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61. 发明申请

US20080275069A1 Quinazoline Derivative 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US20080275069A1
公开(公告)日：2008-11-06
申请号：US11628087
申请日：2005-05-30
申请人： Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A61K31/519 , C07D239/91 , A61P1/16 , A61P3/04 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/14 , A61P25/18 , C07D471/04 , C07D401/12 , A61P43/00 , A61P25/32 , A61P25/28 , A61P25/24 , A61P25/22 , A61P25/16 , A61P25/02 , A61P13/12 , A61P9/10 , A61P3/10 , A61P3/00 , A61K31/517
CPC分类号： C07D239/91 , C07D401/12 , C07D403/04 , C07D471/04
摘要： This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (I) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
摘要翻译：本发明提供式（I）的化合物或其药学上可接受的盐，其中R 1表示低级烷基等; R 2和R 3相同且不同，表示氢原子; R 4表示式（I）等的取代基; X 1表示NH，O或S; Y表示N或C; Ar是通过从其中除去两个氢原子而衍生自芳基等的二价取代基; 环A表示5-或6-元杂芳基; 该化合物具有组胺H3受体拮抗作用或组胺H3受体反向激动作用，可用于预防或治疗代谢系统疾病，循环系统疾病或神经系统疾病。

62. 发明申请

US20080188507A1 Novel azole derivatives 失效
标题翻译：新型唑衍生物
公开(公告)号：US20080188507A1
公开(公告)日：2008-08-07
申请号：US12071808
申请日：2008-02-26
申请人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
IPC分类号： A61K31/4747 , C07D491/14
CPC分类号： C07D491/10
摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine.The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立为次甲基或氮，所述次甲基任选被取代基取代，T，U，V和W中的至少两个为所述次甲基; X是氮或次甲基。本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸障碍，炎症性疾病或青光眼等。

63. 发明申请

US20080161326A1 Novel Sulfone Amide Amide Derivatives 失效
标题翻译：新型磺酰胺酰胺衍生物
公开(公告)号：US20080161326A1
公开(公告)日：2008-07-03
申请号：US10589693
申请日：2005-02-15
申请人： Norikazu Otake , Yoshio Ogino , Akio Kanatani
发明人： Norikazu Otake , Yoshio Ogino , Akio Kanatani
IPC分类号： A61K31/52 , C07D235/04 , A61K31/4184 , A61P3/04 , A61P3/10 , C07D473/00
CPC分类号： C07D471/04 , C07D235/14 , C07D473/00 , C07D487/04
摘要： The present invention relates to compounds of the general formula (I): wherein A, B, C and D each independently are a methine group or a nitrogen atom, said methine group optionally having a substituent(s) with at least one of them meaning the methine group; E means a group represented by the following formulae (E1): R1 means a lower alkyl group or an aryl group optionally having a substituent(s) or means a lower alkylene group linked to arbitrary, linkable position(s) of E, and others. The compounds of the present invention are useful as an agent for the treatment of a variety of diseases related to NPY.
摘要翻译：本发明涉及通式（I）的化合物：其中A，B，C和D各自独立地为次甲基或氮原子，所述次甲基任选具有取代基，其中至少一个为含义次甲基; E表示由下式（E1）表示的基团：R 1表示低级烷基或任选具有取代基的芳基，或指与任意可连接位置连接的低级亚烷基（E）等。本发明的化合物可用作治疗与NPY有关的各种疾病的药剂。

64. 发明授权

US07365079B2 Azole derivatives 失效
标题翻译：唑衍生物
公开(公告)号：US07365079B2
公开(公告)日：2008-04-29
申请号：US10536360
申请日：2003-11-25
申请人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
IPC分类号： A61K31/4355 , C07D471/04
CPC分类号： C07D491/10
摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立为次甲基或氮，所述次甲基任选被取代基取代，T，U，V和W中的至少两个为所述次甲基; X是氮或次甲基。本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸系统疾病，炎症性疾病疾病或青光眼等。

