公开(公告)号：US20050245743A1

公开(公告)日：2005-11-03

申请号：US10518675

申请日：2003-07-03

Applicant: Mohammad Marzabadi ,  Jiang Yu ,  Kai Lu ,  Chien-An Chen ,  John De Leon ,  John Wetzel

Inventor： Mohammad Marzabadi ,  Jiang Yu ,  Kai Lu ,  Chien-An Chen ,  John De Leon ,  John Wetzel

IPC: A61K31/44 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/506 ,  A61P3/04 ,  A61P13/02 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D211/26 ,  C07D211/70 ,  C07D401/12 ,  C07D211/68 ,  C07D41/02 ,  C07D43/02

CPC classification number: C07D211/26 ,  C07D401/12

Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compounds of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject=s depression and/or anxiety. This invention further provides a method of treating a subject suffering from a urinary disorder.

Abstract translation: 本发明涉及作为黑色素浓缩激素-1（MCH1）受体的选择性拮抗剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明提供通过将治疗有效量的本发明化合物与药学上可接受的载体组合而成的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物与药学上可接受的载体组合。 本发明还提供减少受试者体重的方法，其包括向受试者施用一定量的有效减少受试者体重的本发明化合物。 本发明进一步提供了治疗患有抑郁症和/或焦虑症的受试者的方法，其包括向受试者施用有效治疗受试者抑郁症和/或焦虑的量的本发明化合物。 本发明还提供了治疗患有尿失禁的受试者的方法。

公开(公告)号：US20050245578A1

公开(公告)日：2005-11-03

申请号：US11110682

申请日：2005-04-21

Applicant: Pietro Allegrini ,  Gianpiero Ventimiglia ,  Antonio Sommei ,  Graziano Castaldi

Inventor： Pietro Allegrini ,  Gianpiero Ventimiglia ,  Antonio Sommei ,  Graziano Castaldi

IPC: A61K31/4184 ,  A61K31/4439 ,  A61P1/04 ,  C07D401/12 ,  C07D43/02

CPC classification number: C07D401/12

Abstract: Novel crystalline forms of pantoprazole sodium salt solvate with ketone solvents, a process for the preparation thereof, the use of the forms for the purification of pantoprazol, pharmaceutical compositions therefrom and the use thereof in therapy.

Abstract translation: 泮托拉唑钠盐的新型结晶形式用酮溶剂溶剂合物，其制备方法，使用泮托​​拉唑纯化形式，其药物组合物及其在治疗中的用途。

公开(公告)号：US20050245530A1

公开(公告)日：2005-11-03

申请号：US11111144

申请日：2005-04-21

Applicant: Robert Borzilleri ,  Lyndon Cornelius ,  Robert Schmidt ,  Gretchen Schroeder ,  Kyoung Kim

Inventor： Robert Borzilleri ,  Lyndon Cornelius ,  Robert Schmidt ,  Gretchen Schroeder ,  Kyoung Kim

IPC: A61K31/44 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61P35/00 ,  C07D213/68 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D239/34 ,  C07D239/42 ,  C07D239/46 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/02 ,  C07D417/02 ,  C07D417/12 ,  C07D43/02

CPC classification number: C07D213/82 ,  C07D213/68 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/89 ,  C07D239/34 ,  C07D239/42 ,  C07D239/47 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12

Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.

Abstract translation: 本发明涉及具有下式的化合物及其用于治疗癌症的方法。

公开(公告)号：US20050245513A1

公开(公告)日：2005-11-03

申请号：US10508261

申请日：2003-03-17

Applicant: Michel Gallant ,  Denis Deschenes ,  Daniel Dube ,  Laurence Dube ,  Patrick Lacombe ,  Dwight MacDonald

Inventor： Michel Gallant ,  Denis Deschenes ,  Daniel Dube ,  Laurence Dube ,  Patrick Lacombe ,  Dwight MacDonald

IPC: A61K31/4709 ,  A61K31/5377 ,  A61P11/00 ,  A61P25/00 ,  C07D215/04 ,  C07D215/12 ,  C07D215/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/02 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12 ,  C07D487/04 ,  C07D43/02

CPC classification number: C07D215/04 ,  C07D215/12 ,  C07D215/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04

Abstract: 8-arylquinolines wherein the aryl group at the 8-position contains a meta one or two atom bridge to a phenyl, 5 or 6 member heteroaryl or fused bicyclic heteroaryl group, and wherein at least one of the bridge atoms is not carbon, are PDE4 inhibitors.

