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1. 发明授权

US08044069B2 Compounds as calcium channel blockers 有权
标题翻译：化合物作为钙通道阻滞剂
公开(公告)号：US08044069B2
公开(公告)日：2011-10-25
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： A61K31/4015 , A61K31/4025 , A61K31/45 , A61K31/4523 , C07D207/12 , C07D211/40
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。

2. 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。

3. 发明授权

US08648069B2 5-substituted indazoles as kinase inhibitors 有权
标题翻译： 5-取代的吲唑作为激酶抑制剂
公开(公告)号：US08648069B2
公开(公告)日：2014-02-11
申请号：US12327991
申请日：2008-12-04
申请人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, Jr. , Thomas D. Penning
发明人： Irini Akritopoulou-Zanze , Brian D. Wakefield , Helmut Mack , Sean C. Turner , Alan F. Gasiecki , Vijaya J. Gracias , Kathy A. Sarris , Douglas M. Kalvin , Melissa J. Michmerhuizen , Qi Shuai , Jyoti R. Patel , Margaretha Bakker , Nicole Teusch , Eric F. Johnson , Peter J. Kovar , Stevan W. Djuric , Andrew J. Long , Anil Vasudevan , Dawn George , Lu Wang , Biqin Li , N. St. John Moore , Adrian D. Hobson , Keith W. Woods , Julie M. Miyashiro , Steven L. Swann, Jr. , Thomas D. Penning
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4192 , C07D417/14 , C07D405/14 , C07D401/14 , C07D403/04 , C07D403/14
CPC分类号： C07D413/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶例如糖原合成酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），Cdc7，AKT ，PAK4，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。

4. 发明申请

US20140005227A1 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抑制剂V
公开(公告)号：US20140005227A1
公开(公告)日：2014-01-02
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： C07D401/04
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。

5. 发明授权

US08283363B2 Carboxamide compounds and their use as calpain inhibitors 有权
公开(公告)号：US08283363B2
公开(公告)日：2012-10-09
申请号：US12940339
申请日：2010-11-05
申请人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
发明人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
IPC分类号： A61P35/00 , A61P25/00 , A61P29/00 , A61P31/00 , A61P9/00 , A61P27/02 , A61K31/425 , A61K31/451 , A61K31/4015 , A61K31/4439 , A61K31/4164 , C07D211/40 , C07D207/12 , C07D401/02 , C07D233/02 , C07D275/03
CPC分类号： C07D207/22 , C07D207/26 , C07D207/28 , C07D211/76 , C07D211/78 , C07D213/81 , C07D233/32 , C07D233/34 , C07D239/10 , C07D275/03 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
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, R4, Q, Y, A 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 Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

6. 发明申请

US20120122842A1 NAMPT AND ROCK INHIBITORS 有权
标题翻译： NAMPT和ROCK INHIBITORS
公开(公告)号：US20120122842A1
公开(公告)日：2012-05-17
申请号：US13294303
申请日：2011-11-11
申请人： Michael L. Curtin , Bryan K. Sorensen , Howard R. Heyman , Richard F. Clark , Kevin R. Woller , Omar J. Shah , Michael Michaelides , Chris Tse , Anil Vasudevan , Helmut Mack , Todd M. Hansen , Ramzi Sweis , Marina A. Pliushchev
发明人： Michael L. Curtin , Bryan K. Sorensen , Howard R. Heyman , Richard F. Clark , Kevin R. Woller , Omar J. Shah , Michael Michaelides , Chris Tse , Anil Vasudevan , Helmut Mack , Todd M. Hansen , Ramzi Sweis , Marina A. Pliushchev
IPC分类号： A61K31/541 , C07D491/048 , C07D401/14 , C07D401/12 , C07D495/04 , C07D403/14 , C07D405/12 , C07D403/12 , C07D417/12 , A61K31/4035 , A61K31/496 , A61K31/4439 , A61K31/501 , A61K31/4155 , A61P9/12 , A61P9/04 , A61P9/00 , A61P13/12 , A61P9/10 , A61P11/06 , A61P15/10 , A61P15/00 , A61P13/10 , A61P25/00 , A61P29/00 , A61P25/28 , A61P25/16 , A61P19/02 , A61P19/08 , A61P1/00 , A61P17/06 , A61P35/00 , A61P35/04 , A61P31/12 , A61P31/04 , A61P3/10 , A61P25/24 , A61P25/18 , A61P25/08 , A61P35/02 , A61P11/00 , C07D209/44
CPC分类号： C07D209/44 , A61K31/437 , A61K31/496 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/048 , C07D495/04 , C07D519/00
摘要： Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.
摘要翻译：公开了抑制NAMPT活性的化合物，含有该化合物的组合物和治疗其中NAMPT表达的疾病的方法。公开了抑制ROCK活性的化合物，含有化合物的组合物和治疗ROCK表达疾病的方法。

