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31. 发明申请

US20100093730A1 NOVEL COMPOUNDS AS CALCIUM CHANNEL BLOCKERS 有权
标题翻译：新型化合物作为钙通道阻塞剂
公开(公告)号：US20100093730A1
公开(公告)日：2010-04-15
申请号：US12571862
申请日：2009-10-01
申请人： Pramila A. Bhatia , George A. Doherty , Irene Drizin , Helmut Mack , Richard J. Perner , Andrew O. Stewart , Qingwei Zhang
发明人： Pramila A. Bhatia , George A. Doherty , Irene Drizin , Helmut Mack , Richard J. Perner , Andrew O. Stewart , Qingwei Zhang
IPC分类号： A61K31/5377 , C07D403/02 , C07D401/02 , C07D413/02 , A61K31/497 , A61K31/4439
CPC分类号： C07D487/10 , C07D207/27 , C07D207/48 , C07D209/52 , C07D211/76 , C07D211/96 , C07D241/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, Ar2, L1, L2, n, R1, R4, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
摘要翻译：本申请涉及含有式（I）化合物的钙通道抑制剂，其中Ar1，Ar2，L1，L2，n，R1，R4，X和Y如说明书中所定义。本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗病症和病症的方法。

32. 发明申请

US20090166581A1 Additive Comprising Azomethine Compounds 有权
标题翻译：包括偶氮甲碱化合物的添加剂
公开(公告)号：US20090166581A1
公开(公告)日：2009-07-02
申请号：US12282508
申请日：2007-02-15
申请人： Helmut Mack
发明人： Helmut Mack
IPC分类号： C09K3/00
CPC分类号： C08G77/26 , C08K5/29 , C08K5/5465 , C08L83/08
摘要： The present invention relates to a mixture of an oligomeric, blocked aminosilane (azomethine structure) and a monomeric, blocked, primary amine (azomethine structure). This mixture is suitable in particular as a curing agent, crosslinker and adhesion promoter.
摘要翻译：本发明涉及低聚封闭的氨基硅烷（偶氮甲碱结构）和单体封闭的伯胺（偶氮甲碱结构）的混合物。该混合物特别适合作为固化剂，交联剂和粘合促进剂。

33. 发明授权

US07491729B2 3-Substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof 有权
标题翻译： 3-取代的3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，的制备和用途
公开(公告)号：US07491729B2
公开(公告)日：2009-02-17
申请号：US10539708
申请日：2003-12-17
申请人： Margaretha Bakker , Wilfried Hornberger , Andreas Kling , Udo Lange , Helmut Mack , Achim Moeller , Reinhold Mueller , Kurt Schellhaas , Martin Schmidt , Gerd Steiner , Karsten Wicke
发明人： Margaretha Bakker , Wilfried Hornberger , Andreas Kling , Udo Lange , Helmut Mack , Achim Moeller , Reinhold Mueller , Kurt Schellhaas , Martin Schmidt , Gerd Steiner , Karsten Wicke
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D495/14
摘要： 3-Substituted 3,4-dihydrothieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof. The invention relates to 3,4-dihydrothieno[2,3-d]pyrimidin-4-one derivatives which are substituted in position 3 by 5-membered heteroaryl which may be fused to an aryl or heteroaryl radical, where the heteroaryl and, if appropriate, the fused aryl or heteroaryl radical may have 1, 2 or 3 substituents selected independently of one another from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halo-C1-5-alkyl, halo-C1-5-alkoxy, hydroxy, —NH2, —N(R6)2, —NH(R6), aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl, where the substituents aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl may have 1, 2 or 3 substituents selected independently of one another from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halo-C1-5-alkyl, halo-C1-5-alkoxy, hydroxy, —NH2, —N(R6)2 and —NH(R6). The preparation and use of these derivatives, especially for therapeutic purposes, e.g. for the treatment of depressions, are likewise described.
摘要翻译： 3-取代的3,4-二氢噻吩并[2,3-d]嘧啶-4-酮衍生物，的制备和用途。本发明涉及在3位被5位杂芳基取代的3,4-二氢噻吩并[2,3-d]嘧啶-4-酮衍生物，其可以与芳基或杂芳基稠合，其中杂芳基和稠合的芳基或杂芳基可以具有1,2或3个彼此独立地选自C 1-5 - 烷基，C 1-5 - 烷氧基，C 1-5 - 烷硫基，卤素，CN，卤代-C 1-5 - 烷基，卤代C 1-5 - 烷氧基，羟基，-NH 2，-N（R 6）2，-NH（R 6），芳基，芳氧基，芳烷基，芳烷氧基和杂芳基，其中芳基，芳氧基，芳烷基，芳烷氧基和杂芳基可以具有1,2或3个彼此独立地选自C 1-5 - 烷基，C 1-5 - 烷氧基，C 1-5 - 烷硫基，卤素，CN，卤代C 1-5 - 烷基，卤代-C 1-5 - 烷氧基，羟基，-NH 2，-N（R 6）2和-NH（R 6）。这些衍生物的制备和使用，特别是用于治疗目的，例如为了处理凹陷，同样地描述。

