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13 条记录 (耗时 0.036 秒)

    Quinoline derivatives(2)
    3.
    发明授权
    Quinoline derivatives(2) 失效

    公开(公告)号：US06608083B1

    公开(公告)日：2003-08-19

    申请号：US08450437

    申请日：1995-05-25

    申请人： Carlo Farina ,  Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Luca Francesco Raveglia

    发明人： Carlo Farina ,  Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Luca Francesco Raveglia

    IPC分类号： C07D21500

    CPC分类号： C04B35/632 ,  A61K31/00 ,  A61K31/4709 ,  C07D215/52 ,  C07D221/18 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04

    摘要： NK3 receptor antagonists of formula (I): in which: Ar is an optionally substituted phenyl group, or a naphthyl or C5-7 cycloalkdienyl group, or an optionally substituted single or fused ring heterocyclic group, having aromatic character, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from S, O, N; R is linear or branched C1-8 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, an optionally substituted phenyl group or a phenyl C1-6 alkyl group, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxyxcarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or is a group —(CH2)p— when cyclized onto Ar, where p is 2 or 3; R1 and R2, which may be the same or different, are independently hydrogen or C1-6 linear or branched alkyl, or together form a —(CH2)n— group in which n represents 3, 4, or 5; or R1 together with R forms a group —(CH2)q—, in which q is 2, 3, 4 or 5; R3 and R4, which may be the same or different are independently hydrogen, C1-6 linear or branched alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino, mono- and di-C1-6 alkylamino, —O(CH2)r—NT2, in which r is 2, 3, or 4 and T is hydrogen or C1-6 alkyl or it forms with the adjacent nitrogen a group  in which V and V1 are independently hydrogen or oxygen and u is 0,1 or 2; —O(CH2)s—OW2 in which s is 2, 3, or 4 and W is hydrogen or C1-6 alkyl; hydroxyalkyl, aminoalkyl, mono-or di-alkylaminoalkyl, acylamino, alkylsulphonylamino, aminoacylamino, mono- or di-alkylaminoacylamino; with up to four R3 substituents being present in the quinoline nucleus; or R4 is a group —(CH2)t— when cyclized onto R5 as aryl, in which t is 1, 2, or 3; R5 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, wherein an optional substituent is hydroxy, halogen, C1-6 alkoxy or C1-6 alkyl, or an optionally substituted single or fused ring heterocyclic group, having aromatic character, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from S, O, N; in which inter alia, Ar is phenyl, optionally substituted by C1-6 alkyl or halogen; thienyl or a C5-7 cycloalkdienyl group; R is C1-6 alkyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl or hydroxy C1-6 alkyl; R1 and R2 are each hydrogen or C1-6 alkyl; R3 is hydrogen, hydroxy, halogen, C1-6 alkoxy or C1-6 alkyl; R4 is hydrogen, C1-6 alkyl, C1-6 alkoxy, hydroxy, anino, halogen, aminoalkoxy, mono- or di-alkylaminoalkoxy, mono- or di-alkylaminoalkyl, phthaloylalkoxy, mono- or di-alkylaminoacylarnino or acylamino; R5 is phenyl, thienyl, furyl, pyrryl or thiazolyl, and X is oxygen. X is O, S, or N—C≡N.

    Quinoline derivatives
    4.
    发明授权
    Quinoline derivatives 失效
    喹啉衍生物

    公开(公告)号：US06277862B1

    公开(公告)日：2001-08-21

    申请号：US09077151

    申请日：1998-05-22

    申请人： Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Luca Francesco Raveglia ,  Carlo Farina

    发明人： Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Luca Francesco Raveglia ,  Carlo Farina

    IPC分类号： A61K3147

    CPC分类号： C07D215/52

    摘要： A compound, or a solvate or a salt thereof, of formula (I), wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or an optionally substituted single or fused ring aromatic heterocyclic group; R, R1, R2 and R3 are as defined in the description; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound or composition in medicine.

    摘要翻译： 式（I）的化合物或其溶剂合物或其盐，其中Ar为任选取代的芳基或C 5-7环二烯基，或任选取代的单环或稠环芳族杂环基; R，R1，R2和R3如说明书中所定义; 制备这种化合物的方法，在药物中含有这种化合物或组合物的药物组合物。

    Quinoline derivatives as NK-2 and NK-3 receptor ligands
    8.
    发明授权
    Quinoline derivatives as NK-2 and NK-3 receptor ligands 失效
    喹啉衍生物作为NK-2和NK-3受体配体

    公开(公告)号：US06613770B1

    公开(公告)日：2003-09-02

    申请号：US09856385

    申请日：2001-09-28

    申请人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Guy Marguerite Marie Gerard Nadler ,  Luca Francesco Raveglia

