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11. 发明申请

US20070185104A1 Benzoxazole acetonitriles 审中-公开
标题翻译：苯并恶唑乙腈
公开(公告)号：US20070185104A1
公开(公告)日：2007-08-09
申请号：US10571323
申请日：2004-09-10
申请人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
发明人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
IPC分类号： A61K31/5377 , A61K31/506 , C07D413/14
CPC分类号： C07D491/10 , C07D413/06 , C07D413/14
摘要： The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylamino moiety. R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, C1C6-alkYl, C2-C6-alkenYl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, carboxy, aminocarbonyl, cyano or hydroxy.
摘要翻译：本发明涉及苯并恶唑乙腈和含有该苯并恶唑乙腈的配方（I）的药物制剂。所述苯并恶唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）。本发明还涉及制备苯并恶唑乙腈（I）的方法。 A是嘧啶基，L是含有至少一个杂原子的仲或叔氨基或3-8元杂环烷基。选自N，O，S或L是酰氨基部分。 R 1选自包含或由氢，磺酰基，氨基，C 1 -C 6 - 烷基，C 2 -C 6 - 亚烷基，C 2 -C 6 - 炔基或C 1 -C 烷氧基，芳基，卤素，羧基，氨基羰基，氰基或羟基。

12. 发明授权

US07211601B2 Pharmaceutically active pyrrolidine derivatives 有权
标题翻译：药用活性吡咯烷衍生物
公开(公告)号：US07211601B2
公开(公告)日：2007-05-01
申请号：US10239912
申请日：2001-03-20
申请人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J Thomas , Anthony Baxter
发明人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J Thomas , Anthony Baxter
IPC分类号： A61K31/40 , C07D207/10 , C07D207/14
CPC分类号： C07D401/12 , C07D207/22 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present invention is related to pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO22-, —SO2NH—, —CH2-, B is either a group —(C═O)—NR8R9 or represents a heterocyclic residue having the formula (a) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5–6 membered aryl or heteroaryl ring.
摘要翻译：本发明涉及式（I）的吡咯烷衍生物。所述化合物优选用作药物活性化合物。具体地，式（I）的吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。本发明还涉及新型吡咯烷衍生物及其制备方法，其中X选自CR 6 R 7，NOR 6，NNR 6 R 7; A选自 - （CO） - ， - （CO）-O - ， - C（-NH） - ， - （CO）-NH-， - （CS）-NH，-SO 2 2-， SO 2 NH - ， - CH 2 - ，B为基团 - （CO）-NR 8 R 9，或表示具有式（a）的杂环残基，其中Q为NR10，O或S; n是选自0,1或2的整数; Y，Z和E与它们所连接的2个碳原子一起形成5-6元芳基或杂芳基环。

13. 发明申请

US20050187275A1 Triazoles as oxytocin antagonists 失效
标题翻译：三唑作为催产素拮抗剂
公开(公告)号：US20050187275A1
公开(公告)日：2005-08-25
申请号：US10498356
申请日：2002-12-19
申请人： Anna Quattropani , Matthias Schwarz , Russell Thomas , Thomas Coulter
发明人： Anna Quattropani , Matthias Schwarz , Russell Thomas , Thomas Coulter
IPC分类号： A61K31/4196 , A61P1/16 , A61P9/04 , A61P9/12 , A61P13/12 , A61P15/06 , A61P15/12 , A61P15/14 , A61P27/02 , C07D249/10 , C07D249/12 , C07D249/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D407/12
CPC分类号： C07D403/12 , C07D249/10 , C07D249/12 , C07D249/14 , C07D405/06 , C07D405/12
摘要： The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.
摘要翻译：本发明涉及特别用作药物活性化合物的式（I）的三唑衍生物以及含有这种三唑衍生物的药物制剂。所述三唑可用于治疗和/或预防早产，早产，痛经，不适当的血管加压素分泌，充血性心力衰竭，动脉高血压，肝硬化，肾病综合征和高眼压症。特别地，本发明涉及显示催产素和/或加压素受体的显着调节，特别是拮抗活性的三唑衍生物。更优选地，所述化合物可用于治疗和/或预防由催产素和/或加压素介导的疾病状态。本发明还涉及新的三唑衍生物及其制备方法。

