公开(公告)号：US09108961B2

公开(公告)日：2015-08-18

申请号：US14184453

申请日：2014-02-19

Applicant: EnVivo Pharmaceuticals, Inc.

Inventor： Patricia Oliver-Shaffer ,  Gideon Shapiro ,  Richard Chesworth ,  Muneki Kishida ,  Takayuki Ishige

IPC: A61K31/44 ,  C07D453/02

CPC classification number: C07D453/02 ,  A61K9/4833 ,  A61K31/439 ,  C07B2200/13 ,  C30B29/54

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract translation: （R）-7-氯-N-（奎宁环-3-基）苯并[b]噻吩-2-甲酰胺盐酸盐一水合物的结晶形式I和II及其制备方法及其治疗用途。

公开(公告)号：US20140187786A1

公开(公告)日：2014-07-03

申请号：US13945500

申请日：2013-07-18

Applicant: EnVivo Pharmaceuticals, Inc.

Inventor： Gideon Shapiro ,  Richard Chesworth

IPC: C07D471/04 ,  C07D213/64 ,  C07C317/46 ,  C07C317/44 ,  C07C229/34 ,  C07C59/64 ,  C07D217/22 ,  C07D213/55

CPC classification number: C07C229/34 ,  C07C59/64 ,  C07C59/68 ,  C07C59/72 ,  C07C69/734 ,  C07C205/37 ,  C07C205/56 ,  C07C255/57 ,  C07C317/44 ,  C07C317/46 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/04 ,  C07D213/30 ,  C07D213/55 ,  C07D213/64 ,  C07D217/22 ,  C07D231/12 ,  C07D271/08 ,  C07D285/10 ,  C07D471/04

Abstract: Compounds that are 1,3,4-trisubstituted benzenes which modulate (e.g., inhibit) the activity of γ-secretase. The compounds are expected to reduce the level of Aβ42 in patients and be useful in the treatment of diseases (e.g., Alzheimer's disease) characterized by elevated levels of Aβ42 and/or the formation of Aβ plaques.

Abstract translation: 作为调节（例如抑制）γ-分泌酶活性的1,3,4-三取代苯的化合物。 这些化合物预期会降低患者的A＆BGR 42水平，可用于治疗以升高的水平和/或形成A＆bgr为特征的疾病（如阿尔茨海默病）。 斑块

公开(公告)号：US20140038965A1

公开(公告)日：2014-02-06

申请号：US13919516

申请日：2013-06-17

Applicant: EnVivo Pharmaceuticals, Inc.

Inventor： Amy RIPKA ,  Gideon SHAPIRO ,  Richard CHESWORTH

IPC: C07D405/14 ,  C07D413/14

CPC classification number: A61K31/53 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comparing cognitive deficits or schizophrenic symptoms.

Abstract translation: 作为磷酸二酯酶10的抑制剂的5-和6-元杂环化合物被描述为方法，药物组合物，药物制剂和化合物在治疗哺乳动物（包括中枢神经系统（CNS）病症的人）中的药物用途 和其他可能影响CNS功能的疾病。 还描述了治疗神经系统，神经变性和精神病学障碍，包括但不限于那些比较认知缺陷或精神分裂症症状的疾病。

公开(公告)号：US08815933B2

公开(公告)日：2014-08-26

申请号：US14175654

申请日：2014-02-07

Applicant: EnVivo Pharmaceuticals, Inc.

Inventor： Richard Chesworth ,  Gideon Shapiro ,  Gerhard Koenig

IPC: A61K31/403 ,  C07D487/02 ,  A61K31/439

CPC classification number: A61K31/439 ,  A61P25/00

Abstract: (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide has been found to have procognitive effects in humans at unexpectedly low doses. Thus, (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and pharmaceutically acceptable salts thereof can be used at unexpectedly low doses to improve cognition.

Abstract translation: 已经发现（R）-7-氯-N-（奎宁环-3-基）苯并[b]噻吩-2-甲酰胺在意想不到的低剂量下对人体具有认知作用。 因此，可以以意想不到的低剂量使用（R）-7-氯-N-（奎宁环-3-基）苯并[b]噻吩-2-甲酰胺及其药学上可接受的盐，以改善认知。

公开(公告)号：US08569354B2

公开(公告)日：2013-10-29

申请号：US13674290

申请日：2012-11-12

Applicant: EnVivo Pharmaceuticals, Inc.

Inventor： Richard Chesworth ,  Gideon Shapiro ,  Gerhard Koenig

IPC: A61K31/403 ,  C07D487/02

CPC classification number: A61K31/439 ,  A61P25/00

Abstract: (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide has been found to have procognitive effects in humans at unexpectedly low doses. Thus, (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and pharmaceutically acceptable salts thereof can be used at unexpectedly low doses to improve cognition.

Abstract translation: 已经发现（R）-7-氯-N-（奎宁环-3-基）苯并[b]噻吩-2-甲酰胺在意想不到的低剂量下对人体具有认知作用。 因此，可以以意想不到的低剂量使用（R）-7-氯-N-（奎宁环-3-基）苯并[b]噻吩-2-甲酰胺及其药学上可接受的盐，以改善认知。

公开(公告)号：US20130165486A1

公开(公告)日：2013-06-27

申请号：US13756871

申请日：2013-02-01

Applicant: ENVIVO PHARMACEUTICALS, INC.

