公开(公告)号：US20110021761A1

公开(公告)日：2011-01-27

申请号：US12898687

申请日：2010-10-05

Applicant: Antoni Kozlowski ,  Xiaoming Shen ,  Michael D. Bentley ,  Zhihao Fang ,  Tony L. Sander

Inventor： Antoni Kozlowski ,  Xiaoming Shen ,  Michael D. Bentley ,  Zhihao Fang ,  Tony L. Sander

IPC: C07K14/00 ,  C07C309/64 ,  C07C271/06 ,  C07D207/40 ,  C07C223/02 ,  C07C229/02

CPC classification number: C08G65/329 ,  A61K47/56 ,  A61K47/60 ,  Y10S530/815

Abstract: Segmented water soluble polymers, containing a higher molecular weight segment linked to a lower molecular weight segment, are described. In one embodiment, the polymer segments are poly(ethylene glycol) segments. The segmented polymers are functionalized and are useful for conjugation to various moieties such as pharmacologically active substances. Also described are conjugates of such polymers and methods of their preparation.

Abstract translation: 描述了含有与较低分子量链段连接的较高分子量链段的分段水溶性聚合物。 在一个实施方案中，聚合物链段是聚（乙二醇）链段。 分段的聚合物被官能化并且可用于与各种部分缀合，例如药理学活性物质。 还描述了这些聚合物的共轭物及其制备方法。

公开(公告)号：US5608109A

公开(公告)日：1997-03-04

申请号：US350462

申请日：1994-12-07

Applicant: Kazuhiro Takagi ,  Tetsuji Ohshima ,  Nobuyoshi Hasegawa ,  Chiaki Katoh ,  Atsushi Kanaoka ,  Hideo Kanno

Inventor： Kazuhiro Takagi ,  Tetsuji Ohshima ,  Nobuyoshi Hasegawa ,  Chiaki Katoh ,  Atsushi Kanaoka ,  Hideo Kanno

IPC: A01N47/34 ,  A01N47/38 ,  A01N47/40 ,  C07C11/02 ,  C07C281/14 ,  C07C311/03 ,  C07C311/08 ,  C07C317/28 ,  C07C323/48 ,  C07C323/52 ,  C07C323/56 ,  C07C323/60 ,  C07C327/30 ,  C07C327/58 ,  C07C331/12 ,  C07D239/38 ,  C07D295/185 ,  C07D295/205 ,  C07D295/215 ,  C07D295/26 ,  C07D307/52 ,  C07F9/40 ,  C07C309/64 ,  C07C309/71 ,  C07C309/72

CPC classification number: C07D295/185 ,  A01N47/34 ,  A01N47/38 ,  A01N47/40 ,  C07C281/14 ,  C07C311/03 ,  C07C311/08 ,  C07C317/28 ,  C07C323/48 ,  C07C323/52 ,  C07C323/56 ,  C07C323/60 ,  C07C327/30 ,  C07C327/58 ,  C07C331/12 ,  C07D239/38 ,  C07D295/205 ,  C07D295/215 ,  C07D295/26 ,  C07D307/52 ,  C07F9/4006 ,  C07F9/4056 ,  C07C2101/14

Abstract: The present invention relates to a hydrazine derivative represented by the formula (I): ##STR1## (wherein each of Ar.sup.1 and Ar.sup.2 is a substituted or unsubstituted phenyl group, a substituted or unsubstituted heteroaryl group, or the like, R.sup.1 is an alkyl group or the like, and A is a divalent radical having --C.dbd.N--N-- or --CH--NH--N-- as a fundamental skeleton), which is a useful compound as an agricultural and horticultural insecticide.

