公开(公告)号：US09428506B2

公开(公告)日：2016-08-30

申请号：US14394467

申请日：2013-04-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Peng Li ,  Lawrence Wennogle ,  Kimberly Vanover

IPC: A61K31/4985 ,  C07D241/38 ,  C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  C07D471/16 ,  A61K31/445

CPC classification number: C07D471/14 ,  A61K31/445 ,  A61K31/4985 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/16 ,  A61K2300/00

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, of Formula I, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems, such as disease of the central nervous system.

Abstract translation: 本发明涉及如本文所述的游离，固体，药学上可接受的盐和/或基本上纯的形式的式I的特定取代的杂环稠合的γ-咔啉，其药物组合物，以及用于治疗涉及5- HT2A受体，血清素转运蛋白（SERT）和/或涉及多巴胺D2受体信号传导系统的途径，例如中枢神经系统疾病。

公开(公告)号：US09408393B2

公开(公告)日：2016-08-09

申请号：US13765514

申请日：2013-02-12

Applicant: Microbion Corporation

Inventor： Brett Hugh James Baker

IPC: A61K9/06 ,  A61K9/10 ,  A01N55/02 ,  A01N43/16 ,  A01N47/44 ,  A01N45/00 ,  A01N37/18 ,  A01N43/90 ,  A01N43/78 ,  A61K9/00 ,  A61K9/70

CPC classification number: A01N55/02 ,  A01N25/08 ,  A01N37/18 ,  A01N43/16 ,  A01N43/36 ,  A01N43/40 ,  A01N43/54 ,  A01N43/60 ,  A01N43/78 ,  A01N43/84 ,  A01N43/90 ,  A01N45/00 ,  A01N47/44 ,  A01N57/24 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/10 ,  A61K9/16 ,  A61K9/7023 ,  A61K31/407 ,  A61K31/427 ,  A61K31/431 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/546 ,  A61K31/555 ,  A61K31/65 ,  A61K31/665 ,  A61K31/7028 ,  A61K31/7036 ,  A61K31/7048 ,  A61K38/12 ,  A61K38/14 ,  A61L24/0015 ,  A61L24/0031 ,  A61L24/06 ,  A61L2300/404 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/481

Abstract: Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating natural and artificial surfaces that contain bacterial biofilm, including unexpected synergy or enhancing effects between bismuth-thiol (BT) compounds and certain antibiotics, to provide formulations including antiseptic formulations. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating certain gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating certain gram-negative bacterial infections.

Abstract translation: 描述了包含新颖的均匀微粒悬浮液的组合物和方法，用于处理含有细菌生物膜的天然和人造表面，包括铋 - 硫醇（BT）化合物和某些抗生素之间的意外协同作用或增强作用，以提供包括防腐制剂的制剂。 还描述了所公开的BT化合物和BT化合物 - 抗生素组合的以前不可预测的抗菌性质和抗生物膜性质，包括某些此类组合物用于治疗某些革兰氏阳性细菌感染的优先功效，以及某些此类组合物的明显优势 治疗某些革兰氏阴性细菌感染。

公开(公告)号：US20160213640A1

公开(公告)日：2016-07-28

申请号：US14917724

申请日：2014-09-12

Applicant: NIHON NOHYAKU CO., LTD. ,  PITNEY PHARMACEUTICALS PTY LIMITED

Inventor： Nobuharu ANDOH ,  Osamu SANPEI ,  Tetsuo TOGA ,  David Lawson MORRIS ,  Roger ASTON ,  Koji TANAKA ,  Tomokazu HINO

IPC: A61K31/277 ,  A61K31/44 ,  A61K31/433 ,  A61K31/426 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/42 ,  A61K31/421 ,  A61K31/341 ,  A61K31/4245 ,  A61K31/5383 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/381 ,  A61K31/5377 ,  A61K31/415

CPC classification number: A61K31/277 ,  A61K31/341 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/433 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383

Abstract: The present invention relates to an anticancer agent having a high safety and a superior anticancer activity, and an anticancer agent containing, as an active ingredient, an aminoacetonitrile compound represented by the formula (I) wherein R1 is a hydrogen atom, an alkyl group and the like, R2, R3, and R4 are the same or different and each is a hydrogen atom, an alkyl group and the like, R5 and R6 are the same or different and each is a hydrogen atom, a halogen atom and the like, m is 0 or 1, R is a halogen atom, a cyano group, a nitro group, a phenyl group optionally substituted by an alkyl group and the like, an alkyl group and the like, Ar1 is a phenyl group, a naphthyl group, a pyridyl group, a pyrazolyl group, or the like, each of which is optionally substituted by a halogen atom, a cyano group, a nitro group, alkyl group and the like, and W is —O—, —S—, —SO2—, or —N(R7)— wherein R7 is a hydrogen atom, a (C1-C6)alkyl group and the like, or a pharmacologically acceptable salt thereof.

