公开(公告)号：US10301285B2

公开(公告)日：2019-05-28

申请号：US14692597

申请日：2015-04-21

Applicant: University of Tennessee Research Foundation ,  GTx, Inc.

Inventor： Duane D. Miller ,  Jianjun Chen ,  James T. Dalton ,  Chien-Ming Li ,  Sunjoo Ahn ,  Wei Li

IPC: C07D403/04 ,  A61K31/4178 ,  C07D233/02 ,  C07D233/22 ,  C07D233/54 ,  C07D401/04 ,  C07D401/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D263/06 ,  C07D263/14 ,  C07D263/32 ,  C07D277/04 ,  C07D277/24 ,  C07D277/28 ,  C07D277/56 ,  A61K45/06

Abstract: The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.

公开(公告)号：US20190091222A1

公开(公告)日：2019-03-28

申请号：US16156902

申请日：2018-10-10

Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education ,  The United States Government as represented by the Department of Veterans Affairs

Inventor： Beibei Chen ,  Rama K. Mallampalli

IPC: A61K31/506 ,  C07D211/14 ,  A61K31/402 ,  A61P11/06 ,  C07C211/01 ,  A61K31/444 ,  A61P35/00 ,  C07D277/28 ,  C07D207/06 ,  C07C229/38 ,  A61K31/341 ,  A61K31/381 ,  C07C211/53 ,  C07D213/36 ,  C07D233/61 ,  C07D265/30 ,  C07D231/12 ,  A61K31/4155 ,  A61K31/137 ,  A61K31/4418 ,  C07D239/26 ,  C07D213/06 ,  A61K31/5375 ,  C07D213/38 ,  A61K31/427 ,  A61P19/00 ,  A61P3/10 ,  A61K31/4178 ,  C07D233/64 ,  A61P25/00 ,  A61K31/435 ,  C07D295/135 ,  C07D403/12 ,  C07D401/12

CPC classification number: A61K31/506 ,  A61K31/137 ,  A61K31/341 ,  A61K31/381 ,  A61K31/402 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/435 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/5375 ,  A61P3/10 ,  A61P11/06 ,  A61P19/00 ,  A61P25/00 ,  A61P35/00 ,  C07C211/01 ,  C07C211/53 ,  C07C229/38 ,  C07D207/06 ,  C07D211/14 ,  C07D213/06 ,  C07D213/36 ,  C07D213/38 ,  C07D231/12 ,  C07D233/61 ,  C07D233/64 ,  C07D239/26 ,  C07D265/30 ,  C07D277/28 ,  C07D295/135 ,  C07D401/12 ,  C07D403/12 ,  Y02A50/411 ,  Y02A50/473

Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.

公开(公告)号：US10206394B2

公开(公告)日：2019-02-19

申请号：US15520233

申请日：2015-10-13

Applicant: Syngenta Participations AG

Inventor： Alan Joseph Hennessy ,  Shuji Hachisu ,  Jeffrey Steven Wailes ,  Nigel James Willetts ,  Ian Stuart Cloudsdale ,  Janice Black ,  Emma Briggs ,  Suzanna Jane Dale

IPC: A01N37/18 ,  A01N43/60 ,  A01N43/16 ,  A01N43/40 ,  C07D213/40 ,  A01N43/78 ,  A01N37/34 ,  A01N43/54 ,  A01N43/56 ,  C07D309/04 ,  C07D309/14 ,  C07D231/16 ,  C07D331/04 ,  C07D333/20 ,  C07D333/28 ,  C07D401/12 ,  C07D239/30 ,  C07D409/12 ,  C07D417/12 ,  C07D277/24 ,  C07D277/28 ,  C07D277/56 ,  C07D277/64 ,  C07D295/185 ,  C07D213/50 ,  C07D213/61 ,  C07D305/08 ,  C07D307/52 ,  A01N43/08 ,  A01N43/10 ,  A01N43/58 ,  A01N43/80 ,  A01N43/84

Abstract: The present invention relates to a compound of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and G are as defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.

公开(公告)号：US20180346422A1

公开(公告)日：2018-12-06

申请号：US16059270

申请日：2018-08-09

Applicant: Ono Pharmaceutical Co., Ltd.

