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公开(公告)号：US20190167800A1
公开(公告)日：2019-06-06
申请号：US16123209
申请日：2018-09-06
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Nair , Martin Maier , Laxman Eltepu
IPC分类号： A61K47/44 , C07D317/28 , A61K47/10 , C12N15/113 , C07C229/30 , C07D319/06 , C07D203/10 , A61K31/713 , A61K39/39 , A61K47/28 , C07C229/08 , C07C271/12 , C07C251/38 , C07D317/72 , A61K9/127 , C07C323/25 , C12N15/11 , A61K47/18 , C07D491/113 , C07C271/20 , C07C237/16 , A61K31/7088 , C07D405/12 , C07D317/46 , A61K47/20 , A61K39/00 , C07C251/78 , C07D317/44 , C07D491/056
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalky, ω-phosphoalkyl or ω-thiophosphoalkyl.
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公开(公告)号：US10117941B2
公开(公告)日：2018-11-06
申请号：US15603069
申请日：2017-05-23
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Jayaprakash K. Nair , Martin Maier , Laxman Eltepu
IPC分类号： A61K39/39 , C07D203/10 , A61K47/18 , A61K47/28 , A61K31/713 , A61K39/00 , A61K47/44 , C07C229/08 , C07C229/30 , C07D317/28 , C07D319/06 , C12N15/113 , A61K9/127 , C12N15/11 , A61K47/10 , A61K47/20 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , A61K31/7088 , C07D317/44 , C07D317/46 , C07D317/72 , C07D405/12 , C07D491/056 , C07D491/113
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalky, ω-phosphoalkyl or ω-thiophosphoalkyl.
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公开(公告)号：US10035754B2
公开(公告)日：2018-07-31
申请号：US15309070
申请日：2015-05-01
IPC分类号： C07C69/533 , C07C43/205 , C07C37/00 , C07D303/23 , C07C43/20 , C07C69/60 , C07C67/16 , C07C69/54 , C07D303/28 , C07C67/26 , C07C69/593 , C07D203/10 , C08F220/32 , C08F122/20 , C08F222/20 , C08F22/20
CPC分类号： C07C69/533 , C07C37/001 , C07C37/002 , C07C43/20 , C07C43/205 , C07C43/2055 , C07C67/16 , C07C67/26 , C07C69/54 , C07C69/593 , C07C69/60 , C07D203/10 , C07D303/23 , C07D303/28 , C08F22/20 , C08F122/20 , C08F220/32 , C08F222/20 , C08F2220/325 , C08F2222/205 , C08F2500/17 , C07C39/19
摘要： Methacrylated cardanol glycidyl ethers, diglycidyl ethers, intermediates and derivatives thereof are described herein. Compositions and polymers made with such compounds as well as methods of preparation thereof are also described. For example, compounds of Formulas: wherein n, R1, R2, R3, R4, R5, and R6 can each represent various different entities are described in the present disclosure.
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公开(公告)号：US09707292B2
公开(公告)日：2017-07-18
申请号：US14884489
申请日：2015-10-15
发明人： Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev , Laxman Eltepu , Steven Ansell , Jianxin Chen
IPC分类号： A61K39/39 , A61K9/127 , C07C229/08 , A61K31/713 , C07D203/10 , C12N15/113 , C07C229/30 , C07D317/28 , C07D319/06 , A61K39/00 , C12N15/11 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25
CPC分类号： A61K47/44 , A61K9/1272 , A61K31/7088 , A61K31/713 , A61K39/00 , A61K39/39 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , A61K2039/55555 , A61K2039/55561 , C07C229/08 , C07C229/30 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , C07D203/10 , C07D317/28 , C07D317/44 , C07D317/46 , C07D317/72 , C07D319/06 , C07D405/12 , C07D491/056 , C07D491/113 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/3515 , C12N2320/32 , Y02A50/464
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure wherein: R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40 K), optionally substituted mPEG (mw 120-40 K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).
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公开(公告)号：US20160199485A1
公开(公告)日：2016-07-14
申请号：US14884489
申请日：2015-10-15
发明人： Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev , Laxman Eltepu , Steven Ansell , Jianxin Chen
IPC分类号： A61K39/39 , A61K31/713 , C12N15/113 , C07D317/28 , C07D203/10 , C07C229/30 , C07C229/08 , C07D319/06
CPC分类号： A61K47/44 , A61K9/1272 , A61K31/7088 , A61K31/713 , A61K39/00 , A61K39/39 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , A61K2039/55555 , A61K2039/55561 , C07C229/08 , C07C229/30 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , C07D203/10 , C07D317/28 , C07D317/44 , C07D317/46 , C07D317/72 , C07D319/06 , C07D405/12 , C07D491/056 , C07D491/113 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/3515 , C12N2320/32 , Y02A50/464
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure wherein: R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40 K), optionally substituted mPEG (mw 120-40 K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).
摘要翻译： 本发明提供有利地用于脂质颗粒以用于体内递送治疗剂至细胞的脂质。 特别地，本发明提供了具有以下结构的脂质，其中：R1和R2各自独立地为每次出现任选取代的C 10 -C 30烷基，任选取代的C 10 -C 30烯基，任选取代的C 10 -C 30炔基，任选取代的C 10 -C 30酰基， 或 - 连接子 - 配体; R 3为H，任选取代的C 1 -C 10烷基，任选取代的C 2 -C 10烯基，任选取代的C 2 -C 10炔基，烷基硫代烷基磷酸酯，烷基硫代磷酸酯，烷基二硫代磷酸酯，烷基膦酸酯，烷基胺，羟基烷基，ω-氨基烷基，ω-（取代的）氨基烷基， ω-磷酸烷基酯，ω-硫代磷酰基烷基酯，任选取代的聚乙二醇（PEG，mw 100-40K），任选取代的mPEG（mw 120-40K），杂芳基，杂环或连接体 - 配体; 并且E是C（O）O或OC（O）。
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6.发明授权公开(公告)号：US09365510B2
公开(公告)日：2016-06-14
申请号：US13863849
申请日：2013-04-16
IPC分类号： C07C41/00 , C07C43/02 , A61K31/075 , C07D203/10 , A61K31/396 , A61K45/06
CPC分类号： C07D203/10 , A61K31/396 , A61K45/06 , A61K2300/00
摘要： Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R1, R2, R3, R4, M1, M2, X, L1, L2, J1, J2, a1, a2, b1 and b2 are as defined herein, and wherein at least one of M2 or L2 is a moiety comprising an aziridine, acrylamide or sulfonate functional group, are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.