Abstract translation: 本发明涉及一种安全性高，抗癌活性优异的抗癌剂，以及含有式（I）所示氨基乙腈化合​​物作为活性成分的抗癌剂，其中R1为氢原子，烷基和 R 2，R 3和R 4相同或不同，各自为氢原子，烷基等，R 5和R 6相同或不同，分别为氢原子，卤素原子等， m为0或1，R为卤素原子，氰基，硝基，任选被烷基取代的苯基等，烷基等，Ar 1为苯基，萘基， 吡啶基，吡唑基等，它们各自任选被卤素原子，氰基，硝基，烷基等取代，W是-O - ， - S - ， - SO 2 - 或-N（R7） - 其中R7是氢原子，（C1-C6）烷基等，或药理学上 其食盐。

公开(公告)号：US09387189B2

公开(公告)日：2016-07-12

申请号：US13899980

申请日：2013-05-22

Applicant: Professional Compounding Centers of America

Inventor： Andrew B. Glasnapp

IPC: A61K31/202 ,  A61K38/06 ,  A61K45/06 ,  A61K38/20 ,  A61K38/02 ,  A23L1/00 ,  A61K38/17 ,  A61K38/19 ,  A61K47/10 ,  A61K47/12 ,  A61K47/18 ,  A61L27/16 ,  A61L27/52 ,  A61L27/54 ,  A61K31/496 ,  A61K31/7036

CPC classification number: A61K38/12 ,  A23L5/00 ,  A61K31/202 ,  A61K31/351 ,  A61K31/496 ,  A61K31/5383 ,  A61K31/7036 ,  A61K38/06 ,  A61K38/1725 ,  A61K38/195 ,  A61K38/2053 ,  A61K45/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/183 ,  A61K47/26 ,  A61K47/34 ,  A61K47/42 ,  A61L27/16 ,  A61L27/52 ,  A61L27/54 ,  A61L2430/00 ,  Y02A50/473

Abstract: Compositions and methods for treating infectious diseases produced by biofilms are disclosed. More specifically, the present disclosure refers to pharmaceutical compositions which may be used for treating biofilm infections, specifically, biofilms formed by bacteria such as Pseudomonas, E. coli, Klebsiella, and other human pathogens. Pharmaceutical compositions may include a nutrient dispersion. Pharmaceutical compositions disclosed may employ chemotactic agents in order to disrupt biofilms and therefore enhance the antibiotic response. Pharmaceutical compositions disclosed may include suitable vehicles which may depend on the dosage form.

Abstract translation: 公开了用于治疗由生物膜产生的感染性疾病的组合物和方法。 更具体地，本公开涉及可用于治疗生物膜感染的药物组合物，具体地，由诸如假单胞菌属，大肠杆菌，克雷伯杆菌和其他人类病原体的细菌形成的生物膜。 药物组合物可以包括营养分散体。 所公开的药物组合物可以使用趋化剂以破坏生物膜并因此增强抗生素反应。 所公开的药物组合物可包括可能取决于剂型的合适的载体。

公开(公告)号：US09359332B2

公开(公告)日：2016-06-07

申请号：US14060123

申请日：2013-10-22

Applicant: Symphony Evolution, Inc.

Inventor： Kenneth D. Rice ,  Neel K. Anand ,  Joerg Bussenius ,  Simona Costanzo ,  Abigail R. Kennedy ,  Csaba J. Peto ,  Tsze H. Tsang ,  Charles M. Blazey

IPC: C07D209/52 ,  C07D239/94 ,  C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

CPC classification number: C07D403/12 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/7064 ,  C07D239/94 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

Abstract: The present disclosure provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. The compounds are generally of formula (I): Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.Also disclosed are methods of making compounds for formula 8: comprising introducing group E2 into a compound of formula 7: wherein Ar, Z, P, and E2 are defined herein.

Abstract translation: 本公开提供了用于调节受体激酶活性的化合物，特别是ephrin和EGFR，以及利用其化合物及其药物组合物治疗由受体激酶活性介导的疾病的方法。 化合物通常为式（I）：由受体激酶活性介导的疾病包括但不限于以部分由细胞增殖异常水平（即肿瘤生长），程序性细胞死亡（细胞凋亡），细胞迁移和 与肿瘤生长相关的侵袭和血管生成。 本发明的化合物包括“光谱选择性”激酶调节剂，抑制，调节和/或调节受体型酪氨酸激酶（包括ephrin和EGFR）亚家族的信号转导的化合物。 还公开了制备式8化合物的方法：包括将E2组导入式7化合物中：其中Ar，Z，P和E2在本文中定义。

公开(公告)号：US09346765B2

公开(公告)日：2016-05-24

申请号：US14672679

申请日：2015-03-30

Applicant: Rajinder Singh ,  Ankush Argade ,  Donald Payan ,  Susan Molineaux ,  Sacha Holland ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Catherine Sylvain ,  Hui Li ,  Alexander Rossi

