公开(公告)号：US20070238136A1

公开(公告)日：2007-10-11

申请号：US11733232

申请日：2007-04-10

申请人： Jeffrey Miller ,  Elizabeth Arner ,  Robert Copeland ,  Gary Davis ,  Ruiqin Liu ,  Michael Pratta ,  Micky Tortorella

发明人： Jeffrey Miller ,  Elizabeth Arner ,  Robert Copeland ,  Gary Davis ,  Ruiqin Liu ,  Michael Pratta ,  Micky Tortorella

IPC分类号： G01N33/53 ,  C12Q1/34

CPC分类号： C12N9/6489 ,  A61K38/00 ,  C07K16/40 ,  C12Q1/37 ,  G01N33/6887 ,  G01N2333/96486 ,  G01N2500/00 ,  G01N2800/102

摘要： This invention is directed to assays to determine the presence or absence of proteins that exhibit aggrecanase or ADMP activity. This invention also relates to peptides that acts as a substrates for ADMPs, their use in various assays to determine the presence or absence of ADMP activity, and their use as inhibitors of ADMP activity.

摘要翻译： 本发明涉及确定存在或不存在表现出聚集蛋白聚糖蛋白聚糖酶或ADMP活性的蛋白质的测定法。 本发明还涉及作为ADMP底物的肽，其用于各种测定以确定ADMP活性的存在或不存在，以及它们作为ADMP活性抑制剂的用途。

公开(公告)号：US07250435B2

公开(公告)日：2007-07-31

申请号：US11064758

申请日：2005-02-24

申请人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Anup P. Vidwans ,  Eddy Yue

发明人： David A. Nugiel ,  David J. Carini ,  Susan V. Di Meo ,  Anup P. Vidwans ,  Eddy Yue

IPC分类号： A61K31/415 ,  C07D231/54

CPC分类号： C07D401/04 ,  C07D231/54 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14

摘要： The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

摘要翻译： 本发明涉及新一类式（I）的茚并[1,2-c]吡唑-4-酮的合成：其是称为细胞周期蛋白依赖性激酶的酶类的有效抑制剂，其涉及 催化亚基cdk1-7及其调控亚基称为细胞周期蛋白AG。 本发明还提供了通过施用治疗有效量的这些化合物之一或其药学上可接受的盐形式来治疗癌症或其它增殖性疾病的新方法。 或者，可以通过施用本发明的一种化合物和一种或多种其它已知的抗癌或抗增殖剂的治疗有效组合来治疗癌症或其它增殖性疾病。

公开(公告)号：US20070173491A1

公开(公告)日：2007-07-26

申请号：US11655637

申请日：2007-01-19

申请人： Qi Han ,  Hong Liu ,  Richard Olson ,  Michael Yang

发明人： Qi Han ,  Hong Liu ,  Richard Olson ,  Michael Yang

IPC分类号： A61K31/55 ,  A61K31/5513 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07D401/04 ,  C07D223/12 ,  C07D223/18 ,  C07D243/12 ,  C07D243/24 ,  C07D403/02

摘要： This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

摘要翻译： 本发明涉及式（I）的新型内酰胺：具有药物和生物影响性质，其药物组合物和使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。

公开(公告)号：US20070161790A1

公开(公告)日：2007-07-12

申请号：US11717440

申请日：2007-03-13

申请人： James Sherbine ,  Shawn Pack ,  Jaan Pesti ,  Robert Yule ,  Kenneth McNulty

发明人： James Sherbine ,  Shawn Pack ,  Jaan Pesti ,  Robert Yule ,  Kenneth McNulty

IPC分类号： C07D487/04

CPC分类号： C07D231/38 ,  C07D487/04

摘要： The present invention provides novel processes and intermediates for preparing corticotropin releasing factor (CRF) receptor antagonists having the structure below which are useful in treating CRF-related disorders such as anxiety and depression.

摘要翻译： 本发明提供了用于制备具有以下结构的促肾上腺皮质激素释放因子（CRF）受体拮抗剂的新方法和中间体，其可用于治疗CRF相关疾病如焦虑和抑郁。

公开(公告)号：US20070140973A1

公开(公告)日：2007-06-21

申请号：US11610216

申请日：2006-12-13

申请人： D. Edwards ,  David Casebier

发明人： D. Edwards ,  David Casebier

IPC分类号： A61K49/10

CPC分类号： A61K49/0002 ,  A61K49/1809 ,  A61K49/1812 ,  A61K49/223 ,  B82Y5/00

摘要： The present invention is directed, in part, to compounds and methods for diagnostic imaging, comprising administering to a patient a contrast agent which has an overall negative charge.

