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21. 发明申请

WO2007148774A1 環状アミン化合物审中-公开
标题翻译：循环胺化合物
公开(公告)号：WO2007148774A1
公开(公告)日：2007-12-27
申请号：PCT/JP2007/062562
申请日：2007-06-22
申请人：第一三共株式会社 , 宮崎正二郎 , 中村勇二 , 永山貴弘 , 徳井太郎 , 小川泰之
发明人：宮崎正二郎 , 中村勇二 , 永山貴弘 , 徳井太郎 , 小川泰之
IPC分类号： C07D241/06 , A61K31/495 , A61K31/496 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , C07D241/08 , C07D401/04 , C07D403/04 , C07D409/04
CPC分类号： C07D401/04 , C07D211/18 , C07D211/22 , C07D211/70 , C07D241/04 , C07D241/08
摘要： Disclosed is an excellent drug for treatment of hypertension. Specifically disclosed is a pharmaceutical agent containing a compound represented by the general formula (I) below or the like. [In the formula, R 1 represents H, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted cyclic hydrocarbon, an optionally substituted heterocyclyl or the like; R 2 represents H, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted cycloalkyl or the like; R 3 and R 4 independently represent H, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted cycloalkyl or the like; R 5 and R 6 independently represent H, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted alkoxy or the like; R 7 and R 8 independently represent H, an optionally substituted alkyl, an optionally substituted cycloalkyl or the like; X represents a group represented by the above formula (II) or the like; A represents an optionally substituted cyclic hydrocarbon, an optionally substituted heterocyclyl or the like; Y represents a single bond, an optionally substituted alkylene, an optionally substituted alkenylene, -(CH 2 ) a -X 1 -(CH 2 ) b - (wherein X 1 represents -NH-, -O- or the like, and a and b respectively represent a number of 0-5) or the like; and B represents an optionally substituted cyclic hydrocarbon, an optionally substituted heterocyclyl or the like.]
摘要翻译：公开了治疗高血压的优良药物。具体公开了含有下述通式（I）表示的化合物等的药剂。 [式中，R 1表示H，可以具有取代基的烷基，可以具有取代基的烯基，任意取代的环状烃，任意取代的杂环基等; R 2表示H，任选取代的烷基，任选取代的烯基，任选取代的环烷基等; R 3和R 4独立地表示H，任选取代的烷基，任选取代的烯基，任选取代的环烷基等; R 5和R 6独立地表示H，任选取代的烷基，任选取代的环烷基，任选取代的烷氧基等; R 7和R 8独立地表示H，任选取代的烷基，任选取代的环烷基等; X表示由上述式（II）表示的基团等; A表示任选取代的环状烃，任选取代的杂环基等; Y表示单键，任选取代的亚烷基，任选取代的亚烯基， - （CH 2）n - （CH 2）（其中X 1表示-NH-，-O-等，a和b分别表示0的整数） -5）等; 和B代表任选取代的环烃，任选取代的杂环基等。]

22. 发明申请

WO2007067629A1 BRADYKININ 1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： BRADYKININ 1受体拮抗剂
公开(公告)号：WO2007067629A1
公开(公告)日：2007-06-14
申请号：PCT/US2006/046566
申请日：2006-12-06
申请人： AMGEN INC. , CHEN, Jian, Jeffrey , HUMAN, Jason, Brooks , QIAN, Wenyuan , ZHU, Jiawang
发明人： CHEN, Jian, Jeffrey , HUMAN, Jason, Brooks , QIAN, Wenyuan , ZHU, Jiawang
IPC分类号： C07D241/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D453/02 , C07D487/08 , C07D487/10 , A61K31/4965 , A61K31/497 , A61P29/00
CPC分类号： C07D401/12 , C07D241/08 , C07D401/14 , C07D403/12 , C07D405/12 , C07D453/02 , C07D487/08 , C07D487/10
摘要： The invention encompasses novel compounds and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for treatment of diseases mediated by B1 bradykinin receptor.
摘要翻译：本发明包括新颖的化合物及其药学上可接受的衍生物，用于治疗由B1缓激肽受体介导的疾病的药物组合物和方法。

