 , C07D473/08 , C07D473/12 , C07D473/34 , C07H19/16 , C07H19/20
摘要： A compound represented by the following formula I:(HET)Ar--X--CH.sub.2 --Y--CH.sub.2 --O--R (I)wherein:(HET)Ar represents a bicyclic hetero aryl nucleus which is unsubstituted or is substituted;X represents --S--;Y represents --CO--, --C.dbd.N--R.sub.2, in which R.sub.2 is hydrogen or a linear or branched alkyl having 1 to 10 carbon atoms, OH, an alkoxy having 1 to 10 carbon atoms, aryloxy, arylalkoxy, --NH.sub.2, --NHCONH.sub.2, --NHCSNH.sub.2 ; and R represents a phenyl substituted at para position with a carboxyl or a (C.sub.1 -C.sub.20) alkoxycarbonyl group in which the alkoxy group is linear or branched.
摘要翻译：由下式I表示的化合物：（HET）Ar-X-CH 2 -Y-CH 2 -O-R（I）其中：（HET）Ar表示未被取代或被取代的双环杂芳基核; X表示-S-; Y表示-CO-，-C = N-R2，其中R2是氢或具有1-10个碳原子的直链或支链烷基，OH，具有1-10个碳原子的烷氧基，芳氧基，芳基烷氧基，-NH2， NHCONH 2，-NHCSNH 2; 并且R表示在对位被羧基或（C1-C20）烷氧基羰基取代的苯基，其中烷氧基是直链或支链的。

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