Inventor： Kentaro Yashiro ,  Daisuke WAKAMATSU ,  Tetsuji SAITO

IPC: C07D213/61 ,  C07D307/52 ,  A61K31/17 ,  C07D213/40 ,  C07D209/30 ,  C07D277/28 ,  C07D271/06 ,  C07C233/29 ,  C07C233/26 ,  C07D241/12 ,  C07D413/06 ,  C07D239/26 ,  C07D233/64 ,  C07D333/28 ,  C07D333/20 ,  C07C275/40 ,  C07C275/32 ,  C07D309/04 ,  C07D213/74 ,  A61K31/505 ,  A61K31/4965 ,  A61K31/4545 ,  A61K31/435 ,  A61K31/426 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/417 ,  A61K31/4045 ,  A61K31/381 ,  A61K31/351 ,  A61K31/341

Abstract: The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.

公开(公告)号：US10016418B2

公开(公告)日：2018-07-10

申请号：US15205608

申请日：2016-07-08

Applicant: Senomyx, Inc.

Inventor： Chad Priest ,  Alain Noncovich ,  Andrew Patron ,  Jane Ung

IPC: A61K31/497 ,  A61K31/165 ,  A61K31/381 ,  A61K31/4155 ,  A61K31/415 ,  A61K31/422 ,  A61K31/426 ,  A61K31/437 ,  A61K31/4409 ,  A61K31/4436 ,  C07C233/11 ,  C07C235/20 ,  C07C235/24 ,  C07C235/34 ,  C07D213/40 ,  C07D213/75 ,  C07D231/40 ,  C07D277/28 ,  C07D307/52 ,  C07D333/20 ,  C07D333/24 ,  C07D333/32 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  A61K8/42 ,  A61K8/49 ,  A61K8/69 ,  A61Q19/00 ,  A01N43/10 ,  A01N43/40 ,  A01N43/56 ,  A01N43/60 ,  A01N43/76 ,  A01N43/80 ,  A01N43/90 ,  A23L27/00 ,  A23L33/10 ,  A01N37/18 ,  A01N43/78 ,  A61Q1/02 ,  A61Q5/02 ,  A61Q5/12 ,  A61Q9/02 ,  A61Q11/00 ,  A61Q15/00 ,  A61Q17/02 ,  A61Q17/04 ,  A61Q19/10

CPC classification number: A61K31/497 ,  A01N37/18 ,  A01N43/10 ,  A01N43/40 ,  A01N43/56 ,  A01N43/60 ,  A01N43/76 ,  A01N43/78 ,  A01N43/80 ,  A01N43/90 ,  A23L27/88 ,  A23L33/10 ,  A23V2002/00 ,  A61K8/42 ,  A61K8/49 ,  A61K8/4926 ,  A61K8/494 ,  A61K8/4973 ,  A61K8/4986 ,  A61K8/69 ,  A61K31/165 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/426 ,  A61K31/437 ,  A61K31/4409 ,  A61K31/4436 ,  A61K2800/10 ,  A61K2800/40 ,  A61Q1/02 ,  A61Q5/02 ,  A61Q5/12 ,  A61Q9/02 ,  A61Q11/00 ,  A61Q15/00 ,  A61Q17/02 ,  A61Q17/04 ,  A61Q19/00 ,  A61Q19/001 ,  A61Q19/10 ,  C07C233/11 ,  C07C235/20 ,  C07C235/24 ,  C07C235/34 ,  C07C2601/14 ,  C07D213/40 ,  C07D213/75 ,  C07D231/40 ,  C07D277/28 ,  C07D307/52 ,  C07D333/20 ,  C07D333/24 ,  C07D333/32 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.

公开(公告)号：US20180079709A1

公开(公告)日：2018-03-22

申请号：US15497556

申请日：2017-04-26

Applicant: Oryzon Genomics S.A.

Inventor： Alberto ORTEGA MUÑOZ ,  Matthew Colin Thor Fyfe ,  Marc Martinell Pedemonte ,  Maria de los Àngeles Estiarte Martinez ,  Nuria Valls Vidal ,  Guido Kurz ,  Julio Cesar Castro Palomino Laria

IPC: C07C211/36 ,  C07D333/20 ,  C07C273/00 ,  C07D213/57 ,  C07D213/73 ,  C07D231/56 ,  C07C213/00 ,  C07C215/64 ,  C07C217/74 ,  C07C211/40 ,  C07C217/54 ,  C07C215/46 ,  C07C311/21 ,  C07C311/08 ,  C07C273/18 ,  C07C209/28 ,  C07C211/38 ,  C07C269/00 ,  C07D213/74 ,  C07D307/52 ,  C07D213/38 ,  C07D213/30 ,  C07D295/26 ,  C07D295/135 ,  C07D295/096 ,  C07D277/28 ,  C07D207/14 ,  C07D231/12 ,  C07C275/26 ,  C07C271/24

