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1. 发明申请

US20190269785A1 CYTOTOXIC AND ANTI-MITOTIC COMPOUNDS, AND METHODS OF USING THE SAME 审中-公开
公开(公告)号：US20190269785A1
公开(公告)日：2019-09-05
申请号：US16273045
申请日：2019-02-11
申请人： Geoffrey C. WINTERS , Alexander Laurence MANDEL , James R. RICH , Bradley John HEDBERG , Tom Han Hsiao HSIEH , Elyse Marie Josée BOURQUE , John BABCOOK
发明人： Geoffrey C. WINTERS , Alexander Laurence MANDEL , James R. RICH , Bradley John HEDBERG , Tom Han Hsiao HSIEH , Elyse Marie Josée BOURQUE , John BABCOOK
IPC分类号： A61K47/64 , A61K38/05 , A61K31/445 , A61K47/54 , A61K38/06 , A61K39/395 , C07K5/02 , C07D333/34 , C07D213/71 , C07D213/56 , C07D211/60 , C07D211/34 , C07D207/452 , C07D207/08 , C07C381/08 , C07C327/06 , C07C323/67 , C07C323/12 , C07C311/51
摘要： Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

2. 发明授权

US09090662B2 Dithioamine reducing agents 有权
标题翻译：二硫代胺还原剂
公开(公告)号：US09090662B2
公开(公告)日：2015-07-28
申请号：US13768937
申请日：2013-02-15
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION
发明人： Ronald T. Raines , John Lukesh
IPC分类号： A61K38/00 , C07K1/113 , C12N9/96 , C07D339/08 , C07C329/16 , C07C323/25 , C07C327/06
CPC分类号： C07K1/113 , C07B2200/07 , C07C323/25 , C07C327/06 , C07C329/16 , C07D339/08 , C07K1/1133 , C12N9/96
摘要： Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. The invention provides S-acylated dithioamines which can be selectively activated reducing agents by removal of the S-acyl groups enzymatically or chemically. The invention further provides dithiane precursors of thioamino reducing agents. The invention provides dithioamine reducing agents, S-acylated dithioamines and dithianes which are immobilized on surfaces, including among others, glass, quartz, microparticles, nanoparticles and resins.
摘要翻译：可用于还原二硫键的二硫代胺还原剂。本发明的还原剂可用于例如减少二硫键，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。本发明的还原剂可用于和适用于各种生物应用，特别是作为研究和合成试剂。本发明提供S-酰化二硫代胺，其可通过酶或化学去除S-酰基来选择性活化还原剂。本发明还提供了硫代氨基还原剂的二硫代前体。本发明提供固定在玻璃，石英，微粒，纳米颗粒和树脂等表面上的二硫代胺还原剂，S-酰化二硫胺和二噻吩。

3. 发明授权

US5760270A Process of producing ether-type thio-phospholipids 失效
标题翻译：生产醚型硫代磷脂的方法
公开(公告)号：US5760270A
公开(公告)日：1998-06-02
申请号：US847771
申请日：1997-04-23
申请人： Mitsuaki Ohtani , Masahiro Fuji
发明人： Mitsuaki Ohtani , Masahiro Fuji
IPC分类号： C07C327/20 , C07C323/12 , C07C327/06 , C07C327/28 , C07F9/10 , C07F9/117
CPC分类号： C07C327/28 , C07C323/12 , C07C327/06 , C07F9/10 , C07F9/117 , Y02P20/55
摘要： A method of producing an ether-type thio-phospholipid of the formula (I): ##STR1## wherein: n is an integer of 13 to 17; A is C.sub.14 -C.sub.20 acyl group; G is a group selected from the group consisting of: ##STR2## which is useful as synthetic substrate of cytosolic phospholipase A.sub.2 inhibitors, said method being applicable to mass production of the compound (I), intermediates therefor and the preparation of the same are provided.
摘要翻译：制备式（I）的醚型硫代磷脂的方法：其中：n为13〜17的整数; A为C 14 -C 20酰基; G是选自以下的基团：作为细胞溶质磷脂酶A2抑制剂的合成底物有用的，所述方法适用于批量生产化合物（I），其中间体及其制备方法同样提供。

