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61. 发明授权

US07465725B2 Pyrimidine compounds 失效
标题翻译：嘧啶化合物
公开(公告)号：US07465725B2
公开(公告)日：2008-12-16
申请号：US11193001
申请日：2005-07-29
申请人： Mitsunori Ono , Lijun Sun , Teresa Przewloka , Shijie Zhang , Elena Kostik , Weiwen Ying , Yumiko Wada , Keizo Koya
发明人： Mitsunori Ono , Lijun Sun , Teresa Przewloka , Shijie Zhang , Elena Kostik , Weiwen Ying , Yumiko Wada , Keizo Koya
IPC分类号： A61K31/506 , A61P17/06 , A61P19/02 , A61P25/28 , C07D401/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D239/24
CPC分类号： C07D239/48 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D401/14 , C07D403/12
摘要： This invention features pyrimidine compounds of formula (I): R1 is aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C═N—Rc, C═N—ORc, C═N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
摘要翻译：本发明具有式（I）的嘧啶化合物：R1是芳基或杂芳基; R 2和R 4各自独立地是Rc，卤素，硝基，氰基，异硫脲，SRc或ORc; 或R 2和R 4一起是羰基; R3是Rc，烯基，炔基，ORc，OC（O）Rc，SO2Rc，S（O）Rc，S（O2）NRcRd，SRc，NRcRd，NRcCORd，NRcC（O）ORd，NRcC（O）NRcRd，NRcSO2Rd， CORc，C（O）ORc或C（O）NRcRd; R5是H或烷基; n是0，1，2，3，4，5或6; X是O，S，S（O），S（O 2）或NR c; Y是共价键，CH2，C（O），C-N-Rc，C-N-ORc，C-N-SRc，O，S，S（O），S（O 2）或NRc; Z是N或CH; U和V之一是N，另一个是CRc; 并且W是O，S，S（O），S（O 2），NR c或NC（O）R c; 其中R a和R b各自独立地为H，烷基，芳基，杂芳基; R c和R d各自独立地为H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基。

62. 发明申请

US20080214655A1 Paclitaxel enhancer compounds 失效
标题翻译：紫杉醇增强剂化合物
公开(公告)号：US20080214655A1
公开(公告)日：2008-09-04
申请号：US12009641
申请日：2008-01-18
申请人： Keizo Koya , Lijun Sun , Shoujun Chen , Noriaki Tatsuta , Yaming Wu , Mitsunori Ono
发明人： Keizo Koya , Lijun Sun , Shoujun Chen , Noriaki Tatsuta , Yaming Wu , Mitsunori Ono
IPC分类号： A61K31/337
CPC分类号： A61K47/48176 , A61K31/16 , A61K31/165 , A61K31/277 , A61K31/337 , A61K31/381 , A61K31/44 , A61K31/505 , A61K31/53 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D305/14 , C07D307/68 , C07D333/38 , C07D333/68 , C07D407/12
摘要： Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—.R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group.Z is ═O or ═S.Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with Paclitaxel or an analog of Paclitaxel.
摘要翻译：公开了由结构式（I）表示的化合物：Y是共价键，亚苯基或取代或未取代的直链烃基。此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选地，Y是共价键或-C（R 7 R 8） - 。 R 1和R 2分别独立地是芳基或取代的芳基，R 3和R 4是独立的-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 5 -R 6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团或R 7为-H， 8是取代或未取代的芳基，或者R 7和R 8一起是C2-C6取代或未取代的亚烷基。 Z是-O或-S。还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。还公开了通过向受试者施用结合式（I）的化合物与紫杉醇或紫杉醇的类似物组合来治疗患有癌症的受试者的方法。

63. 发明申请

US20080167300A1 PYRIDINE COMPOUNDS 有权
标题翻译：吡啶化合物
公开(公告)号：US20080167300A1
公开(公告)日：2008-07-10
申请号：US12041662
申请日：2008-03-03
申请人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Teresa Przewloka , Hao Li , Howard P. Ng , Zachary Demko
发明人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Teresa Przewloka , Hao Li , Howard P. Ng , Zachary Demko
IPC分类号： A61K31/5377 , A61P43/00
CPC分类号： C07D413/12 , C04B35/632 , C07D213/77 , C07D401/12 , C07D405/12
摘要： This invention features compounds of formula (I): pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12-related diseases and disorders.
摘要翻译：本发明的特征在于式（I）化合物：化合物的药物组合物，以及使用该化合物治疗特别是IL-12相关疾病和病症的方法。

