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11. 发明申请

US20060148807A1 Pyrrolo[1,2b]pyridazine compounds and their uses 审中-公开
标题翻译：吡咯并[1,2b]哒嗪化合物及其用途
公开(公告)号：US20060148807A1
公开(公告)日：2006-07-06
申请号：US11378537
申请日：2006-03-17
申请人： Jian-min Fu
发明人： Jian-min Fu
IPC分类号： A61K31/503 , G01N33/53
CPC分类号： A61K31/503 , G01N33/566 , G01N2500/00
摘要： Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I): including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) R is H or Me.
摘要翻译：公开了新的CRF受体拮抗剂及其用于治疗多种疾病的用途，包括表现出CRF过度分泌或与CRF或CRF受体如焦虑和抑郁症相关的疾病。本发明的CRF受体拮抗剂具有式（I）的结构：包括立体异构体或立体异构体的混合物，药学上可接受的前药或其药学上可接受的盐，其中在式（I）中R是H或Me。

12. 发明申请

US20060128710A1 Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof 审中-公开
标题翻译：对香草素受体亚型1（VR1）的拮抗剂及其用途
公开(公告)号：US20060128710A1
公开(公告)日：2006-06-15
申请号：US11292979
申请日：2005-12-02
申请人： Chih-Hung Lee , Brian Brown , Ryan Keddy , Richard Perner , John Koenig
发明人： Chih-Hung Lee , Brian Brown , Ryan Keddy , Richard Perner , John Koenig
IPC分类号： A61K31/519 , A61K31/503 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： C07D471/04
摘要： Compounds having formula (I) or formula (II) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A, N, X, Y, R1, R2 and R3 are as defined in the specification. These compounds are particularly useful in the treatment of pain, inflammatory hyperalgesia, and urinary dysfunctions, such as bladder overactivity and urinary incontinence.
摘要翻译：具有式（I）或式（II）的化合物或其前药的药学上可接受的盐，前药或盐，其中A，N，X，Y，R 1，R 2 ＆lt;＆gt;和＆lt; 3＆gt;＆gt;如说明书中所定义。这些化合物特别可用于治疗疼痛，炎性痛觉过敏和尿功能障碍，例如膀胱过度活动和尿失禁。

13. 发明申请

US20060074087A1 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes 有权
公开(公告)号：US20060074087A1
公开(公告)日：2006-04-06
申请号：US10542694
申请日：2004-01-27
申请人： Wallace Ashton , Charles Caldwell , Joseph Duffy , Robert Mathvink , Liping Wang , Ann Weber
发明人： Wallace Ashton , Charles Caldwell , Joseph Duffy , Robert Mathvink , Liping Wang , Ann Weber
IPC分类号： A61K31/519 , A61K31/503 , A61K31/498 , C07D487/02
CPC分类号： C07D471/04 , C07D217/06 , C07D217/26
摘要： The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

14. 发明申请

US20060041125A1 Substituted pyrido-pyridazine derivatives which enhance cognition via the gaba-a receptors 失效
标题翻译：取代的吡啶并哒嗪衍生物，其通过gaba-α受体增强认知
公开(公告)号：US20060041125A1
公开(公告)日：2006-02-23
申请号：US10531517
申请日：2003-10-29
申请人： Simon Goodacre , David Hallett
发明人： Simon Goodacre , David Hallett
IPC分类号： C07D487/02 , A61K31/503
CPC分类号： C07D471/04
摘要： The present invention discloses a compound of formula 1, or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, —CO2Ra, —CONRaRb or —CRa&=NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; a pharmaceutical composition comprising it; its use in a method of treatment; use of it to manufacture a medicament; and a method of using it to prevent or treat anxiety, convulsions or cognitive disorders.
摘要翻译：本发明公开了式1化合物或其药学上可接受的盐：其中X 1表示氢，卤素，C 1-6烷基，三氟甲基或C _{1-6烷氧基; X 2表示氢或卤素; Y表示化学键，氧原子或-NH-键; Z表示任选取代的芳基或杂芳基; R 1表示氢，烃，杂环基，卤素，氰基，三氟甲基，硝基，-OR a，-SR a，-SOR 一个或两个以上的一个或多个，其中，R 1，R 2，R 2，其中，R a，R b，R b，R b，R b， CO 2，CO 2 CO 2 SO 2，-SO 2 R 2，或者 - a 并且R a和R b独立地表示氢，烃或杂环基; 包含它的药物组合物; 其用于治疗方法; 使用它制造药物; 以及使用它来预防或治疗焦虑，抽搐或认知障碍的方法。}