23. 发明申请

WO2006105304A3 PHENYL AND PYRIDYL LTA4H MODULATORS 审中-公开
公开(公告)号：WO2006105304A3
公开(公告)日：2006-10-05
申请号：PCT/US2006/011663
申请日：2006-03-30
申请人： JANSSEN PHARMACEUTICA N.V. , BUTLER, Christopher, R. , EDWARDS, James, P. , FOURIE, Anne, M. , GRICE, Cheryl, A. , KARLSSON, Lars , SAVALL, Brad, M. , TAYS, Kevin, L. , WEI, Jianmei
发明人： BUTLER, Christopher, R. , EDWARDS, James, P. , FOURIE, Anne, M. , GRICE, Cheryl, A. , KARLSSON, Lars , SAVALL, Brad, M. , TAYS, Kevin, L. , WEI, Jianmei
IPC分类号： A61K31/445 , A61K31/135 , C07D211/44 , C07D401/04 , C07D207/06 , C07D223/04 , C07D409/12 , C07D401/12 , C07D241/08 , C07D211/58 , C07D471/10 , C07D401/14 , C07D265/30 , A61P29/00
摘要： Leukotrfene A4 hydrolase (LTA4H) inhibitors, compositions containing them, and methods of use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and inflammatory conditions.

24. 发明申请

WO2005049583A1 SYNTHESIS OF 2-CHLORO-3,6-DIALKYL PYRAZINES 审中-公开
标题翻译： 2-氯代-3,6-二甲基吡咯烷的合成
公开(公告)号：WO2005049583A1
公开(公告)日：2005-06-02
申请号：PCT/IB2004/003702
申请日：2004-11-10
申请人： PHARMACIA & UPJOHN COMPANY LLC , RAPPATH, David, Warner
发明人： RAPPATH, David, Warner
IPC分类号： C07D241/08
CPC分类号： C07D241/08 , C07D241/16
摘要： A process for the production of 3,6-dialkyl-2,5-piperazinediones is disclosed.
摘要翻译：公开了制备3,6-二烷基-2,5-哌嗪二酮的方法。

26. 发明申请

WO2002070493A1 BISARYL DERIVATIVES HAVING FSH RECEPTOR MODULATORY ACTIVITY 审中-公开
标题翻译：具有FSH受体调节剂活性的双联衍生物
公开(公告)号：WO2002070493A1
公开(公告)日：2002-09-12
申请号：PCT/US2002/003777
申请日：2002-01-18
申请人： PHARMACOPEIA, INC. , GUO, Tao , HO, Koc-Kan , MCDONALD, Edward , DOLLE, Roland, Ellwood , SAIONZ, Kurt, W. , KULTGEN, Steven, G. , LIU, Ruiyan , DONG, Guizhen , GENG, Peng , ADANG, Anton, Egbert, Peter , VAN STRATEN, Nicole, Corine, Renee
发明人： GUO, Tao , HO, Koc-Kan , MCDONALD, Edward , DOLLE, Roland, Ellwood , SAIONZ, Kurt, W. , KULTGEN, Steven, G. , LIU, Ruiyan , DONG, Guizhen , GENG, Peng , ADANG, Anton, Egbert, Peter , VAN STRATEN, Nicole, Corine, Renee
IPC分类号： C07D241/08
CPC分类号： C07D207/273 , A61K38/00 , C07C237/22 , C07C271/22 , C07C275/14 , C07C2601/02 , C07D223/10 , C07D233/76 , C07D241/08 , C07D243/08 , C07K5/06078 , C07K5/06191
摘要： The invention relates to a bisaryl derivative of the formula I, wherein (R, R) is selected from (H, H), O, (H, CH 3 ), (H, OH) and (H, CN); Ar is substituted phenyl; and A is a group of following formula II, III, IV or V: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.
摘要翻译：本发明涉及式I的二芳基衍生物，其中（R，R）选自（H，H），O，（H，CH 3），（H，OH）和（H，CN）; Ar是取代的苯基; 并且A是以下式II，III，IV或V的组：本发明的化合物具有FSH受体调节活性，并且可用于控制生育力，避孕或用于治疗激素依赖性疾病。