Abstract translation: 本发明涉及由式（I）表示的肼衍生物：其中Ar1和Ar2各自为取代或未取代的苯基，取代或未取代的杂芳基等，R 1为烷基 A是具有-C = NN-或-CH-NH-N-作为基本骨架的二价基团），其作为农业和园艺杀虫剂是有用的化合物。

公开(公告)号：US5512450A

公开(公告)日：1996-04-30

申请号：US413769

申请日：1995-03-30

Applicant: Gary M. Johnson ,  Robert J. Schaeper

Inventor： Gary M. Johnson ,  Robert J. Schaeper

IPC: G01N33/50 ,  C07C69/12 ,  C07C69/22 ,  C07C69/67 ,  C07C69/68 ,  C07C69/76 ,  C07C69/92 ,  C07C309/64 ,  C07C309/72 ,  C07D207/36 ,  C07D307/58 ,  C07D333/32 ,  C12Q1/00 ,  C12Q1/04 ,  C12Q1/37 ,  C12Q1/44 ,  G01N33/52 ,  C07C69/74

CPC classification number: C12Q1/44 ,  C12Q1/37 ,  C12Q2334/00 ,  C12Q2334/70 ,  Y10S435/805 ,  Y10S436/903

Abstract: A test device for determining the presence of leukocyte cells, esterase or protease in a test sample is disclosed. The test device comprises a carrier matrix having a reagent composition incorporated therein, wherein the reagent composition comprises a lactate ester having the structure ##STR1## wherein A is an alcohol blocking group, and wherein B--O-- is a residue of compound B--OH and provides a detectable response when the lactate ester is hydrolyzed; and a buffer. In a preferred embodiment, the lactate ester has the structure ##STR2## wherein X is O, S or NR.sup.2, R is aryl or lower alkyl, R.sup.1 is hydrogen or lower alkyl, and R.sup.2 is hydrogen, lower alkyl or aryl.

Abstract translation: 公开了一种用于测定测试样品中白细胞，酯酶或蛋白酶的存在的测试装置。 测试装置包括其中掺入试剂组合物的载体基质，其中所述试剂组合物包含具有结构为“IMAGE”的乳酸酯，其中A为醇封闭基团，其中BO为化合物B-OH的残基，并提供 当乳酸酯水解时可检测到的反应; 和缓冲区。 在优选的实施方案中，乳酸酯具有其中X为O，S或NR 2，R为芳基或低级烷基，R 1为氢或低级烷基，且R 2为氢，低级烷基或芳基的结构。

公开(公告)号：US4927807A

公开(公告)日：1990-05-22

申请号：US240567

申请日：1988-09-08

Applicant: Herman H. Stein ,  Jacob J. Pattner ,  Steven R. Crowley

Inventor： Herman H. Stein ,  Jacob J. Pattner ,  Steven R. Crowley

IPC: A61K31/16 ,  A61K31/21 ,  A61K31/215 ,  A61K31/255 ,  A61K31/265 ,  A61K31/42 ,  A61K31/421 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61K38/55 ,  A61P27/02 ,  A61P27/06 ,  A61P43/00 ,  C07C233/16 ,  C07C235/08 ,  C07C237/08 ,  C07C271/22 ,  C07C271/34 ,  C07C305/04 ,  C07C307/06 ,  C07C309/64 ,  C07C317/28 ,  C07C317/44 ,  C07C323/52 ,  C07C323/60 ,  C07C323/64 ,  C07D211/44 ,  C07D211/46 ,  C07D211/74 ,  C07D233/64 ,  C07D263/22 ,  C07D263/24 ,  C07D295/20 ,  C07D405/12 ,  C07D413/06

CPC classification number: A61K38/553 ,  Y10S514/913 ,  Y10S530/86

Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is a substituted amino group; or pharmaceutically acceptable salts or esters thereof.Also disclosed are compositions, methods and kits for treating glaucoma or reducing and/or controlling intraocular pressure wherein the renin inhibiting compound is administered in combination with a beta-adrenergic antagonist, a steroidal antiinflammatory agent or an angiotensin converting enzyme inhibiting compound.

