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    Peroxisome proliferator activated receptor alpha agonists
    1.
    发明申请
    Peroxisome proliferator activated receptor alpha agonists 失效
    过氧化物酶体增殖物激活受体α激动剂

    公开(公告)号：US20040102500A1

    公开(公告)日：2004-05-27

    申请号：US10415673

    申请日：2003-09-11

    发明人： Ivan Collado Cano ,  Samuel James Dominianni ,  Garret Jay Etgen ,  Cristina Garcia-Paredes ,  Richard Duane Johnston ,  Michael Edward Letourneau ,  Nathan Bryan Mantlo ,  Michael John Martinelli ,  Daniel Ray Mayhugh ,  Ashraf Saeed ,  Richard Craig Thompson ,  Xiaodong Wang ,  David Scott Coffey ,  Christopher Randall Schmid ,  Jeffrey Thomas Vicenzi ,  Yanping Xu

    IPC分类号： A61K031/4196 ,  C07D249/12 ,  C07D43/02

    CPC分类号： C07C281/06 ,  C07C257/22 ,  C07C281/04 ,  C07D249/12 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12

    摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.

    摘要翻译： 本发明涉及由以下结构式表示的化合物及其药学上可接受的盐，溶剂合物和水合物，R 1是选自C 1 -C 8烷基，芳基-C 0-2 - 烷基，杂芳基-C 0 - C 3 -C 6环烷基芳基-C 0-2 - 烷基或苯基。 W是O或S.R 2是H或选自C 1 -C 6烷基，C 3 -C 6环烷基和杂芳基的取代或未取代的基团。 X是C2-C5亚烷基连接体，连接体的一个碳原子可被O，NH或S取代.Y是C，O，S，NH或单键。 此外，E是（CH 2）n COOH，其中n是0,1,2或3或C（R3）（R4）A，其中A是酸性官能团如羧基，甲酰胺取代或未取代的磺酰胺，或取代或未取代的 未取代的四唑。 R3是H，饱和或不饱和的C1-C5烷基，C1-C5烷氧基。 另外，R 4为H，卤素，取代或未取代的选自C 1 -C 5烷基，C 1 -C 5烷氧基，C 3 -C 6环烷基，芳基C 0 -C 4烷基和苯基，或R 3和R 4的基团，形成C 3 -C 4环烷基。

    Antivirally active heterocyclic azahexane derivatives
    3.
    发明授权
    Antivirally active heterocyclic azahexane derivatives 有权
    抗病毒活性杂环氮杂己烷衍生物

    公开(公告)号：US06300519B1

    公开(公告)日：2001-10-09

    申请号：US09448328

    申请日：1999-11-23

    申请人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    发明人： Alexander Fässler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    IPC分类号： C07C20904

    CPC分类号： C07D213/42 ,  C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20

    摘要： There are described compounds of formula I*, wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (—SO—) and sulfonyl (—SO2—) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

    摘要翻译： 描述式I *的化合物，其中R 1是低级烷氧基羰基，R 2是仲或叔低级烷基或低级烷硫基 - 低级烷基，R 3是未被取代或被一个或多个低级烷氧基取代的苯基或C 4 -C 8环烷基，R 4 是通过环碳原子键合的不饱和杂环基在4-位上被取代的苯基或环己基，具有5-8个环原子，含有1-4个选自氮，氧，硫，脯氨酰基的杂原子（ -SO-）和磺酰基（-SO 2 - ），并且是未取代的或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2中提及的含义之一，R 6独立地为R 1，为低级烷氧基羰基 或其盐，条件是存在至少一种成盐基团。化合物是天冬氨酸逆转录病毒蛋白酶的抑制剂，并且可以用于例如AIDS的治疗。 它们具有出色的药效学性质。

    Combinations of HIV protease inhibitors with reverse transcriptase inhibitors
    5.
    发明授权
    Combinations of HIV protease inhibitors with reverse transcriptase inhibitors 有权
    HIV蛋白酶抑制剂与逆转录酶抑制剂的组合

    公开(公告)号：US6166004A

    公开(公告)日：2000-12-26

    申请号：US399627

    申请日：1999-09-20

    申请人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    发明人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Marc Lang ,  Satish Chandra Khanna

    IPC分类号： C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D213/42 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20 ,  A61K31/435 ,  A61K31/41 ,  A61K31/425 ,  C07D257/06 ,  C07D277/02

    CPC分类号： C07D213/42 ,  C07C271/22 ,  C07C281/02 ,  C07C281/04 ,  C07D241/12 ,  C07D257/04 ,  C07D277/28 ,  C07D333/20

    摘要： There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

    摘要翻译： 描述式I *的化合物，其中R 1是低级烷氧基羰基，R 2是仲或叔低级烷基或低级烷硫基 - 低级烷基，R 3是未被取代或被一个或多个低级烷氧基取代的苯基或C 4 -C 8环烷基， R4是通过环碳原子连接的不饱和杂环基在4-位上被取代的苯基或环己基，具有5-8个环原子，含有1-4个选自氮，氧，硫，亚硫酰基的杂原子 （-SO-）和磺酰基（-SO 2 - ），并且未被取代或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2中所提及的含义之一，R 6独立地为R 1， 低级烷氧基羰基或其盐，条件是存在至少一个成盐基团。 这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，可以用于例如艾滋病的治疗。 它们具有出色的药效学性质。

    Process for the preparation of alkoxytriazolinones
    6.
    发明授权
    Process for the preparation of alkoxytriazolinones 失效
    制备烷氧基三唑啉酮的方法

