公开(公告)号：US08987335B2

公开(公告)日：2015-03-24

申请号：US13586603

申请日：2012-08-15

Applicant: Hariprasad Vankayalapati ,  Venkataswamy Sorna ,  Steven L. Warner ,  Bret Stephens ,  David J. Bearss ,  Sunil Sharma

Inventor： Hariprasad Vankayalapati ,  Venkataswamy Sorna ,  Steven L. Warner ,  Bret Stephens ,  David J. Bearss ,  Sunil Sharma

IPC: A01N33/26 ,  A01N31/08 ,  A61K31/05 ,  C07C241/00 ,  C07C243/00 ,  C07D295/26 ,  C07C311/16 ,  C07C311/46 ,  C07D205/04 ,  C07D295/155

CPC classification number: A61K31/4453 ,  A61K31/18 ,  A61K31/397 ,  A61K31/40 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/5377 ,  C07C311/16 ,  C07C311/46 ,  C07D205/04 ,  C07D295/155 ,  C07D295/26

Abstract: In one aspect, the invention relates to substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract translation: 一方面，本发明涉及可用作赖氨酸特异性组蛋白脱甲基酶（包括LSD1）的抑制剂的取代的（E）-N' - （1-苯基亚乙基）苯甲酰肼类似物，其衍生物和相关化合物。 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用化合物和组合物治疗与LSD1功能障碍相关的疾病的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

公开(公告)号：US20150038687A1

公开(公告)日：2015-02-05

申请号：US14373828

申请日：2013-01-23

Applicant: BAKHU LIMITED

Inventor： Lee Proctor

IPC: C07C241/00

CPC classification number: C07C241/00 ,  C07C243/04 ,  C07C245/16 ,  C07C2531/02

Abstract: The present invention relates to a method of forming diazoalkanes. One aspect of the present invention provides a method for the production of a N-alkyl-N-nitroso compound from a starting material, comprising the use of a tribasic acid to acidify an amine. A second aspect of the present invention provides a method for the production of a diazoalkane, comprising reacting a N-alkyl-N-nitroso compound with a base and a phase transfer catalyst, wherein no organic solvent is used.

Abstract translation: 本发明涉及形成重氮烷烃的方法。 本发明的一个方面提供了从原料制备N-烷基-N-亚硝基化合物的方法，其包括使用三元酸酸化胺。 本发明的第二方面提供了一种制备重氮烷的方法，包括使N-烷基-N-亚硝基化合物与碱和相转移催化剂反应，其中不使用有机溶剂。

公开(公告)号：US08754260B2

公开(公告)日：2014-06-17

申请号：US13682767

申请日：2012-11-21

Applicant: Xerox Corporation

Inventor： Adrien P Cote ,  Amanda L Bongers

IPC: C07C241/00 ,  C07C243/00 ,  C07C249/00 ,  C07C251/00 ,  C07C211/00

CPC classification number: C07C209/74 ,  C07C221/00 ,  C07C225/22

Abstract: A method for making fluoroacyl arylamines is disclosed.

Abstract translation: 公开了一种制备氟酰基芳基胺的方法。

公开(公告)号：US08748411B2

公开(公告)日：2014-06-10

申请号：US11920031

申请日：2006-05-05

Applicant: Rolando Eduardo Rodriguez Fernandez ,  Roberto Vera Alvarez ,  Ania De La Nuez Veulens ,  Yuliet Mazola Reyes ,  Silvio Ernesto Perea Rodriguez ,  Boris Ernesto Acevedo Castro ,  Alexis Musacchio Lasa ,  Raimundo Ubieta Gómez

Inventor： Rolando Eduardo Rodriguez Fernandez ,  Roberto Vera Alvarez ,  Ania De La Nuez Veulens ,  Yuliet Mazola Reyes ,  Silvio Ernesto Perea Rodriguez ,  Boris Ernesto Acevedo Castro ,  Alexis Musacchio Lasa ,  Raimundo Ubieta Gómez

IPC: A61K31/66 ,  A61K31/53 ,  A61K31/505 ,  A61K31/47 ,  A61K31/415 ,  A61K31/40 ,  C07D251/42 ,  C07D473/00 ,  C07D239/02 ,  C07D215/38 ,  C07D235/00 ,  C07D233/96 ,  C07D209/14 ,  C07D307/02 ,  C07D229/00 ,  C07F9/02 ,  C07C281/02 ,  C07C273/02 ,  C07C303/00 ,  C07C241/00

