公开(公告)号：US20180134633A1

公开(公告)日：2018-05-17

申请号：US15573224

申请日：2016-05-11

Applicant: BASF SE

Inventor： Barbara Nave ,  Joachim Dickhaut ,  Peter Nesvadba ,  Mihiret Tekeste Sisay ,  Alexander Wissemeier ,  Wolfram Zerulla ,  Gregor Pasda ,  Olof Wallquist ,  Allan F. Cunningham

IPC: C05G3/08 ,  C07C323/48 ,  C07D249/12 ,  C07D233/42 ,  C07D235/28 ,  C07D239/38 ,  C07C317/08 ,  C07C323/47 ,  C07D495/04 ,  C07D221/04 ,  C07D285/125 ,  C07D405/04 ,  C07D417/04 ,  C07D277/74 ,  C07D401/04 ,  C07C317/18 ,  C07C317/10 ,  C07C323/07 ,  C07C321/20 ,  C07D285/135 ,  C07C321/28 ,  C07D241/18 ,  C07D241/44 ,  C05C3/00 ,  C05F11/00 ,  C05C9/00

CPC classification number: C05G3/08 ,  C05C3/00 ,  C05C9/00 ,  C05F11/00 ,  C07C317/08 ,  C07C317/10 ,  C07C317/18 ,  C07C321/20 ,  C07C321/28 ,  C07C323/07 ,  C07C323/47 ,  C07C323/48 ,  C07C337/08 ,  C07D221/04 ,  C07D233/42 ,  C07D235/28 ,  C07D239/38 ,  C07D241/18 ,  C07D241/44 ,  C07D249/12 ,  C07D277/74 ,  C07D285/125 ,  C07D285/135 ,  C07D401/04 ,  C07D405/04 ,  C07D417/04 ,  C07D495/04 ,  Y02E50/343 ,  Y02P60/218 ,  Y02W30/47

Abstract: Provided herein are a use of thioether compounds of formula I as nitrification inhibitors, and agricultural mixtures and compositions including the thioether compounds.

公开(公告)号：US20180009764A1

公开(公告)日：2018-01-11

申请号：US15708827

申请日：2017-09-19

Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC. ,  ADVANCED CANCER THERAPEUTICS, LLC

Inventor： Robert A. Mitchell ,  John O. Trent ,  Pooran Chand ,  Gilles Hugues Tapolsky

IPC: C07D239/30 ,  C07D401/04 ,  C07D239/38 ,  C07D239/42 ,  C07D409/04 ,  C07D405/04

CPC classification number: C07D239/30 ,  C07D239/38 ,  C07D239/42 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

Abstract: Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula I: wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions that contain a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions that include administering a safe and effective amount of a Formula I compound.

公开(公告)号：US20160326103A1

公开(公告)日：2016-11-10

申请号：US15109741

申请日：2015-01-05

Applicant: BRISTROL-MYERS SQUIBB COMPANY

Inventor： Jingwu Duan ,  T.G. Murali Dhar ,  Bin Jiang ,  Zhonghui Lu ,  Ananta Karmakar ,  Arun Kumar Gupta ,  Carolyn A. Weigelt

IPC: C07C317/14 ,  C07C317/32 ,  C07D303/34 ,  C07D317/44 ,  C07D295/185 ,  C07C317/44 ,  C07C317/50 ,  C07D309/14 ,  C07D231/12 ,  C07D213/30 ,  C07D213/85 ,  C07D239/38 ,  C07D261/08 ,  C07D319/20 ,  C07D213/75 ,  C07D213/40 ,  C07D211/62 ,  C07D295/108 ,  C07D295/155 ,  C07D205/04 ,  C07D471/04 ,  C07D471/10 ,  C07D401/04 ,  C07D237/08 ,  C07C317/22

CPC classification number: C07C317/14 ,  C07C317/20 ,  C07C317/22 ,  C07C317/30 ,  C07C317/32 ,  C07C317/44 ,  C07C317/46 ,  C07C317/50 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/08 ,  C07D205/04 ,  C07D211/36 ,  C07D211/62 ,  C07D213/30 ,  C07D213/40 ,  C07D213/56 ,  C07D213/75 ,  C07D213/81 ,  C07D213/85 ,  C07D231/12 ,  C07D237/08 ,  C07D239/38 ,  C07D241/12 ,  C07D257/04 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D285/06 ,  C07D295/108 ,  C07D295/155 ,  C07D295/18 ,  C07D295/185 ,  C07D295/20 ,  C07D295/22 ,  C07D303/06 ,  C07D303/34 ,  C07D305/14 ,  C07D309/04 ,  C07D309/14 ,  C07D317/44 ,  C07D319/20 ,  C07D401/04 ,  C07D471/04 ,  C07D471/10

