公开(公告)号：US20140073670A1

公开(公告)日：2014-03-13

申请号：US14082415

申请日：2013-11-18

Applicant: AVENTIS PHARMACEUTICALS INC.

Inventor： Sudhakara Rao BADABHAGNI ,  Nilesh JAISWAL ,  Praveen KHULLAR ,  Kum PRASAD

IPC: A61K31/445

CPC classification number: A61K31/445 ,  A61K9/4816 ,  A61K9/4866

Abstract: The present invention relates to a pharmaceutical formulation of fexofenadine hydrochloride in a solvent system suitable as a liquid fill composition.In another aspect, the invention also relates to a process for the preparation of the pharmaceutical formulation and the use of the composition for the treatment of allergic reactions in a patient.

Abstract translation: 本发明涉及在适合作为液体填充组合物的溶剂体系中盐酸非索非那定的药物制剂。 在另一方面，本发明还涉及制备药物制剂的方法和该组合物用于治疗患者过敏反应的用途。

公开(公告)号：US08288425B2

公开(公告)日：2012-10-16

申请号：US11029064

申请日：2005-01-04

Applicant: Michael L. Edwards ,  Paul J. Cox ,  Shelley Amendola ,  Stephanie D. Deprets ,  Timothy A. Gillespy ,  Christopher D. Edlin ,  Andrew D. Morley ,  Charles J. Gardner ,  Brian Pedgrift ,  Herve Bouchard ,  Didier Babin ,  Laurence Gauzy ,  Alain Le-Brun ,  Tahir N. Majid ,  John C. Reader ,  Lloyd J. Payne ,  Nawaz M. Khan ,  Michael Cherry

Inventor： Michael L. Edwards ,  Paul J. Cox ,  Shelley Amendola ,  Stephanie D. Deprets ,  Timothy A. Gillespy ,  Christopher D. Edlin ,  Andrew D. Morley ,  Charles J. Gardner ,  Brian Pedgrift ,  Herve Bouchard ,  Didier Babin ,  Laurence Gauzy ,  Alain Le-Brun ,  Tahir N. Majid ,  John C. Reader ,  Lloyd J. Payne ,  Nawaz M. Khan ,  Michael Cherry

IPC: A61K31/4184 ,  C07D235/18

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Abstract translation: 本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

公开(公告)号：US20120114660A1

公开(公告)日：2012-05-10

申请号：US12503778

申请日：2009-07-15

Applicant: Michael C. Jaye ,  Kim-Anh Thi Doan ,  John A. Krawiec ,  Kevin J. Lynch ,  Dilip V. Amin ,  Victoria J. South

Inventor： Michael C. Jaye ,  Kim-Anh Thi Doan ,  John A. Krawiec ,  Kevin J. Lynch ,  Dilip V. Amin ,  Victoria J. South

IPC: A61K39/395 ,  A61P3/06

CPC classification number: C07K16/40 ,  A01K2217/05 ,  A61K38/00 ,  C12N9/18 ,  C12N9/20

Abstract: Lipoprotein Lipase like polypeptides, nucleic acids encoding said polypeptides, antisense sequences, and antibodies to said polypeptides are disclosed. Also disclosed are methods for the preparation of said polypeptides in a recombinant system and for the use of said polypeptides to screen for agonists and or antagonists of said polypeptides. Also disclosed are methods and compositions for the treatment of disorders of lipid metabolism.

Abstract translation: 公开了脂蛋白脂肪酶样多肽，编码所述多肽的核酸，反义序列和针​​对所述多肽的抗体。 还公开了在重组系统中制备所述多肽的方法，以及所述多肽用于筛选所述多肽的激动剂和/或拮抗剂的方法。 还公开了用于治疗脂质代谢紊乱的方法和组合物。

公开(公告)号：US20120034188A1

公开(公告)日：2012-02-09

申请号：US13195392

申请日：2011-08-01

Applicant: Kun Guo ,  Marco F. Pagnoni ,  Kenneth L. Clark ,  Yuri D. Ivashchenko

Inventor： Kun Guo ,  Marco F. Pagnoni ,  Kenneth L. Clark ,  Yuri D. Ivashchenko

IPC: A61K48/00 ,  C07K16/40 ,  A61P9/10 ,  G01N33/53 ,  C12Q1/68 ,  C12N5/07 ,  C12N9/12 ,  A61K35/76

CPC classification number: C12N9/1205 ,  A61K48/00 ,  C07K14/47 ,  C12N2799/021 ,  C12N2799/022 ,  C12N2799/027 ,  C12N2799/028

Abstract: The present invention relates to human Akt3 proteins and polypeptides. The invention also relates to isolated nucleic acids encoding human Akt3, to vectors containing them and to their therapeutic uses, in particular for gene therapy. Expression of Akt3 inhibits cell death associated with hypoxia, apoptosis or necrosis.