Inventor： Rajinder Singh ,  Ankush Argade ,  Donald Payan ,  Susan Molineaux ,  Sacha Holland ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Catherine Sylvain ,  Hui Li ,  Alexander Rossi

IPC: C07D239/30 ,  C07D239/42 ,  C07D239/48 ,  A61K31/519 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K45/06 ,  C07D498/04 ,  C07D265/36 ,  A61K31/5395 ,  C07D495/04 ,  C07F5/02 ,  C07D498/14 ,  C07D407/14

CPC classification number: A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5395 ,  A61K31/551 ,  A61K45/06 ,  C07D239/48 ,  C07D265/36 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14 ,  C07F5/027

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

公开(公告)号：US20160129032A1

公开(公告)日：2016-05-12

申请号：US14845763

申请日：2015-09-04

Applicant: Kenneth D. Rice ,  Neel K. Anand ,  Joerg Bussenius ,  Simona Costanzo ,  Abigail R. Kennedy ,  Csaba J. Peto ,  Tsze H. Tsang ,  Charles M. Blazey

Inventor： Kenneth D. Rice ,  Neel K. Anand ,  Joerg Bussenius ,  Simona Costanzo ,  Abigail R. Kennedy ,  Csaba J. Peto ,  Tsze H. Tsang ,  Charles M. Blazey

IPC: A61K31/7064 ,  A61K31/5513 ,  A61K31/5377 ,  A61K31/553 ,  A61K31/517 ,  A61K31/5383

CPC classification number: C07D403/12 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/7064 ,  C07D239/94 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04

Abstract: The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

Abstract translation: 本发明提供用于调节受体激酶活性的化合物，特别是ephrin和EGFR，以及利用其化合物及其药物组合物治疗由受体激酶活性介导的疾病的方法。 由受体激酶活性介导的疾病包括但不限于由细胞增殖异常水平（即肿瘤生长），程序性细胞死亡（细胞凋亡），细胞迁移和与肿瘤生长相关的血管生成的特征的疾病。 本发明的化合物包括“光谱选择性”激酶调节剂，抑制，调节和/或调节受体型酪氨酸激酶（包括ephrin和EGFR）亚家族的信号转导的化合物。

公开(公告)号：US20160106753A1

公开(公告)日：2016-04-21

申请号：US14976998

申请日：2015-12-21

Applicant: Giorgio CARAVATTI ,  Sylvie CHAMOIN ,  Pascal FURET ,  Klemens HOGENAUER ,  Konstanze HURTH ,  Christoph KALIS ,  Karen KAMMERTOENS ,  Ian LEWIS ,  Henrik MOEBITZ ,  Alexander Baxter SMITH ,  Nicolas SOLDERMANN ,  Romain WOLF ,  Frederic ZECRI

Inventor： Giorgio CARAVATTI ,  Sylvie CHAMOIN ,  Pascal FURET ,  Klemens HOGENAUER ,  Konstanze HURTH ,  Christoph KALIS ,  Karen KAMMERTOENS ,  Ian LEWIS ,  Henrik MOEBITZ ,  Alexander Baxter SMITH ,  Nicolas SOLDERMANN ,  Romain WOLF ,  Frederic ZECRI

IPC: A61K31/5383 ,  A61K31/538

CPC classification number: A61K31/5383 ,  A61K31/538 ,  C07D413/14 ,  C07D498/04 ,  C12N9/12 ,  C12Q1/25 ,  C12Q1/686 ,  Y02A50/409 ,  Y02A50/411

Abstract: The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

公开(公告)号：US20160106731A1

公开(公告)日：2016-04-21

申请号：US14885181

申请日：2015-10-16

Applicant: Vanderbilt University

Inventor： Taekyu Lee ,  Jason P. Burke ,  Edward T. Olejniczak ,  Johannes Belmar ,  Zhiguo Bian ,  Stephen W. Fesik

IPC: A61K31/4745 ,  A61K31/542 ,  A61K45/06 ,  C07D498/06 ,  A61K31/5383 ,  A61K31/554 ,  C07D513/06 ,  C07D471/08

CPC classification number: A61K31/4745 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/554 ,  A61K45/06 ,  C07D471/08 ,  C07D498/06 ,  C07D513/06

Abstract: The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.

Abstract translation: 本发明提供抑制抗凋亡Bcl-2家族成员骨髓细胞白血病-1（Mcl-1）蛋白的活性的化合物。 本发明还提供药物组合物以及使用化合物治疗特征在于Mcl-1蛋白过度表达或失调的疾病和病症（例如癌症）的方法。

公开(公告)号：US20160102106A1

公开(公告)日：2016-04-14

申请号：US14884397

申请日：2015-10-15

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： John Emmerson Campbell ,  Philip Jones ,  Michael Charles Hewitt

IPC: C07D519/00 ,  A61K31/5383 ,  A61K31/4745 ,  A61K31/519 ,  A61K31/4985 ,  C07D471/04

CPC classification number: C07D519/00 ,  A61K31/4375 ,  A61K31/4745 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04

Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.