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1. 发明授权

US11345668B2 Formation of N-protected 3,6-bis-(4-aminobutyl)-2,5-diketopiperazine through a cyclic α-N-protected amino ester 有权
公开(公告)号：US11345668B2
公开(公告)日：2022-05-31
申请号：US17130729
申请日：2020-12-22
申请人： MannKind Corporation
发明人： John J. Freeman , Otto Phanstiel , William Elliot Bay , Kelly Sullivan Kraft
IPC分类号： C07D241/08 , C07D241/10 , C07D241/04
摘要： A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic α-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.

2. 发明授权

US09944609B2 Formation of N-protected bis-3,6-(4-aminobutyl)-2, 5-diketopiperazine through a cyclic alpha-N-protected amino ester 有权
公开(公告)号：US09944609B2
公开(公告)日：2018-04-17
申请号：US14942410
申请日：2015-11-16
申请人： MannKind Corporation
发明人： John J. Freeman , Otto Phanstiel , William Elliot Bay , Kelly Sullivan Kraft
IPC分类号： C07D241/08 , C07D241/10 , C07D241/04
CPC分类号： C07D241/08 , C07D241/04 , C07D241/10
摘要： A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic α-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.

3. 发明申请

US20170304279A1 PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY 审中-公开
公开(公告)号：US20170304279A1
公开(公告)日：2017-10-26
申请号：US15496318
申请日：2017-04-25
申请人： Curis, Inc.
发明人： Xiong Cai , Haixiao Zhai , Chengjung Lai , Chenggeng Qian
IPC分类号： A61K31/4365 , C07D241/10 , C07D213/30 , C07D495/04 , A61K31/166
CPC分类号： A61K31/4365 , A61K31/166 , C07D213/30 , C07D241/10 , C07D495/04
摘要： The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

4. 发明授权

US09371521B2 Substituted pyrazinedithiol reducing agents 有权
标题翻译：取代的吡嗪硫基还原剂
公开(公告)号：US09371521B2
公开(公告)日：2016-06-21
申请号：US14319972
申请日：2014-06-30
申请人： Wisconsin Alumni Research Foundation
发明人： Ronald Thaddeus Raines , John C. Lukesh, III
IPC分类号： C07D241/10 , C07D241/38 , C12N9/50 , C07D495/04 , C07D241/12 , C12N9/12
CPC分类号： C12N9/63 , C07D241/12 , C07D495/04 , C12N9/1223 , C12Y207/03002 , C12Y304/22002
摘要： Substituted dithiol pyrazine compounds useful as reducing agents in biologically relevant media having formula: where variables are defined herein and corresponding oxidized pyrazine dithianes. Reducing agents useful to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins, and other biological molecules. Reducing agents useful to regulate protein function in proteins in which a sulfhydryl group is associated with biological activity. Reducing agents useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. S-acylated dithiol pyrazine compounds, where R3 is an acyl group, are selectively activated as reducing agents by removal of the S-acyl groups enzymatically or chemically. Dithiol pyrazine reducing agents and corresponding S-acylated dithiol pyrazines, immobilized on surfaces or conjugated to other chemical species, are provided.
摘要翻译：可用作生物相关介质中还原剂的取代的二硫酚吡嗪化合物，其具有式：其中变量在本文中定义，并且相应的氧化吡嗪二噻烷。可用于减少二硫键的还原剂，特别是在蛋白质中，或防止形成二硫键，特别是在蛋白质和其它生物分子中。可用于调节蛋白质功能的还原剂，其中巯基与生物活性相关。有用的并适用于各种生物应用的还原剂，特别是作为研究和合成试剂。其中R3是酰基的S-酰化二硫酚吡嗪化合物通过酶或化学去除S-酰基来选择性活化作为还原剂。提供固定在表面上或与其它化学物质结合的二硫醇吡嗪还原剂和相应的S-酰化二硫酚吡嗪。

5. 发明授权

US09193722B2 Tri-cyclic pyrazolopyridine kinase inhibitors 有权
标题翻译：三环吡唑并吡啶激酶抑制剂
公开(公告)号：US09193722B2
公开(公告)日：2015-11-24
申请号：US13873591
申请日：2013-04-30
申请人： Vertex Pharmaceuticals Incorporated
发明人： Juan-Miguel Jimenez , John Studley , Ronald Knegtel , Luca Settimo , Christopher John Davis , Damien Fraysse , Philip N. Collier , Guy Brenchley , Dean Boyall , Andrew Miller , Heather Twin , Stephen Young
IPC分类号： C07D239/24 , C07D241/10 , A61K31/496 , A61K31/506 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/496 , A61K31/506 , C07D239/24 , C07D241/10 , C07D519/00
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. The compounds of the present invention are represented by the structure of formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。本发明还提供了制备本发明化合物的方法。本发明的化合物由式I的结构或其药学上可接受的盐表示，其中变量在本文中定义。

