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61. 发明申请

US20140302604A1 RADICAL INHIBITOR 有权
标题翻译：放射性抑制剂
公开(公告)号：US20140302604A1
公开(公告)日：2014-10-09
申请号：US14354379
申请日：2012-09-27
申请人： Yoshihiro ISHIKAWA , IHI Corporation
发明人： Yoshihiro Ishikawa , Haruki Eguchi
IPC分类号： C09K15/20
CPC分类号： C09K15/20 , A61K8/49 , A61K2800/522 , A61Q17/04 , C07C225/14 , C07C251/08 , C07C251/10 , C07D211/58 , C07D307/52 , C07D307/58 , C07F15/025 , C09K15/326
摘要： A new radical inhibitor, a composition containing the new radical inhibitor, and a radical generation inhibition method using the new radical inhibitor are provided. A radical inhibitor according to the present invention contains a salen complex compound of a bivalent metal.
摘要翻译：提供了一种新的自由基抑制剂，含有新的自由基抑制剂的组合物和使用新的自由基抑制剂的自由基产生抑制方法。根据本发明的自由基抑制剂含有二价金属的salen络合物。

62. 发明申请

US20130184263A1 Derivatives of Betulin 有权
公开(公告)号：US20130184263A1
公开(公告)日：2013-07-18
申请号：US13714627
申请日：2012-12-14
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： C07C69/34 , C07D217/04 , A61K31/472 , A61K31/495 , C07D265/32 , A61K45/06 , C07D243/08 , A61K31/551 , A61K31/54 , C07D239/26 , A61K31/505 , A61K31/225 , A61K31/5375
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.

63. 发明申请

US20120302534A1 DERIVATIVES OF BETULIN 审中-公开
标题翻译：贝母的衍生物
公开(公告)号：US20120302534A1
公开(公告)日：2012-11-29
申请号：US13577452
申请日：2011-02-09
申请人： Daxin Gao , Nianhe Han , Zhimin Jin , Fangxian Ning , Jun Tang , Yongyong Wu , Heping Yang
发明人： Daxin Gao , Nianhe Han , Zhimin Jin , Fangxian Ning , Jun Tang , Yongyong Wu , Heping Yang
IPC分类号： A61K31/568 , A61P31/18 , A61K31/58 , C07J53/00
CPC分类号： A61K31/50 , A61K31/56 , C07C225/14 , C07C233/76 , C07C235/78 , C07C275/30 , C07C311/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/52 , C07D205/04 , C07D213/40 , C07D231/12 , C07D295/185 , C07D295/26 , C07D333/20
摘要： The present invention relates to a compound characterized by the following Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X, and Y are as described herein. Compounds of the present invention are useful for the treatment of HIV-1.
摘要翻译：本发明涉及以下式I表征的化合物或其药学上可接受的盐，其中R 1，R 2，R 3，X和Y如本文所述。本发明的化合物可用于治疗HIV-1。