摘要翻译： 本发明部分地涉及用于诊断成像的化合物和方法，包括向患者施用具有总负电荷的造影剂。

公开(公告)号：USRE39679E1

公开(公告)日：2007-06-05

申请号：US11356423

申请日：2006-02-16

申请人： Albert J. Robichaud ,  Taekyu Lee ,  Wei Deng ,  Ian S. Mitchell ,  Michael Guang Yang ,  Simon Haydar ,  Wenting Chen ,  Christopher D. McClung ,  Emile J. B. Calvello ,  David M. Zawrotny ,  Parthasarathl Rajagopalan

发明人： Albert J. Robichaud ,  Taekyu Lee ,  Wei Deng ,  Ian S. Mitchell ,  Michael Guang Yang ,  Simon Haydar ,  Wenting Chen ,  Christopher D. McClung ,  Emile J. B. Calvello ,  David M. Zawrotny ,  Parthasarathl Rajagopalan

IPC分类号： C07D267/22 ,  C07D281/18 ,  C07D267/02 ,  C07D279/00 ,  C07D265/34

CPC分类号： C07D471/06 ,  C07D221/18 ,  C07D223/32 ,  C07D491/06 ,  C07D495/06

摘要： The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

公开(公告)号：US07223834B2

公开(公告)日：2007-05-29

申请号：US09975813

申请日：2001-10-12

申请人： Jeffrey A. Miller ,  Elizabeth C. Arner ,  Robert A. Copeland ,  Gary L. Davis ,  Ruiqin Liu ,  Michael A. Pratta ,  Micky D. Tortorella

发明人： Jeffrey A. Miller ,  Elizabeth C. Arner ,  Robert A. Copeland ,  Gary L. Davis ,  Ruiqin Liu ,  Michael A. Pratta ,  Micky D. Tortorella

IPC分类号： A61K38/00 ,  A61K38/17 ,  C12N9/00 ,  C12N9/14

CPC分类号： C12N9/6489 ,  A61K38/00 ,  C07K16/40 ,  C12Q1/37 ,  G01N33/6887 ,  G01N2333/96486 ,  G01N2500/00 ,  G01N2800/102

摘要： This invention is directed to assays to determine the presence or absence of proteins that exhibit aggrecanase or ADMP activity. This invention also relates to peptides that acts as a substrates for ADMPs, their use in various assays to determine the presence or absence of ADMP activity, and their use as inhibitors of ADMP activity.

摘要翻译： 本发明涉及确定存在或不存在表现出聚集蛋白聚糖蛋白聚糖酶或ADMP活性的蛋白质的测定法。 本发明还涉及作为ADMP底物的肽，其用于各种测定以确定ADMP活性的存在或不存在，以及它们作为ADMP活性抑制剂的用途。

公开(公告)号：US07179446B2

公开(公告)日：2007-02-20

申请号：US09995388

申请日：2001-11-27

申请人： Alan P. Carpenter, Jr.

发明人： Alan P. Carpenter, Jr.

IPC分类号： A61K49/00

CPC分类号： A61K49/14 ,  A61K38/00 ,  A61K49/0004 ,  A61K49/085 ,  A61K49/223 ,  A61K51/0476 ,  A61K51/082 ,  A61K51/088 ,  C07D259/00 ,  C07K7/52

摘要： The present invention describes a method of concurrent imaging in a mammal comprising: a) administering to said mammal a vitronectin receptor targeted imaging agent and a perfusion imaging agent; and b) concurrently detecting the vitronectin target imaging agent bound at the vitronectin receptor and the perfusion imaging agent; and c) forming an image from the detection of said vitronectin receptor targeted imaging agent and said perfusion imaging agent.

摘要翻译： 本发明描述了哺乳动物同时成像的方法，包括：a）向所述哺乳动物施用玻连蛋白受体靶向成像剂和灌注成像剂; 和b）同时检测在玻连蛋白受体和灌注显像剂结合的玻连蛋白目标显像剂; 和c）从所述玻连蛋白受体靶向成像剂和所述灌注成像剂的检测中形成图像。

公开(公告)号：US20060258638A1

公开(公告)日：2006-11-16

申请号：US11492593

申请日：2006-07-25

申请人： Richard Olson ,  Thomas Maduskuie ,  Lorin Thompson

发明人： Richard Olson ,  Thomas Maduskuie ,  Lorin Thompson

IPC分类号： A61K31/554 ,  A61K31/553 ,  A61K31/5513 ,  A61K31/55

CPC分类号： C07D223/12 ,  C07D243/24 ,  C07D401/06 ,  C07D401/10 ,  C07D405/12

摘要： This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

公开(公告)号：US20060135762A1

公开(公告)日：2006-06-22

申请号：US11327721

申请日：2006-01-06

申请人： Richard Olson ,  Michael Yang

发明人： Richard Olson ,  Michael Yang

IPC分类号： C07D267/02 ,  C07D243/12

CPC分类号： C07D223/16 ,  A61K31/4015 ,  A61K31/445 ,  A61K31/55 ,  A61K38/00 ,  C07D223/10 ,  C07D223/12 ,  C07D223/18 ,  C07D243/14 ,  C07D243/24 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/0812

摘要： This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

摘要翻译： 本发明涉及具有式（I）的新型环状丙二酰胺：其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。