64. 发明申请

US20080058297A1 Heterocyclic Compounds For Preventing And Treating Disorders Associated With Excessive Bone Loss 审中-公开
标题翻译：用于预防和治疗与过度骨丢失相关的疾病的杂环化合物
公开(公告)号：US20080058297A1
公开(公告)日：2008-03-06
申请号：US10561025
申请日：2004-05-28
申请人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Keizo Koya , Masazumi Nagai
发明人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Keizo Koya , Masazumi Nagai
IPC分类号： A61K31/56 , A61K31/496 , A61K31/5377 , C12N5/02 , C07D295/00 , A61K31/541
CPC分类号： C07D413/14 , C07D239/48 , C07D251/18 , C07D251/52 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/12 , C07D473/16
摘要： This invention relates to pyrimidine compounds of formula (I), formula (I′), and formula (I″): and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, R5, U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Pagers-disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcemia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).
摘要翻译：本发明涉及式（I），式（I'）和式（I“）的嘧啶化合物及其药学上可接受的盐，溶剂合物，包合物和前药，其中R 1， R 2，R 3，R 4，R 5，U，V，W，X，Y， Z和n在本文中定义。本发明还涉及包含这些化合物的组合物和使用它们的方法。本发明的化合物和组合物可用于治疗或预防与过量骨丢失相关的疾病，包括但不限于牙周病，非恶性骨病（例如骨质疏松症，骨骼传播者疾病，成骨不全，纤维性发育异常和原发性甲状旁腺功能亢进）雌激素缺乏，炎性骨丢失，骨恶性肿瘤，关节炎，骨硬化和某些癌症相关疾病（如恶性高钙血症（HCM），多发性骨髓瘤溶骨性骨损伤和乳腺癌和其他转移性癌症的溶骨性骨转移）。

65. 发明授权

US07338951B2 Pyridine compounds 有权
标题翻译：吡啶化合物
公开(公告)号：US07338951B2
公开(公告)日：2008-03-04
申请号：US10985696
申请日：2004-11-10
申请人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Teresa Przewloka , Hao Li , Howard P. Ng , Zachary Demko
发明人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Teresa Przewloka , Hao Li , Howard P. Ng , Zachary Demko
IPC分类号： C07D413/04 , A61K31/5377
CPC分类号： C07D413/12 , C04B35/632 , C07D213/77 , C07D401/12 , C07D405/12
摘要： This invention features compounds of formula (I): pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12-related diseases and disorders.
摘要翻译：本发明的特征在于式（I）化合物：化合物的药物组合物，以及使用该化合物治疗特别是IL-12相关疾病和病症的方法。

66. 发明授权

US07182972B2 Water-soluble bean-based extracts 失效
标题翻译：水溶性豆类提取物
公开(公告)号：US07182972B2
公开(公告)日：2007-02-27
申请号：US10747021
申请日：2003-12-23
申请人： Mitsunori Ono , Keizo Koya , Noriaki Tatsuta , Naoto Yamaguchi , Lan Bo Chen
发明人： Mitsunori Ono , Keizo Koya , Noriaki Tatsuta , Naoto Yamaguchi , Lan Bo Chen
IPC分类号： A23L1/20 , A23L1/40 , A23L1/48 , A23L2/00 , A23F5/00 , A23F3/00 , A23G3/00
CPC分类号： C07H17/07 , A23L33/105 , A23V2002/00 , A23V2250/2116
摘要： This invention relates to a water-soluble bean-based extract including one or more isoflavone glycosides. Also INCLUDED is a method of preparing such a water-soluble bean-based extract.
摘要翻译：本发明涉及包含一种或多种异黄酮糖苷的水溶性豆类提取物。还包括制备这种水溶性豆类提取物的方法。

67. 发明授权

US07001923B2 Taxol enhancer compounds 失效
标题翻译：紫杉醇增强剂化合物
公开(公告)号：US07001923B2
公开(公告)日：2006-02-21
申请号：US10803798
申请日：2004-03-18
申请人： Keizo Koya , Lijun Sun , Shoujun Chen , Noriaki Tatsuta , Yaming Wu , Mitsunori Ono , Zhi-Qiang Xia
发明人： Keizo Koya , Lijun Sun , Shoujun Chen , Noriaki Tatsuta , Yaming Wu , Mitsunori Ono , Zhi-Qiang Xia
IPC分类号： A61K31/16 , A61K31/335 , C07C327/00 , C07D305/00
CPC分类号： C07D307/68 , A45D2008/006 , A61K31/337 , A61K31/505 , A61K31/53 , A61K31/5377 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D333/38 , C07D333/68
摘要： One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—.R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, or a substituted non-aromatic hetereocyclic group, R2–R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, a substituted non-aromatic hetereocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.R5–R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2–C6 substituted or unsubstituted alkylene group.Z is ═O or ═S.Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.
摘要翻译：本发明的一个实施方案是由结构式（I）表示的化合物：<化学式id =“CHEM-US-00001”num =“000