64. 再颁专利

USRE42802E1 Phenylethylamines and condensed rings variants as prodrugs of catecholamines, and their use 失效
标题翻译：苯乙胺和稠环变体作为儿茶酚胺的前药，及其用途
公开(公告)号：USRE42802E1
公开(公告)日：2011-10-04
申请号：US11790465
申请日：2007-04-25
申请人： Hâkan Vilheim Wikström , Durk Dijkstra , Bastiaan Johan Venhuis
发明人： Hâkan Vilheim Wikström , Durk Dijkstra , Bastiaan Johan Venhuis
IPC分类号： A61K31/45 , C07D221/06 , C07D219/06
CPC分类号： C07D221/14 , C07C225/14 , C07C225/20 , C07C2601/16 , C07C2603/26 , C07D211/32 , C07D211/70 , C07D221/08 , C07D221/10 , C07D221/18
摘要： Compounds of the general formula I wherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings B, C and E being aliphatic whereas ring D may be aliphatic or aromatic/heteroaromatic, and wherein X is —(CH2)m—, in which m is an integer 1-3, to form a ring E or, when E is absent, a group R1 bound to the nitrogen atom, wherein R1 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 3 carbon atoms, cycloalkyl(alkyl) groups of 3 to 5 carbon atoms (i.e. including cyclopropyl, cyclopropylmethyl, cyclobutyl and cyclobutylmethyl) and wherein Y is —(CH2)n—, in which n is an integer 1-3, to form a ring C or when C is absent, a group R2 bound to the nitrogen atom, wherein R2 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 7 carbon atoms, cycloalkyl(alkyl) groups of 3 to 7 carbon atoms, alkenyl or alkylnyl groups of 3 to 6 carbon atoms, arylalkyl, heteroarylalkyl having 1 to 3 carbon atoms in the alkyl moiety, whilst the aryl/heteroaryl nucleus may be substituted, provided that when rings B, C, D and E are absent NR1R2 is different from dimethylamino, N-methyl-N-ethylamino, N-methyl-N-propynyl-amino, N-methyl-N-propylamino and N-hydroxipropyl-N-methylamino, and salts thereof with pharmaceutically acceptable acids or bases are disclosed as well as the use of such compounds for the manufacturing of pharmaceutical compositions for the treatment of Parkinson's disease, psychoses, Huntington's disease, impotence, renal failure, heart failure or hypertension, such pharmaceutical compositions and methods of treating Parkinson's disease and schizophrenia.
摘要翻译：其中环B，C，D和E可以存在或不存在，并且当存在时与A组合为A + C，A + E，A + B + C，A + B + D， A + B + E，A + C + E，A + B + C + D或A + B + C + D + E，环B，C和E为脂族环，而环D可为脂族或芳族/杂芳族，其中X是 - （CH 2）m - ，其中m是整数1-3，以形成环E，或当E不存在时，与氮原子结合的基团R1，其中R1选自具有1-3个碳原子的氢原子，烷基或卤代烷基，3至5个碳原子的环烷基（烷基）（即包括环丙基，环丙基甲基，环丁基和环丁基甲基），其中Y是 - （CH 2）n - ，其中 n为整数1-3，形成环C或当不存在C时，与氮原子结合的基团R 2选自氢原子，碳原子数为1〜7的烷基或卤代烷基 3〜7个碳原子的原子，环烷基（烷基），烯基或烷基 3至6个碳原子，芳基烷基，烷基部分具有1至3个碳原子的杂芳基烷基，而芳基/杂芳基核可以被取代，条件是当环B，C，D和E不存在时，NR 1 R 2不同于二甲基氨基， N-甲基-N-乙基氨基，N-甲基-N-丙炔基 - 氨基，N-甲基-N-丙基氨基和N-羟基丙基-N-甲基氨基及其与药学上可接受的酸或碱的盐以及其用途的这种化合物用于制备用于治疗帕金森病，精神病，亨廷顿氏病，阳ence，肾衰竭，心力衰竭或高血压的药物组合物，用于治疗帕金森病和精神分裂症的药物组合物和方法。

65. 发明授权

US07416868B2 Polyene polyketides, processes for their production and their use as a pharmaceutical 失效
标题翻译：聚烯烃聚合物，其生产方法及其作为药物的用途
公开(公告)号：US07416868B2
公开(公告)日：2008-08-26
申请号：US10760494
申请日：2004-01-21
申请人： Emmanuel Zazopoulos , Chris M. Farnet
发明人： Emmanuel Zazopoulos , Chris M. Farnet
IPC分类号： C12N9/00
CPC分类号： C07H15/203 , C07C215/24 , C07C225/14 , C07C235/28 , C07C237/16 , C07C279/22 , C07C305/14 , C07C2601/10 , C07C2601/14 , C07H15/10 , C07H15/18 , C07H15/26 , C12P7/42 , C12P11/00 , C12P13/001 , C12P13/02 , C12P19/44 , C12R1/465 , Y10S435/886
摘要： This invention relates to a new class of polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for obtaining the compounds. One method of obtaining these compounds is by cultivation of novel strains of Streptomyces aizunensis; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to the novel strains of Streptomyces aizunensis used to produce these compounds, to the use of these compounds and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of fungal cell growth and cancer cell growth. The invention also relates to pharmaceutical compositions comprising these novel polyketides or a pharmaceutically acceptable salts or derivatives thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of these novel polyketides.
摘要翻译：本发明涉及新类型的多烯聚酮化合物，其药学上可接受的盐和衍生物，以及获得化合物的方法。获得这些化合物的一种方法是通过培养新的链霉菌链霉菌菌株; 另一种方法涉及在转化的宿主细胞中表达生物合成途径基因。本发明还涉及用于制备这些化合物的新型链霉菌Streptomyces aizunensis菌株，使用这些化合物及其药学上可接受的盐和衍生物作为药物，特别是其作为真菌细胞生长抑制剂和癌细胞生长的用途。本发明还涉及包含这些新型聚酮化合物或其药学上可接受的盐或衍生物的药物组合物。最后，本发明涉及参与这些新型聚酮化合物的生物合成的新型多核苷酸序列及其编码的蛋白质。

