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    Spiro compounds
    2.
    发明授权
    Spiro compounds 失效
    螺环化合物

    公开(公告)号：US07205417B2

    公开(公告)日：2007-04-17

    申请号：US10485955

    申请日：2002-08-02

    申请人： Takehiro Fukami ,  Katsumasa Nonoshita ,  Takeshi Sagara ,  Hiroyuki Kishino

    发明人： Takehiro Fukami ,  Katsumasa Nonoshita ,  Takeshi Sagara ,  Hiroyuki Kishino

    IPC分类号： C07D307/94 ,  C07D407/12 ,  A61K31/4525

    CPC分类号： C07D401/12 ,  A61K31/4747 ,  C07D209/96 ,  C07D307/94 ,  C07D403/12 ,  C07D405/12 ,  C07D471/10 ,  C07D491/10

    摘要： Compounds of the formula (I): (wherein A is an optionally substituted straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom; Ar1 is aryl or heteroaryl, any of which is optionally substituted; n is 0 or 1; R0 is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; T, U, V and W are independently nitrogen atom or optionally substituted methine, and at least two of T, U, V and W are said methine group; X is —N(SO2R1)—, —N(COR2)— or —CO—; Y is —C(R3)(R4)—, —O— or —N(R5)—; Z is methine or nitrogen atom) exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, and gastro-intestinal motility disorder.

    摘要翻译： 式（I）的化合物：

    Spiro compounds
    3.
    发明授权
    Spiro compounds 有权
    螺环化合物

    公开(公告)号：US06649624B2

    公开(公告)日：2003-11-18

    申请号：US10226225

    申请日：2002-08-23

    申请人： Takehiro Fukami ,  Akio Kanatani ,  Akane Ishihara ,  Yasuyuki Ishii ,  Toshiyuki Takahashi ,  Yuji Haga ,  Toshihiro Sakamoto ,  Takahiro Itoh

    发明人： Takehiro Fukami ,  Akio Kanatani ,  Akane Ishihara ,  Yasuyuki Ishii ,  Toshiyuki Takahashi ,  Yuji Haga ,  Toshihiro Sakamoto ,  Takahiro Itoh

    IPC分类号： A61K31438

    CPC分类号： C07D405/12 ,  C07D213/61 ,  C07D307/94 ,  C07D471/10 ,  C07D491/10

    摘要： A method for treating a central nervous system disorder, which involves administering to a patient in need a therapeutically effective amount of a compound of formula (I): wherein Ar1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, nitro, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, cyclo(lower) alkyl, lower alkenyl, lower alkoxy, halo(lower) alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, hydroxy, lower alkoxy, halo(lower) alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl: n represents 0 or 1; Q represents a single bond or carbonyl; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine; Y represents an imino which may be substituted with lower alkyl, or oxygen; or a salt or ester thereof

    摘要翻译： 一种治疗中枢神经系统疾病的方法，其涉及向需要的患者施用治疗有效量的式（I）化合物：其中Ar 1表示可被取代的芳基或杂芳基，所选择的取代基 卤代低级烷基，羟基（低级）烷基，环（低级）烷基，低级烯基，低级烷氧基，卤代（低级）烷氧基，低级烷硫基，羧基，低级烷酰基， 低级烷氧基羰基，任选被氧代取代的低级亚烷基和由式-Q-Ar 2表示的基团; Ar 2表示可被取代的芳基或杂芳基，该取代基选自卤素， 氰基，低级烷基，卤代（低级）烷基，羟基（低级）烷基，羟基，低级烷氧基，卤代（低级）烷氧基，低级烷基氨基，二低级烷基氨基，低级烷酰基和芳基：n表示0或1; Q表示 单键或羰基; T，U，V和W各自独立地表示 反应可以具有选自卤素，低级烷基，羟基和低级烷氧基的取代基的氮原子或次甲基，其中至少两个表示所述次甲基; X表示次甲基; Y表示亚氨基， 被低级烷基或氧取代; 或其盐或酯

    Novel benzimidazole derivatives
    7.
    发明申请
    Novel benzimidazole derivatives 失效

    公开(公告)号：US20060205750A1

    公开(公告)日：2006-09-14

    申请号：US11431274

    申请日：2006-05-10

    申请人： Norikazu Otake ,  Minoru Moriya ,  Yoshio Ogino ,  Kenji Matsuda ,  Yoshikazu Nagae ,  Akio Kanatani ,  Takehiro Fukami

    发明人： Norikazu Otake ,  Minoru Moriya ,  Yoshio Ogino ,  Kenji Matsuda ,  Yoshikazu Nagae ,  Akio Kanatani ,  Takehiro Fukami