14. 发明授权

US4896520A Lockable glove compartment cover arrangement for vehicles 失效
标题翻译：用于车辆的可锁定手套箱盖布置
公开(公告)号：US4896520A
公开(公告)日：1990-01-30
申请号：US237383
申请日：1988-08-29
申请人： Ulrich Bruhnke , Helmut Fischer , Matthias Schwarz , Erwin Uecker , Reinhard Wittwer
发明人： Ulrich Bruhnke , Helmut Fischer , Matthias Schwarz , Erwin Uecker , Reinhard Wittwer
IPC分类号： E05B13/00 , E05B53/00 , E05B77/50 , E05B79/20 , E05B83/30
CPC分类号： E05B13/005 , E05B79/20 , E05B77/50 , E05B83/30 , Y10T70/5124 , Y10T70/5544 , Y10T70/5973
摘要： The invention relates to a lockable glove and auxiliary compartment cover system for motor cars having a lock which is transferable into its tripping position by the stressing of a tripping lever by means of an actuating element. A closing member is provided which can be rotated between positions permitting and blocking the operative connection between the actuating element and the lock to change the security condition of the system. The change of the security condition occurs by means of a toothed-wheel gear which comprises a spur gear element rotatable with the closing element and a further gear element meshing with the spur gear element. In order to permit a handier arrangement of the actuating elements, the further gear element is likewise constructed as a rotatably mounted spur gear element, at least one of the spur gear elements, which belongs to a push-button, is guided for axial sliding, and a tripping stud protrudes eccentrically from the spur gear elements guided for axial sliding by means of which the tripping lever is pivotable in order to trip the lock.
摘要翻译：本发明涉及一种用于机动车辆的可锁定手套和辅助舱盖系统，其具有通过致动元件对脱扣杆的应力可转移到其脱扣位置的锁。提供闭合构件，其可以在允许和阻止致动元件和锁之间的操作连接的位置之间旋转以改变系统的安全状态。安全条件的改变是通过齿轮齿轮发生的，该齿轮包括可与闭合元件一起旋转的正齿轮元件和与正齿轮元件啮合的另一个齿轮元件。为了允许致动元件的更方便的布置，另外的齿轮元件同样被构造为可旋转地安装的正齿轮元件，属于按钮的至少一个正齿轮元件被引导用于轴向滑动，并且跳闸螺栓从被引导用于轴向滑动的正齿轮元件偏心地突出，通过该螺栓将脱扣杆可枢转以便跳闸。

15. 发明授权

US09643162B2 Activated base metal catalysts 有权
公开(公告)号：US09643162B2
公开(公告)日：2017-05-09
申请号：US12601816
申请日：2007-05-29
申请人： Daniel Ostgard , Monika Berweiler , Markus Göttlinger , Steffen Laporte , Matthias Schwarz
发明人： Daniel Ostgard , Monika Berweiler , Markus Göttlinger , Steffen Laporte , Matthias Schwarz
IPC分类号： C07C209/00 , B01J25/02 , C07C209/36 , B01J23/89
CPC分类号： B01J25/02 , B01J23/892 , C07C209/36 , C07C211/46 , C07C211/50
摘要： Nitro-compounds are hydrogenated with an activated Ni catalyst whose Ni/Al alloy also contained one or more elements from the list of Cu, Ag and Au prior to activation. In combination with the Group IB elements mentioned above, this catalyst can also be doped with other elements via their addition to the Ni/Al alloy prior to activation and/or they can be adsorbed onto the surface of the catalyst either during or after the activation of the alloy. The suitable doping elements for the alloy prior to activation in combination with the group IB elements mentioned above are one or more of the elements from the list of Mg, Ti, Ce, Cr, V, Mo, W, Mn, Re, Fe, Co, Tr, Ru, Rh, Pd, Pt and Bi. The suitable doping elements that may be adsorbed onto the surface of the catalyst that was previously doped in the alloy prior to activation with the group IB elements mentioned above are one or more elements from the list Mg, Ca, Ba, Ti, Ce, V, Cr, Mo, W, Mn, Re, Fe, Ru, Co, Rh, Ir, Pd, Pt, Ni, Cu, Ag, Au and Bi.