66. 发明授权

US06551987B1 Pro-fragrances 有权
标题翻译：亲香料
公开(公告)号：US06551987B1
公开(公告)日：2003-04-22
申请号：US10030758
申请日：2001-10-22
申请人： Gregory Scott Miracle , Lon Montgomery Gray
发明人： Gregory Scott Miracle , Lon Montgomery Gray
IPC分类号： A61K746
CPC分类号： A61Q13/00 , A61K8/41 , A61K2800/57 , C07C225/14 , C07C225/20 , C07C255/14 , C07C2601/08 , C07C2601/16 , C11D3/507
摘要： The present invention relates to fragrance delivery systems which comprise: a) one or more pro-fragrances having formula (I) wherein G1 and G2 are methyl, or a cyclic hydrocarbyl unit derived from the isomers of ionone and/or damascone; R and R1 are each independently C1-C22 substituted or unsubstituted, branched or unbranched alkyl, C2-C22 substituted or unsubstituted, branched or unbranched alkenyl, C2-C20 substituted or unsubstituted, branched or unbranched hydroxyalkyl, C7-C20 substituted or unsubstituted alkylenearyl, C3-C20 substituted or unsubstituted cycloalkyl, alkyleneoxy, C6-C20 aryl, C5-C20 heteroaryl comprising one or more heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur, and mixtures thereof; two of the units Y1, Y2, R or R1 can be taken together to form one or more aromatic or non-aromatic, heterocyclic or non-heterocyclic, single rings, fused rings, bicyclo rings, spiroannulated rings, or mixtures thereof, said rings comprising from 3 to 20 carbon atoms and one or more heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur, and mixtures thereof; b) one or more aldehyde releasing oxazolidine pro-fragrances; and c) the balance carriers, pro-fragrances, pro-accords, other perfume ingredients.
摘要翻译：本发明涉及香料递送系统，其包括：a）一种或多种具有其中G1和G2是甲基的式（I）的一种或多种亲香料或衍生自紫罗酮和/或大蠊的异构体的环状烃基单元; R和R 1各自独立地为C 1 -C 22取代或未取代的支链或非支链烷基，C2-C22取代或未取代的支链或非支链烯基，C2-C20取代或未取代的支链或非支链羟烷基，C7-C20取代或未取代的亚烷基硬脂基， C 3 -C 20取代或未取代的环烷基，亚烷氧基，C 6 -C 20芳基，C 5 -C 20杂芳基，其包含一个或多个选自氮，氧，硫及其混合物的杂原子; 两个单元Y 1，Y 2，R或R 1可以一起形成一个或多个芳族或非芳族，杂环或非杂环单环，稠合环，双环，螺环或其混合物，所述环包含3至20个碳原子和一个或多个选自氮，氧，硫及其混合物的杂原子; b）一种或多种醛释放恶唑烷亲香料; 和c）平衡载体，亲香料，亲和剂，其他香料成分。

67. 发明授权

US06281295B1 Enamines as vulcanization accelerators for natural or synthetic rubbers 失效
标题翻译：作为天然或合成橡胶的硫化促进剂
公开(公告)号：US06281295B1
公开(公告)日：2001-08-28
申请号：US08961497
申请日：1997-10-30
申请人： Fabio Broussard , Mauro Adovasio , José Roncalli , Gianbattista Taroni , Corrado Callierotti
发明人： Fabio Broussard , Mauro Adovasio , José Roncalli , Gianbattista Taroni , Corrado Callierotti
IPC分类号： C08F830
CPC分类号： C07D295/104 , C07C225/14 , C07C229/30 , C07D295/145 , C08K5/17 , C08K5/3415 , C08K5/3435 , C08K5/35 , C08L21/00
摘要： Vulcanization accelerators consisting of compounds belonging to the group of enamines having general formula (I):
摘要翻译：由具有通式（I）的烯胺类化合物组成的硫化促进剂：

