公开(公告)号：US11078157B1

公开(公告)日：2021-08-03

申请号：US16262281

申请日：2019-01-30

Applicant: University of Oregon

Inventor： Michael D. Pluth ,  Matthew M. Cerda

IPC: C07D311/16 ,  C07C325/00 ,  C07C327/22 ,  C07C327/26 ,  G01N33/84

Abstract: Disclosed herein are embodiments of a donor compound that releases H2S by reacting with a reactive compound. The donor compound embodiments described herein can be used to deliver H2S to a subject or a sample and further can be used to administer therapeutic agents. The donor compound embodiments also can facilitate bioconjugation. Methods of making and using the donor compound embodiments also are disclosed.

公开(公告)号：US20190315683A1

公开(公告)日：2019-10-17

申请号：US16443793

申请日：2019-06-17

Applicant: Promentis Pharmaceuticals, Inc.

Inventor： Michael Neary ,  James Nieman ,  Steven Tanis ,  Daniel Lawton ,  Garry Smith

IPC: C07C327/34 ,  C07C323/60 ,  C07D277/14 ,  C07C327/26 ,  C07D277/08 ,  C07C327/32 ,  C07C329/06 ,  C07C323/59 ,  C07C323/58 ,  C07C323/57 ,  C07D241/08 ,  C07D327/04

Abstract: Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.

公开(公告)号：US10005860B2

公开(公告)日：2018-06-26

申请号：US15428940

申请日：2017-02-09

Applicant: Basell Poliolefine Italia S.r.l.

Inventor： Alessandro Mignogna ,  Reynald Chevalier ,  Igor Kashulin ,  Ilya Nifant'ev ,  Giampiero Morini ,  Martin Schneider

IPC: C08F110/06 ,  C07C327/26 ,  C07C327/28 ,  C07C329/10 ,  C07C333/04

CPC classification number: C08F110/06 ,  C07C327/26 ,  C07C327/28 ,  C07C329/10 ,  C07C333/04 ,  C08F4/651 ,  C08F2500/12 ,  C08F2500/15 ,  C08F4/6545

Abstract: Catalyst component for the polymerization of olefins comprising Mg, Ti and an electron donor of formula (I) In which X and Y are selected from, R1, and —OR1 and —NR2, B is oxygen or sulphur S is sulphur, R1 is selected from C1-C15 hydrocarbon groups, optionally contain a heteroatom selected from halogen, P, S, N, O and Si, which can be fused together to form one or more cycles, R is hydrogen or R1 and A is a bivalent bridging group with chain length between the two bridging bonds being 1-10 atoms.

公开(公告)号：US20030187288A1

公开(公告)日：2003-10-02

申请号：US10385725

申请日：2003-03-09

Applicant: Nippon Shokubai Co., Ltd.

Inventor： Yoshiyuki Takahashi ,  Yoichi Hino ,  Tatsuhito Matsuda

IPC: C07C327/00 ,  C07C327/26

CPC classification number: C08F22/105 ,  C07C327/22 ,  C07C327/28

Abstract: A thiol carboxylate ester as shown by general formula (I) below, which has a half ester content of 0.0001 to 2 mass %, and favorably, which has a halogen content of not more than 2 mass % and/or to which a polymerization inhibitor such as a catechol family member is added. 1

Abstract translation: 如下述通式（I）所示的硫醇羧酸酯，其半酯含量为0.0001〜2质量％，有利地为卤素含量为2质量％以下，和/或聚合抑制剂 如儿茶酚家族成员。

公开(公告)号：US5986129A

公开(公告)日：1999-11-16

申请号：US903663

申请日：1997-07-31

Applicant: Guido Di Napoli

Inventor： Guido Di Napoli

IPC: A61K8/30 ,  A61K8/00 ,  A61K8/35 ,  A61K8/36 ,  A61K8/368 ,  A61K8/41 ,  A61K31/19 ,  A61P43/00 ,  A61Q19/00 ,  C07C51/06 ,  C07C51/09 ,  C07C51/353 ,  C07C51/367 ,  C07C51/373 ,  C07C66/02 ,  C07C67/00 ,  C07C69/02 ,  C07C69/16 ,  C07C69/95 ,  C07C227/20 ,  C07C229/66 ,  C07C229/74 ,  C07C237/30 ,  C07C237/40 ,  C07C327/16 ,  C07C327/26 ,  C07C59/76 ,  C07C67/02

CPC classification number: C07C66/02 ,  C07C229/66 ,  Y02P20/55

Abstract: The following description sets forth a process for producing rhein, diacerhein and other diacyl derivatives thereof, which comprises the following steps: treatment of a diphenylketone ##STR1## in which R.sub.1 is --OR', --NR'R", --SR', where R' and R" are H, an alkyl or aromatic group; R.sub.2 is H or a protective group, R.sub.3 is --OH or C.sub.1 -C.sub.4 alkyl, with an acid or superacid to give a 1-aminoanthraquinone derivative, diazotisation, replacement of the --NH.sub.2 group by --OH, optional removal of the protective group, and acylation.