    IPC分类号： A61K31/4747 ,  A61K31/4184 ,  C07D487/10

    CPC分类号： C07D473/30 ,  C07D405/04 ,  C07D471/04 ,  C07D471/10 ,  C07D473/00 ,  C07D491/04

    摘要： The present invention relates to a compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is —N(SO2R4)—, —N(COR5)— or —CO—; Y is —C(R6)(R7)—, —O— or —N(R8)—, provided that the compound (I) when E is nitrogen, n is 0, X is —CO—, and Y is —O— is excluded) and the like, which are useful as an agent for the treatment of various diseases related to NPY, for example cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorder, inflammatory diseases or glaucoma, and the like, also for example, atherosclerosis, hypogonadism, hyperandrogenism, polycystic ovary syndrome (Pickwickian syndrome), hirsutism, gastro-intestinal motility disorder, obesity-related gastro-esophageal reflux, obesity hypoventilation, sleep apnea, inflammation, systemic inflammation of the vasculature, osteoarthritis, insulin resistance, bronchoconstriction, alcohol preference, metabolic syndrome, Alzheimer's disease, cardiac hypertrophy, left ventricular hypertrophy, hypertriglyceridemia, low HDL cholesterol, cardiovascular disorders such as coronary heart disease (CHD), cerebrovascular disease, stroke, peripheral vascular disease, sudden death, gallbladder diseases, cancer (breast, endometrial, colon), breathlessness, hyperuricemia, impaired fertility, low back pain, or increased anesthetic risk, and the like.

    Spiro compounds
    8.
    发明授权
    Spiro compounds 有权
    螺环化合物

    公开(公告)号：US06388077B1

    公开(公告)日：2002-05-14

    申请号：US09983598

    申请日：2001-10-25

    申请人： Takehiro Fukami ,  Akio Kanatani ,  Akane Ishihara ,  Yasuyuki Ishii ,  Toshiyuki Takahashi ,  Yuji Haga ,  Toshihiro Sakamoto ,  Takahiro Itoh

    发明人： Takehiro Fukami ,  Akio Kanatani ,  Akane Ishihara ,  Yasuyuki Ishii ,  Toshiyuki Takahashi ,  Yuji Haga ,  Toshihiro Sakamoto ,  Takahiro Itoh

    IPC分类号： C07D491107

    CPC分类号： C07D405/12 ,  C07D213/61 ,  C07D307/94 ,  C07D471/10 ,  C07D491/10

    摘要： Compounds of the general formula VI-1 and processes for their preparation: wherein t, u, v and w each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and optionally protected hydroxy; and wherein at least two of which represent the methine group. These compounds serve as intermediates for novel spiro compounds which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.

    摘要翻译： 通式VI-1的化合物及其制备方法：其中t，u，v和w各自独立地表示氮原子或次甲基，其可以具有选自卤素，低级烷基，低级烷氧基 和任选保护的羟基; 并且其中至少两个表示次甲基。 这些化合物用作新的螺旋化合物的中间体，其表现出神经肽Y受体（NPY）拮抗活性，并且可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，中枢神经系统疾病，代谢疾病等 。

    Spiro compounds
    9.
    发明授权
    Spiro compounds 有权
    螺环化合物

    公开(公告)号：US06335345B1

    公开(公告)日：2002-01-01

    申请号：US09928431

    申请日：2001-08-14

    申请人： Takehiro Fukami ,  Akio Kanatani ,  Akane Ishihara ,  Yasuyuki Ishii ,  Toshiyuki Takahashi ,  Yuji Haga ,  Toshihiro Sakamoto ,  Takahiro Itoh

    发明人： Takehiro Fukami ,  Akio Kanatani ,  Akane Ishihara ,  Yasuyuki Ishii ,  Toshiyuki Takahashi ,  Yuji Haga ,  Toshihiro Sakamoto ,  Takahiro Itoh

    IPC分类号： A61K31506

    CPC分类号： C07D405/12 ,  C07D213/61 ,  C07D307/94 ,  C07D471/10 ,  C07D491/10

    摘要： Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents methine; Y represents an optionally substituted imino or oxygen atom. These novel spiro compounds exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.

    摘要翻译： 通式（I）的螺环化合物：其中Ar1表示任选取代的芳基或杂芳基; n表示0或1; T，U，V和W各自表示氮原子或任选取代的次甲基，其中至少两个 其表示次甲基; X表示次甲基; Y表示任选取代的亚氨基或氧原子。这些新型螺环化合物表现出神经肽Y受体（NPY）拮抗活性，可用作治疗与NPY有关的各种疾病的药剂，例如 心血管疾病，中枢神经系统疾病，全身性疾病等。