34. 发明申请

US20080234329A1 Carboxamide compounds and their use as calpain inhibitors 有权
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：US20080234329A1
公开(公告)日：2008-09-25
申请号：US12070941
申请日：2008-02-22
申请人： Andreas Kling , Wilfried Hornberger , Helmut Mack , Achim Moeller , Volker Nimmrich , Dietmar Seemann , Wilfried Lubisch
发明人： Andreas Kling , Wilfried Hornberger , Helmut Mack , Achim Moeller , Volker Nimmrich , Dietmar Seemann , Wilfried Lubisch
IPC分类号： A61K31/4439 , C07D401/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D491/048 , C07D493/04 , C07D513/04
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a′ and I-A.a″ in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3，R 3，R 3， >，W，Y和X具有权利要求书和说明书中所述的含义，其互变异构体及其药学上合适的盐。特别地，化合物具有通式IA.a'和IA.a“，其中m，E，R 1，R 3a，R 3b， R 2，R 2，R 2，W 2和R 6具有如下的含义：权利要求书，n为0,1或2，其互变异构体及其药学上合适的盐。

35. 发明授权

US06780955B2 Mixture of catenate and cyclic siloxane oligomers, its preparation and use 失效
标题翻译：联苯胺和环状硅氧烷低聚物的混合物，其制备和用途
公开(公告)号：US06780955B2
公开(公告)日：2004-08-24
申请号：US10348959
申请日：2003-01-23
申请人： Dieter Barfurth , Helmut Mack
发明人： Dieter Barfurth , Helmut Mack
IPC分类号： C08G7708
CPC分类号： C08G77/20 , C08G77/045 , C08G77/06 , C09D183/04
摘要： The present invention provides a process for preparing a mixture, which mixture includes catenate and cyclic siloxanes of formula I R3Si—O—(SiR2—O—)mSiR3 (I) and cyclic siloxanes of formula II wherein m is an integer from 0 to 40 and n is an integer from 2 to 40, wherein R2 and R3 are each independently an organic functional group selected from the group including alkyl, aryl, vinyl, and alkoxy groups, and wherein there is not more than one vinyl group or aryl group per silicon atom, said process including a controlled hydrolysis, condensation or cocondensation reaction of at least one monomeric silane in alcoholic solution in the presence of an acidic catalyst, which reaction includes contacting alcohol, water, and at least one chlorosilane component selected from the group including (i), (ii), (iii): (i) at least one arylchlorosilane; (ii) at least one admixture selected from the group including alkylchlorosilane and arylchlorosilane, arylchlorosilane and vinylchlorosilane, alkylchlorosilane and vinylchlorosilane, and arylchlorosilane and vinylchlorosilane and alkylchlorosilane; (iii) at least one selected from the group including chlorosilane, alkylchlorosilane, arylchlorosilane, and vinylchlorosilane in two or more separate batches to obtain two or more separate mixtures and thereafter combining the mixtures; to form the mixture of the catenate and cyclic siloxanes. The present invention also provides the mixtures and the use of such mixtures.
摘要翻译：本发明提供一种制备混合物的方法，该混合物包括式I的链环和环状硅氧烷和式II的环状硅氧烷，其中m为0至40的整数，n为2至40的整数，其中R 2和R 3各自为独立地是选自包括烷基，芳基，乙烯基和烷氧基的有机官能团，并且其中每个硅原子不超过一个乙烯基或芳基，所述方法包括受控的水解，缩合或共缩聚反应在酸性催化剂存在下，醇溶液中的至少一种单体硅烷，该反应包括使醇，水和至少一种选自（i），（ii），（iii）：（i）中的氯硅烷组分与至少一种芳基氯硅烷;（ii）至少一种选自烷基氯硅烷和芳基氯硅烷，芳基氯硅烷和乙烯基氯硅烷，烷基氯硅烷和乙烯基氯硅烷的混合物， nd芳基氯硅烷和乙烯基氯硅烷和烷基氯硅烷;（iii）选自包括氯硅烷，烷基氯硅烷，芳基氯硅烷和乙烯基氯硅烷的组中的至少一种，分两批以上分批，以获得两种或更多种分离的混合物，然后混合该混合物; 链状和环状硅氧烷。本发明还提供了这些混合物的混合物和用途。