Abstract translation: 下面的描述阐述了生产大黄酸，二烯酰亚胺和其它二酰基衍生物的方法，其包括以下步骤：处理其中R 1是-OR'， - NR'R“，-SR'的二苯基酮，其中R' 和R“是H，烷基或芳基; R2是H或保护基团，R3是-OH或C1-C4烷基，与酸或超酸反应得到1-氨基蒽醌衍生物，重氮化，-NH 2基团被-OH取代，任选地除去保护基团， 和酰化。

公开(公告)号：US5807889A

公开(公告)日：1998-09-15

申请号：US504847

申请日：1995-06-06

Applicant: Jens K. Perregaard

Inventor： Jens K. Perregaard

IPC: C07D295/12 ,  A61K31/136 ,  A61K31/34 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/445 ,  A61K31/495 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/30 ,  C07C211/58 ,  C07C211/60 ,  C07C233/15 ,  C07C233/43 ,  C07C233/80 ,  C07C255/58 ,  C07C275/26 ,  C07C275/28 ,  C07C275/40 ,  C07C311/05 ,  C07C311/08 ,  C07C311/21 ,  C07C327/22 ,  C07C327/26 ,  C07D209/14 ,  C07D233/32 ,  C07D233/36 ,  C07D307/81 ,  C07D333/58 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12

CPC classification number: C07D233/32 ,  C07C211/60 ,  C07C233/43 ,  C07C233/80 ,  C07C275/40 ,  C07C311/08 ,  C07D209/14 ,  C07D307/81 ,  C07D333/58 ,  C07C2101/08 ,  C07C2101/14 ,  C07C2102/08

Abstract: Compounds of formula I ##STR1## wherein R1=(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2=H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5=H, halo, alkyl, alkoxy, etc.; R6,R7=H, alkyl; R6R7=atoms to complete a ring; R8,R9=groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other=CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8-OH DPAT cue agonism test in rats.

Abstract translation: 式I的化合物其中R 1 =（环）烷（烯）基，芳烷基，烷基（氧基）羰基，CONH 2等; R2 = H，（环）烷（en）基，芳烷基等; R3-R5 = H，卤素，烷基，烷氧基等; R6，R7 = H，烷基; R6R7 =原子完成环; R8，R9 = R2，2-氧代咪唑烷基烷基等引用的基团; NR8R9 =杂环基; 1的X，Y = CH 2，另一个= CH 2，O，S。 因此，将1-二氢化茚羧酸按5分钟转化为ED50为0.0055.mu.M / kg·s的1-（N，N-二丙基氨基甲基）-6-甲酰氨基茚满草酸盐。 在大鼠的8-OH DPAT提示激动试验中。

公开(公告)号：US5770758A

公开(公告)日：1998-06-23

申请号：US770353

申请日：1996-12-20

Applicant: Walter Kunz ,  Beat Jau

Inventor： Walter Kunz ,  Beat Jau

IPC: C07C323/62 ,  C07C20060101 ,  C07C319/02 ,  C07C319/12 ,  C07C323/33 ,  C07C323/34 ,  C07C323/47 ,  C07C323/49 ,  C07C323/63 ,  C07C323/64 ,  C07C327/26 ,  C07C335/16 ,  C07C335/22 ,  C07D20060101 ,  C07D277/82 ,  C07D285/00 ,  C07D285/01 ,  C07D285/06 ,  C07D285/14 ,  C07D417/04 ,  C07C255/07 ,  C07C321/08 ,  C07C327/16

CPC classification number: C07D285/14 ,  C07C319/02 ,  C07C319/12 ,  C07C323/63 ,  C07C327/26 ,  C07C335/22 ,  C07D277/82

Abstract: Compounds of the formula I ##STR1## and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III ##STR2## In the compounds of the formulae I and III: X is halogen, n is 0,1,2 or 3; Z is CN, CO-A or CS-A, A is hydrogen, halogen, OR.sub.1, SR.sub.2 and N(R.sub.3)R.sub.4 ; R.sub.1 to R .sub.4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R.sub.3 and R.sub.4, together with the nitrogen atom to which they are bonded, are a 5- or 6-membered, substituted or unsubstituted heterocyclic radical having 1-3 heteroatoms O,S and/or N. Processes for the preparation of compounds of the formula I are described.

Abstract translation: 式I的化合物及其二硫化物及其盐是制备具有式III的杀微生物和植物免疫作用的化合物的重要的中间产物。在式I和III的化合物中 X为卤素，n为0,1,2或3; Z是CN，CO-A或CS-A，A是氢，卤素，OR1，SR2和N（R3）R4; R 1至R 4为氢，取代或未取代的含有不超过8个碳原子的开链，饱和或不饱和烃基，取代或未取代的含有不多于10个碳原子的环状，饱和或不饱和烃基，取代或未取代的 未取代的苄基或苯乙基，取代或未取代的不超过8个碳原子的烷酰基，取代或未取代的苯甲酰基或取代或未取代的杂环基; 或R 3和R 4与它们所键合的氮原子一起是具有1-3个杂原子O，S和/或N的5或6元取代或未取代的杂环基。用于制备 描述了式I。

