公开(公告)号：US08987318B2

公开(公告)日：2015-03-24

申请号：US14474490

申请日：2014-09-02

Applicant: Alexar Therapeutics, Inc.

Inventor： Raju Mohan

IPC: C07D231/10 ,  A61K31/4155 ,  A61K31/415 ,  C07D417/04 ,  C07D413/04 ,  C07D403/04 ,  C07D409/04 ,  C07D231/12 ,  C07D405/04

CPC classification number: C07D417/04 ,  C07D231/12 ,  C07D231/16 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04

Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Abstract translation: 本文描述的是肝X受体（LXR）调节剂和利用LXR调节剂治疗真皮疾病，病症或病症的方法。 本文还描述含有这些化合物的药物组合物。

公开(公告)号：US20150073141A1

公开(公告)日：2015-03-12

申请号：US14332207

申请日：2014-07-15

Applicant: Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter I. Dosa

Inventor： Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter I. Dosa

IPC: C07D405/12 ,  C07D401/12 ,  C07D231/12

CPC classification number: A61K31/415 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.The present invention also relates to the method of prophylaxis or treatment of 5-HT2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.

Abstract translation: 本发明涉及式（I）的某些吡唑衍生物及其药物组合物，其调节5-HT2A 5-羟色胺受体的活性。 化合物及其药物组合物涉及可用于预防或治疗血小板凝集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血块形成风险，哮喘或其症状的方法， 激动或症状，行为障碍，药物诱发的精神病，兴奋性精神病，杜蕾特勒杜勒特综合征，躁狂症，有机或非精神病精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症和精神分裂症以及相关疾病和睡眠障碍， 睡眠障碍，糖尿病相关疾病等。 本发明还涉及与单独或一起施用的多巴胺D2受体拮抗剂如氟哌啶醇组合预防或治疗5-HT2A 5-羟色胺受体介导的病症的方法。

公开(公告)号：US20150045399A1

公开(公告)日：2015-02-12

申请号：US14474490

申请日：2014-09-02

Applicant: Alexar Therapeutics, Inc.

Inventor： Raju Mohan

IPC: C07D417/04 ,  C07D405/04 ,  C07D409/04 ,  C07D231/12 ,  C07D413/04 ,  C07D403/04

CPC classification number: C07D417/04 ,  C07D231/12 ,  C07D231/16 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04

Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Abstract translation: 本文描述的是肝X受体（LXR）调节剂和利用LXR调节剂治疗真皮疾病，病症或病症的方法。 本文还描述含有这些化合物的药物组合物。

公开(公告)号：US20150018337A1

公开(公告)日：2015-01-15

申请号：US14446127

申请日：2014-07-29

Applicant: ChemoCentryx, Inc.

Inventor： Trevor T. Charvat ,  Cheng Hu ,  Anita Melikian ,  Aaron Novack ,  Andrew M.K. Pennell ,  Edward J. Sullivan ,  William D. Thomas ,  Solomon Ungashe ,  Penglie Zhang ,  Jay Powers ,  Sreenivas Punna

IPC: C07D473/00 ,  A61K31/496 ,  A61K31/52 ,  A61K31/437 ,  A61K31/4192 ,  A61K31/4164 ,  A61K31/415 ,  A61K31/404 ,  C07D471/04 ,  C07D249/06 ,  C07D233/61 ,  C07D231/14 ,  C07D231/12 ,  C07D209/08 ,  A61K45/06 ,  A61K31/5377

CPC classification number: C07D473/00 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/496 ,  A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/08 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/56 ,  C07D233/61 ,  C07D235/06 ,  C07D235/08 ,  C07D249/06 ,  C07D249/18 ,  C07D401/04 ,  C07D401/14 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C12N2501/999

Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

Abstract translation: 提供了作为CCR9受体的有效拮抗剂的化合物。 动物实验表明，这些化合物可用于治疗炎症，CCR9的特征性疾病。 化合物通常为芳基磺酰胺衍生物，并且可用于药物组合物，用于治疗CCR9介导的疾病的方法，以及用于鉴定CCR9拮抗剂的测定中的对照。

公开(公告)号：US20140349848A1

公开(公告)日：2014-11-27

申请号：US14344579

申请日：2012-09-10

Applicant: Christoph Braun ,  Haruko Sawada ,  Helene Lachaise ,  Stephane Brunet ,  Philippe Rinolfi ,  Christophe Dubost ,  Pierre-Yves Coqueron ,  Simon Maechling ,  Anne-Sophie Rebstock ,  Ulrike Wachendorff-Neumann

