公开(公告)号：US08883837B2

公开(公告)日：2014-11-11

申请号：US12140686

申请日：2008-06-17

申请人： Jean-Francois Bonfanti ,  Koenraad Jozef Lodewijk Andries ,  Jérôme Michel Claude Fortin ,  Philippe Muller ,  Frédéric Marc Maurice Doublet ,  Christophe Meyer ,  Rudy Edmond Willebrords ,  Tom Valerius Josepha Gevers ,  Philip Maria Martha Bern Timmerman

发明人： Jean-Francois Bonfanti ,  Koenraad Jozef Lodewijk Andries ,  Jérôme Michel Claude Fortin ,  Philippe Muller ,  Frédéric Marc Maurice Doublet ,  Christophe Meyer ,  Rudy Edmond Willebrords ,  Tom Valerius Josepha Gevers ,  Philip Maria Martha Bern Timmerman

IPC分类号： A01N43/52 ,  A61K31/415 ,  C07D233/00 ,  C07D235/02 ,  C07D487/04 ,  C07D487/06 ,  C07D413/12

CPC分类号： C07D413/12 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14

摘要： The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.

摘要翻译： 本发明涉及对具有对呼吸道合胞病毒复制具有抑制活性的含有吗啉基的苯并咪唑，其具有前药，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构形式。 还涉及其制备方法和包含这些化合物的组合物，以及作为药物的用途。

公开(公告)号：US08673281B2

公开(公告)日：2014-03-18

申请号：US13584999

申请日：2012-08-14

申请人： Lasse Leino ,  Jarmo Laihia

发明人： Lasse Leino ,  Jarmo Laihia

IPC分类号： C07D233/00 ,  A61K31/417

CPC分类号： A61K31/4172 ,  A61K9/0014 ,  A61K31/00 ,  A61K47/10 ,  A61K47/32 ,  A61K47/44

摘要： A pharmaceutically acceptable agent able to acidify the cell cytoplasm, for the manufacture of a pharmaceutical composition useful for causing immunosuppression in a person or animal, where an effective amount of the agent is administered in an essentially non-dissociated form to the person or animal, and where the agent is admixed with a carrier to adjust the pH of the composition to the pH range 6.1 to 7.0. A pharmaceutical composition is also disclosed.

摘要翻译： 能够使细胞质酸化的药学上可接受的试剂，用于制造用于在人或动物中引起免疫抑制的药物组合物，其中有效量的药剂以基本上非离解形式施用于人或动物， 并且其中将试剂与载体混合以将组合物的pH调节至pH6.0至7.0的pH范围。 还公开了药物组合物。

公开(公告)号：US08410141B2

公开(公告)日：2013-04-02

申请号：US13319287

申请日：2010-05-18

申请人： Tetsuya Murata ,  Yasushi Yoneta ,  Hidetoshi Kishikawa ,  Jun Mihara ,  Daiei Yamazaki ,  Mamoru Hatazawa ,  Norio Sasaki ,  Kei Domon ,  Eiichi Shimojo ,  Teruyuki Ichihara ,  Katsuhiko Shibuya ,  Masashi Ataka ,  Ulrich Görgens

发明人： Tetsuya Murata ,  Yasushi Yoneta ,  Hidetoshi Kishikawa ,  Jun Mihara ,  Daiei Yamazaki ,  Mamoru Hatazawa ,  Norio Sasaki ,  Kei Domon ,  Eiichi Shimojo ,  Teruyuki Ichihara ,  Katsuhiko Shibuya ,  Masashi Ataka ,  Ulrich Görgens

IPC分类号： A61K31/4427 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4192 ,  A61K31/4196 ,  C07D401/14 ,  C07D257/02 ,  C07D249/04 ,  C07D249/08 ,  C07D233/00 ,  C07D231/00 ,  C07D207/00

CPC分类号： A01N43/40 ,  A01N43/36 ,  A01N43/50 ,  A01N43/56 ,  A01N43/647 ,  A01N43/653 ,  A01N43/713 ,  C07D207/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14

摘要： The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.