7. 发明申请

US20110132144A1 Method For Producing Metal Nanoparticles In Polyols 审中-公开
标题翻译：在多元醇中生产金属纳米粒子的方法
公开(公告)号：US20110132144A1
公开(公告)日：2011-06-09
申请号：US13003785
申请日：2009-07-15
申请人： Jochen Mezger , Laurent Marc , Simone Klapdohr , Burkhard Walther , Zhizhong Cai , Tobias Austermann , Silke Flakus , Helmut Mack
发明人： Jochen Mezger , Laurent Marc , Simone Klapdohr , Burkhard Walther , Zhizhong Cai , Tobias Austermann , Silke Flakus , Helmut Mack
IPC分类号： B22F9/18 , B22F9/00 , B82Y40/00
CPC分类号： B22F9/24
摘要： The invention relates to a process for the preparation of metal nanoparticles, selected from the group consisting of lead, bismuth, zinc, antimony, indium, gold, nickel, cobalt, palladium, platinum, iridium, osmium, rhodium, ruthenium, rhenium, vanadium, chromium, manganese, niobium, molybdenum, tungsten, tantalum, cadmium, silver and/or copper, on a rotating body, characterized in that a reduction of corresponding metal salts, corresponding metal salt complexes, corresponding metal hydroxides and/or corresponding metal oxides by polyols having a number of hydroxyl groups in the polyol of 1 to 10 and a molecular weight of the polyols of 2000 to 18 000 Da is effected.
摘要翻译：本发明涉及一种选自铅，铋，锌，锑，铟，金，镍，钴，钯，铂，铱，锇，铑，钌，铼，钒的金属纳米颗粒的制备方法，铬，锰，铌，钼，钨，钽，镉，银和/或铜，其特征在于相应的金属盐，相应的金属盐络合物，相应的金属氢氧化物和/或相应的金属氧化物的还原通过在多元醇中具有多个羟基的多元醇为1至10，多元醇的分子量为2000至18000Da。

8. 发明申请

US20100275950A1 METHOD AND DEVICE FOR THE TREATMENT OF SURFACES 审中-公开
标题翻译：用于处理表面的方法和装置
公开(公告)号：US20100275950A1
公开(公告)日：2010-11-04
申请号：US12741861
申请日：2008-12-09
申请人： Helmut Mack , Tobias Austermann , Martin Ebner , Michael Leck , Wolfgang Viöl
发明人： Helmut Mack , Tobias Austermann , Martin Ebner , Michael Leck , Wolfgang Viöl
IPC分类号： C03C23/00 , C23F1/08
CPC分类号： H05H1/2406 , H05H2001/2412 , H05H2245/125
摘要： The invention relates to a device and a method for the treatment of surfaces with a plasma produced under atmospheric pressure. The device according to the invention is formed as a portable handheld unit and comprises a plasma nozzle (16) for producing a plasma jet (18), which comprises a nozzle opening (17) and at least one electrode and counter-electrode pair (27, 28) arranged upstream of the nozzle opening, the effective electrode surfaces of which pair of electrodes each have a dielectric coating (29, 30), the electrode (27) and the counter-electrode (28) defining between them a working space (34) in which a working gas can be at least partially ionized by means of a dielectric barrier gas discharge, a high-voltage generator (19, 20), which is electrically connected to the electrode and counter-electrode pair (27, 28), a feeding means (15), which produces a gas flow of the working gas from a working gas source into the working space (34) and through the nozzle opening (17), the working gas source being ambient air, and a mains-independent energy source (12) for supplying the high-voltage generator (19, 20) and the feeding means (19).
摘要翻译：本发明涉及用于在大气压下产生的等离子体处理表面的装置和方法。根据本发明的装置形成为便携式手持单元，并且包括用于产生等离子体射流（18）的等离子体喷嘴（16），其包括喷嘴开口（17）和至少一个电极和对电极对（27 ，28）布置在所述喷嘴开口的上游，所述有效电极表面的一对电极各自具有电介质涂层（29,30），所述电极（27）和所述对电极（28）在它们之间限定工作空间 34），其中工作气体可以通过介电阻挡气体放电至少部分地离子化，电连接到电极和对电极对（27,28）的高压发生器（19,20）（15），其将工作气体从工作气体源产生气体流入工作空间（34）并通过喷嘴开口（17），工作气体源是环境空气，以及主干 - 用于供应高压发生器（19,20）的独立能量源（12）和进给装置（19）。

9. 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。

10. 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。

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