Inventor： Christoph Braun ,  Haruko Sawada ,  Helene Lachaise ,  Stephane Brunet ,  Philippe Rinolfi ,  Christophe Dubost ,  Pierre-Yves Coqueron ,  Simon Maechling ,  Anne-Sophie Rebstock ,  Ulrike Wachendorff-Neumann

IPC: C07D413/12 ,  C07F7/10 ,  A01N55/00 ,  C07D277/40 ,  C07D213/73 ,  A01N43/82 ,  C07D417/12 ,  C07D213/75

CPC classification number: C07D413/12 ,  A01N43/82 ,  A01N55/00 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D231/16 ,  C07D231/38 ,  C07D271/07 ,  C07D277/40 ,  C07D277/46 ,  C07D277/48 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07F7/0812 ,  C07F7/10

Abstract: The present invention provides fungicidal 4-substituted-3-{phenyl[(heterocyclylmethoxy)imino]methyl}-1,2,4-oxadiazol-5(4H)-one derivatives of formula (I) wherein A represents a pyridyl or thiazole group and X1, Y1 to Y5 represent independently different substituents.

Abstract translation: 本发明提供式（I）的杀真菌剂4-取代-3- {苯基[（杂环基甲氧基）亚氨基]甲基} -1,2,4-恶二唑-5（4H） - 酮衍生物，其中A代表吡啶基或噻唑基 X1，Y1〜Y5独立地表示不同的取代基。

公开(公告)号：US20140171474A1

公开(公告)日：2014-06-19

申请号：US14183965

申请日：2014-02-19

Applicant: Philippe DESBORDES ,  Ralf DUNKEL ,  Stephanie GARY ,  Marie-Claire GROSJEAN-COURNOYER ,  Benoit HARTMANN ,  Philippe RINOLFI ,  Jean-Pierre VORS ,  Rachel RAMA

Inventor： Philippe DESBORDES ,  Ralf DUNKEL ,  Stephanie GARY ,  Marie-Claire GROSJEAN-COURNOYER ,  Benoit HARTMANN ,  Philippe RINOLFI ,  Jean-Pierre VORS ,  Rachel RAMA

IPC: A01N43/78 ,  A01N43/76 ,  A01N43/36 ,  A01N43/56 ,  A01N43/10

CPC classification number: A01N43/78 ,  A01N43/10 ,  A01N43/36 ,  A01N43/56 ,  A01N43/76 ,  C07D207/34 ,  C07D231/14 ,  C07D231/16 ,  C07D263/34 ,  C07D277/56 ,  C07D333/38

Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions

Abstract translation: 本发明涉及式（I）的N-环烷基-N-联苯甲基 - 甲酰胺衍生物，其中A，Z 1，Z 2，Z 3，X，n，Y和m代表各种取代基，其制备方法，制备中间体化合物， 用作杀真菌活性剂，特别是以杀真菌剂组合物的形式和用于控制植物病原真菌（特别是植物）的方法，使用这些化合物或组合物

公开(公告)号：US08754238B2

公开(公告)日：2014-06-17

申请号：US10895789

申请日：2004-07-21

Applicant: Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter Ian Dosa

Inventor： Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter Ian Dosa

IPC: C07D231/12

CPC classification number: A61K31/415 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.The present invention also relates to the method of prophylaxis or treatment of 5-HT2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.

Abstract translation: 本发明涉及式（I）的某些吡唑衍生物及其药物组合物，其调节5-HT2A 5-羟色胺受体的活性。 化合物及其药物组合物涉及可用于预防或治疗血小板聚集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血块形成风险，哮喘或其症状的方法， 激动或症状，行为障碍，药物诱发的精神病，兴奋性精神病，杜蕾特勒杜勒特综合征，躁狂症，有机或非精神病精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症和精神分裂症以及相关疾病和睡眠障碍， 睡眠障碍，糖尿病相关疾病等。 本发明还涉及与单独或一起施用的多巴胺D2受体拮抗剂如氟哌啶醇组合预防或治疗5-HT2A 5-羟色胺受体介导的病症的方法。

公开(公告)号：US08754219B2

公开(公告)日：2014-06-17

申请号：US13643537

申请日：2011-04-27

Applicant: Jeffrey P. Whitten ,  Yazhong Pei ,  Jianguo Cao ,  Zhijun Wang ,  Evan Rogers ,  Brian Dyck ,  Jonathan Grey

Inventor： Jeffrey P. Whitten ,  Yazhong Pei ,  Jianguo Cao ,  Zhijun Wang ,  Evan Rogers ,  Brian Dyck ,  Jonathan Grey

