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1. 发明申请

US20050054651A1 Compositions and methods for the treatment of disease associated with Trp-p8 expression 有权
标题翻译：用于治疗与Trp-p8表达相关的疾病的组合物和方法
公开(公告)号：US20050054651A1
公开(公告)日：2005-03-10
申请号：US10923413
申请日：2004-08-20
申请人： Sateesh Natarajan , Ofir Moreno , Thomas Graddis , David Duncan , Reiner Laus , Feng Chen
发明人： Sateesh Natarajan , Ofir Moreno , Thomas Graddis , David Duncan , Reiner Laus , Feng Chen
IPC分类号： A61K31/498 , A61K31/517 , A61K45/06 , C07C311/20 , C07C311/37 , C07C323/40 , C07C323/44 , C07C333/06 , C07D207/06 , C07D207/09 , C07D207/32 , C07D207/325 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/48 , C07D213/40 , C07D215/04 , C07D215/08 , C07D215/46 , C07D217/06 , C07D231/12 , C07D231/14 , C07D231/56 , C07D235/18 , C07D235/26 , C07D239/42 , C07D241/18 , C07D241/44 , C07D251/54 , C07D263/34 , C07D263/56 , C07D263/57 , C07D279/12 , C07D295/096 , C07D295/135 , C07D295/26 , C07D307/52 , C07D317/66 , C07D333/34 , C07D401/04 , C07D405/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D493/08 , C07D495/04 , C07D513/04 , G01N33/68
CPC分类号： C07C233/60 , A61K31/498 , A61K31/517 , A61K45/06 , C07C233/58 , C07C243/36 , C07C243/38 , C07C311/20 , C07C311/37 , C07C323/40 , C07C323/44 , C07C333/06 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/06 , C07D207/09 , C07D207/325 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/20 , C07D209/48 , C07D211/06 , C07D213/40 , C07D215/04 , C07D215/08 , C07D215/46 , C07D217/06 , C07D223/04 , C07D231/12 , C07D231/14 , C07D231/56 , C07D235/18 , C07D235/26 , C07D239/42 , C07D241/18 , C07D241/44 , C07D241/54 , C07D251/54 , C07D263/34 , C07D263/57 , C07D279/12 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/26 , C07D307/52 , C07D311/16 , C07D317/66 , C07D333/34 , C07D401/04 , C07D403/14 , C07D405/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D493/08 , C07D495/04 , C07D513/04 , G01N33/5011 , G01N33/6872 , G01N2500/10 , A61K2300/00
摘要： Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
摘要翻译：提供的是小分子Trp-p8调节剂，包括Trp-p8激动剂和Trp-p8拮抗剂，以及包含小分子Trp-p8激动剂的组合物以及用于鉴定和表征新型小分子Trp-p8调节剂的方法和方法降低Trp-p8表达细胞的生存力和/或抑制Trp-p8表达细胞的生长，用于激活Trp-p8介导的阳离子流入的方法，用于刺激细胞凋亡和/或坏死的方法以及用于治疗疾病的相关方法，包括癌症如肺，乳腺，结肠癌和/或前列腺癌以及与Trp-p8表达相关的其它疾病，例如良性前列腺增生。

2. 发明授权

US11046645B2 Isothiocyanate production method, composition for transporting and storing N-substituted O-substituted thiocarbamate, and isothiocyanate composition 有权
公开(公告)号：US11046645B2
公开(公告)日：2021-06-29
申请号：US16382738
申请日：2019-04-12
申请人： Asahi Kasei Kabushiki Kaisha
发明人： Masaaki Shinohata , Yuji Kosugi , Nobuhisa Miyake
IPC分类号： C07C331/20 , C07C331/30 , C07C333/04 , C07C333/06 , C07C333/08 , C07C335/08 , C07C335/14 , C07C329/04 , C07C335/10 , C07C335/16 , C07C331/22 , C07C333/20 , C07C333/22 , C07C333/24
摘要： The present invention relates to an isothiocyanate production method using an organic primary amine and thiourea as starting materials; to a composition for transporting and storing an N-substituted O-substituted thiocarbamate that includes an N-substituted O-substituted thiocarbamate and a hydroxy compound, the equivalent weight ratio of hydroxy groups of the hydroxy compound with respect to the carbamate groups of the N-substituted O-substituted thiocarbamate being in the range of 1 to 100; to a composition for transporting and storing a compound with a thioureido group that includes a compound with a thioureido group and a hydroxy compound, the equivalent weight ratio of hydroxy groups of the hydroxy compound with respect to the thioureido groups of the compound with a thioureido group being in the range of 1 to 100; and to an isothiocyanate composition containing an isothiocyanate and a compound with a specific functional group.

