公开(公告)号：US20100249197A1

公开(公告)日：2010-09-30

申请号：US12477493

申请日：2009-06-03

Applicant: Clare J. Watkins ,  Maria Rosario Romero-Martin ,  Kathryn G. Moore ,  James Ritchie ,  Paul W. Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Igor Starchenkov ,  Klara Dikovska ,  Rasma Bokaldere ,  Vija Gailite ,  Maxim Vorona ,  Victor Andrianov ,  Daina Lolya ,  Valentina Semenikhina ,  Andris Amolins ,  C. John Harris ,  James E.S. Duffy

Inventor： Clare J. Watkins ,  Maria Rosario Romero-Martin ,  Kathryn G. Moore ,  James Ritchie ,  Paul W. Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Igor Starchenkov ,  Klara Dikovska ,  Rasma Bokaldere ,  Vija Gailite ,  Maxim Vorona ,  Victor Andrianov ,  Daina Lolya ,  Valentina Semenikhina ,  Andris Amolins ,  C. John Harris ,  James E.S. Duffy

IPC: A61K31/4406 ,  C07C259/06 ,  A61K31/165 ,  A61P35/00 ,  A61P17/06 ,  C07C259/08 ,  C07D317/54 ,  A61K31/36 ,  C07D213/56 ,  C07D307/54 ,  A61K31/341

CPC classification number: C07D207/337 ,  A61K31/16 ,  A61K31/195 ,  A61K31/198 ,  A61K31/277 ,  A61K31/38 ,  A61K31/381 ,  A61K31/426 ,  C07C233/49 ,  C07C233/83 ,  C07C235/34 ,  C07C237/36 ,  C07C255/57 ,  C07C259/06 ,  C07C259/08 ,  C07C2603/18 ,  C07D207/40 ,  C07D207/404 ,  C07D209/14 ,  C07D209/16 ,  C07D209/18 ,  C07D209/22 ,  C07D213/06 ,  C07D213/55 ,  C07D213/56 ,  C07D233/04 ,  C07D233/08 ,  C07D235/14 ,  C07D235/24 ,  C07D271/06 ,  C07D307/34 ,  C07D307/54 ,  C07D317/60 ,  C07D333/24 ,  C07D333/60 ,  C07D403/12 ,  Y02A50/411

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(═O)— and —C(═O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psorias

Abstract translation: 本发明涉及抑制HDAC活性的一些活性氨基甲酸化合物，其具有式（1）其中：A为芳基; Q1是具有至少2个碳原子的骨架的芳基前导基团; J是选自：-NR 1 C（= O） - 和-C（= O）NR 1 - 的酰胺键; R1是酰氨基取代基; 而Q2是酸性引导组; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，并且例如抑制增殖性疾病如癌症和牛皮癣

公开(公告)号：US20090258901A1

公开(公告)日：2009-10-15

申请号：US12403311

申请日：2009-03-12

Applicant: Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Joanne M. Holland ,  Paul E. Persons ,  Heike Radeke ,  Fengjiang Wang ,  Liming Ahao

Inventor： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Joanne M. Holland ,  Paul E. Persons ,  Heike Radeke ,  Fengjiang Wang ,  Liming Ahao

IPC: A61K31/445 ,  C07D211/22 ,  C07D211/20 ,  A61P35/00

CPC classification number: C40B40/04 ,  C07B2200/11 ,  C07C255/46 ,  C07C2601/04 ,  C07D205/02 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D211/12 ,  C07D211/16 ,  C07D211/18 ,  C07D211/20 ,  C07D211/26 ,  C07D211/32 ,  C07D211/40 ,  C07D211/42 ,  C07D211/60 ,  C07D233/04 ,  C07D233/10 ,  C07D265/30 ,  C07D267/10 ,  C07D303/08 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C40B30/04 ,  C40B50/14

Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

Abstract translation: 本发明的一个方面涉及杂环化合物。 本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。 本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病， 精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。 本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。

公开(公告)号：US06911546B2

公开(公告)日：2005-06-28

申请号：US10330853

申请日：2002-12-26

Applicant: James Lupton Hedrick ,  Pinar Kilickiran ,  Gregory Walker Nyce ,  Robert M. Waymouth

Inventor： James Lupton Hedrick ,  Pinar Kilickiran ,  Gregory Walker Nyce ,  Robert M. Waymouth

IPC: C07C59/285 ,  C07C67/03 ,  C07C68/06 ,  C07D233/02 ,  C07D233/04 ,  C07D233/06 ,  C07D233/16 ,  C07D233/54 ,  C07D307/33 ,  C07F1/00 ,  C07D233/38 ,  C07F2/46

