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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：US06462053B1

    公开(公告)日：2002-10-08

    申请号：US10101221

    申请日：2002-03-20

    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： A61K34355

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

    摘要： A method for treating a cardiovascular 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： 一种治疗心血管疾病的方法，其涉及向需要的患者施用治疗有效量的式（I）化合物：其中Ar1表示可被取代的芳基或杂芳基，所述取代基选自 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，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， 任选被氧代取代的基团和由式-Q-Ar 2表示的基团; Ar 2表示可被取代的芳基或杂芳基，所述取代基选自卤素，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， W各自独立地表示硝基 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表示可以被取代的亚氨基 与低级烷基或氧; 或其盐或酯。

    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

    Spiro compounds
    5.
    发明授权
    Spiro compounds 有权
    螺环化合物

    公开(公告)号：US06803372B2

    公开(公告)日：2004-10-12

    申请号：US10092549

    申请日：2002-03-08

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

    摘要： Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.

    摘要翻译： 通式（I）的化合物：其中Ar 1表示任选取代的芳基或杂芳基; n表示0或1; T，U，V和W各自独立地表示氮原子或任选取代的次甲基，其中至少两个 代表所述次甲基; X表示次甲基或羟基取代的次甲基; Y表示任选取代的亚氨基或氧原子。 这些新颖的螺环化合物可用作神经肽Y受体拮抗剂和用作治疗各种心血管疾病，中枢神经系统疾病，代谢疾病等的药剂。

    Spiro compounds
    7.
    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
    8.
    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。

    Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient
    10.
    发明授权
    Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient 失效
    黑色素浓缩激素受体拮抗剂含有哌啶衍生物作为活性成分

    公开(公告)号：US07727998B2

    公开(公告)日：2010-06-01

    申请号：US10544261

    申请日：2004-02-09

    申请人： Minoru Moriya ,  Toshihiro Sakamoto ,  Makoto Ishikawa ,  Akio Kanatani ,  Takehiro Fukami

    发明人： Minoru Moriya ,  Toshihiro Sakamoto ,  Makoto Ishikawa ,  Akio Kanatani ,  Takehiro Fukami

    IPC分类号： A61K31/4545 ,  C07D491/10

    CPC分类号： C07D401/04 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/445 ,  C07D211/26 ,  C07D491/10

    摘要： The invention provides melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: [wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for —O—, —CH2—, or the like; Y1, Y2, Y3 and Y4 stand for —CH—, —CF—, —N—, or the like; Z stands for lower alkyl, an aliphatic heterocyclic group, or the like; Ar is a mono- or bi-cyclic aliphatic heterocycle or an aromatic heterocycle; and n is an integer of 1 to 8]. The compounds act as antagonist against melanin-concentrating hormone receptor and are useful as drugs for central diseases, circulatory diseases, or metabolic diseases.

    摘要翻译： 本发明提供了含有作为活性成分的通式[I]表示的哌啶衍生物的黑色素浓缩激素受体拮抗剂：其中R1是氢，羟基，低级烷基等; R2，R3a，R3b，R4a，R4b，R5a，R5b和R6各自代表氢，卤素等; W1和W2各自独立地代表-O-，-CH2-等; Y1，Y2，Y3和Y4代表-CH-，-CF-，-N-等; Z代表低级烷基，脂族杂环基等; Ar是单环或双环脂族杂环或芳族杂环; n为1〜8的整数]。 该化合物作为拮抗黑素浓缩激素受体的拮抗剂，可用作中枢疾病，循环系统疾病或代谢疾病的药物。