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82. 发明申请

WO2009042013A1 PROCESS FOR THE SYNTHESIS OF E1 ACTIVATING ENZYME INHIBITORS 审中-公开
标题翻译：合成E1活化酶抑制剂的方法
公开(公告)号：WO2009042013A1
公开(公告)日：2009-04-02
申请号：PCT/US2008/009338
申请日：2008-08-01
申请人： MILLENNIUM PHARMACEUTICALS, INC. , ARMITAGE, Ian , ELLIOT, Eric, L. , LANGSTON, Marianne , LANGSTON, Steven, P. , MCCUBBIN, Quentin, J. , MIZUTANI, Hirotake , STIRLING, Matthew , ZHU, Lei
发明人： ARMITAGE, Ian , ELLIOT, Eric, L. , LANGSTON, Marianne , LANGSTON, Steven, P. , MCCUBBIN, Quentin, J. , MIZUTANI, Hirotake , STIRLING, Matthew , ZHU, Lei
IPC分类号： C07D487/04 , C07C215/44 , C07C217/52 , C07C219/24
CPC分类号： C07D487/04 , C07C215/44 , C07C217/52 , C07C219/24 , C07C315/04 , C07C317/50 , C07C2601/08 , C07D211/96 , C07D213/89 , C07D241/50 , C07D295/22 , C07D305/08 , C07D471/08 , Y02P20/55
摘要： The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((1S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2/3-d]pyrimidin-7- yl}cyclopentyl)methyl sulfamates, which are El activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with El activity.
摘要翻译：本发明提供合成4-取代的（（1S，2S，4R）-2-羟基-4- {7H-吡咯并[2,3-d]嘧啶-7-基}环戊基）甲基的方法和合成中间体氨基磺酸盐，其是E1活化酶抑制剂，并且可用于治疗细胞增殖，特别是癌症和与El活性相关的其它病症的病症。

83. 发明申请

WO2008149053A1 BICYCL0 [2. 2. 1] HE PT- 2-YLAMINE DERIVATES AND THEIR USE 审中-公开
标题翻译： BICYCL0 [2。 2. 1] PT-2-氨基衍生物及其用途
公开(公告)号：WO2008149053A1
公开(公告)日：2008-12-11
申请号：PCT/GB2007/002130
申请日：2007-06-08
申请人： ARGENTA DISCOVERY LTD. , ASTRAZENECA AB , FINCH, Harry , JENNINGS, Andrew, Stephan, Robert , van NIEL, Monique, Bodil , RAY, Nicholas, Charles , SMITH, Philip
发明人： FINCH, Harry , JENNINGS, Andrew, Stephan, Robert , van NIEL, Monique, Bodil , RAY, Nicholas, Charles , SMITH, Philip
IPC分类号： C07C211/38 , C07C211/63 , C07D311/84 , C07D311/86 , C07D333/24 , C07D409/12 , A61K31/216 , A61K31/352 , A61K31/381 , A61P1/00 , A61P9/00 , A61P11/00 , A61P13/00 , A61P37/00
CPC分类号： C07C219/24 , C07C2601/14 , C07C2602/42 , C07C2603/18 , C07D311/82 , C07D333/24 , C07D409/06 , C07D409/14
摘要： A named compound of formula (I): having M3 receptor antagonist activity; a composition comprising such a compound; the use of such a compound in therapy (such as asthma or COPD); and a method of treating a patient with such a compound.
摘要翻译：命名的式（I）化合物：具有M3受体拮抗剂活性; 包含这种化合物的组合物; 在治疗（如哮喘或COPD）中使用这种化合物; 以及用这种化合物治疗患者的方法。

