公开(公告)号：US07569576B2

公开(公告)日：2009-08-04

申请号：US11332607

申请日：2006-01-12

Applicant: Mark A Gallop ,  Jia-Ning Xiang ,  Fenmei Yao ,  Laxminarayan Bhat

Inventor： Mark A Gallop ,  Jia-Ning Xiang ,  Fenmei Yao ,  Laxminarayan Bhat

IPC: A61K31/515 ,  A61K31/44 ,  C07D317/00 ,  C07D407/00 ,  C07D313/16

CPC classification number: C07D307/89 ,  C07D309/30 ,  C07D313/04

Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.

Abstract translation: 本发明提供GABA类似物的环状1-（酰氧基） - 烷基前体药物，制备GABA类似物的环状1-（酰氧基） - 烷基前体药物的方法和GABA类似物的环状1-（酰氧基）烷基前体药物的组合物。 本发明还提供了使用GABA类似物的环状1-（酰氧基） - 烷基前体药物和GABA类似物的环状1-（酰氧基） - 烷基前体药物组合物的方法。

公开(公告)号：US07321046B2

公开(公告)日：2008-01-22

申请号：US11139949

申请日：2005-05-27

Applicant: Dennis P. Curran ,  Youseung Shin ,  Jean-Hugues Fournier ,  John Mancuso ,  Billy W. Day ,  Arndt Bruckner ,  Yoshikazu Fukui

Inventor： Dennis P. Curran ,  Youseung Shin ,  Jean-Hugues Fournier ,  John Mancuso ,  Billy W. Day ,  Arndt Bruckner ,  Yoshikazu Fukui

IPC: C07D313/04 ,  C07D313/16

CPC classification number: C07C33/02 ,  C07B2200/07 ,  C07C59/10 ,  C07C59/42 ,  C07C69/732 ,  C07C69/734 ,  C07D309/10 ,  C07D309/30 ,  C07D313/00 ,  C07D319/06 ,  C07D407/06 ,  C07F7/1804 ,  Y02P20/55

Abstract: Dictyostatin and its analogs show great promise as new anticancer agents. The present invention provides dictyostatin analogs, synthetic intermediates for the synthesis of dictyostatin analogs, and synthetic methods for the synthesis of such analogs and intermediates. Dictyostatin analogs can have the following structure or its enantiomer wherein R1 is H, an alkyl group, an aryl group, an alkenyl group, an alkynyl group, or a halogen atom; R2 is H, a protecting group, an alkyl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; Ra, Rb and Rc are independently an alkyl group or an aryl group; Rd is an alkyl group, an aryl group, an alkoxylalkyl group, —RiSiRaRbRc or a benzyl group, wherein Ri is an alkylene group; Re is an alkyl group, an allyl group, a benzyl group, an aryl group, an alkoxy group, or —NRgRh, wherein Rg and Rh are independently H, an alkyl group or an aryl group; R3 is (CH2)n where n is and integer in the range of 0 to 5, —CH2CH(CH3)—, —CH═CH—, —CH═C(CH3)—, or —C≡C—; R4 is wherein R23a is H, a protecting group, an alkyl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; R23b is H, a protecting group, an alkyl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe, or R23a and R23b together form a portion of six-membered acetal ring incorporating CRtRu; Rt and Ru are independently H, an alkyl group, an aryl group or an alkoxyaryl group; and R5 is H or OR2b, wherein R2b is H, a protecting group, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; provided that the compound is not dictyostatin 1.

公开(公告)号：US07214705B2

公开(公告)日：2007-05-08

申请号：US10517788

申请日：2003-06-30

Applicant: Jacobus Alphonsus Josephus Van Dun ,  Walter Boudewijn Leopold Wouters ,  Michel Marie François Janicot ,  Ursula Maria Mocek ,  Jodi Ann Laakso

Inventor： Jacobus Alphonsus Josephus Van Dun ,  Walter Boudewijn Leopold Wouters ,  Michel Marie François Janicot ,  Ursula Maria Mocek ,  Jodi Ann Laakso

IPC: A01N43/02 ,  A61K31/335 ,  C07D313/04 ,  C07D313/16

CPC classification number: A61K31/70 ,  C07D313/00 ,  C07H17/04 ,  C12P17/162 ,  C12R1/29

Abstract: The invention provides a compound of formula (I) and pharmaceutically acceptable salts thereof. Processes for the isolating of this bafilomycin metabolite from a novel Micromonospora species, pharmaceutical compositions containing this metabolite and methods of treatment using said metabolite are also described

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐。 还描述了用于从新型小单孢菌属物种分离该巴夫洛霉素代谢物的方法，含有该代谢物的药物组合物和使用所述代谢物的治疗方法

公开(公告)号：US08574607B2

公开(公告)日：2013-11-05

申请号：US13322831

申请日：2010-05-21

Applicant: Jürgen Harry Schaetzer ,  Thomas Pitterna ,  Long Lu ,  Yaming Wu ,  Peter Renold ,  Francesca Perruccio ,  Jérome Yves Cassayre ,  Michel Mueglebach

Inventor： Jürgen Harry Schaetzer ,  Thomas Pitterna ,  Long Lu ,  Yaming Wu ,  Peter Renold ,  Francesca Perruccio ,  Jérome Yves Cassayre ,  Michel Mueglebach

IPC: A01N25/00 ,  A01N43/40 ,  A01N43/42 ,  A61K31/44 ,  C07D215/00 ,  C07D333/64 ,  C07D313/16 ,  C07D311/96 ,  C07D317/72 ,  C07C69/76 ,  C07C229/00 ,  C07C323/00

CPC classification number: C07D491/10 ,  A01N43/90 ,  C07D211/94 ,  C07D495/10

Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.