    发明人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Guy Marguerite Marie Gerard Nadler ,  Luca Francesco Raveglia

    IPC分类号： A61K314725

    CPC分类号： C07D401/06 ,  C07D215/52 ,  C07D401/14

    摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein R is linear or branched alkyl; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety —(CH2)n—NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or alkyl or R4 and R together with the carbon atom to which they are attached form an optionally substituted C3-12 cycloalkyl group; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

    摘要翻译： 式（I）的化合物或其溶剂化物或其盐：其中R是直链或支链烷基; R1代表氢或最多四个选自下列的任选取代基：C 1-6烷基，C 1-6烯基 芳基，C 1-6烷氧基，羟基，卤素，硝基，氰基，羧基，甲酰胺基，磺酰氨基，C 1-6烷氧基羰基，三氟甲基，酰氧基，苯二甲酰亚氨基，氨基或单-C2和二-C6烷基氨基; R2代表 - （CH2）n-NY1Y2其中n是1至9的整数，Y1和Y2独立地选自氢; C 1-6 - 烷基; 被羟基，C 1-6烷基氨基或双（C 1-6烷基）氨基取代的C 1-6烷基; C 1-6 - 烯基; 芳基或芳基-C 1-6 - 烷基或Y1和Y2与它们所连接的氮原子一起表示任选取代的N-连接的单或稠环杂环基; R 3是支链或直链C 1-6烷基，C 3-7 环烷基，C 4-7环烷基烷基，任选取代的芳基或任选取代的单环或稠环芳族杂环基; R 4表示氢或烷基或R 4，R与它们所连接的碳原子一起形成任选取代的C 3-12环烷基; 制备这种化合物的方法，包含这些化合物的药物组合物以及这些化合物和组合物在医药中的用途。

    Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists
    9.
    发明授权
    Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists 失效
    喹啉-4-甲酰胺衍生物作为NK-3和NK-2受体拮抗剂

    公开(公告)号：US06780875B2

    公开(公告)日：2004-08-24

    申请号：US10358938

    申请日：2003-02-05

    申请人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Marcel Morvan ,  Guy Marguerite Marie Gérard Nadler ,  Luca Francesco Raveglia

    发明人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Marcel Morvan ,  Guy Marguerite Marie Gérard Nadler ,  Luca Francesco Raveglia

    IPC分类号： A61K314709

    CPC分类号： C07D401/06 ,  C07D215/52 ,  C07D401/12 ,  C07D401/14 ,  C07D413/10 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/10

    摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or an optionally substituted C5-7 cycloalkyl group, or an optionally substituted single or fused ring aromatic heterocyclic group; R is hydrogen, linear or branched C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl; R1 represents hydrogen or up to three optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- and di-C1-6 alkylamino, R2 represents a moiety —(CH2)n—NYY2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from C1-6-alkyl; C1-6 alkyl substituted with hydroxy, alkoxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C3-6 cycloalkyl; C4-6 azacycloalkyl; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl, R5 represents hydrogen or halogen; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

    摘要翻译： 式（I）的化合物或其溶剂化物或其盐：其中，Ar为任选取代的芳基或C 5-7环二烯基，或任选取代的C 5-7环烷​​基，或任选取代的单或稠合 环芳族杂环基团; R是氢，直链或支链C 1-6烷基，C 3-7环烷基，C 3-7环烷基烷基; R 1代表氢或最多三个选自下列的任选取代基：C 1-6烷基， 6-烯基，芳基，C 1-6烷氧基，羟基，卤素，硝基，氰基，羧基，甲酰氨基，磺酰氨基，C 1-6烷氧基羰基，三氟甲基，酰氧基，氨基或单-C 1-6烷基氨基， （CH 2）n -NYY 2，其中n是1至9的整数，Y 1和Y 2独立地选自C 1-6 - 烷基; 被羟基，烷氧基，C 1-6烷基氨基或双（C 1-6烷基）氨基取代的C 1-6烷基; C3-6环烷基; C4-6氮杂环烷基; C 1-6 - 烯基; 芳基或芳基-C 1-6 - 烷基或Y1和Y2与它们所连接的氮原子一起表示任选取代的N-连接的单或稠环杂环基; R 3是支链或直链C 1-6烷基，C 3-7 环烷基，C 4-7环烷基烷基，任选取代的芳基或任选取代的单环或稠环芳族杂环基; R 4表示氢或C 1-6烷基，R 5表示氢或卤素; 制备这种化合物的方法，包含这些化合物的药物组合物以及这些化合物和组合物在医药中的用途。