公开(公告)号：US08318676B2

公开(公告)日：2012-11-27

申请号：US11839633

申请日：2007-08-16

申请人： Rudolf Bimczok ,  Thomas Kripp ,  Beate Grasser ,  Christian Springob

发明人： Rudolf Bimczok ,  Thomas Kripp ,  Beate Grasser ,  Christian Springob

IPC分类号： A61K38/00 ,  A61K31/415 ,  A61K31/155 ,  A61K8/00 ,  A61K8/18 ,  A01N43/50 ,  A01N37/52 ,  A61Q5/00 ,  A61Q9/00 ,  A61Q1/00 ,  C07D233/00 ,  C07C277/00 ,  C07C279/00

CPC分类号： A61Q5/02 ,  A61K8/44 ,  A61K8/4946 ,  A61Q5/04 ,  A61Q5/06 ,  A61Q5/10 ,  A61Q5/12 ,  Y10S514/88

摘要： The invention relates to the use of creatine, creatinine and/or derivatives thereof and/or their salts in an agent for hardening, strengthening, restructuring or increasing the shine, volume or combability of keratin fibers, particularly of human hair.

摘要翻译： 本发明涉及肌酸，肌酸酐和/或其衍生物和/或其盐在药剂中用于硬化，强化，重组或增加角蛋白纤维，特别是人类头发的光泽，体积或梳理性的用途。

公开(公告)号：US08278357B2

公开(公告)日：2012-10-02

申请号：US12591090

申请日：2009-11-06

申请人： Bernard Attali ,  Asher Peretz

发明人： Bernard Attali ,  Asher Peretz

IPC分类号： A61K31/16 ,  C07D233/00 ,  C07D239/00

CPC分类号： A61K31/165 ,  A61K31/195 ,  A61K31/4184

摘要： Compounds, compositions and methods are provided which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing cortical and/or peripheral neuron activity are disclosed. Novel derivatives of N-phenylanthranilic acid are also disclosed.

摘要翻译： 提供了通过通过电压依赖性钾通道调节钾离子通量和/或抑制皮质和/或周围神经元活性而可用于治疗诸如中枢或周围神经系统疾病的病症的化合物，组合物和方法。 还公开了N-苯基邻氨基苯甲酸的新型衍生物。

公开(公告)号：US08242260B2

公开(公告)日：2012-08-14

申请号：US12862418

申请日：2010-08-24

申请人： Abran Q. Costales ,  Shenlin Huang ,  Jeff Xianming Jin ,  Zuosheng Liu ,  Sabina Pecchi ,  Daniel Poon ,  John Tellew ,  Qiong Zhang

发明人： Abran Q. Costales ,  Shenlin Huang ,  Jeff Xianming Jin ,  Zuosheng Liu ,  Sabina Pecchi ,  Daniel Poon ,  John Tellew ,  Qiong Zhang

IPC分类号： C07D345/00 ,  C07D239/00 ,  C07D233/00

CPC分类号： C07D403/04 ,  A61K31/506 ,  A61K45/06

摘要： The present invention provides compounds of Formula I or II: wherein R1, R1b, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds of Formula (I) or (II) and pharmaceutical compositions thereof are useful for the treatment of B-Raf-associated diseases.

摘要翻译： 本发明提供式I或II的化合物：其中R1，R1b，R2，R3，R4，R5，R6和R7如本文所定义。 式（I）或（II）的化合物及其药物组合物可用于治疗B-Raf相关疾病。

公开(公告)号：US08148533B2

公开(公告)日：2012-04-03

申请号：US11072964

申请日：2005-03-04

申请人： Martin A. Paonessa ,  Rajiv R Singh ,  Valentine T Zuba ,  George A Shia ,  John A McFarland

发明人： Martin A. Paonessa ,  Rajiv R Singh ,  Valentine T Zuba ,  George A Shia ,  John A McFarland

IPC分类号： C07D211/00 ,  C07D211/70 ,  C07D277/08 ,  C07D263/02 ,  C07D263/30 ,  C07D233/00 ,  C07D207/00

CPC分类号： C07D213/18 ,  C09K13/08 ,  H01M10/0568 ,  H01M2300/002

摘要： Ionic liquids having melting points below about 100 C formed by reaction of a heterocyclic amine with about 2.8 and about 3.2 moles of anhydrous hydrogen fluoride per mole of amine nitrogen. Electrochemical devices having non-aqueous electrolytes containing the ionic liquids are also disclosed, as well as silicon oxide etching compositions containing the ionic liquids and etching methods in which silicon oxides are selectively removed by the etching compositions in the presence of aluminum.