65. 发明申请

US20070099884A1 Combination therapy for the treatment of diabetes 审中-公开
标题翻译：联合治疗糖尿病治疗
公开(公告)号：US20070099884A1
公开(公告)日：2007-05-03
申请号：US10559206
申请日：2004-06-02
申请人： Ngozi Erondu , Tung Fong , Akio Kanatani , Douglas MacNeil , Leonardus Van Der Ploeg
发明人： Ngozi Erondu , Tung Fong , Akio Kanatani , Douglas MacNeil , Leonardus Van Der Ploeg
IPC分类号： A61K31/498 , A61K31/4747 , A61K31/4196 , A61K31/353
CPC分类号： A61K31/4747 , A61K31/353 , A61K31/4196 , A61K31/498 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compositions comprising an anti-obesity agent and an anti-diabetic agent useful for the treatment of diabetes, diabetes associated with obesity and diabetes-related disorders. The present invention further relates to methods of treating or preventing obesity, and obesity-related disorders, in a subject in need thereof by administering a composition of the present invention. The present invention further provides for pharmaceutical compositions, medicaments, and kits useful in carrying out these methods.
摘要翻译：本发明涉及包含抗肥胖剂和用于治疗糖尿病的抗糖尿病药物，与肥胖相关的糖尿病和糖尿病相关疾病的组合物。本发明还涉及通过给予本发明的组合物来治疗或预防有需要的受试者中肥胖和肥胖相关疾病的方法。本发明进一步提供可用于实施这些方法的药物组合物，药物和试剂盒。

66. 发明申请

US20050009879A1 N-substituted-2-oxodihydropyridine derivatives 失效
标题翻译： N-取代-2-氧代二氢吡啶衍生物
公开(公告)号：US20050009879A1
公开(公告)日：2005-01-13
申请号：US10899162
申请日：2004-07-27
申请人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
发明人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
IPC分类号： A61P3/04 , C07D213/80 , C07D401/04 , C07D401/14 , A61K31/4439 , C07
CPC分类号： C07D213/80 , C07D401/04 , C07D401/14
摘要： A compound of the formula (I): (wherein Ar1 and Ar2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R1 and R2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl; R3, R4 and R5 are independently hydrogen, cyano, halogen or hydroxy, or lower alkyl, lower alkoxy or lower alkylthio, the last three groups being optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl), or a salt or ester thereof is useful as a neuropeptide Y receptor antagonist agent and is also useful as an agent for the treatment of bulimia, obesity or diabetes.
摘要翻译：式（I）的化合物：其中Ar 1和Ar 2独立地为芳基或杂芳基，其中任何一个任选被选自氰基，卤素，硝基，低级烷基，卤代低级烷基，羟基 - 低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基，低级烯基，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，低级烷基磺酰基氨基，芳基磺酰基氨基，羟基，低级烷氧基，低级烷氧基，芳氧基，杂芳氧基，低级烷硫基，羧基，甲酰基，低级烷酰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，二低级烷基氨基甲酰基，低级烷基磺酰基，芳基磺酰基，芳基和杂芳基; R 1和R 2独立地为低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基或低级烷氧基，其中任何一个任选被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰氨基，羟基，低级烷氧基，甲酰基，低级烷基低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 3，R 4和R 5独立地是氢，氰基，卤素或羟基，或低级烷基，低级烷氧基或低级烷硫基，最后三个基团任选地被选自以下的取代基取代：卤素，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，羟基，低级烷氧基，甲酰基，低级烷氧基羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基）或其盐或酯可用作神经肽Y受体拮抗剂，可用作治疗贪食症，肥胖症或糖尿病的药剂。

67. 发明授权

US08044070B2 Heteroaryloxy nitrogenous saturated heterocyclic derivative 有权
标题翻译：杂环氧基含氮饱和杂环衍生物
公开(公告)号：US08044070B2
公开(公告)日：2011-10-25
申请号：US12540534
申请日：2009-08-13
申请人： Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
发明人： Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
IPC分类号： A61K31/445 , C07D211/00
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/501 , A61K31/506 , C07D401/14 , C07D403/12 , C07D413/14 , C07D471/04
摘要： Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.
摘要翻译：提供式（I）化合物及其药学上可接受的盐：其中X1，X2和X3各自独立地表示N或CH; W表示下式（II）：或下式（III）：Y表示式（IV）的基团：所述化合物具有组胺H3受体拮抗或反向激动活性，可用于治疗和/或预防肥胖，糖尿病，激素分泌障碍，睡眠障碍等

68. 发明授权

US07732456B2 Pyridone derivative 失效
标题翻译：吡啶酮衍生物
公开(公告)号：US07732456B2
公开(公告)日：2010-06-08
申请号：US10591373
申请日：2005-03-04
申请人： Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
IPC分类号： A61K31/444 , C07D401/02
CPC分类号： C07D213/69 , C07D237/16 , C07D239/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D451/02 , C07D471/04
摘要： The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].
摘要翻译：本发明提供由通式（I）表示的吡啶酮衍生物[在该式中，R 1和R 2可以相同或不同，代表H等，或者R 1和R 2可以与脂族含氮杂环基一起形成他们绑定的N X1-X3可以相同或不同，代替次甲基或N，但不是全部同时代表氮; X4-X7可以相同或不同，代表次甲基或N，条件是它们中的三个或更多不同时代表N; Y1和Y3可以相同或不同，代表单键，-O-，-NR-，-S-等; Y2代表低级亚烷基等; R代表H等，L代表亚甲基; Z 1和Z 2可以相同或不同，代表单键或低级亚烷基; 或R1，L和Z2可以与R1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。