公开(公告)号：US09816054B2

公开(公告)日：2017-11-14

申请号：US12249584

申请日：2008-10-10

Applicant: Sergei Saveliev ,  Daniel Simpson ,  Keith V. Wood ,  Harry Tetsuo Uyeda ,  Carolyn Woodroofe Hitko ,  Dieter Klaubert

Inventor： Sergei Saveliev ,  Daniel Simpson ,  Keith V. Wood ,  Harry Tetsuo Uyeda ,  Carolyn Woodroofe Hitko ,  Dieter Klaubert

IPC: C07C309/64 ,  C11D1/20 ,  C07C309/10 ,  C07C309/14 ,  C07C309/15 ,  C07C309/16 ,  C07C323/12 ,  C07C329/06 ,  C07D307/40 ,  C07D307/56 ,  C07D317/22 ,  C07D333/16 ,  C11D1/14

CPC classification number: C11D1/20 ,  C07C309/10 ,  C07C309/14 ,  C07C309/15 ,  C07C309/16 ,  C07C323/12 ,  C07C329/06 ,  C07D307/40 ,  C07D307/56 ,  C07D317/22 ,  C07D333/16 ,  C11D1/143

Abstract: The invention provides surfactant compounds of formulas I-IX, which can be used in methods for aiding the solubilization, digestion, preparation, analysis, and/or characterization of biological material, for example, proteins or cell membranes. The compounds can also aid in the recovery of peptides generated during protein digestion, particularly for in-gel digestion protocol. Additionally, the compounds can improve enzymatic protein deglycosylation without interfering with downstream sample preparation steps and mass spectrometric analysis. The compounds can be specifically useful as digestion aids that can be decomposed by an acid, by heat, or a combination thereof. Decomposition of the surfactants allows for facile separation from isolated samples, and/or allows for analysis of the sample without interfering with the sensitivity of various analytical techniques.

公开(公告)号：US5463062A

公开(公告)日：1995-10-31

申请号：US116563

申请日：1993-09-07

Applicant: Horst Hemmerle ,  Peter Schindler ,  Andreas Herling

Inventor： Horst Hemmerle ,  Peter Schindler ,  Andreas Herling

IPC: A61K31/185 ,  A61K31/19 ,  A61K31/215 ,  A61K31/22 ,  A61K31/28 ,  A61K31/357 ,  A61K31/37 ,  A61K31/38 ,  A61K31/381 ,  A61K31/395 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/433 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/47 ,  A61P3/08 ,  A61P3/10 ,  C07C59/205 ,  C07C59/80 ,  C07C62/10 ,  C07C69/65 ,  C07C69/708 ,  C07C69/732 ,  C07C69/734 ,  C07C69/738 ,  C07C69/74 ,  C07C69/75 ,  C07C69/753 ,  C07C69/757 ,  C07C69/76 ,  C07C235/40 ,  C07C235/54 ,  C07C255/31 ,  C07C309/02 ,  C07C309/64 ,  C07C311/02 ,  C07D207/16 ,  C07D209/18 ,  C07D209/42 ,  C07D213/02 ,  C07D213/55 ,  C07D213/79 ,  C07D215/48 ,  C07D215/54 ,  C07D233/54 ,  C07D235/06 ,  C07D235/08 ,  C07D239/26 ,  C07D239/34 ,  C07D257/04 ,  C07D285/06 ,  C07D307/85 ,  C07D311/06 ,  C07D317/72 ,  C07D333/02 ,  C07D333/16 ,  C07D333/24 ,  C07D333/28 ,  C07D333/38 ,  C07D333/68 ,  C07D493/04 ,  C07D493/10 ,  C07D495/00 ,  C07D495/04 ,  C07D495/14 ,  C07D521/00 ,  C07D225/04 ,  C07D401/08 ,  C07D403/08

CPC classification number: C07D213/79 ,  C07C69/757 ,  C07D207/16 ,  C07D209/42 ,  C07D213/55 ,  C07D215/48 ,  C07D231/12 ,  C07D233/56 ,  C07D235/06 ,  C07D239/26 ,  C07D249/08 ,  C07D285/06 ,  C07D307/85 ,  C07D333/16 ,  C07D333/24 ,  C07D333/28 ,  C07D333/38 ,  C07D333/68 ,  C07D493/10 ,  C07D495/14 ,  Y02P20/55

Abstract: Cyclohexane derivatives of the formula I ##STR1## in which the radicals R.sup.1 to R.sup.6, X, Y and Z have the stated meanings, and processes for the preparation of these compounds are described. The compounds have valuable pharmacological properties and can therefore be used as pharmaceuticals.