16. 发明授权

US08889911B2 Activated base metal catalysts 有权
标题翻译：活性贱金属催化剂
公开(公告)号：US08889911B2
公开(公告)日：2014-11-18
申请号：US12601820
申请日：2007-05-29
申请人： Daniel Ostgard , Monika Berweiler , Markus Göttlinger , Steffen Laporte , Matthias Schwarz
发明人： Daniel Ostgard , Monika Berweiler , Markus Göttlinger , Steffen Laporte , Matthias Schwarz
IPC分类号： C07C209/00 , B01J25/02 , C07C209/36
CPC分类号： B01J25/02 , C07C209/36 , C07C211/50
摘要： Nitro-compounds are hydrogenated with an activated Ni catalyst that is doped during and/or after activation with one or more elements from the list of Mg, Ca, Ba, Ti, Zr, Ce, Nb, Cr, Mo, W, Mn, Re, Fe, Co, Ir, Ni, Cu, Ag, Au, Rh, Ru and Bi whereas the Ni/Al alloy may not, but preferentially can contain prior to activation one or more doping elements from the list of Ti, Ce, V, Cr, Mo, W, Mn, Re, Fe, Ru, Co, Rh, Ir, Pd, Pt and Bi. If the Ni/Al alloy contained one or more of the above mentioned suitable alloy doping elements prior to activation, the resulting catalyst can then be doped with one or more of the elements from the list of Mg, Ca, Ba, Ti, Zr, Ce, V, Nb, Cr, Mo, W, Mn, Re, Fe, Ru, Co, Rh, Ir, Ni, Pd, Pt, Cu, Ag, Au and Bi by their adsorption onto the surface of the catalyst.
摘要翻译：硝基化合物用活化的Ni催化剂氢化，所述活化的Ni催化剂在Mg，Ca，Ba，Ti，Zr，Ce，Nb，Cr，Mo，W，Mn的列表中的一种或多种元素的活化期间和/ Re，Fe，Co，Ir，Ni，Cu，Ag，Au，Rh，Ru和Bi，而Ni / Al合金在活化前可能不含有一种或多种来自Ti，Ce， V，Cr，Mo，W，Mn，Re，Fe，Ru，Co，Rh，Ir，Pd，Pt和Bi。如果Ni / Al合金在活化之前含有一种或多种上述合适的合金掺杂元素，则所得到的催化剂然后可以从Mg，Ca，Ba，Ti，Zr的列表中掺入一种或多种元素，通过吸附在催化剂表面上的Ce，V，Nb，Cr，Mo，W，Mn，Re，Fe，Ru，Co，Rh，Ir，Ni，Pd，Pt，Cu，Ag，Au和Bi。

17. 发明授权

US08796280B2 2,3-disubstituted pyrazinesulfonamides as CRTH2 inhibitors 有权
标题翻译： 2,3-二取代吡嗪磺酰胺作为CRTH2抑制剂
公开(公告)号：US08796280B2
公开(公告)日：2014-08-05
申请号：US11918294
申请日：2006-04-20
申请人： Patrick Page , Matthias Schwarz , Eric Sebille , Christophe Cleva , Cedric Merlot , Maurizio Maio
发明人： Patrick Page , Matthias Schwarz , Eric Sebille , Christophe Cleva , Cedric Merlot , Maurizio Maio
IPC分类号： A61K31/4965 , C07D409/12 , C07D401/10 , C07D241/22 , C07D413/10 , C07D405/12 , C07D403/10 , C07D401/12
CPC分类号： C07D241/22 , C07D241/20 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D411/14 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The present invention is related to the use of 2,3 substituted pyrazine sulfonamides of formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.
摘要翻译：本发明涉及式（I）的2,3-取代吡嗪磺酰胺在治疗和/或预防过敏性疾病，炎性皮肤病和其它具有炎性成分的疾病中的应用。具体地说，本发明涉及2,3取代吡嗪磺酰胺用于调节，特别是抑制CRTH2活性的用途。

