公开(公告)号：US20170291886A1

公开(公告)日：2017-10-12

申请号：US15508266

申请日：2015-08-28

Applicant: Neoculi Pty Ltd.

Inventor： Stephen Page ,  Andrew Stevens ,  Adam McCluskey ,  Martine Keenan ,  Rebecca Abraham

IPC: C07D333/58 ,  A61K45/06 ,  C07C281/18 ,  A61K31/505 ,  C07D239/50 ,  C07D295/135 ,  C07C335/40 ,  A61K31/381 ,  A61K31/404 ,  C07D209/08 ,  A61K31/496 ,  A61K31/155 ,  A61K9/00

CPC classification number: C07D333/58 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/155 ,  A61K31/17 ,  A61K31/341 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/496 ,  A61K31/498 ,  A61K31/505 ,  A61K45/06 ,  C07C47/565 ,  C07C211/29 ,  C07C251/24 ,  C07C281/18 ,  C07C335/40 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/08 ,  C07D209/14 ,  C07D239/48 ,  C07D239/50 ,  C07D241/20 ,  C07D249/14 ,  C07D251/54 ,  C07D295/135 ,  C07D307/56 ,  C07D311/58 ,  C07D401/14 ,  A61K2300/00

Abstract: The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention.

公开(公告)号：US09783513B2

公开(公告)日：2017-10-10

申请号：US14421776

申请日：2013-08-16

Applicant: Ohio State Innovation Foundation ,  Research Institute at Nationwide Children's Hospital

Inventor： Chenglong Li ,  Wenying Yu ,  Jiayuh Lin

IPC: C07C50/12 ,  C07D275/06 ,  C07D213/74 ,  C07C307/02 ,  C07D233/54 ,  C07D211/26 ,  C07D295/135 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

CPC classification number: C07D275/06 ,  C07C307/02 ,  C07C311/39 ,  C07C311/58 ,  C07C2601/14 ,  C07C2602/10 ,  C07D211/26 ,  C07D213/74 ,  C07D233/54 ,  C07D233/61 ,  C07D295/135 ,  C07D295/205 ,  C07D309/04 ,  C07D335/02 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

Abstract: In one aspect, the invention relates to substituted 6-amino-5,8-dioxo-5,8-dihydronaphthalene-1-sulfonamide analogs and derivatives thereof, substituted 4-amino-5H-naphtho[1,8-cd]isothiazol-5-one 1,1-dioxide analogs and derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. 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.

公开(公告)号：US20170224679A1

公开(公告)日：2017-08-10

申请号：US15500758

申请日：2015-07-27

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Ebere F. IGBOKO ,  Paul Bryan WREN

IPC: A61K31/495 ,  A61K45/06 ,  A61K31/282 ,  A61K31/341 ,  A61K31/277 ,  A61K31/40 ,  A61K31/17 ,  A61K31/445 ,  A61K31/351

CPC classification number: A61K31/495 ,  A61K31/17 ,  A61K31/277 ,  A61K31/282 ,  A61K31/341 ,  A61K31/351 ,  A61K31/40 ,  A61K31/445 ,  A61K31/4462 ,  A61K31/555 ,  A61K45/06 ,  C07D211/54 ,  C07D295/135 ,  C07D307/18 ,  C07D309/08 ,  A61K2300/00

Abstract: The invention relates to the use of a CXCR2 antagonist for the prevention and/or treatment of chemotherapy induced peripheral neuropathy (CIPN).

公开(公告)号：US20170190681A1

公开(公告)日：2017-07-06

申请号：US15314124

申请日：2015-05-27

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Weichun CHEN ,  Ebere F. IGBOKO ,  Xichen LIN ,  Hongfu LU ,  Feng REN ,  Paul Bryan WREN ,  Zhongmiao XU ,  Ting YANG ,  Lingdong ZHU

IPC: C07D307/18 ,  C07D241/04

CPC classification number: C07D307/18 ,  C07C311/47 ,  C07C317/42 ,  C07C317/50 ,  C07C2101/10 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07D207/10 ,  C07D211/54 ,  C07D213/34 ,  C07D233/64 ,  C07D239/26 ,  C07D241/04 ,  C07D295/135 ,  C07D305/06 ,  C07D309/08 ,  C07D471/04 ,  C07D487/04

Abstract: The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor In addition, the invention relates to compositions containing the derivatives and processes for their preparation

公开(公告)号：US20170114050A1

公开(公告)日：2017-04-27

申请号：US15311817

申请日：2015-05-13

Applicant: NORTHEASTERN UNIVERSITY

Inventor： Michael Malamas ,  Alexandros Makriyannis ,  Kumara Vadivel Subramanian ,  Kyle M. Whitten ,  Nikolai M. Zvonok ,  Jay Matthew West ,  Michael Mccormack ,  Spiro Pavlopoulos