CPC classification number: C07C211/36 ,  C07B2200/07 ,  C07C209/28 ,  C07C211/37 ,  C07C211/38 ,  C07C211/40 ,  C07C213/00 ,  C07C215/46 ,  C07C215/64 ,  C07C217/54 ,  C07C217/74 ,  C07C269/00 ,  C07C271/24 ,  C07C273/00 ,  C07C273/18 ,  C07C275/26 ,  C07C311/08 ,  C07C311/21 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/08 ,  C07D207/14 ,  C07D213/30 ,  C07D213/38 ,  C07D213/57 ,  C07D213/73 ,  C07D213/74 ,  C07D231/12 ,  C07D231/56 ,  C07D277/28 ,  C07D295/096 ,  C07D295/135 ,  C07D295/26 ,  C07D307/52 ,  C07D333/20

Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

公开(公告)号：US09920042B2

公开(公告)日：2018-03-20

申请号：US14430604

申请日：2013-09-27

Applicant: Universite de Droit et de la Sante de Lille 2

Inventor： Nicolas Willand ,  Benoit Deprez ,  Alain Baulard ,  Priscille Brodin ,  Olivier Sperando ,  Vincent Villeret ,  Baptiste Villemagne

IPC: C07D277/26 ,  C07D277/30 ,  C07D417/04 ,  C07D213/81 ,  C07D249/06 ,  C07D249/08 ,  C07D271/06 ,  C07D277/56 ,  C07D277/66 ,  C07D285/08 ,  C07D285/12 ,  C07D291/04 ,  C07C255/57 ,  C07C311/37 ,  C07C247/18 ,  A61K31/155 ,  A61K31/175 ,  A61K31/4192 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/428 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/277 ,  A61K31/4439 ,  A61K45/06 ,  C07C255/60 ,  C07D263/32 ,  C07D277/28

CPC classification number: C07D417/04 ,  A61K31/155 ,  A61K31/175 ,  A61K31/277 ,  A61K31/4192 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/428 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/4439 ,  A61K45/06 ,  C07C247/18 ,  C07C255/57 ,  C07C255/60 ,  C07C311/37 ,  C07D213/81 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/26 ,  C07D277/28 ,  C07D277/30 ,  C07D277/56 ,  C07D277/66 ,  C07D285/08 ,  C07D285/12 ,  C07D291/04 ,  A61K2300/00

Abstract: The present invention concerns compounds of general formula (I): in which Y and Z are chosen from CH and N; T is chosen from CO or SO2; n is 1 to 3; R1 represents a group chosen, for example, from C1-C3 alkyl chains unsubstituted or substituted by fluorine, the unsubstituted or substituted cyclic, cyano, azido, alkoxy and phenyl groups; and R is chosen from the azido, cyano, alkinyl and 2-benzothiazolyl groups and an optionally substituted aromatic heterocycle with five vertices; and the use thereof in the treatment of bacterial and mycobacterial infections such as, for example, tuberculosis, leprosy and atypical mycobacterial infections. The present invention also concerns pharmaceutical compositions comprising, as the active ingredient, at least one of the abovementioned compounds and optionally an antibiotic activatable via the EthA pathway.

公开(公告)号：USRE46592E1

公开(公告)日：2017-10-31

申请号：US14938526

申请日：2015-11-11

Applicant: Aerpio Therapeutics, Inc.

Inventor： Jeffrey Lyle Gray ,  Kande K. D. Amarasinghe ,  Cynthia Monesa Clark ,  Ryan Matthew Nichols ,  Matthew B. Maier

IPC: A61K31/4965 ,  A61K31/425 ,  A61K31/426 ,  C07D277/64 ,  C07D417/04 ,  A61K9/00 ,  A61K31/428 ,  A61K31/497 ,  C07D277/60 ,  C07D277/30 ,  C07D277/28 ,  A61K31/427

CPC classification number: A61K31/426 ,  A61K9/0019 ,  A61K31/427 ,  A61K31/428 ,  A61K31/497 ,  C07D277/28 ,  C07D277/30 ,  C07D277/60 ,  C07D277/64 ,  C07D417/04 ,  Y02A50/401

Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.

公开(公告)号：US09718812B2

公开(公告)日：2017-08-01

申请号：US15115963

申请日：2015-02-04

Applicant: Axxam S.P.A.