摘要翻译： 通过杂环胺与每摩尔胺氮约2.8和约3.2摩尔无水氟化氢的反应形成熔点低于约100℃的离子液体。 还公开了具有含有离子液体的非水电解质的电化学装置，以及含有离子液体的氧化硅蚀刻组合物和在铝存在下通过蚀刻组合物选择性除去氧化硅的蚀刻方法。

公开(公告)号：US07973067B2

公开(公告)日：2011-07-05

申请号：US12331787

申请日：2008-12-10

申请人： Zhaoning Zhu ,  Brian McKittrick ,  Zhong-Yue Sun ,  Yuanzan C. Ye ,  Johannes H. Voigt ,  Corey Strickland ,  Elizabeth M. Smith ,  Andrew Stamford ,  William J. Greenlee ,  Robert D. Mazzola, Jr. ,  John P. Caldwell ,  Jared N. Cumming ,  Lingyan Wang ,  Yusheng Wu ,  Ulrich Iserloh ,  Tao Guo ,  Thuy X. H. Le ,  Kurt W. Saionz ,  Suresh D. Babu ,  Rachel C. Hunter ,  Michelle L. Morris ,  Huizhong Gu ,  Gang Qian ,  Dawit Tadesse

发明人： Zhaoning Zhu ,  Brian McKittrick ,  Zhong-Yue Sun ,  Yuanzan C. Ye ,  Johannes H. Voigt ,  Corey Strickland ,  Elizabeth M. Smith ,  Andrew Stamford ,  William J. Greenlee ,  Robert D. Mazzola, Jr. ,  John P. Caldwell ,  Jared N. Cumming ,  Lingyan Wang ,  Yusheng Wu ,  Ulrich Iserloh ,  Tao Guo ,  Thuy X. H. Le ,  Kurt W. Saionz ,  Suresh D. Babu ,  Rachel C. Hunter ,  Michelle L. Morris ,  Huizhong Gu ,  Gang Qian ,  Dawit Tadesse

IPC分类号： A01N43/50 ,  A61K31/415 ,  C07D233/00

CPC分类号： C07D233/46 ,  C07D233/70 ,  C07D233/88 ,  C07D239/22 ,  C07D239/70 ,  C07D271/07 ,  C07D273/00 ,  C07D401/04 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06

摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

公开(公告)号：US07906539B2

公开(公告)日：2011-03-15

申请号：US12192589

申请日：2008-08-15

申请人： Matthias Eckhardt ,  Frank Himmelsbach ,  Elke Langkopf ,  Leo Thomas ,  Mohammad Tadayyon

发明人： Matthias Eckhardt ,  Frank Himmelsbach ,  Elke Langkopf ,  Leo Thomas ,  Mohammad Tadayyon

IPC分类号： A61K31/41 ,  A61K31/426 ,  A61K31/4192 ,  C07D249/08 ,  C07D233/00

CPC分类号： C07D471/04 ,  C07D249/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14

摘要： The present invention relates to imidazoles and triazoles of general formula wherein R1 to R4 and X are defined as in claims 1 to 8, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

摘要翻译： 本发明涉及通式的咪唑和三唑，其中R 1至R 4和X如权利要求1至8中所定义，互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质，特别是 对二肽基肽酶-IV（DPP-IV）的活性具有抑制作用。

公开(公告)号：US07863459B2

公开(公告)日：2011-01-04

申请号：US12094563

申请日：2006-12-18

申请人： Robert Lines

发明人： Robert Lines

IPC分类号： C07D233/00

CPC分类号： C09B69/04

摘要： An 'onium salt, e.g. a quaternary ammonium salt, of an anionic dye may be prepared by mixing an aqueous solution of a salt of the dye with a solution of a water-insoluble 'onium salt in an organic solvent, and separating a solution of the 'onium salt of the anionic dye in the organic solvent from the residual aqueous solution.

摘要翻译： “盐”，例如 阴离子染料的季铵盐可以通过将染料盐的水溶液与水不溶性“鎓盐”在有机溶剂中的溶液混合，并将 阴离子染料在有机溶剂中残留水溶液。