68. 发明申请

US20060030560A1 Pyrimidine compounds 失效
标题翻译：嘧啶化合物
公开(公告)号：US20060030560A1
公开(公告)日：2006-02-09
申请号：US11193002
申请日：2005-07-29
申请人： Lijun Sun , Mitsunori Ono , Teresa Przewloka , Elena Kostik , Yumiko Wada
发明人： Lijun Sun , Mitsunori Ono , Teresa Przewloka , Elena Kostik , Yumiko Wada
IPC分类号： A61K31/541 , A61K31/5377
CPC分类号： C07D239/48 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D401/14 , C07D403/12
摘要： This invention features pyrimidine compounds of formula (I): R1 is each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C═N—Rc, C═N—ORc, C═N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
摘要翻译：本发明具有式（I）的嘧啶化合物：R 1和R 2各自为H; R 3是H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基; R 5是H或烷基; n是0，1，2，3，4，5或6; X是NR c; Y是共价键，CH 2，C（O），CNR C，O，CN-OR C， O，S，S（O），S（O 2 2）或NR C 2 O。 Z是N或CH; U和V之一是N，另一个是CR ; 和W是O，S，S（O），S（O 2 2），NR C或O或O（O）R c。其中R a，R b和R b各自独立地是H，烷基，芳基，杂芳基; 和R c是H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基。

69. 发明申请

US20060004044A1 3-glyoxylamideindoles for treating cancer 审中-公开
标题翻译： 3-乙醛酰胺吲哚治疗癌症
公开(公告)号：US20060004044A1
公开(公告)日：2006-01-05
申请号：US11136074
申请日：2005-05-24
申请人： Keizo Koya , Lijun Sun , Mitsunori Ono , Guiqing Liang , David James , Hao Li , Zhi-Qiang Xia
发明人： Keizo Koya , Lijun Sun , Mitsunori Ono , Guiqing Liang , David James , Hao Li , Zhi-Qiang Xia
IPC分类号： A61K31/4709 , A61K31/425 , A61K31/42 , A61K31/4196 , A61K31/405
CPC分类号： C07D249/08 , C07D209/12 , C07D209/18 , C07D231/12 , C07D233/56 , C07D401/12 , C07D403/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by Structural Formula (I) (preferably an effective amount). Also disclosed is a method of treating a subject with cancer by administering to the subject an effective amount of a compound represented by Structural Formula (I).
摘要翻译：公开了由结构式（I）表示的抗癌化合物：结构式（I）中的变量如下所述。还公开了包含药学上可接受的载体或稀释剂和由结构式（I）表示的化合物（优选有效量））的药物组合物。还公开了通过向受试者施用有效量的由结构式（I）表示的化合物来治疗患有癌症的受试者的方法。

70. 发明申请

US20050272766A1 1-Glyoxylamide indolizines for treating lung and ovarian cancer 审中-公开
标题翻译： 1-乙酰氧基吲哚啉用于治疗肺癌和卵巢癌
公开(公告)号：US20050272766A1
公开(公告)日：2005-12-08
申请号：US11088253
申请日：2005-03-23
申请人： Keizo Koya , Lijun Sun , Hao Li , Mitsunori Ono
发明人： Keizo Koya , Lijun Sun , Hao Li , Mitsunori Ono
IPC分类号： A61K31/437 , A61K31/4745
CPC分类号： A61K31/437 , A61K31/4745
摘要： A method of treating a subject having lung cancer or ovarian cancer, comprising administering to the subject an effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt, solvate, or polymorph thereof: Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z1 and Z2 are independently ═O, ═S, ═N—OR12 or ═NR12 R1 and R2 are independently —H, an aliphatic group, a substituted aliphatic group, an unsubstituted non-aromatic heterocylic group, a substituted non-aromatic heterocylic group, an aryl group or a substituted aryl group, provided that R1 and R2 are not both —H. Alternatively, —NR1R2, taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, —C(R4R5)—, —N(R4)—, —O—, —S—, —S(O)—, —S(O)2—, —C(═O)—, —C(═O)—N(R4)—, or —N(R4)—C(═O)—. R4 and R5 are independently —H or a substituted or unsubstituted aliphatic group. R12 is —H or a substituted or unsubstituted alkyl group.
摘要翻译：一种治疗患有肺癌或卵巢癌的受试者的方法，其包括向所述受试者施用有效量的由结构式（I）表示的化合物或其药学上可接受的盐，溶剂化物或多晶型物：环A是取代或未取代的，任选地与芳基稠合。 Z 1和Z 2独立地是-O，-S，-N-OR 12或-NR 12， R 1和R 2独立地是-H，脂族基团，取代的脂族基团，未取代的非芳族杂环基团，取代的非芳族杂环基团，芳基或取代的芳基，条件是R 1和R 2不同时为-H。或者，-NR 1 R 2 R 2一起是取代或未取代的非芳族含氮杂环基或取代或未取代的含氮杂芳基。 R 3是取代或未取代的芳基或取代或未取代的脂族基。 X是共价键，-C（R 4 R 5） - ， - N（R 4） - ， - O - ， - ，-S（O） - ， - S（O）2 - ， - C（ - ） - >） - 或-N（R 4） - C（-O） - 。 R 4和R 5独立地是-H或取代或未取代的脂族基团。 R 12是-H或取代或未取代的烷基。

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