3. 发明授权

US10308601B2 Isothiocyanate production method, composition for transporting and storing N-substituted O-substituted thiocarbamate, and isothiocyanate composition 有权
公开(公告)号：US10308601B2
公开(公告)日：2019-06-04
申请号：US14772943
申请日：2014-02-28
申请人： Asahi Kasei Chemicals Corporation
发明人： Masaaki Shinohata , Yuji Kosugi , Nobuhisa Miyake
IPC分类号： C07C209/60 , C07C263/20 , C07C331/00 , C07C331/30 , C07C333/04 , C07C333/06 , C07C333/08 , C07C331/20 , C07C331/22 , C07C335/08 , C07C335/14 , C07C329/04 , C07C335/10 , C07C335/16
摘要： The present invention relates to an isothiocyanate production method using an organic primary amine and thiourea as starting materials; to a composition for transporting and storing an N-substituted O-substituted thiocarbamate that includes an N-substituted O-substituted thiocarbamate and a hydroxy compound, the equivalent weight ratio of hydroxy groups of the hydroxy compound with respect to the carbamate groups of the N-substituted O-substituted thiocarbamate being in the range of 1 to 100; to a composition for transporting and storing a compound with a thioureido group that includes a compound with a thioureido group and a hydroxy compound, the equivalent weight ratio of hydroxy groups of the hydroxy compound with respect to the thioureido groups of the compound with a thioureido group being in the range of 1 to 100; and to an isothiocyanate composition containing an isothiocyanate and a compound with a specific functional group.

4. 发明授权

US4987130A Substituted amine derivatives, their production and use 失效
标题翻译：取代的胺衍生物，其生产和使用
公开(公告)号：US4987130A
公开(公告)日：1991-01-22
申请号：US453346
申请日：1989-12-22
申请人： Susumu Tsushima , Muneo Takatani , Minoru Hirata
发明人： Susumu Tsushima , Muneo Takatani , Minoru Hirata
IPC分类号： C07C271/10 , A61K20060101 , A61K31/27 , A61K31/325 , A61K31/335 , A61K31/395 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61P9/06 , C07C20060101 , C07C269/02 , C07C271/06 , C07C271/12 , C07C271/24 , C07C271/28 , C07C275/00 , C07C275/14 , C07C275/28 , C07C323/25 , C07C333/04 , C07C333/06 , C07C333/10 , C07D209/48 , C07D211/04 , C07D211/34 , C07D211/58 , C07D213/24 , C07D213/36 , C07D213/38 , C07D213/53 , C07D295/10 , C07D295/12 , C07D295/125 , C07D295/13 , C07D521/00
CPC分类号： C07D295/13 , C07C275/14 , C07C275/28 , C07D211/34 , C07D213/38
摘要： Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.

5. 发明授权

US3883343A Method of tobacco sucker inhibition 失效
标题翻译：烟草吸盘抑制方法
公开(公告)号：US3883343A
公开(公告)日：1975-05-13
申请号：US34053473
申请日：1973-03-12
申请人： ISHIHARA MINING & CHEMICAL CO
发明人： FUJIKAWA KANICHI , TAKAHASHI RYOHEI , YOKOMICHI ISAO , KIMURA FUMIO , KAJI TAKEO , SAKASHITA NOBUYUKI
IPC分类号： A01N47/12 , A01N47/16 , A01N47/18 , A01P21/00 , C07C67/00 , C07C325/00 , C07C333/02 , C07C333/04 , C07C333/06 , C07C333/10 , A01N9/20
CPC分类号： A01N47/12 , C07C333/02
摘要： The inhibition of the growth of tobacco plant suckers by the application to the tobacco plant of benzylthiolcarbamate having the formula,

WHEREIN R1 and R2 are selected from the group consisting of acetyl, cyclohexyl, and C1-6 alkyl group; X and Y are selected from the group consisting of nitro, acetyl, amino, C1-3 alkyl, C1-3 alkoxyl, and halogen; and M AND N ARE 0 OR 1.
摘要翻译：通过应用于具有式WHEREIN R 1和R 2的硫代氨基甲酸苄酯的烟草植物对烟草植物吸盘的生长的抑制选自乙酰基，环己基和C 1-6烷基; X和Y选自硝基，乙酰基，氨基，C 1-3烷基，C 1-3烷氧基和卤素; M AND N为0或1。