CPC classification number: C07D233/16 ,  C07C59/285 ,  C07C67/03 ,  C07C68/06 ,  C07D233/02 ,  C07D233/04 ,  C07D233/06 ,  C07D233/54 ,  C07D307/33 ,  C07F1/00 ,  C07C69/82 ,  C07C69/96

Abstract: A method is provided for carrying out depolymerization of a polymer containing electrophilic linkages in the presence of a catalyst and a nucleophilic reagent, wherein production of undesirable byproducts resulting from polymer degradation is minimized. The reaction can be carried out at a temperature of 80° C. or less, and generally involves the use of an organic, nonmetallic catalyst, thereby ensuring that the depolymerization product(s) are substantially free of metal contaminants. In an exemplary depolymerization method, the catalyst is a carbene compound such as an N-heterocyclic carbene, or is a precursor to a carbene compound. The method provides an important alternative to current recycling techniques such as those used in the degradation of polyesters, polyamides, and the like.

Abstract translation: 提供了一种在催化剂和亲核试剂的存在下进行含有亲电键的聚合物解聚的方法，其中由聚合物降解产生的不需要的副产物的产生最小化。 反应可以在80℃或更低的温度下进行，通常涉及使用有机非金属催化剂，从而确保解聚产物基本上不含金属污染物。 在示例性的解聚方法中，催化剂是卡宾化合物如N-杂环卡宾，或是卡宾化合物的前体。 该方法提供了当前回收技术的重要替代方法，例如用于降解聚酯，聚酰胺等的那些。

公开(公告)号：US20030149273A1

公开(公告)日：2003-08-07

申请号：US10279895

申请日：2002-10-24

Inventor： Hans-Christian Militzer ,  Ulrich Scholz ,  Wolfgang A. Herrmann ,  Christian Gstottmayr

IPC: C07F015/00 ,  C07D207/46

CPC classification number: C07D233/56 ,  C07C1/321 ,  C07C2531/22 ,  C07D233/04 ,  C07F15/006 ,  C07F15/0086 ,  C07F15/04 ,  C07C15/14

Abstract: The present invention relates to a process for preparing polyaryl compounds by coupling aryl halides or aryl sulphonates and reactive aryl compounds in the presence of novel transition metal complexes of N-heterocyclic carbenes which, just like the N-heterocyclic carbenes themselves and the salts from which they are derived, form part of the invention.

Abstract translation: 本发明涉及在N-杂环卡宾的新型过渡金属络合物存在下偶合芳基卤化物或芳基磺酸盐和反应性芳基化合物来制备聚芳基化合物的方法，其正如N-杂环卡宾本身及其盐 它们是衍生的，构成本发明的一部分。

公开(公告)号：US4127489A

公开(公告)日：1978-11-28

申请号：US708980

申请日：1976-07-27

Applicant: Hans J. Pracht ,  Joseph P. Nirschl

Inventor： Hans J. Pracht ,  Joseph P. Nirschl

IPC: C07D233/04 ,  D06M13/473 ,  D06M13/34

CPC classification number: D06M13/473 ,  C07D233/04

Abstract: A process for making quaternary imidazolinium fabric conditioning agents essentially free of amines, amine salts and alkoxylated forms of the quaternary imidazolinium salts. An aqueous liquid fabric conditioning composition containing quaternary imidazolinium conditioning agents essentially free of amines and amine salts possesses desirable stability and conditioning properties.

Abstract translation: 制备基本上不含季胺咪唑鎓盐的胺，胺盐和烷氧基化形式的季咪唑啉织物调理剂的方法。 含有基本上不含胺和胺盐的季咪唑啉调理剂的水性液体织物调理组合物具有期望的稳定性和调理性能。

公开(公告)号：US3926994A

公开(公告)日：1975-12-16

申请号：US47275974

申请日：1974-05-23

Applicant: WYETH JOHN & BROTHER LTD

Inventor： WHITE ALAN CHAPMAN ,  BLACK ROBIN MICHAEL

IPC: C07D209/38 ,  C07D233/04 ,  C07D233/20 ,  C07D233/22 ,  C07D239/06 ,  C07D243/04 ,  C07D245/02 ,  C07D487/04 ,  C07D491/20 ,  C07D239/00

CPC classification number: C07D487/04 ,  C07D209/38 ,  C07D233/04 ,  C07D233/20 ,  C07D233/22 ,  C07D239/06 ,  C07D243/04 ,  C07D245/02 ,  Y10S514/866

Abstract: OR AN ACID ADDITION SALT THEREOF WHEREIN N REPRESENTS 0, 1, 2 OR 3, R3 and R4 which may be the same or different represent hydrogen or lower alkyl radicals or R3 represents hydrogen and R4 represents hydroxy, Ph is a phenyl group optionally substituted by one or more hydroxyl, lower alkyl, lower alkoxy, haloloweralkyl, halogen, amino or mono or di(lower)alkylamino groups,, R is a hydroxyl, acyloxy, alkoxy or halo group, R1 is a substituted or unsubstituted phenyl or naphthyl radical and R6 is hydrogen, lower alkyl, or acyl. The compounds have hypoglycemic activity.