6. 发明授权

US08969351B2 Crystalline form of an inhibitor of MDM2/4 and p53 interaction 有权
公开(公告)号：US08969351B2
公开(公告)日：2015-03-03
申请号：US13298351
申请日：2011-11-17
申请人： Joerg Berghausen , Haixia Ren
发明人： Joerg Berghausen , Haixia Ren
IPC分类号： A61K31/497 , C07D241/10 , C07D401/12
CPC分类号： C07D401/12
摘要： A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively.

7. 发明授权

US08338431B2 Phosphodiesterase inhibitors 有权
标题翻译：磷酸二酯酶抑制剂
公开(公告)号：US08338431B2
公开(公告)日：2012-12-25
申请号：US12528649
申请日：2008-02-26
申请人： Ravindra Babu Bollu , Jakob Felding , Simon Feldbæk Nielsen , Jens Christian Højland Larsen
发明人： Ravindra Babu Bollu , Jakob Felding , Simon Feldbæk Nielsen , Jens Christian Højland Larsen
IPC分类号： A61K31/497 , A61K31/4433 , A61K31/382 , A61P17/00 , A61P35/00 , A61P29/00 , C07D213/02 , C07D491/10 , C07D241/10 , C07D335/04
CPC分类号： C07D495/10 , C07D491/10 , C07D493/10
摘要： The present invention relates to a compound according to formula I, wherein X, A, G, E, R1, R2, R3 are as shown herein; and pharmaceutically acceptable salts, hydrates, N-oxides or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
摘要翻译：本发明涉及式I化合物，其中X，A，G，E，R 1，R 2，R 3如本文所示; 及其药学上可接受的盐，水合物，N-氧化物或溶剂合物。本发明还涉及用于治疗的所述化合物，包含所述化合物的药物组合物，治疗疾病的方法，例如，所述化合物的皮肤病，以及所述化合物在制备药物中的用途。

8. 发明申请

US20120020915A1 Compounds and Methods for Treating Cancer and Diseases of the Central Nervous System 失效
标题翻译：治疗中枢神经系统癌症和疾病的化合物和方法
公开(公告)号：US20120020915A1
公开(公告)日：2012-01-26
申请号：US13006338
申请日：2011-01-13
申请人： Ajay Gupta , Hyman M. Schipper , Moulay Alaoui-Jamali , Walter A. Szarek , Kanji Nakatsu , Jason Z. Vlahakis
发明人： Ajay Gupta , Hyman M. Schipper , Moulay Alaoui-Jamali , Walter A. Szarek , Kanji Nakatsu , Jason Z. Vlahakis
IPC分类号： A61K31/4178 , A61K31/4164 , C07D233/54 , A61K31/4184 , C07D235/06 , A61K31/41 , C07D257/04 , A61K31/4439 , C07D405/14 , A61K31/4196 , C07D249/08 , A61K31/4965 , C07D241/10 , A61K31/496 , C07D403/04 , A61K39/395 , A61K39/00 , A61K48/00 , A61K31/7052 , A61K38/21 , A61K35/76 , A61K38/18 , A61K38/20 , A61K33/24 , A61K31/505 , A61P35/00 , C07D405/06
CPC分类号： C07D233/60 , C07D231/12 , C07D233/24 , C07D233/61 , C07D233/90 , C07D235/06 , C07D235/30 , C07D249/08 , C07D249/12 , C07D249/18 , C07D257/04 , C07D403/12 , C07D405/06 , C07D405/14 , C07D409/06
摘要： Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.
摘要翻译：公开了通式（I）的化合物：包含单独或与其它化学治疗剂组合的有效量的所述化合物的组合物，以及可用于治疗或预防癌症和抑制肿瘤组织生长的方法。这些化合物减弱与增加的血红素氧合酶活性相关的氧化损伤，并可以减少转化细胞中的细胞增殖。此外，所述的化合物和组合物可用作神经保护剂并用于治疗或预防神经变性疾病和中枢神经系统的其它疾病。