CPC classification number: C07C211/14 ,  C07C237/06 ,  C07C237/22 ,  C07C243/28 ,  C07C255/42 ,  C07C257/14 ,  C07C271/22 ,  C07C271/64 ,  C07C275/08 ,  C07C275/16 ,  C07C275/24 ,  C07C281/12 ,  C07C317/28 ,  C07C327/42 ,  C07C337/08 ,  C07D207/34 ,  C07D209/14 ,  C07D213/81 ,  C07D213/82 ,  C07D215/46 ,  C07D233/88 ,  C07D233/91 ,  C07D235/14 ,  C07D239/36 ,  C07D239/46 ,  C07D239/54 ,  C07D251/22 ,  C07D307/52 ,  C07D487/04 ,  C07F9/224

Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.

Abstract translation: 通过在硅分子模拟中得到的化学化合物通过化学物质与酪蛋白激酶2酶底物磷酸化结构域或其邻域的特异性相互作用具有适合于阻断磷酸化事件的良好定义的结构。 本发明还包含含有这些化合物的药物组合物及其在制备用于治疗与肿瘤过程相关的疾病或病症的药物或试剂中的用途。

公开(公告)号：US08729111B2

公开(公告)日：2014-05-20

申请号：US12671990

申请日：2008-08-07

Applicant: Lijun Sun ,  Jun Jiang

Inventor： Lijun Sun ,  Jun Jiang

IPC: A01N43/78 ,  A61K31/425 ,  C07C241/00 ,  C07C243/00 ,  C07C249/00 ,  C07C251/00

CPC classification number: C07C391/00 ,  A61K31/16 ,  A61K31/165 ,  C07C243/34 ,  C07C327/56 ,  C07C333/28

Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

公开(公告)号：US08637678B2

公开(公告)日：2014-01-28

申请号：US13142110

申请日：2009-12-16

Applicant: George Robert Hodges ,  Lisa Mitchell ,  Alan James Robinson

Inventor： George Robert Hodges ,  Lisa Mitchell ,  Alan James Robinson

IPC: C07D231/10 ,  C07C22/04 ,  C07C49/12 ,  C07C43/30 ,  C07C241/00 ,  C07D333/02

CPC classification number: C07D333/28 ,  C07C25/18 ,  C07C43/192 ,  C07C49/693 ,  C07C251/82 ,  C07D231/14

Abstract: The present invention relates to methods of initiating a reaction represented by scheme (1), wherein Q is optionally substituted aryl or optionally substituted heteroaryl; X is halogen or a sulphonate; P is an organic radical; R is hydrogen or an organic radical; wherein the catalyst comprises copper and a ligand; comprising providing the compound of formula III in liquid form prior to contacting the compound of formula III with the catalyst.

Abstract translation: 本发明涉及引发由方案（1）表示的反应的方法，其中Q是任选取代的芳基或任选取代的杂芳基; X是卤素或磺酸盐; P是有机基团; R是氢或有机基团; 其中所述催化剂包含铜和配体; 在将式III化合物与催化剂接触之前，提供液态的式III化合物。

公开(公告)号：US20120215009A1

公开(公告)日：2012-08-23

申请号：US13504558

申请日：2010-10-28

Applicant: Maximilian Dochnahl ,  Michael Keil ,  Roland Goetz

Inventor： Maximilian Dochnahl ,  Michael Keil ,  Roland Goetz

IPC: C07D231/14 ,  C07C241/00

CPC classification number: C07D231/14

Abstract: Process for preparing aminale and their use for preparing 1,3-disubstituted pyrazole compounds.

