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81. 发明申请

US20020013498A1 Process for the reduction of cyano-substituted sulfones to aminoalkylene-substituted sulfones 有权
公开(公告)号：US20020013498A1
公开(公告)日：2002-01-31
申请号：US09843986
申请日：2001-04-27
发明人： Jack ChanKou Hwang , Eugene Tarlton , Anthony D. Piscopio
IPC分类号： C07C317/28
CPC分类号： C07C315/04 , C07C317/28
摘要： Disclosed is a process for selectively reducing a nitrile containing organic compound that also contains a sulfone moiety, the nitrile being reduced to a primary amine.

82. 发明授权

US6153648A Iodopropargylamine compounds, and industrial antimicrobial and antifungal agents, algicides, and antifouling agents containing the same 失效
标题翻译：碘代炔丙胺化合物，工业抗微生物和抗真菌剂，杀藻剂和含有它们的防污剂
公开(公告)号：US6153648A
公开(公告)日：2000-11-28
申请号：US486121
申请日：2000-02-23
申请人： Kenji Makino , Shinichi Igarashi , Mitsugu Futagawa
发明人： Kenji Makino , Shinichi Igarashi , Mitsugu Futagawa
IPC分类号： A01N37/44 , A01N41/10 , C07C225/14 , C07C229/30 , C07C255/30 , C07C255/40 , C07C317/28 , C07C317/48 , A01N37/06 , A01N33/04 , C07C69/73
CPC分类号： A01N37/44 , A01N41/10 , C07C225/14 , C07C229/30 , C07C255/30 , C07C255/40 , C07C317/28 , C07C317/48 , C07C2101/14
摘要： Iodopropargylamine compound of the general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 combine with each other to form a tetramethylene group or a pentamethylene group, R.sup.3 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, and X and Y each independently represent a cyano group, an alkoxycarbonyl group having 2 to 7 carbon atoms, an alkylcarbonyl group having 2 to 7 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, a phenylcarbonyl group or a phenylsulfonyl group, provided that the phenyl group of a phenylcarbonyl group or a phenylsulfonyl group may be optionally substituted by halogen atoms, alkyl groups having 1 to 3 carbon atoms, alkoxy groups having 1 to 3 carbon atoms, nitro groups or trifluoromethyl groups. The compound are useful as the active ingredient for industrial antibacterial and antifungal agents, algicides, and agents for preventing adhesion of organisms.
摘要翻译： PCT No.PCT / JP98 / 03806 Sec。 371日期2000年2月23日 102（e）日期2000年2月23日PCT提交1998年8月27日PCT公布。 WO99 / 11601 PCT出版物日期1999年3月11日通式（1）的二丙炔胺化合物：其中R1和R2各自独立地表示氢原子或具有1至3个碳原子的烷基，或者R1和R2彼此结合形成四亚甲基或五亚甲基，R 3表示氢原子或碳原子数1〜3的烷基，X和Y各自独立地表示氰基，碳原子数2〜7的烷氧基羰基，碳原子数2〜7的烷基羰基，具有1至6个碳原子的烷基磺酰基，苯基羰基或苯基磺酰基，条件是苯基羰基或苯基磺酰基的苯基可以任选被卤素原子，具有1-3个碳原子的烷基，烷氧基具有1至3个碳原子的基团，硝基或三氟甲基。该化合物可用作工业抗细菌和抗真菌剂，杀藻剂和防止生物粘附的试剂的活性成分。