IPC: C07D405/12 ,  C07C331/20 ,  C07D213/36 ,  C07D295/13 ,  C07D295/135 ,  C07D211/26 ,  C07D241/18 ,  C07D239/26 ,  C07C331/26 ,  C07D319/18 ,  C07D317/54 ,  C07D213/64 ,  C07D213/30 ,  C07D261/08 ,  C07D231/12 ,  C07D317/58 ,  C07D205/04 ,  C07D413/12 ,  C07D403/12 ,  C07D207/12 ,  C07D211/46 ,  C07C255/46 ,  C07D239/28 ,  C07C331/24

CPC classification number: C07D405/12 ,  C07B2200/07 ,  C07C255/46 ,  C07C331/20 ,  C07C331/24 ,  C07C331/26 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D205/04 ,  C07D207/12 ,  C07D211/10 ,  C07D211/26 ,  C07D211/46 ,  C07D213/30 ,  C07D213/36 ,  C07D213/46 ,  C07D213/64 ,  C07D231/12 ,  C07D239/26 ,  C07D239/28 ,  C07D241/18 ,  C07D261/08 ,  C07D295/13 ,  C07D295/135 ,  C07D317/54 ,  C07D317/58 ,  C07D319/18 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

Abstract: A compound is represented as Formula I, a tautomer thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Compounds of Formula I are inhibitors of N-acylethanolamine hydrolyzing acid amidase (NAAA). The present technology is directed to compounds, compositions, and methods to inhibit N-acylethanolamine hydrolyzing acid amidase and to treat N-acylethanolamine hydrolyzing acid amidase mediated conditions in a subject.

公开(公告)号：US09617239B2

公开(公告)日：2017-04-11

申请号：US13641713

申请日：2011-03-10

Applicant: Alfred L. Williams ,  John Scott ,  Li-An Yeh ,  Matthew Robert Redinbo

Inventor： Alfred L. Williams ,  John Scott ,  Li-An Yeh ,  Matthew Robert Redinbo

IPC: A61K31/38 ,  C07D333/34 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/137 ,  A61K31/42 ,  A61K31/4409 ,  A61K31/4709 ,  A61K31/553 ,  C07D295/135 ,  C07D409/06 ,  C12Q1/34

CPC classification number: C07D333/34 ,  A61K31/137 ,  A61K31/42 ,  A61K31/4409 ,  A61K31/4709 ,  A61K31/553 ,  C07D295/135 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C12Q1/34 ,  G01N2333/924 ,  G01N2500/02

Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. Glucuronidase inhibitors described include phenoxy thiophene sulfonamides. Other compounds, for instance pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls, are also contemplated. Also contemplated are compositions including one or more of such compounds for use inhibiting glucuronidase and methods of using one or more of such compounds as a co-drug to be used in combination with the anticancer drug CPT-11.

公开(公告)号：US09580386B2

公开(公告)日：2017-02-28

申请号：US14459540

申请日：2014-08-14

Applicant: GRÜNENTHAL GMBH

Inventor： Bert Nolte ,  Wolfgang Schröder ,  Klaus Linz ,  Werner Englberger ,  Hans Schick ,  Heinz Graubaum ,  Birgit Braun ,  Sigrid Ozegowski ,  József Bálint ,  Helmut Sonnenschein

IPC: C07C211/00 ,  C07D209/20 ,  C07C211/40 ,  C07C215/14 ,  C07C215/42 ,  C07C217/74 ,  C07C223/04 ,  C07C229/16 ,  C07C233/36 ,  C07C233/40 ,  C07C233/41 ,  C07C233/62 ,  C07C233/79 ,  C07C235/54 ,  C07C237/06 ,  C07C275/24 ,  C07C311/07 ,  C07C311/18 ,  C07D209/12 ,  C07D209/14 ,  C07D211/62 ,  C07D213/12 ,  C07D213/82 ,  C07D231/14 ,  C07D251/54 ,  C07D295/135 ,  C07D309/08 ,  C07D333/20 ,  C07D403/08 ,  C07D409/08 ,  A61K31/135 ,  A61K45/06 ,  A61K31/136 ,  A61K31/165 ,  A61K31/18 ,  A61K31/404 ,  A61K31/53 ,  A61K31/5377 ,  C07C211/54 ,  C07C237/24 ,  C07C311/37 ,  C07D251/48