68. 发明授权

US5731133A Process for the production of a chromogenically developed color photographic image using a compound capable of reacting with primary aromatic amines 失效
标题翻译：使用能够与伯芳香胺反应的化合物生产显色显影的彩色照相图像的方法
公开(公告)号：US5731133A
公开(公告)日：1998-03-24
申请号：US647640
申请日：1996-05-15
申请人： Thomas Hubsch , Arno Schmuck
发明人： Thomas Hubsch , Arno Schmuck
IPC分类号： G03C7/00 , C07C225/12 , C07C225/14 , C07C225/20 , C07C229/12 , C07C229/30 , C07C229/34 , C07C233/31 , C07C255/30 , C07D295/104 , C07D295/145 , G03C7/392 , G03C7/407 , G03C7/42 , G03C11/00
CPC分类号： C07D295/104 , C07C225/12 , C07C225/14 , C07C225/20 , C07C229/12 , C07C229/30 , C07C229/34 , C07C233/31 , C07C255/30 , C07D295/145 , G03C7/39208 , G03C7/407 , C07C2101/14 , C07C2101/16
摘要： The storage stability of photographic color images obtained by chromogenic development may be improved by compounds of the formula I, which are capable of reacting with primary amines, in particular color developer compounds (reagent for primary amines). The compounds of the formula may be added to the color photographic recording material or to a treatment bath downstream from color development. Compounds of the formula I are moreover suitable as an additive to a spent photographic processing bath or its overflow in order to reduce therein the content of color developer compounds before the processing bath or the overflow is disposed of or regenerated for further use. ##STR1## In formula I: A means --OR.sup.2, --SR.sup.2 or --NR.sup.2 R.sup.3 ; R.sup.1 means H, alkyl, aryl, acyl, sulphonyl or a residue as in A or a residue which, together with A or together with Z.sup.1, completes a ring;R.sup.2 means H, alkyl, aryl, acyl, sulphonyl; R.sup.3 means a residue as in R.sup.2 or optionally a residue which, together with R.sup.2 and the N atom, forms a heterocyclic ring, Z.sup.1 and Z.sup.2 mutually independently mean: H, halogen, cyano, alkyl, aryl, acyl, a heterocyclic group, alkoxycarbonyl, aroxycarbonyl, sulphonyl, imino, imido, sulphamoyl, carbonamido or sulphonamido; wherein Z.sup.1 and Z.sup.2, together with the C atom to which they are attached, may form a carbocyclic or heterocyclic ring system.
摘要翻译：通过显影发展获得的照相彩色图像的储存稳定性可以通过能够与伯胺反应的式I化合物，特别是彩色显影剂化合物（伯胺试剂）来改善。可以将该配方化合物加入到彩色照相记录材料中，或加入到显影下游的处理浴中。此外，式I化合物适合作为用过的照相处理槽或其溢流剂的添加剂，以便在处理槽或溢出处理或再生以供进一步使用之前将其中的显色剂化合物的含量减少。（I）式Ⅰ中，A表示-OR2，-SR2或-NR2R3; R1表示H中的H，烷基，芳基，酰基，磺酰基或残基，或与A或与Z1一起形成环的残基; R2表示H，烷基，芳基，酰基，磺酰基; R3表示残基，如R2或任选残基，其与R2和N原子一起形成杂环，Z1和Z2相互独立地表示：H，卤素，氰基，烷基，芳基，酰基，杂环基，烷氧基羰基，芳氧基羰基，磺酰基，亚氨基，亚氨基，氨磺酰基，碳酰氨基或磺酰氨基; 其中Z1和Z2与它们所连接的C原子一起可以形成碳环或杂环系。

69. 发明授权

US5416088A Substituted pyridylpyrimidines, their preparation and their use 失效
标题翻译：取代的吡啶基嘧啶，其制备及其用途
公开(公告)号：US5416088A
公开(公告)日：1995-05-16
申请号：US107670
申请日：1993-08-16
申请人： Ulrich Heinemann , Heinz-Wilhelm Dehne , Stefan Dutzmann , Christoph Erdelen
发明人： Ulrich Heinemann , Heinz-Wilhelm Dehne , Stefan Dutzmann , Christoph Erdelen
IPC分类号： A01N25/02 , A01N25/30 , A01N43/54 , C07C225/14 , C07C225/16 , C07C323/27 , C07D401/04
CPC分类号： C07D401/04 , A01N43/54 , C07C225/14 , C07C225/16 , C07C323/27
摘要： ##STR1## Substituted pyridylpyrimidines have formula (I), in which A and Ar have the meaning given in the test of the description. Also disclosed are their preparation, their use and new initial products. The compounds having formula (I) may be prepared from appropriate salts of 2-pyridylamidine with appropriate enamines; said enamines are also new and disclosed by the invention, and may be prepared from appropriate ketones with appropriate formaldehyde derivates.
摘要翻译： PCT No.PCT / EP92 / 00311 Sec。 371日期：1993年8月16日 102（e）日期1993年8月16日PCT提交1992年2月13日PCT公布。第WO92 / 14726号公报（I）取代的吡啶基嘧啶具有式（I），其中A和Ar具有在描述试验中给出的含义。还披露了他们的准备，使用和新的初始产品。具有式（I）的化合物可以由适当的2-吡啶基脒盐与适当的烯胺制备; 所述烯胺也是新的并且由本发明公开，并且可以由具有合适的甲醛衍生物的合适的酮制备。