公开(公告)号：US5340807A

公开(公告)日：1994-08-23

申请号：US989906

申请日：1992-12-11

Applicant: Toshiaki Kumazawa ,  Masashi Yanase ,  Hiroyuki Harakawa ,  Hiroyuki Obase ,  Shoji Oda ,  Shiro Shirakura ,  Koji Yamada ,  Kazuhiro Kubo

Inventor： Toshiaki Kumazawa ,  Masashi Yanase ,  Hiroyuki Harakawa ,  Hiroyuki Obase ,  Shoji Oda ,  Shiro Shirakura ,  Koji Yamada ,  Kazuhiro Kubo

IPC: A61K31/335 ,  A61K31/165 ,  A61K31/18 ,  A61K31/19 ,  A61K31/215 ,  A61K31/235 ,  A61K31/275 ,  A61K31/38 ,  A61K31/435 ,  A61K31/44 ,  A61K31/55 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07C233/65 ,  C07C235/46 ,  C07C235/48 ,  C07C237/40 ,  C07C323/40 ,  C07C323/62 ,  C07C327/26 ,  C07C331/08 ,  C07D221/16 ,  C07D223/20 ,  C07D233/58 ,  C07D313/12 ,  C07D337/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/044 ,  C07D495/04 ,  A01N43/46 ,  C07D273/02 ,  C07D313/06

CPC classification number: C07D491/04 ,  C07C233/65 ,  C07D223/20 ,  C07D313/12 ,  C07D337/12 ,  C07C2103/32 ,  Y10S514/824

Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.

Abstract translation: 公开了由式（I）表示的三环化合物：其中R 1，R 2，R 3和R 4各自独立地表示氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基， C 1-6烷基氨基，卤代C 1-6烷基，卤代C 1-6烷氧基，卤素，硝基，氰基，羧基，C 1-6烷氧基羰基，羟甲基，CR 9 R 10 CO 2 R 11（其中R 9，R 10和R 11各自独立地表示氢或C 1-6烷基） 或CONR 12 R 13（其中R 12和R 13各自独立地表示氢或C 1-6烷基）; R5表示氢或C1-6烷基; R 6，R 7和R 8各自独立地表示氢，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷酰氧基，C 1-6烷硫基，氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O，CH2-（O）n，（其中n表示0,1或2），CH2CH2，CH = CH或CON（R14）（其中R14表示氢或C1-6烷基）和Z 表示氧或硫，或其药学上可接受的盐。 该化合物具有酰基辅酶A：胆固醇酰基转移酶抑制活性，因此预期对高脂血症和动脉硬化具有预防和治疗作用。

公开(公告)号：US5241108A

公开(公告)日：1993-08-31

申请号：US624009

申请日：1990-12-07

Applicant: Gerhard Horpel ,  Karl-Heinz Nordsiek

Inventor： Gerhard Horpel ,  Karl-Heinz Nordsiek

IPC: C07C327/36 ,  C07C327/26 ,  C08G75/14 ,  C08K5/36 ,  C08K5/38 ,  C08L21/00

CPC classification number: C08K5/38 ,  C07C327/26 ,  C08G75/14 ,  C08L21/00

Abstract: Polysulfide derivatives having the general formula (A--S--S--).sub.2 X--S--S--A, processes for their production and their use for crosslinking of reversion-stable rubber vulcanizates are provided. Crosslinking with reduced reversion and loss of elastomeric properties with age is achieved by the crosslinking system provided by the invention.

Abstract translation: 提供了具有通式（A-S-S-）2 X-S-S-A的多硫化物衍生物及其制备方法及其用于交换回复稳定的橡胶硫化橡胶。 通过本发明提供的交联体系实现了具有降低的回复和随着年龄的弹性体特性损失的交联。

公开(公告)号：US5223637A

公开(公告)日：1993-06-29

申请号：US889388

申请日：1992-05-28

Applicant: Kazutoshi Kuroda ,  Hiroshi Kase ,  Katsuhiko Ando ,  Isao Kawamoto ,  Toru Yasuzawa ,  Hiroshi Sano ,  Joji Goto ,  Koji Yamada

Inventor： Kazutoshi Kuroda ,  Hiroshi Kase ,  Katsuhiko Ando ,  Isao Kawamoto ,  Toru Yasuzawa ,  Hiroshi Sano ,  Joji Goto ,  Koji Yamada

IPC: C07C323/20 ,  C07C327/26 ,  C12P7/00

CPC classification number: C07C323/20 ,  C07C327/26 ,  C12P7/00

Abstract: KS-506a, KS-506x and KS-506g having an activity to inhibit cyclic nucleotide phosphodiesterase and KS-506m and KS-506h having an activity to inhibit histamine release are produced by culturing a microorganism belonging to the genus Mortierella.

Abstract translation: 通过培养属于被孢霉属属的微生物来产生具有抑制环核苷酸磷酸二酯酶的活性的KS-506a，KS-506x和KS-506g以及具有抑制组胺释放活性的KS-506m和KS-506h。