27. 发明申请

WO02053546A1 HETEROCYCLE DERIVATIVES AS PPAR-GAMMA AGONISTS 审中-公开
标题翻译：作为PPAR-GAMMA AGONISTS的异构衍生物
公开(公告)号：WO02053546A1
公开(公告)日：2002-07-11
申请号：PCT/US2001/000440
申请日：2001-01-05
IPC分类号： A61K31/495 , A61K31/496 , A61P3/10 , C07D241/08 , C07D401/06 , C07D405/12 , C07D241/04
CPC分类号： C07D401/06 , A61K31/495 , A61K31/496 , C07D241/08 , C07D405/12
摘要： Compounds having the structure are peroxisome proliferator-activated receptor-gamma (PPAR-gamma) selective agonists and as such are useful in the modulation of blood glucose and the increase of insulin sensitivity in mammals. This activity of the piperazine derivatives of the invention make them particularly useful in the treatment of those conditions selected from the group consisting of diabetes, atherosclerosis, hyperglycemia, hyperlipidemia, obesity, syndrome X, insulin resistance, hypertension, heart failure and cardiovascular disease in mammals.
摘要翻译：具有该结构的化合物是过氧化物酶体增殖物激活受体-γ（PPAR-γ）选择性激动剂，因此可用于调节血糖和哺乳动物中胰岛素敏感性的增加。本发明的哌嗪衍生物的这种活性使得它们特别可用于治疗选自以下的那些病症：糖尿病，动脉粥样硬化，高血糖症，高脂血症，肥胖症，综合征X，胰岛素抵抗，高血压，心力衰竭和哺乳动物心血管疾病。

28. 发明申请

WO02048099A1 CARBOXYLIC ACID AMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF THROMBOEMBOLIC DISEASES AND TUMOURS 审中-公开
标题翻译：酰胺及其它们在肿瘤和疾病血栓栓塞治疗的
公开(公告)号：WO02048099A1
公开(公告)日：2002-06-20
申请号：PCT/EP2001/013545
申请日：2001-11-21
IPC分类号： C07D295/12 , A61K31/17 , A61K31/27 , A61K31/381 , A61K31/402 , A61K31/405 , A61K31/4172 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/445 , A61K31/4453 , A61K31/4468 , A61K31/45 , A61K31/453 , A61K31/4535 , A61K31/4545 , A61K31/495 , A61K31/497 , A61K31/5375 , A61K31/55 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P29/00 , A61P35/00 , A61P35/04 , C07C271/28 , C07C273/18 , C07C275/28 , C07C275/30 , C07C303/40 , C07C311/39 , C07C311/46 , C07C315/04 , C07C317/32 , C07C323/60 , C07D207/26 , C07D207/27 , C07D209/18 , C07D209/20 , C07D211/20 , C07D211/26 , C07D211/58 , C07D211/76 , C07D213/56 , C07D213/64 , C07D213/74 , C07D213/75 , C07D223/10 , C07D233/54 , C07D233/64 , C07D241/08 , C07D265/32 , C07D295/135 , C07D295/20 , C07D295/205 , C07D333/24 , C07D401/04 , C07D401/14 , C07D405/04 , C07D409/12 , C07D409/14 , C07D417/14 , A61K31/175 , C07C275/42 , C07C311/45 , C07C323/52 , C07D413/04
CPC分类号： C07D207/27 , C07C271/28 , C07C275/28 , C07C275/30 , C07C311/46 , C07C317/32 , C07C323/60 , C07C2601/02 , C07D209/20 , C07D211/20 , C07D211/58 , C07D211/76 , C07D213/56 , C07D213/64 , C07D213/75 , C07D223/10 , C07D233/64 , C07D241/08 , C07D265/32 , C07D295/135 , C07D295/205 , C07D333/24 , C07D401/04 , C07D401/14 , C07D405/04 , C07D409/12 , C07D409/14 , C07D417/14
摘要： The invention relates to compounds of formula (I), wherein the variables have the following meanings: D means a phenyl or a pyridyl which is unsubstituted or is mono- or polysubstituted by Hal, A, OR , N(R )2, NO2, CN, COOR2 or CON(R )2; R means H, Ar, Het, cycloalkyl or A, which can be substituted by OR , SR , N(R )2, Ar, Het, cycloalkyl, CN, COOR or CON(R )2; R means H or A, E means phenylene which can be mono- or polysubstituted by Hal, A, OR , N(R )2, NO2, CN, COOR or CON(R )2 or piperidin-1,4-diyl, W means AR, Het or N(R )2 and if E=piperidin-1,4-diyl, also R2 or cycloalkyl; and X means NH or O. These compounds are inhibitors of the coagulation factor Xa and can be used for the prevention and/or therapy of thromboembolic diseases and for treating tumours.
摘要翻译：式（I）其中各变量具有以下含义，D为未取代的或单 - 或被Hal，A，OR <2>，N（R <2>）2，NO 2，CN，COOR <2>或多取代的化合物 CON（R <2>）2 - 取代的苯基或吡啶基; R（<2> R）2中，Ar中，Het，环烷基，CN，COOR <2>或CON（<1> H，氩中，Het，环烷基或A，其由或<2>，SR <2>，N R可以被取代<2>）2; [R <2> H或A; E为亚苯基，其是单取代的或被Hal，A，OR <2>，N（R <2>）2，NO 2，CN，COOR可以是<2>或CON（R <2>）2或取代的哌啶取代的 -1,4-二基，W AR，的Het或N（R <2>）2，并且如果E =哌啶-1,4-二基，也可为R <2>或环烷基，X是NH或O，是抑制剂凝血因子Xa的和可用于预防和/或血栓栓塞性疾病的治疗和用于治疗肿瘤。