Abstract: Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：US20160287586A1

公开(公告)日：2016-10-06

申请号：US14535640

申请日：2014-11-07

Applicant: Cellceutix Corporation ,  RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY

Inventor： Richard W. Scott ,  Kathryn B. Freeman ,  Haizhong Tang ,  Gill Diamond

IPC: A61K31/506 ,  A61K9/06 ,  A61K9/00

CPC classification number: A61K31/506 ,  A01N25/00 ,  A61K9/0053 ,  A61K9/06 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4192 ,  A61K31/4436 ,  A61K31/496 ,  A61K31/505 ,  C07C211/27 ,  C07C211/28 ,  C07C211/29 ,  C07C217/20 ,  C07C237/08 ,  C07C279/04 ,  C07C279/06 ,  C07C279/08 ,  C07C279/12 ,  C07D209/86 ,  C07D239/26 ,  C07D239/28 ,  C07D239/38 ,  C07D249/06 ,  C07D277/28 ,  C07D307/52 ,  C07D307/91 ,  C07D333/20 ,  C07D333/76 ,  C07D409/14

Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.

Abstract translation: 本公开内容提供了用于杀死或抑制念珠菌或曲霉菌种的生长或预防或治疗具有念珠菌病（口服和/或播撒）或曲霉属感染的哺乳动物的化合物或其药学上可接受的盐。

公开(公告)号：US09320734B2

公开(公告)日：2016-04-26

申请号：US14589360

申请日：2015-01-05

Applicant: Board of Regents, The University of Texas System ,  Arizona Board of Regents on Behalf of the University of Arizona

Inventor： Daruka Mahadevan ,  Emmanuelle J. Meuillet ,  Eugene A. Mash, Jr. ,  Vijay M. Gokhale ,  Garth Powis ,  Shuxing Zhang

IPC: A61K31/433 ,  C07C59/90 ,  C07C65/40 ,  C07C233/75 ,  C07C235/64 ,  C07C237/42 ,  C07C271/22 ,  C07C311/21 ,  C07C317/14 ,  C07C317/18 ,  C07C317/28 ,  C07C317/44 ,  C07C323/65 ,  C07D213/50 ,  C07D213/643 ,  C07D213/74 ,  C07D213/76 ,  C07D231/06 ,  C07D231/12 ,  C07D231/20 ,  C07D231/38 ,  C07D231/42 ,  C07D233/20 ,  C07D233/26 ,  C07D233/64 ,  C07D237/08 ,  C07D237/18 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/52 ,  C07D261/08 ,  C07D261/20 ,  C07D263/32 ,  C07D263/42 ,  C07D263/56 ,  C07D271/10 ,  C07D271/113 ,  C07D277/52 ,  C07D277/64 ,  C07D285/12 ,  C07D285/125 ,  C07D285/135 ,  C07D295/135 ,  C07D295/192 ,  C07D295/26 ,  C07D333/38 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07F9/6558

CPC classification number: A61K31/433 ,  C07C59/90 ,  C07C65/40 ,  C07C233/75 ,  C07C235/64 ,  C07C237/42 ,  C07C271/22 ,  C07C311/21 ,  C07C317/14 ,  C07C317/18 ,  C07C317/28 ,  C07C317/44 ,  C07C323/65 ,  C07D213/50 ,  C07D213/643 ,  C07D213/74 ,  C07D213/76 ,  C07D231/06 ,  C07D231/12 ,  C07D231/20 ,  C07D231/38 ,  C07D231/42 ,  C07D233/20 ,  C07D233/26 ,  C07D233/64 ,  C07D237/08 ,  C07D237/18 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/52 ,  C07D261/08 ,  C07D261/20 ,  C07D263/32 ,  C07D263/42 ,  C07D263/56 ,  C07D271/10 ,  C07D271/113 ,  C07D277/52 ,  C07D277/64 ,  C07D285/12 ,  C07D285/125 ,  C07D285/135 ,  C07D295/135 ,  C07D295/192 ,  C07D295/26 ,  C07D333/38 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07F9/65583

Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

公开(公告)号：US20160016880A1

公开(公告)日：2016-01-21

申请号：US14774289

申请日：2014-03-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yan Shi ,  Peter T.W. Cheng ,  Ying Wang ,  Shung C. Wu ,  Hao Zhang

IPC: C07C59/13 ,  A61K31/415 ,  A61K31/192 ,  C07D307/79 ,  A61K31/343 ,  C07D333/56 ,  A61K31/381 ,  C07D271/06 ,  A61K31/4245 ,  C07C59/215 ,  C07C323/19 ,  C07C205/34 ,  C07D333/28 ,  C07D239/38 ,  A61K31/505 ,  C07D205/04 ,  A61K31/397 ,  A61K45/06 ,  C07D231/12