IPC: A61K31/44 ,  C07D221/02

CPC classification number: C07D417/12 ,  C07C233/75 ,  C07C233/80 ,  C07C233/92 ,  C07C255/60 ,  C07C2601/02 ,  C07D213/81 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/56 ,  C07D263/57 ,  C07D277/34 ,  C07D277/56 ,  C07D317/62 ,  C07D333/38 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract translation: 本文描述了含有这种化合物的化合物和药物组合物，其调节储存操作的钙（SOC）通道的活性。 本文还描述了使用这种SOC通道调节剂单独和与其它化合物组合用于治疗将受益于SOC通道活性抑制的疾病或病症的方法。

公开(公告)号：US20140155617A1

公开(公告)日：2014-06-05

申请号：US14041938

申请日：2013-09-30

Applicant: E.I. du Pont de Nemours and Company

Inventor： Gary David Annis

IPC: C07C45/70 ,  C07C49/80 ,  C07C25/13 ,  C07D261/04

CPC classification number: C07D261/04 ,  C07C17/35 ,  C07C25/13 ,  C07C45/455 ,  C07C45/70 ,  C07C49/80 ,  C07C49/813 ,  C07C67/343 ,  C07C205/45 ,  C07C209/74 ,  C07C231/12 ,  C07C231/14 ,  C07C235/84 ,  C07D213/40 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D249/08 ,  C07D249/10 ,  C07D277/28 ,  C07C69/94 ,  C07C69/76 ,  C07C211/56

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. Also disclosed is a method for preparing a compound of Formula 2 comprising (1) forming a reaction mixture comprising a Grignard reagent derived from contacting a compound of Formula 5 wherein X is Cl, Br or I with magnesium metal or an alkylmagnesium halide in the presence of an ethereal solvent, and then (2) contacting the reaction mixture with a compound of Formula 6 wherein Y is OR11 or NR12 R13, and R11, R12 and R13 are as defined in the disclosure. Further disclosed is a method for preparing a compound of Formula 7 wherein Q and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.

Abstract translation: 公开了一种制备式1化合物的方法，其中Q和Z如本公开中所定义，包括从包含式2化合物，式3化合物，包含至少一种选自 由式4的碱土金属氢氧化物组成的组，其中M是Ca，Sr或Ba，式4a的碱金属碳酸盐，其中M1是Li，Na或K，1,5-二氮杂双环[4.3.0]壬-5-烯和 1,8-二氮杂双环[5.4.0]十一碳-7-烯，以及能够与水形成低沸点共沸物的非质子传递溶剂。 还公开了制备式2化合物的方法，其包括（1）形成反应混合物，该反应混合物包含衍生自在存在下使式5的化合物（其中X为Cl，Br或I）与镁金属或烷基卤化镁接触的格利雅试剂 的醚溶剂，然后（2）使反应混合物与式6化合物（其中Y是OR 11或NR 12 R 13）和R 11，R 12和R 13如本公开中所定义。 进一步公开的是制备式7化合物的方法，其中Q和Z如本公开所定义，使用式1的化合物，其特征在于通过上述方法制备式1化合物或使用制备的式1化合物 通过上述方法。

公开(公告)号：US20140140973A1

公开(公告)日：2014-05-22

申请号：US14164573

申请日：2014-01-27

Applicant: E I DU PONT DE NEMOURS AND COMPANY

Inventor： GEORGE PHILIP LAHM ,  Stephen Frederick McCann ,  Kanu Maganbhai Patel ,  Thomas Paul Selby ,  Thomas Martin Stevenson

IPC: A01N43/56 ,  A01N43/54 ,  A01N43/58 ,  A01N43/86

CPC classification number: A01N43/56 ,  A01N43/54 ,  A01N43/58 ,  A01N43/86 ,  C07C251/76 ,  C07D213/77 ,  C07D231/06 ,  C07D231/08 ,  C07D231/14 ,  C07D231/16 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14

Abstract: This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure.This invention further relates to a bezoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.

Abstract translation: 本发明涉及一种控制鳞翅目，同翅目，半翅目，鳞翅目和鞘翅目昆虫害虫的方法，包括使昆虫或其环境与节肢动物学有效量的式I化合物，其N-氧化物或农业上合适的盐接触，其中A 并且B和R 1至R 8如本公开中所定义。 本发明还涉及式10的唑嗪酮化合物，其中R 4至R 8如本公开所定义，可用于制备式I化合物。