29. 发明申请

WO0192228A3 PROCESS FOR THE SYNTHESIS OF AMINE ETHERS FROM SECONDARY AMINO OXIDES 审中-公开
标题翻译：从二级氨基氧化合成胺类的方法
公开(公告)号：WO0192228A3
公开(公告)日：2002-05-16
申请号：PCT/EP0105668
申请日：2001-05-17
申请人： CIBA SC HOLDING AG , HAFNER ANDREAS , KIRNER HANS JUERG , SCHWARZENBACH FRANZ , SCHAAF PAUL ADRIAAN V D , NESVADBA PETER
发明人： HAFNER ANDREAS , KIRNER HANS JUERG , SCHWARZENBACH FRANZ , VAN DER SCHAAF PAUL ADRIAAN , NESVADBA PETER
IPC分类号： B01J27/122 , C07B61/00 , C07D209/44 , C07D211/94 , C07D217/26 , C07D241/08 , C07D401/12 , C07D401/14 , C07D405/12 , C08F4/00 , C08K5/3412 , C08K5/3435 , C08L101/00 , C09K15/30 , C09K21/10
CPC分类号： C07D401/14 , C04B35/632 , C07D209/44 , C07D211/94 , C07D217/26 , C07D241/08 , C07D401/12 , C07D405/12 , C08K5/3412
摘要： An amine ether of formula (A) wherein a is 1 or 2; and when a is 1, E is E'; when a is 2, E is L; E' is C1-C36 alkyl; C3-C18 alkenyl; C2-C18 alkinyl; C5-C18 cycloalkyl; C5-C18 cycloalkenyl; a radical of a saturated or unsaturated aliphatic bicyclic or tricyclic hydrocarbon of 7 to 12 carbon atoms; C2-C7alkyl or C3-C7alkenyl substituted by halogen; C7-C15aralkyl or C7-C15 aralkyl substituted by C1-C4 alkyl or phenyl; or E' is a radical of formula (VII) as explained in claim 1; T' is tertiary C4-C18alkyl or phenyl, each of which are unsubstituted or substituted by halogen, OH, COOR21 or C(O)-R22; or T' is C5-C12cycloalkyl; C5-C12cacloalkyl which is interrupted by at least one O or -NR18-; a polycyclic alkyl radical having 7-18 carbon atoms, or the same radical which is interrupted by at least one O or -NR18-; or T' is -C(G1)(G2)-T''; or C1-C18alkyl or C5-C12cycloalkyl substituted by F(I)T'' is hydrogen, halogen, NO2, cyano, or is a monovalent organic radical comprising 1-50 carbon atoms; or T'' and T' together form a divalent organic linking group completing, together with the hindered amine nitrogen atom and the quaternary carbon atom substituted by G1 and G2, an optionally substituted five- or six-membered ring structure; and all other residues are as defined in claim 1, are obtained in good yield from the corresponding N-oxyl hindered amine precursor by reaction with a hydrocarbon E1-H or H-L-H in the presence of an organic hydroperoxide and a catalytic amount of copper or a copper compound. The products of present process find utility as polymerization regulators and/or light stabilizers for organic material.
摘要翻译：式（A）的胺醚，其中a为1或2; 当a为1时，E为E'; 当a为2时，E为L; E'是C 1 -C 36烷基; C3-C18烯基; C2-C18炔基; C5-C18环烷基; C5-C18环烯基; 7-12个碳原子的饱和或不饱和脂族二环或三环烃基团; C 2 -C 7烷基或被卤素取代的C 3 -C 7链烯基; 被C 1 -C 4烷基或苯基取代的C 7 -C 15芳烷基或C 7 -C 15芳烷基; 或E'是如权利要求1所述的式（VII）的基团; T'是叔C4-C18烷基或苯基，其各自为未取代的或被卤素，OH，COOR21或C（O）-R22取代; 或T'为C 5 -C 12环烷基; 被至少一个O或-NR 18 - 中断的C 5 -C 12烷基; 具有7-18个碳原子的多环烷基或被至少一个O或-NR 18 - 中断的相同基团; 或T'为-C（G1）（G2）-T“; 或被F（I）T“取代的C 1 -C 18烷基或C 5 -C 12环烷基是氢，卤素，NO 2，氰基，或是包含1-50个碳原子的一价有机基团; 或T“和T'一起形成二价有机连接基团，与受阻胺氮原子和被G1和G2取代的季碳原子一起形成任选取代的五元或六元环结构; 并且所有其它残基如权利要求1中所定义，通过在有机氢过氧化物和催化量的铜或其盐的存在下与烃E1-H或HLH反应，由相应的N-氧基受阻胺前体以良好的产率获得铜化合物。本发明的产品可用作有机材料的聚合调节剂和/或光稳定剂。