15. 发明申请

US20060004008A1 Topoisomerase-targeting agents 有权
标题翻译：拓扑异构酶靶向剂
公开(公告)号：US20060004008A1
公开(公告)日：2006-01-05
申请号：US11121292
申请日：2005-05-03
申请人： Edmond LaVoie , Alexander Ruchelman , Leroy Liu
发明人： Edmond LaVoie , Alexander Ruchelman , Leroy Liu
IPC分类号： A61K31/503 , A61K31/4745 , C07D471/02 , C07D487/02
CPC分类号： C07D491/04
摘要： The invention provides compounds of formula I or formula II: wherein: the bond represented by — is a single bond or a double bond, and R1-R5, X, and Y have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I or II, processes for preparing compounds of formula I or II, intermediates useful for preparing compounds of formula I or II, and therapeutic methods for treating cancer and other topoisomerase related conditions using compounds of formula I or II.
摘要翻译：本发明提供式I或式II化合物：其中：由 - 表示的键是单键或双键，R 1 -R 5，X，和Y具有本说明书中定义的任何含义及其药学上可接受的盐。本发明还提供了包含式I或II化合物的药物组合物，制备式I或II化合物的方法，可用于制备式I或II化合物的中间体，以及用于治疗癌症和其它拓扑异构酶相关病症的治疗方法，公式I或II。

16. 发明申请

US20050267182A1 Urea derivatives as FLT-3 modulators 审中-公开
标题翻译：脲衍生物作为FLT-3调节剂
公开(公告)号：US20050267182A1
公开(公告)日：2005-12-01
申请号：US10989717
申请日：2004-11-15
申请人： Zdravko Milanov , Shamal Mehta , Robert Grotzfeld , Andiliy Lai , Hitesh Patel , David Lockhart
发明人： Zdravko Milanov , Shamal Mehta , Robert Grotzfeld , Andiliy Lai , Hitesh Patel , David Lockhart
IPC分类号： A61K20060101 , A61K31/42 , A61K31/47 , A61K31/4709 , A61K31/4745 , A61K31/503 , A61K31/517 , A61K31/519 , A61K31/52 , C07D215/38 , C07D231/12 , C07D231/40 , C07D261/06 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/46 , C07D277/82 , C07D405/12 , C07D413/00 , C07D413/02 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D473/10 , C07D487/04 , C07D495/04 , C07D513/04
CPC分类号： C07D231/12 , A61K31/42 , C07D231/40 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/46 , C07D277/82 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D495/04 , C07D513/04 , Y02A50/401 , Y02A50/411
摘要： The invention provides methods and compositions for treating conditions mediated FLT-3. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.
摘要翻译：本发明提供用于治疗介导的FLT-3的病症的方法和组合物。本发明还提供了使用化合物和/或组合物治疗受试者中各种疾病和不需要的病症的方法。

17. 发明申请

US20050261297A1 Nitrogen-containing heterocyclic compound 失效
公开(公告)号：US20050261297A1
公开(公告)日：2005-11-24
申请号：US11190859
申请日：2005-07-28
申请人： Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
发明人： Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
IPC分类号： A61P19/00 , A61P19/08 , A61P19/10 , A61P43/00 , C07D487/04 , A61K31/503 , A61K31/55
CPC分类号： C07D487/04
摘要： As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention. Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.