84. 发明授权

US6077866A Benzophenone hydrazone derivatives as insecticides 失效
标题翻译：二苯甲酮腙衍生物作为杀虫剂
公开(公告)号：US6077866A
公开(公告)日：2000-06-20
申请号：US644139
申请日：1996-05-10
申请人： Yoshinori Kitagawa , Katsuaki Wada , Yoshiko Kyo , Yuichi Otsu , Yumi Hattori , Toru Obinata , Takahisa Abe , Katsuhiko Shibuya , Wolfram Andersch
发明人： Yoshinori Kitagawa , Katsuaki Wada , Yoshiko Kyo , Yuichi Otsu , Yumi Hattori , Toru Obinata , Takahisa Abe , Katsuhiko Shibuya , Wolfram Andersch
IPC分类号： C07C317/28 , A01N33/26 , A01N35/10 , A01N37/28 , A01N41/10 , A01N47/24 , A01N47/34 , C07C317/24 , C07C323/08 , C07C323/22 , C07C323/45 , C07C323/48 , C07C323/60 , C07C327/22 , C07C329/16 , C07C331/04 , C07C335/32 , C07F7/08 , A01N47/12
CPC分类号： C07C335/32 , A01N35/10 , A01N37/28 , A01N47/24 , A01N47/34 , C07C317/24 , C07C317/28 , C07C323/08 , C07C323/22 , C07C323/48 , C07C323/60 , C07C327/22 , C07C329/16 , C07C331/04 , C07F7/0818
摘要： Novel benzophenonehydrazone derivatives represented by the formula (I): ##STR1## wherein, R.sup.1 is halogen; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is cyano, optically substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-4 alkynyl, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl; R.sup.4 is hydrogen, phenyl, optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.2-8 alkenyl, --CO--R.sup.8, --CO--O--R.sup.9 or ##STR2## R.sup.5 is hydrogen, formyl, phenyl, optionally substituted C.sub.1-8 alkyl, optionally substituted C.sub.2-8 alkenyl, optionally substituted C.sub.3-8 alkynyl, optionally substituted C.sub.1-8 alkyl-arbonyl, optionally substituted C.sub.1-6 alkyl-oxalyl, optionally substituted C.sub.1-8 alkoxy-carbonyl, optionally substituted C.sub.1-8 alkoxy-oxalyl, optionally substituted C.sub.3-8 cycloalkyl-carbonyl, optionally substituted C.sub.2-8 alkenyl-carbonyl or optionally substituted benzoyl; R.sup.6 is hydrogen or halogen; R.sup.7 is hydrogen, halogen or C.sub.1-2 alkyl, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl; n is 0, 1 or 2, provided that n is 0 when R.sup.3 is cyano, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl, is a single bond of Anti form or of Syn form.The benzophenonehydrazone derivatives of the formula (I) have excellent insecticidal activities.
摘要翻译：由式（I）表示的新型二苯甲酮腙衍生物：其中，R1为卤素; R2是氢或C1-4烷基; R3是氰基，光学取代的C1-4烷基，C2-4烯基，C3-4炔基，C1-4烷基羰基或C1-4烷氧基 - 硫代羰基; R4是氢，苯基，任选取代的C 1-6烷基，任选取代的C 2-8烯基，-CO-R 8，-CO-O-R 9或R 5是氢，甲酰基，苯基，任选取代的C 1-8烷基，任选取代的C 2 -8-烯基，任选取代的C 3-8炔基，任选取代的C 1-8烷基 - 羰基，任选取代的C 1-6烷基 - 草酰基，任选取代的C 1-8烷氧羰基，任选取代的C 1-8烷氧基 - 草酰基，任选取代的C 3 -8环烷基 - 羰基，任选取代的C 2-8烯基 - 羰基或任选取代的苯甲酰基; R6是氢或卤素; R7是氢，卤素或C1-2烷基，C1-4烷基羰基或C1-4烷氧基 - 硫代羰基; n为0,1或2，条件是当R 3为氰基时，n为0，C 1-4烷基 - 羰基或C 1-4烷氧基 - 硫代羰基，+ Z为抗式或Syn形式的单键。式（I）的二苯甲酮腙衍生物具有优异的杀虫活性。