Abstract translation: 制备胺的方法及其用于制备1,3-二取代吡唑化合物的方法。

公开(公告)号：US20120095103A1

公开(公告)日：2012-04-19

申请号：US13333179

申请日：2011-12-21

Applicant: Keizo KOYA ,  Weiwen Ying ,  Teresa Przewloka ,  Lijun Sun

Inventor： Keizo KOYA ,  Weiwen Ying ,  Teresa Przewloka ,  Lijun Sun

IPC: A61K31/165 ,  A61P35/00 ,  C07C241/00

CPC classification number: C07C391/00 ,  A61K31/165 ,  A61K31/18 ,  A61K45/06 ,  C07C259/20 ,  C07C2601/02

Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

公开(公告)号：US08093424B2

公开(公告)日：2012-01-10

申请号：US11985459

申请日：2007-11-15

Applicant: Robert Greenhouse ,  Ralph New Harris, III ,  Saul Jaime-Figueroa ,  James M. Kress ,  David Bruce Repke ,  Russell Stephen Stabler

Inventor： Robert Greenhouse ,  Ralph New Harris, III ,  Saul Jaime-Figueroa ,  James M. Kress ,  David Bruce Repke ,  Russell Stephen Stabler

IPC: C07C303/00 ,  C07C307/00 ,  C07C309/00 ,  C07C311/00 ,  C07C241/00 ,  C07C243/00 ,  C07C249/00 ,  C07C251/00

CPC classification number: C07C317/32 ,  C07C317/44 ,  C07C2602/08 ,  C07C2602/10 ,  C07D207/16 ,  C07D207/325 ,  C07D207/34 ,  C07D207/36 ,  C07D209/30 ,  C07D231/18 ,  C07D233/20 ,  C07D233/34 ,  C07D233/44 ,  C07D233/48 ,  C07D233/54 ,  C07D233/58 ,  C07D233/64 ,  C07D233/84 ,  C07D233/88 ,  C07D233/90 ,  C07D235/06 ,  C07D239/14 ,  C07D239/42 ,  C07D277/82

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract translation: 式I化合物或其药学上可接受的盐，其中m，p，q，Ar，R 1和R 2如本文所定义。 还提供了制备方法，组合物和使用式I化合物的方法。

公开(公告)号：US08017654B2

公开(公告)日：2011-09-13

申请号：US11918357

申请日：2006-04-13

Applicant: Thomas A. Dahl ,  Matthew McLeod

Inventor： Thomas A. Dahl ,  Matthew McLeod

IPC: A01N37/18 ,  A61K31/16 ,  C07D305/00 ,  C07D407/00 ,  C07D493/00 ,  C07C241/00 ,  C07C243/00 ,  C07C249/00 ,  C07C251/00

CPC classification number: A61K45/06 ,  A61K31/16 ,  A61K31/165 ,  A61K31/337 ,  A61K2300/00

Abstract: A method of treating a subject with cancer includes the step of co-administering to the subject over three to five weeks, a taxane in an amount of between about 243 μmol/m2 to 315 μmol/m2 (e.g., equivalent to paclitaxel in about 210-270 mg/m2); and a bis(thiohydrazide amide) in an amount between about 1473 μmol/m2 and about 1722 μmol/m2 (e.g., Compound (1) in about 590-690 mg/m2). The bis(thiohydrazide amide) is represented by Structural Formula (I), Y is a covalent bond or an optionally substituted straight chained hydrocarbyl group, or, Y, taken together with both >C=Z groups to which it is bonded, is an optionally substituted aromatic group. R1-R4 are independently —H, an optionally substituted aliphatic group, an optionally substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R7-R8 are independently —H, an optionally substituted aliphatic group, or an optionally substituted aryl group. Z is O or S.

Abstract translation: 用癌症治疗受试者的方法包括在三至五周内共同给予受试者的步骤，量为约243μmol/ m 3至315μmol/ m 2的紫杉烷（例如，相当于约210的紫杉醇 -270 mg / m2）; 和约1473μmol/ m 2与约1722μmol/ m 2之间的量的二（硫代酰肼）酰胺（例如化合物（1），约590-690mg / m 2）。 双（硫代酰肼）由结构式（I）表示，Y为共价键或任选取代的直链烃基，或Y与它们所键合的两个> C = Z基团一起为 任选取代的芳族基团。 R 1 -R 4独立地是-H，任选取代的脂族基团，任选取代的芳基，或者R 1和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4与碳和 与它们键合的氮原子形成任选地与芳环稠合的非芳族杂环。 R 7 -R 8独立地为-H，任选取代的脂族基团或任选取代的芳基。 Z是O或S.