6. 发明授权

US5817858A Carbamate compounds having N-substituted thiocarbamoyl group and process for preparing the same 失效
标题翻译：具有N-取代的硫代氨基甲酰基的氨基甲酸酯化合物及其制备方法
公开(公告)号：US5817858A
公开(公告)日：1998-10-06
申请号：US629619
申请日：1996-04-09
申请人： Choi Yong Moon , Han Dong Il , Kim Hyung Cheol
发明人： Choi Yong Moon , Han Dong Il , Kim Hyung Cheol
IPC分类号： C07C333/04 , C07C333/06 , C07C333/10 , C07D295/21 , C07C333/02
CPC分类号： C07D295/21 , C07C333/04 , C07C333/06 , C07C333/10 , C07C2101/02
摘要： There is disclosed 3-N-substituted thiocarbamoyl-2-phenyl-1,3-propanediol carbamate, represented by the following structural formula I, that is very effective for prophylaxis and treatment of central nervous system disorders including nervous muscular pain, epilepsy and cerebral apoplexy: ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl containing 1 to 8 carbon atoms and 5 to 7-membered aliphatic cyclic compound which may comprise two or less nitrogen or oxygen atoms directly unconnected, with a proviso that R.sub.1 and R.sub.2 both should not be hydrogen and the total number of carbon atoms of R.sub.1 and R.sub.2 ranges from 1 to 16.
摘要翻译：公开了由以下结构式I表示的3-N-取代的硫代氨基甲酰基-2-苯基-1,3-丙二醇氨基甲酸酯，其对预防和治疗包括神经性肌肉疼痛，癫痫和脑的中枢神经系统疾病非常有效中和：彼此独立地选自氢，含有1至8个碳原子的低级烷基和5至7元脂肪族环状化合物，其可包含两个或更少个直接未连接的氮原子或氧原子，条件是R1和R2都不应该是氢，R1和R2的总碳原子数范围是1到16。

7. 发明授权

US5380747A Treatment for atherosclerosis and other cardiovascular and inflammatory diseases 失效
标题翻译：治疗动脉粥样硬化和其他心血管和炎症疾病
公开(公告)号：US5380747A
公开(公告)日：1995-01-10
申请号：US969934
申请日：1992-10-30
申请人： Russell M. Medford , Margaret K. Offermann , R. Wayne Alexander
发明人： Russell M. Medford , Margaret K. Offermann , R. Wayne Alexander
IPC分类号： C07D295/10 , A61K31/145 , A61K31/185 , A61K31/198 , A61K31/27 , A61K31/325 , A61K31/40 , A61K31/445 , A61K45/06 , A61P9/00 , A61P9/02 , A61P9/08 , A61P9/10 , A61P29/00 , C07C333/04 , C07C333/06 , G01N33/68
CPC分类号： G01N33/6872 , A61K31/145 , A61K31/185 , A61K31/198 , A61K31/325 , A61K31/40 , A61K45/06 , G01N2333/70503 , G01N2333/7056 , G01N2800/323
摘要： Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
摘要翻译：二硫代羧酸盐，特别是二硫代氨基甲酸盐阻断内皮细胞表面粘附分子VCAM-1的诱导表达，并且可用于治疗心血管疾病，包括动脉粥样硬化，血管成形术后再狭窄，冠状动脉疾病和心绞痛，作为以及由VCAM-1介导的非心血管炎性疾病。