84. 发明申请

WO2007017670A1 BICYCLO[2.2.]HEPT-7-YLAMINE DERIVATIVES AND THEIR USES 审中-公开
标题翻译： BICYCLO [2.2。] HEPT-7-YLAMINE DERIVATIVES及其用途
公开(公告)号：WO2007017670A1
公开(公告)日：2007-02-15
申请号：PCT/GB2006/002957
申请日：2006-08-08
申请人： ARGENTA DISCOVERY LTD. , FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , van NEIL, Monique, Bodil , JENNINGS, Andrew, Stephen, Robert
发明人： FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , van NEIL, Monique, Bodil , JENNINGS, Andrew, Stephen, Robert
IPC分类号： C07C271/38 , C07C219/24 , C07C233/41 , C07D211/14 , C07D311/84 , C07D311/86 , C07D333/16 , C07D409/14 , A61K31/27 , A61K31/381 , A61K31/451 , A61K31/221 , A61K31/352 , A61K31/4704 , A61P29/00
CPC分类号： C07C271/38 , C07C219/24 , C07C235/36 , C07C2602/42 , C07D211/14 , C07D311/84 , C07D311/86 , C07D333/16 , C07D409/06 , C07D409/14
摘要： Compounds of formula (I) have muscarinic M3 receptor modulating activity; Formula(I) wherein A is an oxygen atom or group -N(R 12 )-;(i) R 1 is C 1 -C 6 -alkyl or a hydrogen atom; and R 2 is a hydrogen atom or a group -R 5 , -Z-Y-R 5 -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 ; -Z-NR 9 -CO-R 5 ; or -Z-CO 2 H; and R 3 is a lone pair,or C 1 -C 6 -aIkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R 1 and R 3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R 2 is a hydrogen atom; or a group -R 5 , -Z-Y-R 5 , -Z-NR 9 R 10 , -Z-CO-NR 9 R 10 , -Z-NR 9 -CO-R 5 , or -Z-CO 2 H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R 1 and R 2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group -Y-R 5 , -Z-Y-R 5 , -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 ; -Z-NR 9 -CO-R 5 ; or -Z-CO 2 H and R 3 is a lone pair, or C 1 -C 6 -alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; R 4 is a group of formula (a), (b), (c) or (d); is an C 1 -C 6 -alkyl, aryl, aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C 1 -C 8 -alkyl)-, heteroaryl(C 1- C 8 -alkyl)-, cycloalkyl or heterocycloalkyl group, and the remaining variables are as defined in the specification.
摘要翻译：式（I）化合物具有毒蕈碱M3受体调节活性; 式（I）其中A是氧原子或基团-N（R 12） - ;（i）R 1是C 1 - C 6 - 烷基或氢原子; R 2是氢原子或基团-R 5，-ZYR 5 -Z-NR 9， [R ^{10 ; -Z-CO-NR ^{9 - [R ^{10 ; -Z-NR ^{9 -CO-R ^{5 ; 或-Z-CO 2 H; 且R 3是孤对的或C 1 -C 6 - 烷基，在这种情况下，其所连接的氮原子是季氮并带正电荷; 或（ii）R 1和R 3与它们所连接的氮一起形成杂环烷基环，R 2是氢原子; 或基团-R 5，-ZYR 5，-Z-NR 9，R 10，-Z- CO-NR 9 R 10，-Z-NR 9 -CO-R 5，或-Z- CO 2 H，其中附着的氮原子是季氮并带正电荷; 或（iii）R 1和R 2与它们所连接的氮一起形成杂环烷基环，所述环被基团-YR 5 9，-ZYR 5，-Z-NR 9，R 10， -Z-CO-NR ^{9 - [R ^{10 ; -Z-NR ^{9 -CO-R ^{5 ; 或-Z-CO 2 H和R 3是孤对的或C 1 -C 6 - 烷基，在这种情况下，其所连接的氮原子是季氮并携带正电荷; R 4是式（a），（b），（c）或（d）的基团。是C 1 -C 6 - 烷基，芳基，芳基 - 稠合环烷基，芳基 - 稠合 - 杂环烷基，杂芳基，芳基（C 1〜 C 1 -C 8 - 烷基） - ，杂芳基（C 1 -C 8 - 烷基） - ，环烷基或杂环烷基，剩余的变量如规范中所定义。}}}}}}}}}

85. 发明申请

WO00061541A3 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO00061541A3
公开(公告)日：2001-09-27
申请号：PCT/EP2000/003239
申请日：2000-04-11
IPC分类号： C07D499/64 , A61K31/21 , A61K31/225 , A61K31/366 , A61K31/4172 , A61K31/4178 , A61K31/426 , A61K31/431 , A61K31/4439 , A61K31/473 , A61K31/663 , A61K31/704 , A61K38/00 , A61P1/00 , A61P1/04 , A61P9/00 , A61P9/02 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/10 , A61P15/08 , A61P15/10 , A61P17/00 , A61P17/08 , A61P19/04 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P39/06 , A61P43/00 , C07C211/42 , C07C211/49 , C07C219/06 , C07C219/22 , C07C219/24 , C07C271/28 , C07D219/10 , C07D233/64 , C07D277/06 , C07D277/14 , C07D309/30 , C07D401/12 , C07D405/14 , C07D417/06 , C07D471/04 , C07D473/18 , C07D495/04 , C07D499/68 , C07F9/38 , C07F9/40 , C07H15/252 , C07K5/02 , C07D233/54 , C07D499/00
CPC分类号： C07H15/252 , C07C219/06 , C07C219/22 , C07C219/24 , C07C271/28 , C07C2601/14 , C07F9/3873 , C07K5/0222
摘要： Compounds or their salts having general formulas (I) and (II) wherein: s = is an integer equal to 1 or 2, preferably s = 2; b0 = 0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.
摘要翻译：具有通式（I）和（II）的化合物或其盐，其中：s =等于1或2，优选s = 2的整数; b0 = 0或1; A是一种药物的基础，并且符合说明书中报道的药理学试验，C和C1是两个二价基团。基团B和B1的前体符合说明书中报道的药理学试验。