CPC classification number: C07C59/13 ,  A61K31/192 ,  A61K31/343 ,  A61K31/381 ,  A61K31/397 ,  A61K31/415 ,  A61K31/4245 ,  A61K31/505 ,  A61K45/06 ,  C07C43/192 ,  C07C43/196 ,  C07C47/277 ,  C07C59/215 ,  C07C59/72 ,  C07C62/34 ,  C07C69/675 ,  C07C69/708 ,  C07C69/732 ,  C07C69/734 ,  C07C69/736 ,  C07C69/757 ,  C07C69/76 ,  C07C205/34 ,  C07C235/26 ,  C07C237/22 ,  C07C311/51 ,  C07C323/19 ,  C07C2601/02 ,  C07C2602/08 ,  C07C2602/42 ,  C07D205/04 ,  C07D231/12 ,  C07D239/38 ,  C07D271/06 ,  C07D307/79 ,  C07D333/16 ,  C07D333/28 ,  C07D333/56

Abstract: The present invention provides compounds of Formula (I): (I) or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

Abstract translation: 本发明提供式（I）的化合物：（I）或其立体异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是可用作药物的GPR120G蛋白偶联受体调节剂。

公开(公告)号：US09145354B2

公开(公告)日：2015-09-29

申请号：US14355786

申请日：2012-10-31

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Andrew James Woodhead ,  Christopher Charles Frederick Hamlett ,  Gilbert Ebai Besong ,  Gianni Chessari ,  Maria Grazia Carr ,  Alessia Millemaggi ,  David Norton ,  Susanne Maria Saalau-Bethell ,  Hendrika Maria Gerarda Willems ,  Neil Thomas Thompson ,  Steven Douglas Hiscock

IPC: C07C225/16 ,  C07D213/73 ,  C07D213/74 ,  C07C255/58 ,  C07D213/79 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D231/12 ,  C07D401/04 ,  C07D239/26 ,  C07D239/38 ,  C07C225/18 ,  C07D241/20 ,  C07D261/08 ,  C07D277/28 ,  C07D498/04 ,  C07D213/50 ,  C07D213/64 ,  C07D213/65 ,  C07C225/22 ,  C07C229/38 ,  C07C237/06 ,  C07C237/10 ,  C07C237/24 ,  C07C237/30 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  C07C313/06 ,  A61K31/138 ,  A61K31/277 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/5383 ,  A61K45/06 ,  C07C221/00 ,  C07C253/30 ,  C07D275/02 ,  A61K47/10 ,  A61K47/26 ,  A61K9/19

CPC classification number: C07C225/16 ,  A61K9/0019 ,  A61K9/19 ,  A61K9/2018 ,  A61K9/4858 ,  A61K31/138 ,  A61K31/277 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/5383 ,  A61K45/06 ,  A61K47/10 ,  A61K47/26 ,  C07B2200/05 ,  C07C221/00 ,  C07C225/18 ,  C07C225/22 ,  C07C229/38 ,  C07C237/06 ,  C07C237/10 ,  C07C237/24 ,  C07C237/30 ,  C07C253/30 ,  C07C255/58 ,  C07C313/06 ,  C07C2601/02 ,  C07D213/50 ,  C07D213/64 ,  C07D213/65 ,  C07D213/73 ,  C07D213/74 ,  C07D213/79 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D231/12 ,  C07D239/26 ,  C07D239/38 ,  C07D241/20 ,  C07D261/08 ,  C07D275/02 ,  C07D277/28 ,  C07D401/04 ,  C07D498/04

Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections. The compounds have the formula (1): or a salt, N-oxide, tautomer or stereoisomer thereof, wherein A is CH or N; E is CH or N; R1 is selected from: an optionally substituted acyclic C1-8 hydrocarbon group wherein one carbon atom of the acyclic C1-8 hydrocarbon group may optionally be replaced by O, S, NRc, S(O) or SO2, or two adjacent carbon atoms of the acyclic C1-8 hydrocarbon group may optionally be replaced by CONRc, NRcCO, NRcSO2 or SO2NRc provided that in each case at least one carbon atom of the acyclic C1-8 hydrocarbon group remains; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is hydrogen or X—R8; X is a C1-8 alkanediyl group wherein one carbon atom of the C1-8 alkanediyl group may optionally be bonded to a —CH2—CH2— moiety to form a cyclopropane-1,1-diyl group or two adjacent carbon atoms of the C1-8 alkanediyl group may optionally be bonded to a —(CH2)n moiety, where n is 1 to 5, to form a C3-7-cycloalkane-1,2-diyl group; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyclic carbocyclic or heterocyclic ring containing 0-3 heteroatom ring members selected from N, O and S; R4 is hydrogen or R4a wherein R4a is halogen; cyano; C1-4 alkyl; fluoro-1-4 alkyl; C1-4 alkoxy; fluoro-C1-4 alkoxy; hydroxy-C1-4 alkyl; or C1-2 alkoxy-C1-4 alkyl; R5 is hydrogen or R5a wherein R5a is selected from C1-2 alkyl optionally substituted with fluorine; C1-3 alkoxy optionally substituted with fluorine; halogen; cyclopropyl; and cyano; R8 is hydroxy or C(═O)NR10R11; provided that when R8 is hydroxy, there are at least two carbon atoms in line between the hydroxy group and the nitrogen atom to which X is attached; R10 is hydrogen or C1-4 alkyl; and R11 is hydrogen; amino-C2-4 alkyl or hydroxy-C2-4 alkyl; but excluding the compounds 1-(3-benzoylphenyl)-ethylamine and 1-(3-furan-2-oylcarbonylphenyl)-ethylamine.