    公开(公告)号：US5892054A

    公开(公告)日：1999-04-06

    申请号：US934501

    申请日：1997-09-19

    申请人： Heinz-Jurgen Wroblowsky ,  Klaus Konig

    发明人： Heinz-Jurgen Wroblowsky ,  Klaus Konig

    IPC分类号： C07C281/04 ,  C07C281/16 ,  C07D249/12

    CPC分类号： C07D249/12 ,  C07C281/04

    摘要： Alkoxytriazolinones of the formula (I), ##STR1## in which R.sup.1 and R.sup.2 independently of one another represent in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl,(which can be used as intermediates for the preparation of herbicidal active compounds) are obtained in good yields and in high purity by reacting iminocarbonic diesters (II) with carbazinic esters (III) ##STR2## in which R.sup.2 and R.sup.3 in each case represent, for example, alkyl or aryl,at -20.degree. C. to +120.degree. C. (1st step) and subjecting the semicarbazide derivatives (IV) formed in this process with elimination of R.sup.2 -OH ##STR3## to a cyclizing condensation reaction in the presence of a base at 20.degree. C. to 150.degree. C. with elimination of R.sup.3 --OH, if appropriate (2nd step) and, finally, by reacting the resulting 5-alkoxytriazolinones of the formula (V) �=formula (I) where R.sup.1 =H! with an alkylating agent of the formula R.sup.1 --X (VI) �X, for example,=halogen or --OSO.sub.2 OR.sup.1 ! at 0.degree. C. to 150.degree. C., if appropriate in the presence of a base (3rd step: highly selective 4-alkylation).

    摘要翻译： 式（I）的烷氧基​​三唑啉酮，其中R 1和R 2彼此独立地表示，各自为任选取代的烷基，烯基，炔基，环烷基，环烷基烷基，芳基或芳基烷基（可用作中间体 用于制备除草活性化合物）以良好的产率和高纯度通过使亚氨基碳酸二酯（II）与咔嗪酸酯（III）反应获得，其中R2和R3各自表示例如 ，烷基或芳基，在-20℃至+ 120℃（第一步），并将在该过程中形成的氨基脲衍生物（Ⅳ）与R 2 -OH反应生成环状 在20℃至150℃存在下，在适当的情况下消除R3-OH（第二步），最后通过使得到的式（V）的5-烷氧基三唑啉酮[= 式（I）其中R1 = H]与式R1-X（VI）的烷基化剂[X，例如=卤素或 -OSO2OR1]在0℃至150℃，如果合适的话，在碱的存在下（第3步：高选择性4-烷基化）。

    PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID DERIVATIVES
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID DERIVATIVES 有权
    制备吡唑羧酸衍生物的方法

    公开(公告)号：US20150158818A1

    公开(公告)日：2015-06-11

    申请号：US14623372

    申请日：2015-02-16

    申请人： Hoffmann-La Roche Inc.

    发明人： Bjoern Bartels ,  Fritz Bliss ,  Katrin Groebke Zbinden ,  Matthias Koerner

    IPC分类号： C07D231/14 ,  C07C227/16 ,  C07C269/04 ,  C07C281/02

    CPC分类号： C07D231/14 ,  C07C227/16 ,  C07C269/04 ,  C07C281/02 ,  C07C281/04 ,  Y02P20/55

    摘要： The present invention relates to a novel process for the preparation of a pyrazole carboxylic acid derivative of the formula wherein R1 is C1-7-alkyl and R3 is C1-7-alkyl which is optionally substituted with halogen or C1-4-alkoxy.The pyrazole carboxylic acid derivative of the formula I can be used as building block in the preparation of pharmaceutically active principles e.g. for compounds acting as phosphodiesterase (PDE) inhibitors, particularly PDE10 inhibitors. PDE10 inhibitors have the potential to treat psychotic disorders like schizophrenia.

    摘要翻译： 本发明涉及制备下式的吡唑羧酸衍生物的新方法：其中R 1为C 1-7 - 烷基且R 3为任选被卤素或C 1-4 - 烷氧基取代的C 1-7 - 烷基。 式I的吡唑羧酸衍生物可用作制备药物活性成分的结构单元，例如， 用作磷酸二酯酶（PDE）抑制剂，特别是PDE10抑制剂的化合物。 PDE10抑制剂具有治疗精神病如精神分裂症的潜力。

    Artichoke hybrid named ‘PS-H2015’
    8.
    发明授权
    Artichoke hybrid named ‘PS-H2015’ 有权
    朝鲜蓟混合动物名叫“PS-H2015”

    公开(公告)号：US07868225B2

    公开(公告)日：2011-01-11

    申请号：US12215466

    申请日：2008-06-27

    申请人： William J. Colfer

    发明人： William J. Colfer

    IPC分类号： A01H5/00 ,  A01H5/10

    CPC分类号： C07C281/06 ,  C07C257/22 ,  C07C281/04 ,  C07D249/12 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12

    摘要： A new and distinct hybrid of artichoke named ‘PS-H2015’, characterized by its numerous bud numbers, fleshiness of bracts, fleshiness of hearts, uniformity of head shapes; strong violet blush coloration; and ability to bolt in warm summer conditions (reduced vernalization requirements) allowing spring/summer planting and fall production.

    摘要翻译： 一种名为“PS-H2015”的朝鲜蓟的新鲜而独特的混合物，其特征在于其众多的芽数，苞片的肉质，心脏的肉体，头部形状的均匀性; 强紫色腮红着色; 以及能够在温暖的夏季条件下（春化要求降低），允许春季/夏季播种和秋季生产。