86. 发明申请

WO00069806A1 METHOD FOR PRODUCING CHIRAL AMINES 审中-公开
标题翻译：用于生产手性胺
公开(公告)号：WO00069806A1
公开(公告)日：2000-11-23
申请号：PCT/EP2000/004149
申请日：2000-05-10
IPC分类号： C07C213/02 , C07C219/24
CPC分类号： C07C213/02 , C07B2200/07 , C07C2601/04 , C07C219/24
摘要： The invention relates to amines of general formula (I) or to the mirror image thereof, wherein R means hydrogen, C1-6-alkyl, aryl-C1-4-alkyl or acyl. The inventive amines are produced by means of steteroselective hydrogenation of the corresponding oximes in the presence of a platinum metal-phosphine-complex with homogeneous catalysis. The amines which can be produced by the invention are intermediate products in the synthesis of antiviral active agents such as lobucavir for instance.
摘要翻译：通式（I）或其镜像，其中R <1>为氢，C 1-6 - 烷基，芳基-C 1-4 - 烷基或酰基，由相应的肟的立体选择性氢化在铂金属 - 膦的存在下制备的胺通过均相催化生产复杂。根据胺是抗病毒剂如洛布卡韦的合成中的中间体，本发明可以制备。

87. 发明申请

WO1995029148A1 O-ACYL-4-PHENYL-CYCLOHEXANOLS, THEIR SALTS, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE, AS WELL AS A METHOD OF PREPARING THEM 审中-公开
标题翻译： O-酰基-4-苯基 - 环己醇，它们的盐，药物含有它们的使用和用于生产
公开(公告)号：WO1995029148A1
公开(公告)日：1995-11-02
申请号：PCT/EP1994001276
申请日：1994-04-25
申请人： DR. KARL THOMAE GMBH , WOITUN, Eberhard , MAIER, Roland , MÜLLER, Peter , HURNAUS, Rudolf , MARK, Michael , EISELE, Bernhard , BUDZINSKI, Ralph-Michael , HALLERMAYER, Gerhard
发明人： DR. KARL THOMAE GMBH
IPC分类号： C07C219/24
CPC分类号： C07D295/096 , C07C219/24 , C07C237/06 , C07C2601/14
摘要： The invention concerns O-acyl-4-phenyl-cyclohexanols of the general formula (I) in which n stands for the numbers 0 or 1, m stands for the numbers 1 or 2, p stands for the numbers 0 or 1, R and R each stand for hydrogen, lower alkyl, alkenyl or alkinyl, these groups possibly being further substituted or, together with the intermediate nitrogen atom, forming 5 to 7-member saturated, monocyclic, heterocyclic rings which may possibly be further interrupted by an oxygen or sulphur atom or an imino group, R , R , R and R stand for hydrogen or lower alkyl, R additionally also stands for lower alkoxy, R stands for hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A stands for a chemical bond or alkyl, alkenyl or alkinyl having up to 17 carbon atoms. The invention further concerns a method of preparing said compounds, medicaments containing said compounds and the use of said medicaments which are effective in cholesterol biosynthesis. The anti-hypercholesterolemic substances are used for the treatment and prevention of atherosclerosis and inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase.
摘要翻译：描述了O-酰基-4-苯基 - 环己醇的通式（I），其中n为数字0或1，m是1或2，p个数字0或1，R <1>和R <2> 形成各氢，低级烷基，烯基或炔基，这些基团任选地可以与处于中间的氮原子上被取代，或者一起表示5至7元饱和的单环，杂环还任选被氧或硫原子或亚氨基可以被中断，R <3>，R <4>，R <5>和R <6>是氢或低级烷基，R <5>除，低级烷氧基，R <7>为氢，环烷基，苯基或取代的苯基基，萘基，四氢萘基，噻吩基，呋喃基或吡啶基，且a是最多17个C原子的化学键或烷基，烯基或炔基，还涉及它们的制备方法，含有这些化合物的药物组合物，并且其在使用这些药物的胆囊从事甾醇生物合成。用于治疗动脉粥样硬化和预防的物质antihypercholesterolämischen，它可以抑制酶2,3-环氧角鲨烯 - 羊毛甾醇环化酶。