Abstract translation: 公开了用作农药的式（I）化合物，其中取代基如权利要求1所定义。

公开(公告)号：US20120071547A1

公开(公告)日：2012-03-22

申请号：US13048195

申请日：2011-03-15

Applicant: JYH-HORNG SHEU ,  WEI-HSIEN WANG ,  ZHI-HONG WEN ,  BO-WEI CHEN ,  PING-JYUN SUNG

Inventor： JYH-HORNG SHEU ,  WEI-HSIEN WANG ,  ZHI-HONG WEN ,  BO-WEI CHEN ,  PING-JYUN SUNG

IPC: A61K31/335 ,  C07D313/16 ,  C07D307/87 ,  C07D303/02 ,  C07C69/753 ,  A61P25/00 ,  A61K31/336 ,  A61K31/215 ,  A61P9/10 ,  A61P19/02 ,  A61P37/00 ,  C07D313/00 ,  A61K31/343

CPC classification number: C07C35/23 ,  A61K35/614 ,  C07C69/18 ,  C07C2602/32 ,  C07C2603/26 ,  C07D303/16 ,  C07D307/87 ,  C07D493/08

Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.

Abstract translation: 本发明涉及来自软珊瑚的化合物及其产生。 本发明还涉及来自软珊瑚的化合物在抑制诱导型一氧化氮合酶和/或环加氧酶-2中的用途以及治疗与诱导型一氧化氮合酶和/或环氧合酶-2相关的疾病的用途。

公开(公告)号：US20040087804A1

公开(公告)日：2004-05-06

申请号：US10688926

申请日：2003-10-21

Inventor： Eiji Ohara ,  Ken-ichiro Kawazumi

IPC: C07D313/16

CPC classification number: C07D315/00 ,  B01D3/146

Abstract: A process produces null-caprolactone by the oxidation of cyclohexanone by feeding a crude reaction mixture to a first distillation column; distilling off a first distillate containing low boiling components including unreacted cyclohexanone from the top of the first distillation column; recovering a first side-cut fraction containing unreacted cyclohexanone in a higher concentration than in the first distillate from an intermediate tray; recovering a first bottom liquid containing high boiling components including null-caprolactone from the bottom; introducing the first side-cut fraction to a second distillation column; recovering a second bottom liquid containing unreacted cyclohexanone from the bottom of the second distillation column; recycling the second bottom liquid into the raw material cyclohexanone; introducing the first bottom liquid to a third distillation column to thereby yield a third distillate containing null-caprolactone from the third distillation column.

Abstract translation: 通过将粗反应混合物进料至第一蒸馏塔，通过环己酮的氧化产生ε-己内酯; 从第一蒸馏塔的顶部蒸馏出含有低沸点组分（包括未反应的环己酮）的第一馏出物; 从中间托盘回收含有比在第一馏出物中更高浓度的未反应的环己酮的第一侧馏分; 从底部回收含有高沸点组分（包括ε-己内酯）的第一底液; 将第一侧馏分引入第二蒸馏塔; 从第二蒸馏塔的底部回收含有未反应的环己酮的第二底液; 将第二底液再循环到原料环己酮中; 将第一底液引入第三蒸馏塔，从而从第三蒸馏塔得到含有ε-己内酯的第三馏出物。

公开(公告)号：US20040010152A1

公开(公告)日：2004-01-15

申请号：US10405603

申请日：2003-04-03

Applicant: KYUSHU UNIVERSITY

Inventor： Tsutomu Katsuki ,  Akira Watanabe ,  Tatsuya Uchida

IPC: C07D313/16 ,  C07D313/04 ,  C07D309/00 ,  C07F007/00

CPC classification number: C07D315/00 ,  C07F7/003

Abstract: An optically active lactone compound is produced by using a Zr(salen) complex of the following formula (I) or its enantiomer as a catalyst and subjecting a cyclic ketone compound to a Baeyer-Villiger reaction with at least one oxidizer selected from hydrogen peroxide, aqueous hydrogen peroxide and urea-hydrogen peroxide adduct in a solvent: 1 wherein Ar1 is an aryl group having a carbon number of 10 to 16 and Y is a phenoxy group or an alkoxy group having a carbon number of 1 to 10.