Abstract translation: 本发明涉及人Akt3蛋白和多肽。 本发明还涉及编码人Akt3的分离的核酸，含有它们的载体和其治疗用途，特别是用于基因治疗。 Akt3的表达抑制与缺氧，凋亡或坏死相关的细胞死亡。

公开(公告)号：US08008340B2

公开(公告)日：2011-08-30

申请号：US11675230

申请日：2007-02-15

Applicant: William Arthur Metz, Jr.

Inventor： William Arthur Metz, Jr.

IPC: A01N43/38 ,  A61K31/40 ,  C07D209/04

CPC classification number: A61K31/404

Abstract: A method for inhibiting casein kinase Iε activity, comprising administering to said patient a therapeutically effective amount of a compound of formula I. its stereoisomer, enantiomer, racemate, tautomer or pharmaceutically acceptable salt thereof.

Abstract translation: 一种抑制酪蛋白激酶I的方法 活性，包括向所述患者施用治疗有效量的式I化合物。其立体异构体，对映异构体，外消旋物，互变异构体或其药学上可接受的盐。

公开(公告)号：US07977045B2

公开(公告)日：2011-07-12

申请号：US12728984

申请日：2010-03-22

Applicant: Soo-Il Kim

Inventor： Soo-Il Kim

IPC: C12Q1/70

CPC classification number: A61K9/0043 ,  A61K9/006 ,  A61K9/08 ,  A61K31/573 ,  A61K31/58 ,  A61K47/32 ,  A61K47/36 ,  A61K47/38 ,  B05B11/3018 ,  Y10S514/951 ,  Y10S514/975

Abstract: An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (D) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively high and such that it resists being cleared from the mucosal surfaces by the inherent mucocillary forces which are present in the nasal cavity, a method of use of the composition and a method for preparation of the composition, including in preferred form the use of anti-inflammatory steroid, for example, triamcinolone acetonide, and an odorless form of the composition.

Abstract translation: 一种能够喷洒到个体鼻腔中的水性药物组合物，其包含：（A）药物有效量的药物固体颗粒，其通过存在于粘膜上而有效地治疗身体状况 鼻腔表面; 和（B）有效维持所述颗粒均匀分散在组合物中并赋予组合物以下触变性能的悬浮剂：（i）以非HEED形式的位置的粘度相对较高，其组成为 呈凝胶状; （ii）当组合物经过剪切（摇动）制备用于喷雾时，组合物的粘度变得相对较低，并且使得雾状形式的组合物容易地流入鼻道以沉积在粘膜表面上 鼻腔; 和（D）沉积形式在粘膜表面上，组合物的粘度相对较高，使得其抵抗通过存在于鼻腔中的固有粘膜毛孔而从粘膜表面清除，使用 组合物和组合物的制备方法，包括优选形式使用抗炎类固醇，例如曲安奈德，以及组合物的无味形式。

公开(公告)号：US07923466B2

公开(公告)日：2011-04-12

申请号：US12269216

申请日：2008-11-12

Applicant: William Arthur Metz, Jr. ,  Fa-Xiang Ding

Inventor： William Arthur Metz, Jr. ,  Fa-Xiang Ding

IPC: A61K31/404

CPC classification number: C07D491/10 ,  C07D209/42 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

Abstract: Methods for the treatment of a patient suffering from a disease or disorder ameliorated by inhibition of casein kinase Iε activity comprising the administration of a compounds of formula (I) and formula (II) as inhibitors of human casein kinase Iε, and methods of using the compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) useful in the claimed methods of treatment are also disclosed.