69. 发明授权

US07645756B2 Nitrogenous fused heteroaromatic ring derivative 失效
标题翻译：含氮稠合杂芳环衍生物
公开(公告)号：US07645756B2
公开(公告)日：2010-01-12
申请号：US10589832
申请日：2005-02-17
申请人： Toshiyuki Takahashi , Akio Kanatani , Shigeru Tokita , Ryo Yoshimoto
发明人： Toshiyuki Takahashi , Akio Kanatani , Shigeru Tokita , Ryo Yoshimoto
IPC分类号： C07D487/04 , A61K31/5025 , A61K31/53 , A61P3/04 , A61P3/10 , A61P9/10
CPC分类号： C07D487/04
摘要： The invention provides a compound or its pharmaceutically-acceptable salt of formula wherein A1 is a hydrogen, etc.; j and k are 0 or 1; is a double bond, etc.; is a double bond, etc.; one of W1 and W2 is E—O—W, etc., and the other is a hydrogen atom, etc.; E is a divalent group derived from a benzene ring, etc., by removing two hydrogen atoms therefrom; W is a group of formula (II-1): which has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for prevention or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
摘要翻译：本发明提供了下式的化合物或其药学上可接受的盐：其中A1是氢等; j和k为0或1; “img id =”CUSTOM-CHARACTER-00001“he =”3.13mm“wi =”9.14mm“file =”US07645756-20100112-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>是双键等; “img id =”CUSTOM-CHARACTER-00002“he =”3.13mm“wi =”9.48mm“file =”US07645756-20100112-P00002.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>是双键等; W1和W2之一是E-O-W等，另一个是氢原子等; E是通过从其中除去两个氢原子而衍生自苯环等的二价基团; W是一组式（II-1）：其具有组胺H3受体拮抗作用或组胺H3受体反向激动作用，并且可用于预防或治疗代谢系统疾病，循环系统疾病或神经系统疾病。

70. 发明申请

US20080139589A1 Crystal of 4(3H)-Quinazolinone Derivative 失效
标题翻译： 4（3H） - 喹唑啉酮衍生物的晶体
公开(公告)号：US20080139589A1
公开(公告)日：2008-06-12
申请号：US11884138
申请日：2006-02-13
申请人： Akio Kanatani , Nagaaki Sato , Tsuyoshi Nagase , Shigeru Tokita
发明人： Akio Kanatani , Nagaaki Sato , Tsuyoshi Nagase , Shigeru Tokita
IPC分类号： A61K31/517 , C07D239/72 , A61P3/04 , A61P3/10 , A61P25/00
CPC分类号： C07D239/91 , A61K31/517 , A61K45/06
摘要： A substance that has a potency antagonistic to coupling of histamine with histamine H3 receptor or a potency of inhibiting the constant activity of histamine H3 receptor. There is provided a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that in the powder X- ray diffractometry, has peaks at 6.4°, 9.7°, 10.2°, 12.9°, 14.2°, 14.7°, 16.0°, 16.3°, 16.8°, 17.6°, 19.5°, 20.3°, 20.6°, 21.2°, 21.8°, 22.1°, 22.4°, 22.6°, 24.0°, 24.3°, 24.9°, 25.7°, 25.9°, 26.5°, 26.7°, 27.4°, 29.1°, 29.4°, 32.3° and 39.0° diffraction angles(2θ±0.2°).
摘要翻译：具有拮抗组胺与组胺H3受体的拮抗作用或抑制组胺H3受体的恒定活性的效力的物质。提供2-甲基3- {4- [3-（1-吡咯烷基）丙氧基]苯基} -5-三氟甲基-4（3H） - 喹唑啉酮的晶型I，其在粉末X射线衍射中具有峰在6.4°，9.7°，10.2°，12.9°，14.2°，14.7°，16.0°，16.3°，16.8°，17.6°，19.5°，20.3°，20.6°，21.2°，21.8°，22.1°，22.4° °，22.6°，24.0°，24.3°，24.9°，25.7°，25.9°，26.5°，26.7°，27.4°，29.1°，29.4°，32.3°和39.0°衍射角（2θ±0.2°）。

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