Abstract translation: 8-芳基喹啉，其中8-位上的芳基含有与苯基，5或6元杂芳基或稠合双环杂芳基相连的一个或两个原子桥，并且其中至少一个桥原子不是碳，是PDE4 抑制剂。

公开(公告)号：US20050245499A1

公开(公告)日：2005-11-03

申请号：US11001760

申请日：2004-12-02

Applicant: Judith Straub ,  Michael Hale ,  Francois Maltais ,  Gabriel Martinez-Botella ,  Alex Aronov ,  Guy Bemis

Inventor： Judith Straub ,  Michael Hale ,  Francois Maltais ,  Gabriel Martinez-Botella ,  Alex Aronov ,  Guy Bemis

IPC: A61K31/506 ,  A61K45/06 ,  C07D239/48 ,  C07D251/18 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  A61K31/4545 ,  A61K31/53 ,  C07D43/02

CPC classification number: C07D239/48 ,  A61K31/506 ,  A61K45/06 ,  C07D251/18 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  A61K2300/00

Abstract: Described herein are compounds that are useful as protein kinase inhibitors of formula I: or a pharmaceutically acceptable salt thereof, wherein Ring B, Z1, Z2, U, p, Q, R1, R2, R3, and R3 are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including stroke, inflammatory disorders, autoimmune diseases such as SLE lupus and psoriasis, proliferative disorders such as cancer, and conditions associated with organ transplantation.

Abstract translation: 本文描述了可用作式I的蛋白激酶抑制剂的化合物或其药学上可接受的盐，其中环B，Z 1，Z 2，U，p， Q，R 1，R 2，R 3，R 3和R 3如本文所定义。 这些化合物及其药学上可接受的组合物可用于治疗或减轻各种疾病的严重性，包括中风，炎性疾病，自身免疫性疾病如SLE狼疮和牛皮癣，增殖性疾病如癌症，以及与器官移植相关的病症 。

公开(公告)号：US20050239855A1

公开(公告)日：2005-10-27

申请号：US11112423

申请日：2005-04-22

Applicant: Siegfried Reich ,  Ted Bleckman ,  Susan Kephart ,  William Romines ,  Michael Wallace

Inventor： Siegfried Reich ,  Ted Bleckman ,  Susan Kephart ,  William Romines ,  Michael Wallace

IPC: B22D11/10 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4375 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/5377 ,  A61P9/00 ,  A61P35/00 ,  A61P43/00 ,  B22D41/50 ,  B22D41/56 ,  C07D231/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D521/00 ,  C07D43/02

CPC classification number: C07D249/08 ,  B22D41/56 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/04 ,  C07F7/1804

Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

公开(公告)号：US20050239829A1

公开(公告)日：2005-10-27

申请号：US10515845

申请日：2003-05-29

Applicant: Masami Takahashi ,  Tsutomu Miyake ,  Yasunori Moritani ,  Hidetoshi Asai ,  Taketoshi Ishii ,  Rikako Kono

Inventor： Masami Takahashi ,  Tsutomu Miyake ,  Yasunori Moritani ,  Hidetoshi Asai ,  Taketoshi Ishii ,  Rikako Kono

IPC: A61K31/445 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/513 ,  A61K38/00 ,  C07D211/46 ,  C07D211/54 ,  C07D211/58 ,  C07D211/62 ,  C07D211/74 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12 ,  C07D473/34 ,  C07K5/02 ,  C07K5/06 ,  C07K5/083 ,  C07K5/087 ,  C07K5/097 ,  C07K5/103 ,  C07D43/02

CPC classification number: C07D211/46 ,  A61K38/00 ,  C07D211/54 ,  C07D211/58 ,  C07D211/62 ,  C07D211/74 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12 ,  C07D473/34 ,  C07K5/0202 ,  C07K5/06191 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0821 ,  C07K5/1008

Abstract: The present invention provides a novel piperidine compound of the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted benzene ring, R1 represents an optionally substituted alkyl group, an optionally substituted hydroxyl group, etc., or a group of the formula: (a) wherein R11 and R12 are the same or different, and each represents hydrogen atom, a substituted carbonyl group, a substituted sulfonyl group, an optionally substituted alkyl group, etc., R2 represents hydrogen atom, etc., Z represents oxygen atom or a group represented by —N(R3)—, R3 represents hydrogen atom or an alkyl group, etc., R4 represents hydrogen atom or an alkyl group, etc., or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明提供式[I]的新的哌啶化合物：其中环A表示任选取代的苯环，环B表示任选取代的苯环，R 1表示任选取代的烷基， 任选取代的羟基等，或下式的基团：（a）其中R 11和R 12相同或不同，并且各自表示氢原子 取代的羰基，取代的磺酰基，任意取代的烷基等，R 2表示氢原子等，Z表示氧原子或-N（R' R 3表示氢原子或烷基等，R 4表示氢原子或烷基等， 或其药学上可接受的盐。