Inventor： Gideon SHAPIRO ,  Richard CHESWORTH

IPC: C07D309/08 ,  C07C229/42 ,  C07D285/14 ,  C07C59/64 ,  C07D271/12 ,  C07C205/56 ,  C07C59/72

CPC classification number: C07C51/09 ,  C07C51/42 ,  C07C59/72 ,  C07C67/343 ,  C07C67/48 ,  C07C69/734 ,  C07C69/757 ,  C07C205/37 ,  C07C205/55 ,  C07C205/56 ,  C07C229/42 ,  C07C255/57 ,  C07C323/18 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D271/12 ,  C07D277/64 ,  C07D285/14 ,  C07D309/08

Abstract: Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described.

Abstract translation: 描述了作为γ分泌酶的调节剂的四氮取代的苯及其在治疗治疗神经变性疾病例如阿尔茨海默病的一种或多种症状中的用途。

公开(公告)号：US20040255341A1

公开(公告)日：2004-12-16

申请号：US10852951

申请日：2004-05-25

Applicant: EnVivo Pharmaceuticals, Inc.

Inventor： David A. Lowe ,  Gerhard Koenig ,  Christopher J. Cummings

IPC: G01N033/00 ,  A01K067/00 ,  A01K067/033

CPC classification number: A01K67/0339 ,  A01K2217/05 ,  A01K2227/706 ,  A01K2267/0312 ,  C12N15/8509

Abstract: The present invention discloses a transgenic fly that expresses the Arctic mutant version of the human Anull42 peptide of human amyloid-null precursor protein (APP), and a double transgenic fly that expresses both the Tau protein and the human Anull42Arctic peptide of human amyloid-null precursor protein (APP). The transgenic flies of the present invention provide for models of neurodegenerative disorders, such as Alzheimer's disease. The invention further discloses methods for identifying genetic modifiers, as well as screening methods to identify therapeutic compounds to treat neurodegenerative disorders using the transgenic flies.

Abstract translation: 本发明公开了一种表达人淀粉样蛋白-β前体蛋白（APP）的人Abeta42肽的北极突变体型的转基因飞行物，以及表达人淀粉样蛋白-β的Tau蛋白和人Abeta42Arctic肽的双转基因蝇 前体蛋白（APP）。 本发明的转基因苍蝇提供了神经变性疾病如阿尔茨海默氏病的模型。 本发明进一步公开了用于鉴定遗传修饰剂的方法，以及用于鉴定使用转基因苍蝇治疗神经变性疾病的治疗化合物的筛选方法。

公开(公告)号：US20040126319A1

公开(公告)日：2004-07-01

申请号：US10676424

申请日：2003-10-01

Applicant: Baylor College of Medicine ,  European Molecular Biology Laboratory (EMBL) ,  EnVivo Pharmaceuticals

Inventor： Edvard Falt ,  Luis Serrano ,  Cayetano Gonzalez ,  Christian Boulin ,  Christopher J. Cummings ,  Juan Botas ,  Huda Zoghbi

IPC: C12Q001/68 ,  A61K049/00

CPC classification number: G06T7/20 ,  G06T7/0012 ,  G06T2207/30004

Abstract: The present invention provides a method for screening for the effect of a test agent on a population of biological specimens, preferably insects, comprising the steps of providing a population of specimens, administering at least one test agent to the population, creating a digitized movie showing the movements of members of the population, measuring at least one trait of members of the population, and correlating the traits of the population with the effect of the test agent. The invention also provides a method for preparing a medicament useful for the treatment of a mammalian disease.

Abstract translation: 本发明提供了一种用于筛选测试试剂对生物标本群体（优选昆虫）的影响的方法，其包括以下步骤：提供一组标本，向群体施用至少一种测试试剂，产生数字化电影，其显示 人口的流动，衡量人口的至少一个特征，并将人口的特征与检验人员的影响相关联。 本发明还提供了制备用于治疗哺乳动物疾病的药物的方法。

公开(公告)号：US20140249179A1

公开(公告)日：2014-09-04

申请号：US14184453

申请日：2014-02-19

Applicant: ENVIVO PHARMACEUTICALS, INC.

Inventor： Patricia Oliver-Shaffer ,  Gideon Shapiro ,  Richard Chesworth ,  Muneki Kishida ,  Takayuki Ishige

IPC: C07D453/02

CPC classification number: C07D453/02 ,  A61K9/4833 ,  A61K31/439 ,  C07B2200/13 ,  C30B29/54

Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.

Abstract translation: （R）-7-氯-N-（奎宁环-3-基）苯并[b]噻吩-2-甲酰胺盐酸盐一水合物的结晶形式I和II及其制备方法及其治疗用途。

公开(公告)号：US20140148479A1

公开(公告)日：2014-05-29

申请号：US14139178

申请日：2013-12-23

Applicant: EnVivo Pharmaceuticals, Inc.

Inventor： Richard Chesworth ,  Gideon Shapiro ,  Gerhard Koenig

IPC: A61K31/439

CPC classification number: A61K31/439 ,  A61P25/00

Abstract: (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide has been found to have procognitive effects in humans at unexpectedly low doses. Thus, (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and pharmaceutically acceptable salts thereof can be used at unexpectedly low doses to improve cognition.

Abstract translation: 已经发现（R）-7-氯-N-（奎宁环-3-基）苯并[b]噻吩-2-甲酰胺在意想不到的低剂量下对人体具有认知作用。 因此，可以以意想不到的低剂量使用（R）-7-氯-N-（奎宁环-3-基）苯并[b]噻吩-2-甲酰胺及其药学上可接受的盐，以改善认知。