9. 发明授权

US08101749B2 Process for the preparation of onium salts with a tetrafluoroborate anion having a reduced halide content 失效
标题翻译：用具有降低的卤化物含量的四氟硼酸盐阴离子制备鎓盐的方法
公开(公告)号：US08101749B2
公开(公告)日：2012-01-24
申请号：US11721613
申请日：2005-11-18
申请人： Nikolai (Mykola) Ignatyev , Urs Welz-Biermann , Andriy Kucheryna , Helge Willner
发明人： Nikolai (Mykola) Ignatyev , Urs Welz-Biermann , Andriy Kucheryna , Helge Willner
IPC分类号： C07D207/04 , C07D231/06 , C07D231/10 , C07D233/04 , C07D233/54 , C07D249/04 , C07D249/08 , C07D263/30 , C07D277/20 , C07D215/02 , C07D217/02 , C07D211/80 , C07D211/06 , C07D209/04 , C07D237/06 , C07D239/24 , C07D241/10 , C07D241/36
CPC分类号： C07C209/12 , C07C381/12 , C07D213/20 , C07D213/74 , C07D233/54 , C07D295/023 , C07D295/037 , C07F9/5407 , C07C211/63
摘要： The invention relates to a method for producing onium salts with tetrafluoroborate anion by reacting an onium halide with an oxonium tetrafluoroborate, sulfonium tetrafluoroborate, or triphenylcarbonium tetrafluoroborate.
摘要翻译：本发明涉及通过卤化鎓与四氟硼酸鎓鎓，四氟硼酸锍或四氟硼酸三苯基碳鎓反应，与四氟硼酸根阴离子生成鎓盐的方法。

10. 发明申请

US20110288296A1 PRODUCTION AND USE OF ZINC AMIDES 有权
标题翻译：锌的生产和使用
公开(公告)号：US20110288296A1
公开(公告)日：2011-11-24
申请号：US13147339
申请日：2010-02-11
申请人： Paul Knochel , Marc Mosrin
发明人： Paul Knochel , Marc Mosrin
IPC分类号： C07D473/12 , C07D237/06 , C07D239/24 , C07D333/56 , C07D241/10 , C07C211/52 , C07D213/61 , C07D307/71 , C07F3/06 , C07D405/06
CPC分类号： C07F3/06 , C07D211/10 , C07D237/12 , C07D239/30 , C07D241/16 , C07D405/06 , C07F3/003
摘要： The application relates to a reagent of the general formula R1R2N—ZnY LiY (I) wherein R1, R2 are, independently, selected from H, substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or silyl derivatives thereof; and R1 and R2 together can be part of a cyclic or polymeric structure; and wherein at least one of R1 and R2 is other than H; Y is selected from the group consisting of F; Cl; Br; I; CN; SCN; NCO; Halon, wherein n=3 or 4 and Hal is selected from Cl, Br and I; NO3; BF4; PF6; H; a carboxylate of the general formula RXCO2; an alcoholate of the general formula ORX; a thiolate of the general formula SRX; RXP(O)O2; or SCORX; or SCSRX; OnSRx; wherein n=2 or 3; or NOn, wherein n=2 or 3; and a derivative thereof; wherein Rx is a substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or derivatives thereof, or H; or as adduct with a solvent; as well as to the preparation and use thereof.34
摘要翻译：本申请涉及通式为R 1 R 2 N-ZnY LiY（I）的试剂，其中R 1，R 2独立地选自H，具有直链，支链或环状的取代或未取代的一个或多个杂原子的取代或未取代的芳基或杂芳基烷基，烯基，炔基或甲硅烷基衍生物; R1和R2一起可以是环状或聚合物结构的一部分; 并且其中R 1和R 2中的至少一个不是H; Y选自F; Cl; Br; 一世; CN; SCN; NCO; Halon，其中n = 3或4，Hal选自Cl，Br和I; NO3; BF4; PF6; H; 通式为RXCO2的羧酸酯; 通式ORX的醇化物; 通式SRX的硫醇盐; RXP（O）O2; 或SCORX; 或SCSRX; OnSRx; 其中n = 2或3; 或NO n，其中n = 2或3; 及其衍生物; 其中Rx是取代或未取代的芳基或含有一个或多个杂原子的直链，支链或环状取代或未取代的烷基，烯基，炔基或衍生物，或H; 或作为与溶剂的加合物; 以及其制备和使用。 34

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