Abstract translation: 描述了其中基团R 1至R 6，X，Y和Z具有所述含义的式I的环己烷衍生物及其制备方法。 这些化合物具有有价值的药理学性质，因此可以用作药物。

公开(公告)号：US5329040A

公开(公告)日：1994-07-12

申请号：US871341

申请日：1992-04-21

Applicant: Lothar Schmitt ,  Rudiger Berthold

Inventor： Lothar Schmitt ,  Rudiger Berthold

IPC: C07C315/04 ,  C07C317/34 ,  C07C317/36 ,  C07C309/69 ,  C07C309/64

CPC classification number: C07C315/04

Abstract: In the process for the continuous preparation of aminoaryl or aminoalkyl .beta.-sulfatoethyl sulfones by reaction of the corresponding .beta.-hydroxyethyl sulfones with sulfuric acid in a molar ratio of 1:1 to 1:1.15 at temperatures above 120 .degree. C. a mixture of a .beta.-hydroxyethyl sulfone with sulfuric acid is supplied to a fluidized bed of end product produced by recycling and mechanical stirring. The mixture is reacted at 100.degree. to 200.degree. C.

Abstract translation: 在连续制备氨基芳基或氨基烷基β-磺基乙基砜的过程中，通过相应的β-羟基乙基砜与硫酸在摩尔比为1:1至1:1.15的温度高于120℃下反应， 用硫酸将β-羟乙基砜供给到通过再循环和机械搅拌生产的最终产物的流化床。 混合物在100至200℃下反应

公开(公告)号：US5082832A

公开(公告)日：1992-01-21

申请号：US423803

申请日：1989-10-18

Applicant: Joseph Cadiergue ,  Jean-Pierre Demoute ,  Jean Tessier

Inventor： Joseph Cadiergue ,  Jean-Pierre Demoute ,  Jean Tessier

IPC: C07C69/74 ,  A01N53/00 ,  A01N53/02 ,  A01N53/04 ,  A01N53/06 ,  A01N53/08 ,  A01N55/00 ,  A01N57/12 ,  A01N57/14 ,  A01N57/36 ,  A23K1/16 ,  A61K31/215 ,  A61K31/23 ,  C07C51/377 ,  C07C61/40 ,  C07C62/02 ,  C07C67/00 ,  C07C67/317 ,  C07C69/63 ,  C07C69/65 ,  C07C69/743 ,  C07C69/757 ,  C07C69/76 ,  C07C253/00 ,  C07C253/30 ,  C07C255/10 ,  C07C255/31 ,  C07C255/53 ,  C07C301/00 ,  C07C303/28 ,  C07C303/30 ,  C07C309/63 ,  C07C309/64 ,  C07C309/65 ,  C07C309/66 ,  C07C309/70 ,  C07C309/72 ,  C07C309/73 ,  C07C317/04 ,  C07C317/14 ,  C07D209/48 ,  C07D209/49 ,  C07D213/30 ,  C07D213/57 ,  C07D213/64 ,  C07D213/647 ,  C07D213/65 ,  C07D213/68 ,  C07D233/64 ,  C07D233/72 ,  C07D307/42 ,  C07D307/45 ,  C07D309/38 ,  C07D317/24 ,  C07F9/09 ,  C07F9/117 ,  C07F9/177 ,  C07F9/38 ,  C07F9/40 ,  C07F9/58 ,  C07F9/655 ,  C07F9/6574

CPC classification number: C07D213/647 ,  A01N53/00 ,  A01N55/00 ,  A01N57/14 ,  A01N57/36 ,  A23K20/00 ,  C07C309/00 ,  C07C309/65 ,  C07C309/66 ,  C07C309/72 ,  C07C61/40 ,  C07C69/757 ,  C07D317/24 ,  C07F9/117 ,  C07F9/177 ,  C07F9/581 ,  C07F9/65502 ,  C07F9/65742 ,  C07C2101/02