Inventor： Paolo Pevarello ,  Stefan Lohmer ,  Chiara Llberati ,  Pierfausto Seneci ,  Cristina Pesenti ,  Adolfo Prandi

IPC: C07D417/06 ,  C07D413/14 ,  C07D277/30 ,  C07D417/14 ,  C07F7/18 ,  C07D277/28 ,  C07D263/32 ,  C07D413/06

CPC classification number: C07D417/06 ,  C07D263/32 ,  C07D277/28 ,  C07D277/30 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  C07F7/18

Abstract: The present invention refers to novel substituted thiazole and oxazole compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties. The compounds are useful in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.

公开(公告)号：US09682925B2

公开(公告)日：2017-06-20

申请号：US15005574

申请日：2016-01-25

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Naoki Tomita ,  Shigeo Kajii ,  Douglas Robert Cary ,  Daisuke Tomita ,  Shinichi Imamura ,  Ken Tsuchida ,  Satoru Matsuda ,  Ryujiro Hara

IPC: A61K31/167 ,  A61K31/36 ,  A61K31/366 ,  A61K31/40 ,  A61K31/402 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/428 ,  A61K31/429 ,  A61K31/433 ,  A61K31/451 ,  A61K31/495 ,  A61K31/55 ,  C07C233/80 ,  A61K31/381 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4453 ,  A61K31/4468 ,  C07D309/14 ,  C07C271/22 ,  C07D317/58 ,  C07D223/16 ,  C07D231/14 ,  C07D231/20 ,  C07D231/22 ,  C07D333/20 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D405/04 ,  C07D239/36 ,  C07D409/04 ,  C07D471/04 ,  C07D261/08 ,  C07D261/10 ,  C07D263/32 ,  C07D263/34 ,  C07C235/56 ,  C07D207/06 ,  C07C237/40 ,  C07D495/04 ,  C07D207/337 ,  C07D277/20 ,  C07D277/28 ,  C07D277/30 ,  C07D209/08 ,  C07D277/62 ,  C07D209/42 ,  C07D513/04 ,  C07D209/46 ,  C07D209/48 ,  C07D285/06 ,  C07D211/56 ,  C07D211/58 ,  C07D295/14 ,  C07D211/76 ,  C07D213/04 ,  C07D213/38 ,  C07D213/56 ,  C07D211/98 ,  C07D335/02 ,  C07C237/42 ,  C07C271/20 ,  C07D211/40 ,  C07D231/26 ,  C07D295/135 ,  C07D295/155

CPC classification number: C07C233/80 ,  A61K31/167 ,  A61K31/36 ,  A61K31/366 ,  A61K31/381 ,  A61K31/40 ,  A61K31/402 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/428 ,  A61K31/429 ,  A61K31/433 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4453 ,  A61K31/4468 ,  A61K31/451 ,  A61K31/495 ,  A61K31/55 ,  C07C235/56 ,  C07C237/40 ,  C07C237/42 ,  C07C271/20 ,  C07C271/22 ,  C07C2601/02 ,  C07C2601/18 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/337 ,  C07D209/08 ,  C07D209/42 ,  C07D209/46 ,  C07D209/48 ,  C07D211/40 ,  C07D211/56 ,  C07D211/58 ,  C07D211/76 ,  C07D211/98 ,  C07D213/04 ,  C07D213/38 ,  C07D213/56 ,  C07D223/16 ,  C07D231/14 ,  C07D231/20 ,  C07D231/22 ,  C07D231/26 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D239/36 ,  C07D261/08 ,  C07D261/10 ,  C07D263/32 ,  C07D263/34 ,  C07D277/20 ,  C07D277/28 ,  C07D277/30 ,  C07D277/62 ,  C07D285/06 ,  C07D295/135 ,  C07D295/14 ,  C07D295/155 ,  C07D309/14 ,  C07D317/58 ,  C07D333/20 ,  C07D335/02 ,  C07D405/04 ,  C07D409/04 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

Abstract: The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula wherein A is a hydrocarbon group or heterocyclic group optionally having substituent(s); R is H, a hydrocarbon group or heterocyclic group optionally having substituent(s); A and R are optionally bonded to each other to form a ring optionally having substituent(s); Q1, Q2, Q3 and Q4 are each a hydrogen atom or a substituent; Q1 and Q2, and Q3 and Q4, are each optionally bonded to each other to form a ring optionally having substituent(s); X is H, an acyclic hydrocarbon group or saturated cyclic group optionally having substituent(s); Y1, Y2 and Y3 are each H, a hydrocarbon group or heterocyclic group optionally having substituent(s); X and Y1, and Y1 and Y2, are each optionally bonded to each other to form a ring optionally having substituent(s); and Z1, Z2 and Z3 are each H or a substituent, or a salt thereof.