4. 发明授权

US5464601A Process for preparing sulfides of phosphorus 失效
标题翻译：制备磷硫化物的方法
公开(公告)号：US5464601A
公开(公告)日：1995-11-07
申请号：US219227
申请日：1994-03-29
申请人： Edward J. Griffith , Toan M. Ngo
发明人： Edward J. Griffith , Toan M. Ngo
IPC分类号： C01B25/14 , C01B25/16 , C07C327/06 , C07D237/18 , C07F9/165 , C07F9/18 , C09K3/00
CPC分类号： C01B25/16 , C01B25/14 , C07C327/06 , C07D237/18 , C07F9/165 , C07F9/18
摘要： There is disclosed a novel process for preparing products of the reaction of elemental phosphorus and elemental sulfur under reaction conditions wherein the phosphorus and sulfur are combined in a pre-mix at temperatures below the reaction temperature. The pre-mix may contain a diluent which is preferably the product of the reaction. Phosphorus pentasulfide can be prepared by heating the pre-mix to reaction temperatures wherein lower exotherm temperatures and reduced vibration are observed.
摘要翻译：公开了在反应条件下制备元素磷和元素硫的反应产物的新方法，其中在低于反应温度的温度下将磷和硫组合在预混物中。预混合物可以含有优选为反应产物的稀释剂。五硫化二磷可以通过将预混物加热至观察到较低的放热温度和减少的振动的反应温度来制备。

5. 发明授权

US5393913A N-formylanilines 失效
标题翻译： N-甲酰苯胺
公开(公告)号：US5393913A
公开(公告)日：1995-02-28
申请号：US25503
申请日：1993-03-03
申请人： Thierry Aubert
发明人： Thierry Aubert
IPC分类号： C07C255/23 , C07C233/15 , C07C255/24 , C07C255/25 , C07C323/27 , C07C327/42 , C07D233/84 , C07C255/02 , C07C327/06 , C07D233/04
CPC分类号： C07D233/84 , C07C233/15 , C07C255/24 , C07C255/25 , C07C327/42
摘要： The present invention relates to N-carbonyl anilines which are intermediates for the preparation of pesticidal 1-aryl imidazoles and to processes for making them.
摘要翻译：本发明涉及作为制备杀虫剂1-芳基咪唑的中间体的N-羰基苯胺及其制备方法。

6. 发明授权

US5262436A Acylamino acid antihypertensives in the treatment of congestive heart failure 失效
标题翻译：酰氨基酸抗高血压药治疗充血性心力衰竭
公开(公告)号：US5262436A
公开(公告)日：1993-11-16
申请号：US741025
申请日：1991-08-06
申请人： Martin F. Haslanger , Bernard R. Neustadt , Elizabeth M. Smith
发明人： Martin F. Haslanger , Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： A61K38/00 , A61K45/06 , C07C323/60 , C07C327/06 , C07C327/16 , C07K5/062 , C07K5/065 , C07K14/81 , A61K31/16 , A61K31/165 , A61K31/265 , A61K31/34 , A61K31/38
CPC分类号： C07K14/8146 , A61K45/06 , C07C323/60 , C07C327/06 , C07C327/16 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： Mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
摘要翻译：公开了可用于治疗高血压的巯基 - 酰基氨基酸和用于治疗高血压的巯基酰基氨基酸和心房利钠因子或血管紧张素转换酶抑制剂的组合。

7. 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。

8. 发明授权

US5179121A Thiobutyric acid derivatives 失效
标题翻译：三氢酸衍生物
公开(公告)号：US5179121A
公开(公告)日：1993-01-12
申请号：US745567
申请日：1991-08-15
申请人： Peter Maienfisch , Manfred Boger , Eginhard Steiner
发明人： Peter Maienfisch , Manfred Boger , Eginhard Steiner
IPC分类号： A01N37/02 , A01N37/36 , A01N43/08 , C07C327/06 , C07C327/22 , C07D307/38
CPC分类号： C07C327/22 , A01N37/02 , A01N37/36 , A01N43/08
摘要： Novel 4-chloro-4,4-difluorothiobutyric acid derivatives of the formula I ##STR1## in which R.sub.1 and R.sub.2 are, independently of one another, hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 halogenoalkyl and R.sub.3 is hydrogen or an organic radical can be employed as pest-control agents. Control of insects and arachnids is possible and preferable.
摘要翻译：式I（I）的新型4-氯-4,4-二氟硫代丁酸衍生物，其中R 1和R 2彼此独立地为氢，C 1 -C 4烷基或C 1 -C 4卤代烷基，R 3为氢或有机自由基可以作为害虫防治剂使用。昆虫和蜘蛛的控制是可能的并且是优选的。