Abstract: Novel 2,2-dimethyl-cyclopropane carboxylic acid derivatives of the formula ##STR1## wherein X.sub.1 and X.sub.2 are individually halogen, R.sub.1 is selected from the group consisting of halogen, alkyl of 1 to 8 carbon atoms, optionally substituted aryl of 6 to 14 carbon atoms, perfluoroalkyl of 1 to 8 carbon atoms, --CN and ##STR2## R' is alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of ##STR3## Alk.sub.1 is optionally unsaturated alkyl of 1 to 8 carbon atoms no substituted or substituted with at least one functional group, Ar is aryl of 6 to 14 carbon atoms no substituted or substituted with at least one functional group, Alk.sub.2 and Alk.sub.3 and Alk.sub.2 ' and Alk.sub.3 ' are optionally unsaturated alkyl of 1 to 8 carbon atoms no substituted or substituted with at least one functional group or together with ##STR4## form the rings ##STR5## wherein A is optionally unsaturated alkyl of 1 to 6 carbon atoms optionally substituted with at least one functional group, R" is alkyl of 1 to 6 carbon atoms no substituted or substituted with at least one functional group or aryl of 6 to 14 carbon atoms no substituted or substituted with at least one functional group and R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and residue of an alcohol used in pyrethrinoid esters having pestioidal activity.

公开(公告)号：US20080058542A1

公开(公告)日：2008-03-06

申请号：US11874294

申请日：2007-10-18

Applicant: M. Rahman ,  Francis Houlihan

Inventor： M. Rahman ,  Francis Houlihan

IPC: C07C309/64 ,  C07C323/00 ,  C07C69/00

CPC classification number: G03F7/0045 ,  C07C381/12 ,  G03F7/0392

Abstract: The present invention relates to a novel photoactive compounds that can be used in formulating photoresist compositions.

Abstract translation: 本发明涉及可用于配制光致抗蚀剂组合物的新型光活性化合物。

公开(公告)号：US6121477A

公开(公告)日：2000-09-19

申请号：US230686

申请日：1999-01-29

Applicant: Yoshihiko Yasohara ,  Kenji Miyamoto ,  Shigeru Kawano ,  Junzo Hasegawa

Inventor： Yoshihiko Yasohara ,  Kenji Miyamoto ,  Shigeru Kawano ,  Junzo Hasegawa

IPC: C07C303/30 ,  C07C309/64 ,  C07C309/66 ,  C07C309/73 ,  C07C327/32 ,  C07D317/24 ,  C07C309/75 ,  C07C309/65

CPC classification number: C07C303/30 ,  C07C309/64 ,  C07C309/66 ,  C07C309/73 ,  C07C327/32 ,  C07D317/24 ,  C07B2200/07

Abstract: Optically active 2-aralkyl-3-sulfonyloxy-1-propanol and 2-aralkyl-3-sulfonyloxypropionic acid are provided by using an optically active 2-aralkyl-3-acyloxy-1-propanol as a starting material. Furthermore, an optically active 2-aralkyl-3-thiopropionic acid, which is an important intermediate for synthesis of enkephalinase inhibitors, is provided. According to the present invention, industrially useful optically active sulfonic acid ester derivatives can be provided.

Abstract translation: PCT No.PCT / JP97 / 02699 Sec。 371日期1999年1月29日第 102（e）1999年1月29日PCT PCT 1997年8月1日PCT公布。 公开号WO98 / 05634 日期1998年2月12日光学活性2-芳烷基-3-磺酰氧基-1-丙醇和2-芳烷基-3-磺酰氧基丙酸通过使用光学活性2-芳烷基-3-酰氧基-1-丙醇作为起始原料提供。 此外，提供了作为合成脑啡肽酶抑制剂的重要中间体的光学活性2-芳烷基-3-硫代丙酸。 根据本发明，可提供工业上有用的光学活性磺酸酯衍生物。