36. 发明授权

US5932567A Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US5932567A
公开(公告)日：1999-08-03
申请号：US875515
申请日：1997-07-30
申请人： Werner Seitz , Helmut Mack , Thomas Zierke , Hans-Joachim Bohm , Hans Wolfgang Hoffken , Stefan Koser , Thomas Pfeiffer , Wilfried Hornberger
发明人： Werner Seitz , Helmut Mack , Thomas Zierke , Hans-Joachim Bohm , Hans Wolfgang Hoffken , Stefan Koser , Thomas Pfeiffer , Wilfried Hornberger
IPC分类号： A61K38/55 , A61K38/00 , A61P7/02 , C07K5/06 , C07K5/065 , C07K5/072 , C07K5/087 , C07D239/14
CPC分类号： C07K5/0812 , C07K5/06026 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06113 , C07K5/06191 , A61K38/00
摘要： Thrombin inhibitors of the formula ##STR1## where R.sup.1, A, B and D have the meaning indicated in the description, and intermediates for the preparation thereof are described.The compounds I are suitable for controlling diseases.
摘要翻译： PCT No.PCT / EP96 / 00472 Sec。 371日期1997年7月30日 102（e）日期1997年7月30日PCT提交1996年2月6日PCT公布。出版物WO96 / 24609 日期为1996年8月15日，其中R1，A，B和D的凝血酶抑制剂具有说明书中指出的含义及其制备中间体。化合物I适合于控制疾病。

37. 发明授权

US09382383B2 Composition comprising block cocondensates of propylfunctional alkaline siliconates and silicates, and method for the production thereof 有权
标题翻译：丙基官能的碱性硅酸盐和硅酸盐的嵌段共缩合物的组合物及其制备方法
公开(公告)号：US09382383B2
公开(公告)日：2016-07-05
申请号：US14358437
申请日：2012-10-30
申请人： Spomenko Ljesic , Christopher Studte , Helmut Mack
发明人： Spomenko Ljesic , Christopher Studte , Helmut Mack
IPC分类号： C07F7/04 , C08G77/16 , C04B24/42 , C08G77/42 , C08L83/10 , C08G77/06 , C04B28/14 , C04B103/00 , C04B103/65 , C04B111/27
CPC分类号： C08G77/16 , C04B24/42 , C04B28/14 , C04B2103/0061 , C04B2103/65 , C04B2111/27 , C08G77/06 , C08G77/42 , C08L83/10
摘要： The invention relates to a composition and a method for the production of the composition comprising block cocondensates of propylfunctional alkaline siliconates and silicates.
摘要翻译：本发明涉及一种组合物和制备该组合物的方法，该组合物包含丙基官能的碱性硅酸盐和硅酸盐的嵌段共缩合物。

38. 发明授权

US09150553B2 Carboxamide compounds and their use as calpain inhibitors 有权
公开(公告)号：US09150553B2
公开(公告)日：2015-10-06
申请号：US12810795
申请日：2008-12-29
申请人： Wilfried Hornberger , Helmut Mack , Andreas Kling , Achim Moeller , Barbara Vogg , Jürgen Delzer , Gisela Backfisch , Armin Beyerbach
发明人： Wilfried Hornberger , Helmut Mack , Andreas Kling , Achim Moeller , Barbara Vogg , Jürgen Delzer , Gisela Backfisch , Armin Beyerbach
IPC分类号： C07D405/14 , A61K31/4439 , C07D491/052
CPC分类号： C07D405/14 , C07D491/052
摘要： The present invention relates to novel carboxamide compounds of the formula I and their use for the manufacture of a medicament. The carboxamide compounds are prodrugs of inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. R1 is C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C4-alkyl, aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl, hetaryl-C1-C4-alkyl or hetaryl-C2-C6-alkenyl, R2 is C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C4-alkyl, aryl, O-aryl, O—CH2-aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl, hetaryl-C1-C4-alkyl or hetaryl-C2-C6-alkenyl, R3a and R3b together form a moiety S-Alk-S, O-Alk-S or O-Alk-O, wherein Alk is linear C2-C5-alkandiyl, which may be unsubstituted or substituted with 1, 2, 3 or 4 radicals selected from C1-C4-alkyl or halogen; X is a radical of the formulae C(═O)—O—Rx1, C(═O)—NRx2Rx3, C(═O)—N(Rx4)—(C1-C6-alkylene)-NRx2Rx3, C(═O)—N(Rx4)NRx2Rx3, n is 0, 1 or 2, one of the variables Y1, Y2, Y3 or Y4 is a nitrogen atom, and the remaining variables Y1, Y2, Y3 or Y4 are CH; Ry is e.g. OH, SH, halogen, NO2, NH2, CN, CF3, CHF2, CH2F, O—CF3, O—CHF2, O—CH2F, COOH, OCH2COOH, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkoxy-C1-C4-alkyl, C1-C6-alkylthio etc. W is a radical of the formulae W1 or W2 which is linked via nitrogen: in which * means the linkage to the 6-membered heteroaromatic ring, and # means the linkage to R2, m is 0, 1 or 2, and Rw is e.g. OH, SH, halogen, NO2, NH2, CN, CF3, CHF2, CH2F, O—CF3, O—CHF2, O—CH2F, COOH, OCH2COOH.