公开(公告)号：US20050239796A1

公开(公告)日：2005-10-27

申请号：US11122293

申请日：2005-05-04

Applicant: Christophe Thurieau ,  Jerome Gonzalez ,  Christophe Moinet

Inventor： Christophe Thurieau ,  Jerome Gonzalez ,  Christophe Moinet

IPC: A61K31/445 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/5377 ,  A61P5/00 ,  A61P5/02 ,  A61P5/08 ,  A61P5/48 ,  A61P19/00 ,  A61P35/00 ,  C07D211/58 ,  C07D211/96 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61K31/496 ,  C07D43/02 ,  C07D45/02

CPC classification number: C07D401/12 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

Abstract translation: 本申请的主题是下式的4-氨基哌啶的新衍生物，其中R 1，R 2和R 3代表各种基团， 并通过合成方法在液相和固相中并行制备其制备方法。 这些产品与生长抑素受体的某些亚型具有良好的亲和力，它们特别可用于治疗涉及一种（或更多种）生长抑素受体的病理状态或疾病。

公开(公告)号：US20050239776A1

公开(公告)日：2005-10-27

申请号：US10512248

申请日：2003-04-22

Applicant: Albert Amegadzie ,  Kevin Gardinier ,  Erik Hembre ,  Jian Hong ,  Louis Jungheim ,  Brian Muehl ,  David Remick ,  Michael Robertson ,  Kenneth Savin

Inventor： Albert Amegadzie ,  Kevin Gardinier ,  Erik Hembre ,  Jian Hong ,  Louis Jungheim ,  Brian Muehl ,  David Remick ,  Michael Robertson ,  Kenneth Savin

IPC: A61K31/4192 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P3/10 ,  A61P7/12 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/08 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/04 ,  A61P19/10 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P27/02 ,  A61P29/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D249/04 ,  C07D249/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D413/02 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/02 ,  C07D417/14 ,  C07D43/02

CPC classification number: C07D249/06 ,  C07D249/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.

Abstract translation: 本发明涉及式（I）的选择性NK-1受体拮抗剂; 或其药学上可接受的盐，用于治疗与过速的速激肽相关的病症。

公开(公告)号：US20050236976A1

公开(公告)日：2005-10-27

申请号：US11024798

申请日：2004-12-30

Applicant: Man-Kit Leung ,  Hsien-Chang Lin ,  Meng-Yen Chou ,  Shen-Shen Wang ,  Kuei-Hui Yang

Inventor： Man-Kit Leung ,  Hsien-Chang Lin ,  Meng-Yen Chou ,  Shen-Shen Wang ,  Kuei-Hui Yang

IPC: C07C211/54 ,  C07C211/58 ,  C09K11/06 ,  H01J1/62 ,  H01J63/04 ,  H01L51/00 ,  H01L51/50 ,  H05B33/14 ,  C07D43/02

CPC classification number: H05B33/14 ,  C07C211/54 ,  C07C211/58 ,  C09K11/06 ,  C09K2211/1014 ,  C09K2211/1029 ,  H01L51/0052 ,  H01L51/0059 ,  H01L51/006 ,  H01L51/0061 ,  H01L51/0068 ,  H01L51/0072 ,  H01L51/0081 ,  H01L51/5048 ,  H01L2251/308

Abstract: The present invention relates to an organic electroluminescent device, comprising a first electrode, an organic luminescent layer and a second electrode which disposed over a substrate. The organic electroluminescent layer comprises compound of formula (I) compound, wherein that Ar1—Ar6 are individual hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C3-6 cycloalkyl, substituted or unsubstituted C3-10 alkenyl, substituted or unsubstituted C6-40 aromatic amino, substituted or unsubstituted C6-40 aromatic, substituted or unsubstituted C6-40 poly cyclic aromatic, or substituted or unsubstituted C6-40 aralkyl.

Abstract translation: 本发明涉及一种有机电致发光器件，其包括设置在衬底上的第一电极，有机发光层和第二电极。 有机电致发光层包括式（I）化合物的化合物，其中Ar 1 -Ar 6是单独的氢，取代或未取代的C 1-6 - 取代或未取代的C 3-6环烷基，取代或未取代的C 3-10链烯基，取代或未取代的C 6-6 - 芳族氨基，取代或未取代的C 6-6芳基，取代或未取代的C 6-14-40多环芳族或取代或未取代的C 6-6 - 芳烷基。