85. 发明授权

US5955505A Glutamic acid receptor agonist 失效
标题翻译：谷氨酸受体激动剂
公开(公告)号：US5955505A
公开(公告)日：1999-09-21
申请号：US894433
申请日：1997-08-20
申请人： Jiro Takeo , Shinya Yamashita , Keiji Wada , Yoshiyuki Chiba
发明人： Jiro Takeo , Shinya Yamashita , Keiji Wada , Yoshiyuki Chiba
IPC分类号： A61K31/00 , A61K31/18 , A61K31/192 , A61K31/195 , A61K31/216 , A61K31/4035 , A61K31/4406 , C07C317/28 , C07C323/49 , C07C323/56 , C07C323/62 , A61K31/44
CPC分类号： C07C323/62 , A61K31/00 , A61K31/18 , A61K31/192 , A61K31/195 , A61K31/216 , A61K31/4035 , A61K31/4406 , C07C317/28 , C07C323/49 , C07C323/56
摘要： A method comprising administering a sulfonamide derivative to a patient requiring activation of glutamate receptors, the sulfonamide derivative represented by the formula ##STR1## wherein A is a napthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 40 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, and an acetamido group, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group of --OCH.sub.2 -- or a group of --CH.dbd.CH--; X and Y are the same or different, and are each a hydrogen atom or a fluorine atom; R is a carboxy group, an alkoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of ##STR2## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and R.sub.2 is a hydrogen atom, a hydroxyl group, an alkyl group having 1 to 3 carbon atoms, a carboxymethyl group or an alkoxycarbonylmethyl group having 3 to 6 carbon atoms; m is an integer from 0 to 2; and n is an integer from 0 to 3, or an pharmaceutically acceptable salt thereof, as an effective ingredient. The agonist is efficacious in the medical treatment of nerve degenerative disorders.
摘要翻译： PCT No.PCT / JP96 / 00379 Sec。 371日期1997年8月20日 102（e）日期1997年8月20日PCT提交1996年2月20日PCT公布。公开号WO96 / 25926 日期：1996年8月29日一种方法，包括向需要谷氨酸受体活化的患者施用磺酰胺衍生物，其中A为萘基，吡啶基，苯基，被1〜 5个选自卤素原子，具有1至40个碳原子的烷基，具有1至4个碳原子的烷氧基，硝基和乙酰氨基，或具有1至20个碳的烷基的基团原子 B是具有1至3个碳原子的亚烷基，-OCH 2 - 或-CH = CH-的基团; X和Y相同或不同，分别为氢原子或氟原子; R为羧基，碳原子数2〜5的烷氧基羰基，羟甲基或其中R1为氢原子或碳原子数1〜3的烷基的基团。 R2为氢原子，羟基，碳原子数为1〜3的烷基，羧甲基或碳原子数为3〜6的烷氧基羰基甲基。 m为0〜2的整数; n为0〜3的整数，或其药学上可接受的盐作为有效成分。激动剂在神经退行性疾病的治疗中是有效的。

90. 发明授权

US5817859A .alpha.-acyloxy-.beta.-amino-thiocarboxylic acid esters 失效
标题翻译： α-酰氧基-β-氨基 - 硫代羧酸酯
公开(公告)号：US5817859A
公开(公告)日：1998-10-06
申请号：US878079
申请日：1997-06-18
申请人： Takayuki Suzuki , Yutaka Honda , Kunisuke Izawa
发明人： Takayuki Suzuki , Yutaka Honda , Kunisuke Izawa
IPC分类号： C07C317/28 , C07C323/29 , C07C327/30 , C07C327/22
CPC分类号： C07C323/29 , C07C317/28 , C07C327/30
摘要： The present invention provides a simple and inexpensive method for producing a-hydroxy-.beta.-aminocarboxylic acids and their esters. An ester of an N-protected .alpha.-amino acid ester is converted into a .beta.-ketosulfoxide, which is then processed with an acid to give an .alpha.-ketohemimercaptal. Next, this is acylated and then processed with a base to obtain an N-protected .alpha.-acyloxy-.beta.-amino-thioester, which is then saponified to obtain an intended compound. According to the method of the present invention, it is possible to produce .alpha.-hydroxy-.beta.-aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.
摘要翻译：本发明提供了一种简单且廉价的α-羟基-β-氨基羧酸及其酯的制备方法。将N-保护的α-氨基酸酯的酯转化成β-酮亚砜，然后用酸处理，得到α-酮基二巯基。接下来，将其进行酰化，然后用碱处理，得到N-保护的α-酰氧基-β-氨基 - 硫代酯，然后皂化，得到目标化合物。根据本发明的方法，可以生产α-羟基-β-氨基羧酸衍生物，它们是从α-氨基酸生产各种HIV蛋白酶抑制剂，肾素抑制剂和制癌剂的中间体。该方法包括减少反应步骤，得到所需产物的方法中的选择性高，所得产物的产率高。

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