Abstract translation: 用于治疗患有通过抑制酪蛋白激酶I改变的疾病或病症的患者的方法; 包括施用式（I）和式（II）化合物作为人酪蛋白激酶I的抑制剂的活性;以及使用式（I）和式（II）化合物治疗中枢神经系统疾病和病症的方法 包括情绪障碍和睡眠障碍。 R基取代基在本文中定义，并且也公开了包含用于所要求保护的治疗方法的式（I）或式（II）化合物的药物组合物。

公开(公告)号：US07919508B2

公开(公告)日：2011-04-05

申请号：US11552169

申请日：2006-10-24

Applicant: Gregory Shutske ,  Keith J. Harris ,  Kenneth J. Bordeau ,  Michael R. Angelastro ,  Stanly John ,  Joseph T. Klein ,  Jinqi Lu ,  Catherine Bomont

Inventor： Gregory Shutske ,  Keith J. Harris ,  Kenneth J. Bordeau ,  Michael R. Angelastro ,  Stanly John ,  Joseph T. Klein ,  Jinqi Lu ,  Catherine Bomont

IPC: A61K31/452 ,  C07D405/02

CPC classification number: C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention provides compounds of formula I: a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, X and n are defined as defined herein. Additionally, a method for treating dopamine-related neurological disorders selected form the group consisting of neurological, psychological, cardiovascular, cognitive or attention disorders, substance abuse and addictive behavior, or a combination thereof, comprising administering to a patient in need of such treatment a therapeutically effective amount of compounds of formula I.

Abstract translation: 本发明提供式I化合物：其立体异构体或其药学上可接受的盐，其中变量R1，R2，R3，R4，X和n如本文所定义。 另外，一种治疗多巴胺相关神经系统疾病的方法，其选自神经学，心理学，心血管学，认知或注意障碍，药物滥用和成瘾行为或其组合，其包括向需要这种治疗的患者施用 治疗有效量的式I化合物。

公开(公告)号：US07772252B2

公开(公告)日：2010-08-10

申请号：US12425731

申请日：2009-04-17

Applicant: James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M Shutske ,  Joseph T Strupczewski ,  Kenneth J Bordeau ,  John G Jurcak ,  Thaddeus Nieduzak ,  Sharon A. Jackson ,  Paul Angell ,  James P Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

Inventor： James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M Shutske ,  Joseph T Strupczewski ,  Kenneth J Bordeau ,  John G Jurcak ,  Thaddeus Nieduzak ,  Sharon A. Jackson ,  Paul Angell ,  James P Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

IPC: A61K31/4535 ,  C07D409/04 ,  C07D409/14 ,  C07D495/04

CPC classification number: A61K31/496 ,  C07D209/08 ,  C07D213/74 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D239/42 ,  C07D241/04 ,  C07D241/20 ,  C07D249/08 ,  C07D261/20 ,  C07D295/14 ,  C07D295/155 ,  C07D307/66 ,  C07D307/68 ,  C07D317/58 ,  C07D333/58 ,  C07D333/66 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/06 ,  C07D495/04 ,  C07D498/04

Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D3 receptors.

Abstract translation: 本发明涉及显示与多巴胺D3受体的选择性结合的杂环取代的羰基衍生物。 另一方面，本发明涉及一种治疗需要这种治疗的患者中与多巴胺D3受体活性相关的中枢神经系统障碍的方法，其包括向受试者施用治疗有效量的所述化合物以减轻这种病症。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏综合征和亨廷顿疾病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及本文所述化合物的制备方法以及制备和使用化合物作为多巴胺D3受体的显像剂的方法。

公开(公告)号：US07723074B2

公开(公告)日：2010-05-25

申请号：US12348990

申请日：2009-01-06

Applicant: Ashfaq Parkar ,  Paul August ,  Theresa Kuntzweiler ,  Mohamad Ali Ardati ,  Namadev Baskaran

Inventor： Ashfaq Parkar ,  Paul August ,  Theresa Kuntzweiler ,  Mohamad Ali Ardati ,  Namadev Baskaran

IPC: C12P21/06 ,  C12N1/20 ,  C12N1/00 ,  C12N15/00 ,  C12N5/00 ,  C12N5/02 ,  C12N5/07 ,  C12N5/10 ,  C12N15/74 ,  C07H21/04

CPC classification number: C07K14/72 ,  C07K14/723 ,  C07K2319/00

Abstract: Described herein is a novel member of the prostanoid receptor family, a guinea pig prostaglandin D2 receptor. Described are the receptor, the nucleic acid that encodes it, and various uses for both.

Abstract translation: 本文描述的是前列腺素受体家族的新成员，豚鼠前列腺素D2受体。 描述的是受体，编码它的核酸，以及两者的各种用途。