8. 发明授权

US5179125A N-substituted mercaptopropanamide derivatives 失效
标题翻译： N-取代巯基丙酰胺衍生物
公开(公告)号：US5179125A
公开(公告)日：1993-01-12
申请号：US504654
申请日：1990-04-04
申请人： Tetsutaro Mimura , Yasuhisa Nakamura , Junko Nishino , Tadahiro Sawayama , Takashi Sasagawa , Takashi Deguchi , Hideo Nakamura
发明人： Tetsutaro Mimura , Yasuhisa Nakamura , Junko Nishino , Tadahiro Sawayama , Takashi Sasagawa , Takashi Deguchi , Hideo Nakamura
IPC分类号： C07C229/08 , C07C229/24 , C07C229/26 , C07C229/34 , C07C229/60 , C07C323/60 , C07C327/06 , C07C327/12 , C07C327/16 , C07C327/24 , C07C327/32 , C07C329/06 , C07C333/06 , C07D213/50 , C07D261/20 , C07D265/30 , C07D295/088 , C07D295/155 , C07D307/68 , C07D333/22 , C07D333/38
CPC分类号： C07D265/30 , C07C229/08 , C07C229/24 , C07C229/26 , C07C229/34 , C07C229/60 , C07C323/60 , C07C327/06 , C07C327/12 , C07C327/16 , C07C327/24 , C07C327/32 , C07C329/06 , C07C333/06 , C07D213/50 , C07D261/20 , C07D295/088 , C07D295/155 , C07D307/68 , C07D333/22 , C07D333/38 , C07C2101/02 , C07C2101/08 , C07C2101/16
摘要： Novel N-substituted mercaptopropanamide derivatives of the formula: ##STR1## wherein R.sub.1 is mercapto or a group convertible into mercapto when cleaved within the biobody, W is hydrogen atom, an alkyl or an aralkyl, R.sub.2 is an aryl which may optionally have substituent(s), a heterocyclic group which may optionally have substituent(s), or an alkyl which may optionally have substituent(s), X is a cycloalkylene, a cycloalkylidene, or a phenylene which may optionally have substituent(s) or may optionally be fused with other ring, and R.sub.3 is carboxyl or a group convertible into carboxyl when cleaved within the biobody, or a pharmaceutically acceptable salt thereof, and a solid solution of said N-substituted mercaptopropanamide derivative with an amino acid, which have excellent enkephalinase inhibitory activity and are useful for the treatment of mild to moderate pain, and a pharmaceutical composition containing said compounds as an active ingredient, and processes for preparing these compounds.
摘要翻译：新型N-取代巯基丙酰胺衍生物，其分子式如下：其中R 1为巯基或当在生物体内切割时可转化成巯基的基团，W为氢原子，烷基或芳烷基，R2为可任意选择的芳基具有取代基，可以任选具有取代基的杂环基或可任选具有取代基的烷基，X是可以任选具有取代基的亚环烷基，亚环烷基或亚苯基，可任选地与其它环稠合，并且R3是羧基或当在生物体内切割时可转化成羧基的基团或其药学上可接受的盐，以及所述N-取代的巯基丙酰胺衍生物与氨基酸的固溶体，其具有优异的脑啡肽酶抑制活性，并且可用于治疗轻度至中度疼痛，以及含有所述化合物作为活性成分的药物组合物，以及制备这些化合物的方法 ds。