公开(公告)号：US20150266900A1

公开(公告)日：2015-09-24

申请号：US14435649

申请日：2012-10-30

Applicant: VILNIUS UNIVERSITY

Inventor： Daumantas Matulis ,  Virginija Dudutiene ,  Asta Zubriene

IPC: C07D513/04 ,  C07C323/67 ,  C07D237/18 ,  C07C317/22 ,  C07C311/29 ,  C07D295/096 ,  C07C311/39 ,  C07C317/14

CPC classification number: C07D513/04 ,  C07C311/29 ,  C07C311/37 ,  C07C311/39 ,  C07C317/14 ,  C07C317/18 ,  C07C317/22 ,  C07C317/36 ,  C07C323/67 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2601/20 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/74 ,  C07D233/84 ,  C07D237/18 ,  C07D239/38 ,  C07D277/74 ,  C07D295/096

Abstract: Novel fluorinated benzenesulfonamides compounds of general formula (I) can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression.

Abstract translation: 通式（I）的新型氟化苯磺酰胺化合物可用于生物医药作为药物制剂中的活性成分，因为它们抑制参与疾病进展的酶。

公开(公告)号：US20150225423A1

公开(公告)日：2015-08-13

申请号：US14693345

申请日：2015-04-22

Applicant: Université Laval

Inventor： Giorgio ATTARDO ,  Sasmita TRIPATHY ,  Martin GAGNON

IPC: C07D513/04 ,  C07D239/47 ,  C07D401/12 ,  C07D471/04 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D401/14 ,  C07D239/56 ,  C07D409/12

CPC classification number: C07D513/04 ,  A61K31/435 ,  A61K31/497 ,  A61K31/506 ,  C07D239/38 ,  C07D239/47 ,  C07D239/56 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.

Abstract translation: 本发明的特征在于具有式（Ia）和（Ib）的化合物（例如，式（（Ia-2） - （Ia-21））中任一项的化合物，包括其它互变异构体，立体异构体，E / Z立体异构体， 本发明还涉及通过施用有效量的式（Ia）或（Ib）化合物来治疗或预防患者的疼痛（例如神经性疼痛），炎症或癫痫的方法， 本发明还涉及治疗或预防患者的疼痛（例如神经性疼痛），炎症或癫痫的方法，其包括向有需要的患者施用有效量的式（IIa）或（IIb）化合物， 本文所述的化合物（例如，式（Ia），（Ib），（IIa）或（IIb）的化合物可以是式（（IIa-2） - （IIa-6） ）也可以用作抗惊厥药。

公开(公告)号：US20150051195A1

公开(公告)日：2015-02-19

申请号：US14528130

申请日：2014-10-30

Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN

Inventor： Patrick Chaltin ,  Zeger Debyser ,  Marc De Maeyer ,  Arnaud Marchand ,  Damien Marchand ,  Wim Smets ,  Arnout Voet ,  Frauke Christ

IPC: C07D491/052 ,  C07D239/26 ,  C07D401/04 ,  C07D403/04 ,  C07D239/38 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D401/14 ,  C07D239/42 ,  C07D413/14

CPC classification number: C07D491/052 ,  C07D239/26 ,  C07D239/38 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/14 ,  C07D417/04

Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.

Abstract translation: 本发明涉及一系列具有抗病毒活性的新化合物，更具体地涉及HIV（人类免疫缺陷病毒）复制抑制性质。 本发明还涉及制备这些化合物的方法，以及可用于这种合成的一个或多个步骤的新型中间体。 本发明还涉及包含有效量的这些化合物作为活性成分的药物组合物。 本发明还涉及这些化合物作为药物或制备用于治疗患有病毒感染，特别是HIV感染的动物的药物的用途。 本发明还涉及通过施用治疗量的这种化合物治疗动物中的病毒感染的方法，任选地与一种或多种具有抗病毒活性的其它药物组合。