The disclosure relates to derivatives of tetrahydropyrimidine, imidazoline, tetrahydro-1H-1,3-diazepine and hexahydro-1,3diazocine of the general formula

Abstract translation: 本公开涉及通式为四氢嘧啶，咪唑啉，四氢-1H-1,3-二氮杂和六氢-1,3-二氮辛啶的衍生物或其中N代表0,1,2或3，R3和 可以相同或不同的R 4表示氢或低级烷基，或者R 3表示氢，R 4表示羟基，Ph是任选被一个或多个羟基，低级烷基，低级烷氧基，卤代低级烷基，卤素，氨基或单环或 二（低级）烷基氨基，R是羟基，酰氧基，烷氧基或卤素基团，R 1是取代或未取代的苯基或萘基，R 6是氢，低级烷基或酰基。 该化合物具有降血糖活性。

公开(公告)号：US3148150A

公开(公告)日：1964-09-08

申请号：US10209361

申请日：1961-04-11

Applicant: PETROLITE CORP

Inventor： DE GROOTE MELVIN ,  KWAN-TING SHEN

IPC: C02F5/12 ,  C07C215/00 ,  C07D233/04

CPC classification number: C02F5/12 ,  C07C215/00 ,  C07D233/04 ,  Y10S159/13

公开(公告)号：US2695884A

公开(公告)日：1954-11-30

申请号：US28164952

申请日：1952-04-10

Applicant: PETROLITE CORP

Inventor： HOWARD SMITH ALVIN

IPC: C07D233/04 ,  C10G33/04

CPC classification number: C10G33/04 ,  C07D233/04

公开(公告)号：US09266821B2

公开(公告)日：2016-02-23

申请号：US12580467

申请日：2009-10-16

Applicant: Upali Weerasooriya ,  John Boorem ,  Brian Hodle ,  Aaron Boorem ,  Peter Radford ,  Howard Stevenson ,  G. Gerald Barr

Inventor： Upali Weerasooriya ,  John Boorem ,  Brian Hodle ,  Aaron Boorem ,  Peter Radford ,  Howard Stevenson ,  G. Gerald Barr

IPC: C07D233/04 ,  C07C231/02 ,  C07C233/36

CPC classification number: C07C231/02 ,  C07D233/04 ,  C07C233/36

Abstract: A process for reacting, in the presence of a particular calcium containing catalyst, an amine having an active hydrogen and one or more of a fatty acid ester or a fatty acid.

Abstract translation: 在特定含钙催化剂存在下使具有活性氢和一种或多种脂肪酸酯或脂肪酸的胺反应的方法。

公开(公告)号：US09179675B2

公开(公告)日：2015-11-10

申请号：US14587929

申请日：2014-12-31

Applicant: Marrone Bio Innovations, Inc.

Inventor： Huazhang Huang ,  Ratnakar Asolkar

IPC: A01N37/02 ,  A01N37/06 ,  A01N37/10 ,  A01N37/18 ,  A01N43/36 ,  A01N43/40 ,  A01N43/46 ,  C07C233/05 ,  C07C233/06 ,  C07C233/11 ,  C07D295/185 ,  C07C57/42 ,  C07D207/06 ,  C07D211/16 ,  C07D233/04 ,  C11B1/00 ,  C07C57/44 ,  C07C69/587 ,  C07C233/08

CPC classification number: A01N43/36 ,  A01N37/02 ,  A01N37/06 ,  A01N37/10 ,  A01N37/18 ,  A01N43/40 ,  A01N43/46 ,  C07C57/42 ,  C07C57/44 ,  C07C69/587 ,  C07C233/05 ,  C07C233/06 ,  C07C233/08 ,  C07C233/11 ,  C07C2601/08 ,  C07D207/06 ,  C07D211/16 ,  C07D223/04 ,  C07D233/04 ,  C07D295/185 ,  C11B1/00

Abstract: Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.