18. 发明申请

US20130143893A1 PIPERAZINE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：哌嗪衍生物及其使用方法
公开(公告)号：US20130143893A1
公开(公告)日：2013-06-06
申请号：US13754345
申请日：2013-01-30
申请人： Sharad Magar , Andreas Goutopoulos , Yihua Liao , Matthias Schwarz , Russell J. Thomas
发明人： Sharad Magar , Andreas Goutopoulos , Yihua Liao , Matthias Schwarz , Russell J. Thomas
IPC分类号： C07D409/14 , C07D403/12 , C07D471/04 , C07D403/14
CPC分类号： C07D409/14 , A61K31/496 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D487/04
摘要： The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
摘要翻译：本发明提供2-甲酰胺哌嗪化合物，以及使用或包含一种或多种这些化合物的治疗方法和药物组合物。本发明的化合物可用于治疗哺乳动物不育症。

19. 发明申请

US20120295889A1 3-Arylamino Pyridine Derivatives 有权
标题翻译： 3-芳基氨基吡啶衍生物
公开(公告)号：US20120295889A1
公开(公告)日：2012-11-22
申请号：US13472721
申请日：2012-05-16
申请人： Ulrich Abel , Holger Deppe , Achim Feurer , Ulrich Grädler , Kerstin Otte , Renate Sekul , Meinolf Thiemann , Andreas Goutopoulos , Matthias Schwarz , Xuliang Jiang
发明人： Ulrich Abel , Holger Deppe , Achim Feurer , Ulrich Grädler , Kerstin Otte , Renate Sekul , Meinolf Thiemann , Andreas Goutopoulos , Matthias Schwarz , Xuliang Jiang
IPC分类号： C07D213/81 , A61K31/5377 , A61K31/496 , A61K31/506 , A61K31/4709 , A61K31/4545 , A61K31/444 , A61K31/443 , A61K31/4439 , A61K31/44 , C07D413/12 , C07D401/12 , C07D413/04 , C07D405/12 , C07D213/79 , A61P9/10 , A61K31/4433 , C07D413/06 , C07D213/89 , C07D401/06 , A61P35/00 , A61P29/00 , A61P1/18 , A61P13/12 , A61P17/00 , A61P9/00 , A61P13/08 , A61P17/06 , A61P3/10 , A61P27/02 , A61P1/00 , A61K31/55
CPC分类号： C07D405/12 , C07D213/79 , C07D213/81 , C07D213/89 , C07D295/125 , C07D295/13 , C07D295/32 , C07D401/12
摘要： The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
摘要翻译：本发明提供新的取代的3-芳基氨基吡啶化合物其药学上可接受的盐，溶剂合物和前药化合物，其中W，R 1，R 2，R 9，R 10，R 11，R 12，R 13，R 14如说明书中所定义。这些化合物是MEK抑制剂，可用于治疗过度增殖性疾病，如癌症，再狭窄和炎症。还公开了这样的化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗和含有这些化合物的药物组合物中的应用。

20. 发明申请

US20120238575A1 ANTIPROLIFERATIVE PYRIMIDYL, FUSED PYRIMIDYL AND PYRIMIDYL HYDRAZONES 审中-公开
标题翻译：抗生素PYRIMIDYL，FUSED PYRIMIDYL和PYRIMIDYL HYDRAZONES
公开(公告)号：US20120238575A1
公开(公告)日：2012-09-20
申请号：US13484329
申请日：2012-05-31
申请人： BRIAN HEALEY , Zhong Zhao , Amanda Sutton , Matthias Schwarz
发明人： BRIAN HEALEY , Zhong Zhao , Amanda Sutton , Matthias Schwarz
IPC分类号： A61K31/505 , A61K31/517 , C07D239/42 , C07D413/04 , C12N5/09 , C07D239/47 , C07D413/10 , A61K31/5377 , C07D401/04 , A61P35/00 , C07D239/94 , A61K31/506
CPC分类号： C07D239/94 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D413/04
摘要： The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.
摘要翻译：本发明涉及新的一系列嘧啶基或稠合的嘧啶基腙。其中A选自式（A1），（A2），（A3），（A4），（A5）的式（I）化合物可用于治疗和/或预防增殖性疾病。

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