30. 发明申请

WO01090113A1 HYDROXYLAMINE ESTERS AS POLYMERIZATION INITIATORS 审中-公开
标题翻译：羟基胺酯作为聚合引发剂
公开(公告)号：WO01090113A1
公开(公告)日：2001-11-29
申请号：PCT/EP2001/005447
申请日：2001-05-14
IPC分类号： C07C239/22 , C07D209/44 , C07D211/10 , C07D211/42 , C07D211/74 , C07D211/94 , C07D233/32 , C07D233/38 , C07D241/08 , C07D295/24 , C07D401/14 , C07D487/10 , C07D491/10 , C07D491/113 , C07F9/59 , C08F2/38 , C08F4/00 , C08F8/50 , C08F10/00
CPC分类号： C07D491/10 , C07C239/22 , C07D209/44 , C07D211/94 , C07D233/32 , C07D233/38 , C07D241/08 , C07D295/24 , C07D401/14 , C07D487/10 , C07F9/591 , C08F2/38 , C08F4/00 , C08F8/30 , C08F8/50 , C08F110/02 , C08F110/06 , C08K5/3435 , C08L23/06 , C08L23/10 , C08L2023/44 , C08L2205/02 , C08L2666/06 , C08F8/00
摘要： The invention relates to novel cyclic and open-chain hydroxylamine esters and polymerizable compositions comprising these hydroxylamine esters and an ethylenically unsaturated monomer or oligomer. The invention also relates to use as polymerization initiators and to the use of known hydroxylamine esters selected from the group consisting of HALS compounds and the novel hydroxylamine esters for the controlled degradation of polypropylene and for achieving a controlled increase in the molecular weight of polyethylene.
摘要翻译：本发明涉及新的环状和开链羟胺酯和包含这些羟胺酯和烯属不饱和单体或低聚物的可聚合组合物。本发明还涉及用作聚合引发剂和使用选自HALS化合物和新型羟胺酯的已知羟胺，用于聚丙烯的受控降解和用于实现聚乙烯分子量的受控增加。

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