70. 发明授权

US5281622A Method of treating inflammation and pain with 2-(N-substituted-aminoalkyl)-5-(E)-alkylidene cyclopentanones, 2-(N-substituted-aminoalkyl)-5-(E)-arylalkylidene cyclopentanones, and derivatives thereof 失效
标题翻译：用2-（N-取代 - 氨基烷基）-5-（E） - 亚烷基环戊酮，2-（N-取代 - 氨基烷基）-5-（E） - 芳基亚烷基环戊酮及其衍生物治疗炎症和疼痛的方法
公开(公告)号：US5281622A
公开(公告)日：1994-01-25
申请号：US44983
申请日：1993-04-08
申请人： Lan K. Wong , Hai-Tao Chen , Zhi-Zhong Ji
发明人： Lan K. Wong , Hai-Tao Chen , Zhi-Zhong Ji
IPC分类号： A61K31/13 , C07C225/14 , C07C225/18 , C07D295/116 , A61K31/12 , A61K31/265 , A61K31/36
CPC分类号： C07D295/116 , A61K31/13 , C07C225/14 , C07C225/18 , C07C2101/08 , C07C2101/10
摘要： Novel 2-(N-substituted-aminoalkyl)-5-(E)-alkylidene cyclopentanones, 2-(N-substituted-aminoalkyl)-5-(E)-arylalkylidene cyclopentanones, and derivatives thereof having the formula ##STR1## wherein x is methylene or ethylene; R.sub.1 is dimethylamino, diethylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, anilino or substituted anilino; R.sub.2 is hydrogen, straight or branched alkyl of 1 to 9 carbon atoms, aryl or arylalkyl; R.sub.3 is hydrogen, straight or branched alkyl of 1 to 9 carbon atoms, aryl or arylalkyl; and R.sub.4 is hydrogen, methyl, ethyl, allyl, benzyl, substituted benzyl, cyclopentyl, substituted cyclopentyl, cyclopenten-1-yl, or substituted cyclopenten-1-yl; and wherein aryl is phenyl or phenyl substituted with one or more methoxyl, hydroxyl, methylenedioxy, chloro, bromo, fluoro, ethoxycarbonylmethoxy, benzoxy, alkyl group, or their combination, possess anti-inflammatory, analgesic and anticancer properties. The methods of using these compounds to treat inflammation, pain and cancer in mammals and to resist or substantially prevent inflammation and pain in mammals are also disclosed.
摘要翻译：新的2-（N-取代 - 氨基烷基）-5-（E） - 亚烷基环戊酮，2-（N-取代 - 氨基烷基）-5-（E） - 芳基亚烷基环戊酮及其衍生物具有下式（*化学结构* ）其中x是亚甲基或亚乙基; R1是二甲基氨基，二乙基氨基，1-吡咯烷基，1-哌啶基，4-吗啉基，苯胺基或取代的苯胺基; R2是氢，1至9个碳原子的直链或支链烷基，芳基或芳基烷基; R3是氢，1至9个碳原子的直链或支链烷基，芳基或芳基烷基; R 4是氢，甲基，乙基，烯丙基，苄基，取代的苄基，环戊基，取代的环戊基，环戊烯-1-基或取代的环戊烯-1-基; 羟基，亚甲二氧基，氯，溴，氟，乙氧羰基甲氧基，苯氧基，烷基或它们的组合取代的苯基或苯基被苯基取代，具有抗炎，镇痛和抗癌特性。还公开了使用这些化合物治疗哺乳动物中的炎症，疼痛和癌症并抵抗或基本上预防哺乳动物的炎症和疼痛的方法。

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