9. 发明授权

US4939170A Substituted aminophenyl carbamates 失效
标题翻译：取代氨基苯基氨基甲酸酯
公开(公告)号：US4939170A
公开(公告)日：1990-07-03
申请号：US197009
申请日：1988-05-20
申请人： Bernd-Wieland Kruger , Klaus Sasse , Peter Heitkamper , Klaus Konig , Wilhelm Brandes , Gerd Hanssler , Albrecht Marhold
发明人： Bernd-Wieland Kruger , Klaus Sasse , Peter Heitkamper , Klaus Konig , Wilhelm Brandes , Gerd Hanssler , Albrecht Marhold
IPC分类号： A01N47/22 , A01N47/30 , A01N53/00 , A01N53/06 , C07C67/00 , C07C201/00 , C07C205/26 , C07C205/37 , C07C205/43 , C07C213/00 , C07C213/02 , C07C215/76 , C07C239/00 , C07C271/40 , C07C271/48 , C07C275/28 , C07C275/34 , C07C301/00 , C07C303/40 , C07C311/08 , C07C311/21 , C07C311/31 , C07C311/37 , C07C313/00 , C07C317/36 , C07C317/38 , C07C317/40 , C07C323/39 , C07C323/49 , C07C333/04 , C07C333/06 , C07C333/08 , C07D307/08 , C07D309/08 , C07D319/06 , C07D521/00
CPC分类号： C07D307/08 , C07C205/26 , C07C205/37 , C07C275/34 , C07D319/06
摘要： Fungicidal substituted aminophenyl carbamates of the formula ##STR1## in which X represents --CO--NR.sup.8 R.sup.9 ; --CO--OR.sup.9 ; --CO--SR.sup.9 ; --CO.sup.R.sup.10 ; --SO.sub.2 R.sup.9 or hydrogen, in whichR.sup.8 represents hydrogen or alkyl,R.sup.9 represents optionally substituted aryl, optionally substituted aralkyl, optionally substituted alkyl, alkenyl, halogenoalkenyl, or in each case optionally substituted cycloalkyl, cycloalkenyl or cycloalkylalkyl, andR.sup.10 has the meaning of R.sup.9 or represents an optionally substituted heterocyclic ring,Y.sup.1 to Y.sup.4 are identical or different and represent hydrogen, halogen, nitro, cyano, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, alkylsulfonyl or halogenoalkythio,R.sup.1 to R.sup.7 are identical or different and represent hydrogen, alkyl, halogenoalkyl or alkoxyalkyl,n represents 0 or 1, andZ represents alkyl, halogenoalkyl or a ##STR2## radical, in which R.sup.11 to R.sup.14 are identical or different and represent hydrogen, alkyl, halogenoalkyl or alkoxyalkyl, andR.sup.15 represents alkyl, halogenoalkyl or alkoxyalkyl.
摘要翻译：式（I）的杀真菌取代的氨基苯基氨基甲酸酯，其中X表示-CO-NR8R9; -CO-OR9; -CO-SR9; -COR10; -SO 2 R 9或氢，其中R 8表示氢或烷基，R 9表示任选取代的芳基，任选取代的芳烷基，任选取代的烷基，烯基，卤代烯基，或在每种情况下任选取代的环烷基，环烯基或环烷基烷基，R 10具有R 9 或代表任选取代的杂环，Y 1至Y 4相同或不同，表示氢，卤素，硝基，氰基，烷基，卤代烷基，烷氧基，卤代烷氧基，烷硫基，烷基磺酰基或卤代链烯基，R 1至R 7相同或不同，烷基，卤代烷基或烷氧基烷基，n表示0或1，Z表示烷基，卤代烷基或基团，其中R11至R14相同或不同，表示氢，烷基，卤代烷基或烷氧基烷基，R15表示烷基，卤代烷基或烷氧基烷基。

10. 发明授权

US4617416A Process for the preparation of thiocarbamates 失效
标题翻译：硫代氨基甲酸酯的制备方法
公开(公告)号：US4617416A
公开(公告)日：1986-10-14
申请号：US713603
申请日：1985-03-19
申请人： Renato Ugo , Stefano Campolmi , Vittorio Carletti
发明人： Renato Ugo , Stefano Campolmi , Vittorio Carletti
IPC分类号： C07B61/00 , B01J31/00 , C07C67/00 , C07C325/00 , C07C333/02 , C07C333/04 , C07C333/06 , C07C333/20 , C07C333/22 , C07C155/02
CPC分类号： C07C333/02
摘要： There is disclosed a process for the preparation of thiocarbamates having the following general formula: ##STR1## wherein: R represents alkyl C.sub.1 -C.sub.4 optionally substituted with one or more halogen atoms, alkenyl C.sub.2 -C.sub.4 optionally substituted with one or more halogen atoms, phenyl optionally substituted with one or more halogen atoms, benzyl optionally substituted with one or more halogen atoms on the phenyl ring;R.sup.1 and R.sup.2, equal or different from one another, represent alkyl C.sub.1 -C.sub.4 or cycloalkyl;consisting in reacting organic dithiocarbonates with organic carbamoyl halides, in the presence of an aqueous solution of an inorganic base and a phase transfer catalyst, at a temperature of 10.degree. to 50.degree. C. for time periods of 5 to 10 hours.The thiocarbamates obtained are used as herbicides, fungicides, etc., and in general in various fields of "fine chemicals".
摘要翻译：公开了制备具有以下通式的硫代氨基甲酸酯的方法：其中：R表示任选被一个或多个卤素原子取代的C 1 -C 4烷基，任选被一个或多个卤素原子取代的烯基C 2 -C 4，苯基任选地被一个或多个卤素原子取代，苯基上任选被一个或多个卤素原子取代的苄基; R1和R2彼此相同或不同，表示烷基C1-C4或环烷基; 在有机二硫代碳酸酯与有机氨基甲酰卤反应的条件下，在无机碱和相转移催化剂的水溶液存在下，在10〜50℃的温度下反应5〜10小时。所得的硫代氨基甲酸酯用作除草剂，杀真菌剂等，一般用于“精细化学品”的各个领域。

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