18. 发明申请

US20050192314A1 Urea derivatives as C-kit modulators 审中-公开
标题翻译：尿素衍生物作为C-kit调节剂
公开(公告)号：US20050192314A1
公开(公告)日：2005-09-01
申请号：US10990195
申请日：2004-11-15
申请人： Shamal Mehta , Zdravko Milanov , Robert Grotzfeld , Hitesh Patel , Andiliy Lai , David Lockhart
发明人： Shamal Mehta , Zdravko Milanov , Robert Grotzfeld , Hitesh Patel , Andiliy Lai , David Lockhart
IPC分类号： A61K20060101 , A61K31/42 , A61K31/47 , A61K31/4709 , A61K31/4745 , A61K31/503 , A61K31/517 , A61K31/519 , A61K31/52 , C07D215/38 , C07D231/12 , C07D231/40 , C07D261/06 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/46 , C07D277/82 , C07D405/12 , C07D413/00 , C07D413/02 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D473/10 , C07D487/04 , C07D495/04 , C07D513/04
CPC分类号： C07D231/12 , A61K31/42 , C07D231/40 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/46 , C07D277/82 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D495/04 , C07D513/04 , Y02A50/401 , Y02A50/411
摘要： The invention provides methods and compositions for treating conditions mediated by c-kit kinase. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.
摘要翻译：本发明提供了用于治疗由c-kit激酶介导的病症的方法和组合物。本发明还提供了使用化合物和/或组合物治疗受试者中各种疾病和不需要的病症的方法。

19. 发明申请

US20050171171A1 Amide derivatives as FLT-3 modulators 审中-公开
标题翻译：酰胺衍生物作为FLT-3调节剂
公开(公告)号：US20050171171A1
公开(公告)日：2005-08-04
申请号：US10989766
申请日：2004-11-15
申请人： Shamal Mehta , Robert Grotzfeld , Zdravko Milanov , Andiliy Lai , Hitesh Patel , David Lockhart
发明人： Shamal Mehta , Robert Grotzfeld , Zdravko Milanov , Andiliy Lai , Hitesh Patel , David Lockhart
IPC分类号： A61K20060101 , A61K31/42 , A61K31/47 , A61K31/4709 , A61K31/4745 , A61K31/503 , A61K31/517 , A61K31/519 , A61K31/52 , C07D215/38 , C07D231/12 , C07D231/40 , C07D261/06 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/46 , C07D277/82 , C07D405/12 , C07D413/00 , C07D413/02 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D473/10 , C07D487/04 , C07D495/04 , C07D513/04
CPC分类号： C07D231/12 , A61K31/42 , C07D231/40 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/46 , C07D277/82 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D495/04 , C07D513/04 , Y02A50/401 , Y02A50/411
摘要： The invention provides methods and compositions for treating conditions mediated by flt-3 wherein derivatives of amide compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.
摘要翻译：本发明提供用于治疗由flt-3介导的病症的方法和组合物，其中使用酰胺化合物的衍生物。本发明还提供了使用化合物和/或组合物治疗受试者中各种疾病和不需要的病症的方法。

20. 发明申请

US20050165031A1 Urea derivatives as ABL modulators 审中-公开
标题翻译：尿素衍生物作为ABL调节剂
公开(公告)号：US20050165031A1
公开(公告)日：2005-07-28
申请号：US10989814
申请日：2004-11-15
申请人： Robert Grotzfeld , Hitest Patel , Shamal Mehta , Zdravko Milanov , Andiliy Lai , David Lockhart
发明人： Robert Grotzfeld , Hitest Patel , Shamal Mehta , Zdravko Milanov , Andiliy Lai , David Lockhart
IPC分类号： A61K20060101 , A61K31/42 , A61K31/47 , A61K31/4709 , A61K31/4745 , A61K31/503 , A61K31/517 , A61K31/519 , A61K31/52 , C07D215/38 , C07D231/12 , C07D231/40 , C07D261/06 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/46 , C07D277/82 , C07D405/12 , C07D413/00 , C07D413/02 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D473/10 , C07D487/04 , C07D495/04 , C07D513/04
CPC分类号： C07D231/12 , A61K31/42 , C07D231/40 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/46 , C07D277/82 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D495/04 , C07D513/04 , Y02A50/401 , Y02A50/411
摘要： The invention provides methods and compositions for treating conditions mediated by Bcr-Abl. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.
摘要翻译：本发明提供用于治疗由Bcr-Abl介导的病症的方法和组合物。本发明还提供了使用化合物和/或组合物治疗受试者中各种疾病和不需要的病症的方法。

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