9. 发明授权

US4417918A Herbicidal .alpha.-[3-(2-halo-4-trifluoromethylphenoxy)-6-halophenoxy]propionic acid thio esters and acids 失效
标题翻译：除草剂α-[3-（2-卤代-4-三氟甲基苯氧基）-6-卤苯氧基]丙酸硫酯和酸
公开(公告)号：US4417918A
公开(公告)日：1983-11-29
申请号：US297299
申请日：1981-08-28
申请人： Otto Rohr , Georg Pissiotas , Beat Bohner , Kurt Burdeska
发明人： Otto Rohr , Georg Pissiotas , Beat Bohner , Kurt Burdeska
IPC分类号： C07D295/18 , A01N39/02 , A01N39/04 , A01N47/40 , C07C51/00 , C07C59/125 , C07C59/68 , C07C59/70 , C07C67/00 , C07C69/712 , C07C69/736 , C07C219/06 , C07C231/00 , C07C231/12 , C07C233/00 , C07C233/16 , C07C235/06 , C07C235/20 , C07C235/22 , C07C235/24 , C07C239/00 , C07C253/00 , C07C255/16 , C07C255/49 , C07C255/53 , C07C255/54 , C07C325/00 , C07C327/06 , C07C327/22 , C07D295/08 , C07D295/088 , C07D295/185 , A01N37/10 , C07C149/40 , C07C149/43 , C07C153/023
CPC分类号： C07D295/185 , A01N39/02 , A01N39/04 , C07C255/00 , C07C323/00 , C07C327/00 , C07C59/68 , C07D295/088
摘要： 3-Phenoxy-.alpha.-phenoxy-alkancarboxylic acid derivatives of the formula ##STR1## are disclosed as possessing a surprising selective herbicidal activity. In the formula Hal is a halogen atom, m is an integer 1, 2, or 3, Y is a hydrogen or halogen atom or the cyano group, Z is a halogen atom or the cyano group, R.sub.1 is hydrogen or C.sub.1 -C.sub.8 alkyl, and R is an acid function. Methods are disclosed for combatting weeds in mono- and dicotyledonous cultures such as cereals, corn, rice, soya and cotton, which comprise applying to the locus to be protected from weeds a dosage of from 0.1 to 10.0 kilograms per hectare of the above compounds.
摘要翻译：公开了具有令人惊奇的选择性除草活性的式（I）的3-苯氧基-α-苯氧基 - 链烷羧酸衍生物。式中Hal为卤原子，m为整数1,2或3，Y为氢或卤素原子或氰基，Z为卤素原子或氰基，R1为氢或C1-C8烷基，R为酸官能团。公开了用于防治单谷和双子叶培养物如谷物，玉米，水稻，大豆和棉花中的杂草的方法，其包括以每公顷0.1至10.0千克的上述化合物的剂量施用于要防止杂草的场所。

10. 发明授权

US4414017A Herbicidal 3-butyrolactones 失效
标题翻译：除草剂3-丁内酯
公开(公告)号：US4414017A
公开(公告)日：1983-11-08
申请号：US153476
申请日：1980-05-27
申请人： David C. K. Chan
发明人： David C. K. Chan
IPC分类号： C07D207/273 , A01N33/22 , A01N37/18 , A01N37/38 , A01N39/02 , A01N43/08 , A01N43/10 , A01N43/36 , A01N53/00 , A01N53/08 , C07C51/00 , C07C62/08 , C07C67/00 , C07C69/757 , C07C201/00 , C07C205/38 , C07C231/00 , C07C235/28 , C07C325/00 , C07C327/06 , C07C327/22 , C07D307/33 , C07D333/32 , C07D307/32
CPC分类号： C07D307/33 , A01N39/02 , A01N43/08 , A01N43/10 , A01N43/36 , A01N53/00
摘要： Compounds of the formula ##STR1## wheren X.sup.1 is halo or trihalomethyl, X.sup.2 is hydrogen or halo, R.sup.1 is nitro or --OR.sup.3, R.sup.2 is hydrogen or --OR.sup.4, R.sup.3 ##STR2## R.sup.4 is ##STR3## and R is hydroxy, alkoxy, alkenoxy, alkynoxy, thiol, alkythio, alkenylthio, amino, mono- or di-substituted amino or OM, wherein M is a monovalent cation; R' and R" are hydrogen, alkyl, alkenyl, alkynyl or phenyl; and Y is oxygen, sulfur, or substituted or unsubstituted nitrogen, have herbicidal activity.
摘要翻译：其中X 1为卤素或三卤代甲基，X 2为氢或卤素，R 1为硝基或-OR 3，R 2为氢或-OR 4的化合物，其中R 1为羟基，烷氧基，链烯氧基，炔氧基，硫醇，链炔基，链烯硫基，氨基，单取代或二取代的氨基或OM，其中M是一价阳离子; R'和R“是氢，烷基，烯基，炔基或苯基; 和Y是氧，硫或取代或未取代的氮，具有除草活性。

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