摘要翻译： 具有式I结构的化合物或其药学上可接受的盐，互变异构体或立体异构体，其中R，R1，R2，R3，R4，M1，M2，X，L1，L2，J1，J2，a1，a2，b1和 b2如本文所定义，并且其中M2或L2中的至少一个是包含氮丙啶，丙烯酰胺或磺酸盐官能团的部分。 还提供了这些化合物用于治疗各种适应症的用途，包括前列腺癌以及涉及这些化合物的治疗方法。
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7.发明授权Process for preparing 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole 失效制备6-苯基-2,3,5,6-四氢咪唑并[8,2,1-b {9噻唑
公开(公告)号：US4059588A
公开(公告)日：1977-11-22
申请号：US240826
申请日：1972-04-03
申请人： Asbjorn Baklien , Jan Kolm
发明人： Asbjorn Baklien , Jan Kolm
IPC分类号： C07D203/08 , C07D203/10 , C07D277/18 , C07D513/04
CPC分类号： C07D203/08 , C07D203/10 , C07D277/18
摘要： This disclosure relates to a process for the manufacture of compounds of the formula ##STR1## which comprises ring-closing a compound of the formula ##STR2## wherein the variables are as defined infra.
摘要翻译： 本公开涉及制备式“IMAGE”的化合物的方法，其包括闭合式IMA的化合物，其中变量如下文所定义。
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公开(公告)号：US4025503A
公开(公告)日：1977-05-24
申请号：US486216
申请日：1974-07-05
申请人： Felix Miksovsky , Rolf Fikentscher
发明人： Felix Miksovsky , Rolf Fikentscher
IPC分类号： C07D203/10 , C07D203/08 , C07D203/18
CPC分类号： C07D203/08
摘要： Aziridinecarboxylic acid esters are prepared by trans-esterification of aziridinecarboxylic acid methyl, ethyl or propyl esters in the presence of a high-boiling paraffin hydrocarbon and optionally of an amine.
摘要翻译： 通过在高沸点链烷烃和任选的胺存在下，通过偶氮二羧酸甲基，乙基或丙基酯的酯交换来制备氮杂环丁烷羧酸酯。
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公开(公告)号：US3759937A
公开(公告)日：1973-09-18
申请号：US3759937D
申请日：1966-07-14
申请人： ICI AUSTRALIA LTD
IPC分类号： C07D203/08 , C07D203/10 , C07D277/18 , C07D91/18
CPC分类号： C07D203/08 , C07D203/10 , C07D277/18
摘要： Process for preparing certain 2-imino-thiazolidines which comprises reacting certain aziridines with thiourea or thiocyanic acid.
摘要翻译： 制备某些2-亚氨基 - 噻唑烷的方法，包括使某些氮丙啶与硫脲或硫氰酸反应。
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公开(公告)号：US3583977A
公开(公告)日：1971-06-08
申请号：US3583977D
申请日：1968-06-18
申请人： GEN TIRE & RUBBER CO
发明人： UELZMANN HEINZ
IPC分类号： C07D203/10 , C08G18/10 , C08G18/50 , C08G18/64 , C08G59/10 , C08G59/50 , C08G65/22 , C08G65/26 , C08G73/02 , C08K5/3412 , C08L63/00 , C08L101/08 , C07D23/02 , C07D23/06
CPC分类号： C08L63/00 , C07D203/10 , C08G18/10 , C08G18/5057 , C08G18/6423 , C08G59/10 , C08G59/5066 , C08G65/22 , C08G65/263 , C08G73/0206 , C08G73/0226 , C08K5/3412 , C08L101/08 , Y10S516/06 , C08G18/3293 , C08L2666/20 , C08L2666/02
摘要： AZIRIDINYL COMPOUNDS OF THE FORMULA:
AZ-CH2-CH(-O-R'')-CH2-O-R
WHEREIN
AZ IS AN AZIRIDINO GROUP, R IS HYDROGEN, OR AN ALKENYL, ALKENYL CYCLO ALIPHATIC, ALKENYLARYL, HYDROXYPOLYOXYALKYLENE, OR A HYDROXY POLYOXYALKYLENE (OXYALKYENYL) GROUP, AND R'' IS HYDROGEN, OR A HYDROXYPOLYOXALKYLENE, OR A HYDROXY POLYOXYALKYLENE (OXYALKENYL) GROUP
ARE PREPARED ACCORDING TO THE REACTION ILLUSTRATED BY THE FOLLOWING TYPICAL PREPARATION:
2-(HO-CH2-)-OXIRANE + AZIRIDINE ---->
1-(HO-CH2-CH(-OH)-CH2-)-AZIRIDINE
THE NEW COMPOUNDS CAN BE USED IN FORMING ADHESIVES, COATINGS FOR FABRICS, FOAMS AND SPONGES, BINDERS, EMULSIFIERS AND SURFACTANTS AND AS CROSS-LINKERS FOR POLYMERS.
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