88. 发明申请

US20170348324A1 DERIVATIVES OF BETULIN 审中-公开
公开(公告)号：US20170348324A1
公开(公告)日：2017-12-07
申请号：US15685150
申请日：2017-08-24
申请人： GLAXOSMITHKLINE LLC
发明人： Mark Andrew HATCHER , Brian Alvin Johns , Michael Tolar Martin , Elie Amine Tabet , Jun Tang
IPC分类号： A61K31/568 , C07J53/00 , A61K31/222 , A61K31/225 , A61K31/397 , C07D498/14 , C07D413/06 , C07D265/32 , C07D265/30 , C07D243/08 , C07D239/48 , C07D239/26 , C07D217/04 , C07D213/40 , C07D207/09 , C07D205/04 , C07C233/33 , C07C225/14 , C07C219/24 , C07C219/06 , C07C217/26 , C07C215/08 , C07C211/38 , C07C211/10 , C07C211/04 , C07C69/34 , A61K45/06 , A61K31/58 , A61K31/551 , A61K31/54 , A61K31/5375 , A61K31/506 , A61K31/505 , A61K31/4985 , A61K31/495 , A61K31/472 , A61K31/44 , A61K31/40 , C07J63/00 , A61K31/56 , C07C2601/14 , C07C2603/52 , C07C2601/02
CPC分类号： A61K31/568 , A61K31/222 , A61K31/225 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/472 , A61K31/495 , A61K31/4985 , A61K31/505 , A61K31/506 , A61K31/5375 , A61K31/54 , A61K31/551 , A61K31/56 , A61K31/58 , A61K45/06 , C07C69/34 , C07C211/04 , C07C211/10 , C07C211/38 , C07C215/08 , C07C217/26 , C07C219/06 , C07C219/24 , C07C225/14 , C07C233/33 , C07C2601/02 , C07C2601/14 , C07C2603/52 , C07D205/04 , C07D207/09 , C07D213/40 , C07D217/04 , C07D239/26 , C07D239/48 , C07D243/08 , C07D265/30 , C07D265/32 , C07D413/06 , C07D498/14 , C07J53/002 , C07J63/008
摘要： The present invention relates to compounds characterized by having a structure according to the following Formula I: , or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.

89. 发明授权

US09802938B2 Sulfamoylating reagents 有权
公开(公告)号：US09802938B2
公开(公告)日：2017-10-31
申请号：US14552883
申请日：2014-11-25
申请人： Millennium Pharmaceuticals, Inc.
发明人： Ian Armitage , Eric L. Elliott , Marianne Langston , Steven P. Langston , Quentin J. McCubbin , Hiro Mizutani , Matthew Stirling , Lei Zhu
IPC分类号： C07D487/04 , C07D487/08 , C07D471/08 , C07D241/04 , C07D265/30 , C07C315/04 , C07C317/50 , C07C215/44 , C07C217/52 , C07C219/24 , C07D211/96 , C07D213/89 , C07D241/50 , C07D295/22 , C07D305/08 , C07C305/08
CPC分类号： C07D487/04 , C07C215/44 , C07C217/52 , C07C219/24 , C07C315/04 , C07C317/50 , C07C2601/08 , C07D211/96 , C07D213/89 , C07D241/50 , C07D295/22 , C07D305/08 , C07D471/08 , Y02P20/55
摘要： The present invention provides sulfamoylating reagents of formula RuN−—S(O)2X+, wherein X is a cyclic tertiary amine or a nitrogen-containing heteroaryl and Ru is an amine protecting group or hydrogen.

90. 发明申请

US20170275241A1 TRANSESTERIFICATION REACTION BY MEANS OF IRON CATALYST 审中-公开
公开(公告)号：US20170275241A1
公开(公告)日：2017-09-28
申请号：US15129313
申请日：2015-02-03
申请人： KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION
发明人： Takashi OHSHIMA , Ryo YAZAKI , Chika FUJIMOTO , Rikiya HORIKAWA
IPC分类号： C07C213/06 , C07C269/06 , C07C231/02 , C07B41/12 , B01J23/745 , C07C67/03
CPC分类号： C07C213/06 , B01J23/745 , B01J31/22 , C07B41/12 , C07B2200/07 , C07C67/03 , C07C67/08 , C07C231/02 , C07C269/06 , C07C2601/14 , C07C2603/74 , C07D211/22 , C07D211/46 , C07C69/78 , C07C69/612 , C07C69/618 , C07C69/34 , C07C233/65 , C07C233/75 , C07C233/11 , C07C271/22 , C07C219/14 , C07C219/24 , C07C219/34
摘要： Provided is a catalyst for transesterification reactions, which contains an iron salen complex. Also provided is a method for producing an ester compound, which is characterized by carrying out a transesterification reaction between a starting material ester and a starting material alcohol with use of the catalyst.

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