CPC classification number: C07D209/20 ,  A61K31/135 ,  A61K31/136 ,  A61K31/165 ,  A61K31/18 ,  A61K31/404 ,  A61K31/53 ,  A61K31/5377 ,  A61K45/06 ,  C07C211/40 ,  C07C211/54 ,  C07C215/14 ,  C07C215/42 ,  C07C217/74 ,  C07C223/04 ,  C07C229/16 ,  C07C233/36 ,  C07C233/40 ,  C07C233/41 ,  C07C233/62 ,  C07C233/79 ,  C07C235/54 ,  C07C237/06 ,  C07C237/24 ,  C07C275/24 ,  C07C311/07 ,  C07C311/18 ,  C07C311/37 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07D209/12 ,  C07D209/14 ,  C07D211/62 ,  C07D213/12 ,  C07D213/82 ,  C07D231/14 ,  C07D251/48 ,  C07D251/54 ,  C07D295/135 ,  C07D309/08 ,  C07D333/20 ,  C07D403/08 ,  C07D409/08

Abstract: The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

Abstract translation: 本发明涉及对μ-阿片受体和ORL1-受体具有亲和力的化合物，其生产方法，含有这些化合物的药物以及这些化合物用于治疗疼痛和其它病症的用途。

公开(公告)号：US20170001949A1

公开(公告)日：2017-01-05

申请号：US15169725

申请日：2016-05-31

Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education

Inventor： Xiang-qun XIE ,  Peng YANG ,  Rentian FENG

IPC: C07C233/40 ,  C07D295/135

CPC classification number: C07C233/40 ,  C07C69/78 ,  C07C233/11 ,  C07C233/13 ,  C07C233/22 ,  C07C233/36 ,  C07C233/63 ,  C07C233/78 ,  C07C311/05 ,  C07C311/18 ,  C07C311/20 ,  C07C311/29 ,  C07C311/48 ,  C07C2601/14 ,  C07C2603/74 ,  C07D203/08 ,  C07D211/06 ,  C07D213/56 ,  C07D235/12 ,  C07D295/135

Abstract: Cannabinoid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.

Abstract translation: 其中：R1和R2独立地为H，烷基或烯基; R3是烷基，烯基，芳基，芳烷基，芳烯基，杂环基，杂环基烷基，杂芳基，杂芳基烷基; R4和R5独立地是键，亚烷基或烯基; （C 1 -C 6）烷基，烷氧基，氨基，COOH，CONH 2，SO 3 H，PO 3 H 2，CN，SH，NO 2和CF 3; 且p和q独立地为0,1,2,3,4或5.这些化合物可用于治疗骨质疏松症或多发性骨髓瘤。

公开(公告)号：US09493396B2

公开(公告)日：2016-11-15

申请号：US14915014

申请日：2014-08-26

Applicant: LUPIN ATLANTIS HOLDINGS SA

Inventor： Prathap Sreedharan Nair ,  Ganesh Bhausaheb Gudade ,  Mahadeo Bhaskar Tryambake ,  Chetan Sanjay Pawar ,  Sanjeev Anant Kulkarni ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC: C07D231/12 ,  A61K31/137 ,  A61K31/195 ,  A61K31/415 ,  A61P13/12 ,  A61P5/18 ,  C07C211/30 ,  C07C217/48 ,  C07C217/58 ,  C07C227/18 ,  C07C229/34 ,  C07C229/38 ,  C07C317/32 ,  C07D207/06 ,  C07D295/135 ,  C07C209/22 ,  C07C213/08 ,  C07C315/04 ,  C07D305/08 ,  C07C227/10 ,  C07C237/20

CPC classification number: C07C211/30 ,  A61K31/137 ,  A61K31/195 ,  A61K31/415 ,  C07C209/22 ,  C07C213/08 ,  C07C217/48 ,  C07C217/58 ,  C07C227/10 ,  C07C227/18 ,  C07C229/34 ,  C07C229/38 ,  C07C237/20 ,  C07C315/04 ,  C07C317/32 ,  C07D207/06 ,  C07D231/12 ,  C07D295/135 ,  C07D305/08

Abstract: The invention relates to naphthalene compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium sensing receptor modulators (Ca SR). The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium sensing receptor modulators (Ca SR) channel modulators.

Abstract translation: 本发明涉及式（I）的萘化合物及其药学上可接受的盐，其中取代基如本文所述，以及它们在医学中用于治疗与钙感应受体调节剂（Ca SR）调节相关的疾病， 。 本发明还涉及含有这些化合物治疗与钙感应受体调节剂（Ca SR）通道调节剂相关的疾病障碍的药物组合物。

公开(公告)号：US20160326113A1

公开(公告)日：2016-11-10

申请号：US15147671

申请日：2016-05-05

Applicant: Lin Yi ,  Xiping Su ,  Peter Werth

Inventor： Lin Yi ,  Xiping Su ,  Peter Werth

IPC: C07D209/88 ,  C07D295/135 ,  C07C243/22

CPC classification number: C07D209/88 ,  C07C243/22 ,  C07D295/135 ,  C07D295/14 ,  C07D295/155

Abstract: Methods and intermediates for the synthesis of carprofen and its derivatives starting from cyclohexanone are disclosed.

Abstract translation: 公开了从环己酮开始合成卡洛芬及其衍生物的方法和中间体。