Abstract translation: 通过使用下述式（I）的Zr（salen）配合物或其对映异构体作为催化剂并使环酮化合物与Baeyer-Villiger反应与至少一种选自过氧化氢的氧化剂反应来制备光学活性的内酯化合物， 过氧化氢水溶液和脲 - 过氧化氢加合物，其中Ar 1是碳原子数为10〜16的芳基，Y为苯氧基或碳数为1〜10的烷氧基。

公开(公告)号：US20030175267A1

公开(公告)日：2003-09-18

申请号：US08867612

申请日：1997-06-02

Inventor： YI WANG ,  LOUIS MATIS

IPC: A01N025/00 ,  A01N043/26 ,  A01N043/12 ,  A61K031/335 ,  A61K031/34 ,  C12P021/08 ,  C07K016/00 ,  C07D313/16 ,  C07D313/06 ,  A61K039/395 ,  C07D307/94 ,  C07D311/96

CPC classification number: C07K16/18 ,  A61K38/00 ,  Y10S424/81 ,  Y10S436/821 ,  Y10S514/825 ,  Y10S514/885 ,  Y10S530/868

Abstract: The use of compounds that block complement component or its active fragments C5a and/or C5b (such compounds collectively referred to as nullC5 blockersnull) to treat established joint inflammation (arthritis) is disclosed. Administration of such C5 blockers has been found to: 1) arrest and/or reduce inflammation in joints which are already inflamed, and 2) inhibit the spread of inflammation to unaffected joints.

Abstract translation: 公开了使用封闭补体成分或其活性片段C5a和/或C5b（这些化合物统称为“C5阻断剂”）来治疗已建立的关节炎症（关节炎）的化合物。 已经发现这种C5阻滞剂的施用：1）阻止和/或减少已经发炎的关节炎症，和2）抑制炎症扩散到未受影响的关节。

公开(公告)号：US20010053858A1

公开(公告)日：2001-12-20

申请号：US09729408

申请日：2000-12-04

Inventor： Erik Bruce Tjaden ,  John Robert Briggs ,  Anil Sakharam Guram ,  John Michael Maher

IPC: C07D313/04 ,  C07D313/16

CPC classification number: C07D315/00 ,  C07C67/38 ,  Y02P20/582 ,  C07C69/675

Abstract: This invention relates in part to processes for producing one or more substituted or unsubstituted epsilon caprolactones and/or hydrates and/or esters thereof which comprise subjecting one or more substituted or unsubstituted penten-1-ols to carbonylation in the presence of a carbonylation catalyst, e.g., a metal-organophosphorus ligand complex catalyst, to produce said one or more substituted or unsubstituted epsilon caprolactones and/or hydrates and/or esters thereof. The substituted and unsubstituted epsilon caprolactones and/or hydrates and/or esters thereof produced by the processes of this invention can undergo further reaction(s) to afford desired derivatives thereof, e.g., epsilon caprolactam. This invention also relates in part to reaction mixtures containing one or more substituted or unsubstituted epsilon caprolactones and/or hydrates and/or esters thereof as principal product(s) of reaction.

公开(公告)号：US08853426B2

公开(公告)日：2014-10-07

申请号：US13881544

申请日：2011-10-11

Applicant: Kazuaki Ishihara ,  Muhammet Uyanik

Inventor： Kazuaki Ishihara ,  Muhammet Uyanik

IPC: C07D313/16 ,  C07B33/00 ,  C07D307/83 ,  C07D309/30 ,  C07D313/04 ,  C07D307/935 ,  C07D323/04 ,  C07D307/33 ,  C07D307/77 ,  C07D307/88 ,  C07D307/79

CPC classification number: C07D313/04 ,  C07B33/00 ,  C07C37/56 ,  C07C67/42 ,  C07D307/33 ,  C07D307/77 ,  C07D307/79 ,  C07D307/83 ,  C07D307/88 ,  C07D307/935 ,  C07D309/30 ,  C07D323/04 ,  C07C69/24 ,  C07C39/28

Abstract: The present invention relates to a method for manufacturing an ester from a ketone or an aldehyde, which is a reactive substrate, by a Baeyer-Villiger oxidation reaction using hydrogen peroxide, and in this method, as a catalyst, M(BAr4)n, which is a metal borate, is used (M represents an alkali metal or an alkaline earth metal; Ar represents an aryl; and n is the same number as the valence of M). For example, when cyclohexanone was used as the reactive substrate, and Sr[B(3,5-CF3C6H3)4]2 was used as the catalyst, ε-caprolactone was obtained at an isolated yield of 82%.

Abstract translation: 本发明涉及通过使用过氧化氢的Baeyer-Villiger氧化反应从作为反应性底物的酮或醛制造酯的方法，在该方法中，作为催化剂M（BAr4）n， 使用金属硼酸盐（M表示碱金属或碱土金属; Ar表示芳基; n表示与M的化合价相同的数）。 例如，当使用环己酮作为反应性底物，并且使用Sr [B（3,5-CF 3 C 6 H 3）4] 2作为催化剂时，以82％的分离收率得到ε-己内酯。