39. 发明授权

US09062027B2 Carboxamide compounds and their use as calpain inhibitors V 有权
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：US09062027B2
公开(公告)日：2015-06-23
申请号：US13992582
申请日：2011-12-08
申请人： Andreas Kling , Katja Jantos , Helmut Mack , Achim Moller , Wilfried Hornberger , Yanbin Lao , Gisela Backfisch , Marjoleen Nijsen
发明人： Andreas Kling , Katja Jantos , Helmut Mack , Achim Moller , Wilfried Hornberger , Yanbin Lao , Gisela Backfisch , Marjoleen Nijsen
IPC分类号： C07D401/14 , C07D401/04 , A61K31/4439 , A61P25/28
CPC分类号： C07D401/04 , A61K31/4439 , C07D401/14 , Y02A50/411
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3, R4, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式（I）的化合物，其中R 1，R 2，R 3，R 4，X，m和n具有权利要求书和描述中所述的含义，其互变异构体，其水合物和药学上合适的盐其中。在这些化合物中，优选其中R 1为任选取代的苄基或杂芳基 - 甲基，X为单键或氧原子，R 2为C 1 -C 4烷基，C 1 -C 4卤代烷基，C 2 -C 4 - 烯基，C 3 -C 6 环烷基，C 3 -C 6环烷基-C 1 -C 2烷基，C 3 -C 6杂环烷基-C 1 -C 2烷基，苯基，苯基-C 1 -C 3 - 烷基，吡啶-2-基-C 1 -C 3 - 烷基或CH 2 -C（O）OCH 3，R 3和R 4彼此独立地是卤素，CN，CF 3，CHF 2，CH 2 F，C 1 -C 2 - 烷基或C 1 -C 2 - 烷氧基，m和n彼此独立地为0或1。

40. 发明授权

US09051304B2 Carboxamide compounds and their use as calpain inhibitors V 有权
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：US09051304B2
公开(公告)日：2015-06-09
申请号：US12972663
申请日：2010-12-20
申请人： Andreas Kling , Katja Jantos , Helmut Mack , Achim Möller , Wilfried Hornberger , Gisela Backfisch , Yanbin Lao , Marjoleen Nijsen
发明人： Andreas Kling , Katja Jantos , Helmut Mack , Achim Möller , Wilfried Hornberger , Gisela Backfisch , Yanbin Lao , Marjoleen Nijsen
IPC分类号： C07D401/04 , C07D401/14 , C07D207/28 , C07D409/14 , C07D417/14
CPC分类号： C07D401/04 , C07D207/28 , C07D401/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3 R4, R5, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is optionally substituted aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl or hetaryl-C1-C4-alkyl, R3 is C1-C3-alkyl, C1-C3-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, or phenyl-C1-C3-alkyl, R4 and R5 independently of one another are halogen, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3，R 4，R 5，m和n具有权利要求书和描述中所述的含义，其互变异构体，其水合物及其药学上合适的盐。在这些化合物中，优选其中R 1为任选取代的苯基-C 1 -C 2烷基或杂芳基-C 1 -C 2烷基，R 2为任选取代的芳基，杂芳基，芳基-C 1 -C 6 - 烷基，芳基-C 2 -C 6 - 烯基或杂芳基-C 1 -C 4 - 烷基，R 3是C 1 -C 3 - 烷基，C 1 -C 3 - 卤代烷基，C 2 -C 4 - 烯基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 2烷基或苯基 - C 1 -C 3 - 烷基，R 4和R 5彼此独立地是卤素，CF 3，CHF 2，CH 2 F，C 1 -C 2 - 烷基或C 1 -C 2 - 烷氧基，m和n彼此独立地为0或1。

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