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    N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands
    1.
    发明申请
    N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands 审中-公开
    N-苯基吡咯胍衍生物作为黑皮质素受体配体

    公开(公告)号：US20090018183A1

    公开(公告)日：2009-01-15

    申请号：US12232399

    申请日：2008-09-17

    申请人： Torbjorn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

    发明人： Torbjorn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

    IPC分类号： A61K31/40 ,  A61P3/00 ,  A61P25/00

    CPC分类号： C07D207/335 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D207/42

    摘要： The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

    摘要翻译： 本发明提供了作为黑皮质素受体配体和/或用于治疗黑皮质素系统中的病症的通式（I）的新化合物：其中X是（CH 2）n，其中n是0,1或2; R 1，R 2，R 3，R 4和R 5可以相同或不同，并且选自氢，卤素，具有1-5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，烷基磺酰氧基，氰基，硝基，三卤代烷基，磺基 或方案1中给出的结构之一; 或者R 1，R 2，R 3，R 4和R 5中的两个可以一起形成亚甲二氧基或亚乙二氧基部分; R 6，R 7，R 8和R 9相同或不同，并且选自氢，卤素，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，具有0,1 或2个碳原子，氰基，硝基，三卤代烷基，酰胺或磺基，z表示残基与苯基或吡咯环的连接点; 及其药理学活性盐。

    N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands
    2.
    发明申请
    N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands 失效
    N-苯基吡咯胍衍生物作为黑皮质素受体配体

    公开(公告)号：US20060148798A1

    公开(公告)日：2006-07-06

    申请号：US11374956

    申请日：2006-03-15

    申请人： Torbjorn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

    发明人： Torbjorn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

    IPC分类号： A61K31/5377 ,  A61K31/4025 ,  C07D413/02 ,  C07D403/02 ,  C07D207/30

    CPC分类号： C07D207/335 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D207/42

    摘要： The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

    摘要翻译： 本发明提供了作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的通式（I）的新化合物：其中X是（CH 2） / SUB>其中n为0,1或2; R 1，R 2，R 3，R 4和R 5可以是 羟基，烷基磺酰氧基，氰基，硝基，三卤代烷基，磺基或方案1中给出的结构之一;其中R 1，R 2， 或R 1，R 2，R 3，R 4和R 5中的两个， 可以一起形成亚甲二氧基或亚乙二氧基部分; R 6，R 7，R 8和R 9相同或不同，并且选自氢， 卤素，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，具有0,1或2个碳原子的胺（伯，仲或叔），氰基，硝基，三卤代烷基，酰胺或磺基，和z 显示残基与苯基或吡咯环的连接点; 及其药理学活性盐。

    N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands
    3.
    发明授权
    N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands 失效
    N-苯基吡咯胍衍生物作为黑皮质素受体配体

    公开(公告)号：US07186748B2

    公开(公告)日：2007-03-06

    申请号：US10484444

    申请日：2002-08-06

    申请人： Torbjörn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

    发明人： Torbjörn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

    IPC分类号： A61K31/402 ,  C07D207/335

    CPC分类号： C07D207/335 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D207/42

    摘要： The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

    摘要翻译： 本发明提供了作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的通式（I）的新化合物：其中X是（CH 2） / SUB>其中n为0,1或2; R 1，R 2，R 3，R 4和R 5可以是 羟基，烷基磺酰氧基，氰基，硝基，三卤代烷基，磺基或方案1中给出的结构之一;其中R 1，R 2， 或R 1，R 2，R 3，R 4和R 5中的两个， 可以一起形成亚甲二氧基或亚乙二氧基部分; R 6，R 7，R 8和R 9相同或不同，并且选自氢， 卤素，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，具有0,1或2个碳原子的胺（伯，仲或叔），氰基，硝基，三卤代烷基，酰胺或磺基，和z 显示残基与苯基或吡咯环的连接点; 及其药理学活性盐。

    N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands
    4.
    发明授权
    N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands 失效
    N-苯基吡咯胍衍生物作为黑皮质素受体配体

    公开(公告)号：US07442807B2

    公开(公告)日：2008-10-28

    申请号：US11374956

    申请日：2006-03-15

    申请人： Torbjörn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

    发明人： Torbjörn Lundstedt ,  Anna Skottner ,  Arne Boman ,  Per Andersson ,  Elisabeth Seifert ,  Victor Andrianov

    IPC分类号： C07D207/325 ,  C07D207/335 ,  C07D413/10

    CPC分类号： C07D207/335 ,  C07D207/34 ,  C07D207/36 ,  C07D207/38 ,  C07D207/42

    摘要： The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

    摘要翻译： 本发明提供了作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的通式（I）的新化合物：其中X是（CH 2） / SUB>其中n为0,1或2; R 1，R 2，R 3，R 4和R 5可以是 羟基，烷基磺酰氧基，氰基，硝基，三卤代烷基，磺基或方案1中给出的结构之一;其中R 1，R 2， 或R 1，R 2，R 3，R 4和R 5中的两个， 可以一起形成亚甲二氧基或亚乙二氧基部分; R 6，R 7，R 8和R 9相同或不同，并且选自氢， 卤素，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基，羟基，具有0,1或2个碳原子的胺（伯，仲或叔），氰基，硝基，三卤代烷基，酰胺或磺基，和z 显示残基与苯基或吡咯环的连接点; 及其药理学活性盐。

    Carbamic acid compounds comprising a bicyclic heteroaryl group as HDAC inhibitors
    8.
    发明授权
    Carbamic acid compounds comprising a bicyclic heteroaryl group as HDAC inhibitors 失效
    包含双环杂芳基作为HDAC抑制剂的氨基甲酸化合物

    公开(公告)号：US08071620B2

    公开(公告)日：2011-12-06

    申请号：US12636949

    申请日：2009-12-14

    申请人： Paul W. Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Victor Andrianov ,  Olga Habarova ,  Daina Lolya ,  Irina Piskunova

    发明人： Paul W. Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Victor Andrianov ,  Olga Habarova ,  Daina Lolya ,  Irina Piskunova

    IPC分类号： C07D215/38 ,  A61K31/04

    CPC分类号： C07D263/56 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D241/42 ,  C07D241/44 ,  C07D277/64

    摘要： This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated C1-7alkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the α-position; and with the proviso that A is not benzimidazol-2-yl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

    摘要翻译： 本发明涉及抑制HDAC（组蛋白脱乙酰酶）活性的某些下式的氨基甲酸化合物，其中：A独立地是未取代或取代的双环C 9-10杂芳基（例如喹啉基;喹喔啉基;苯并恶唑基;苯并噻唑基）; Q为酸性引导基团，独立地为骨架长度为4以下的未取代或取代的饱和或不饱和C 1-7亚烷基; 条件是如果A是未取代的苯并噻唑-2-基，则Q是不饱和基团; 并且条件是如果A是未取代的喹啉-6-基，那么Q在α-位是未取代的; 并且条件是A不是苯并咪唑-2-基; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。 本发明还涉及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体外和体内的用途，以抑制HDAC，以及治疗由HDAC，癌症，增殖性病症，牛皮癣等介导的病症 。

    CARBAMIC ACID COMPOUNDS COMPRISING A BICYCLIC HETEROARYL GROUP AS HDAC INHIBITORS
    10.
    发明申请
    CARBAMIC ACID COMPOUNDS COMPRISING A BICYCLIC HETEROARYL GROUP AS HDAC INHIBITORS 失效
    作为HDAC抑制剂包含双相异构体组的碳酸化合物

    公开(公告)号：US20100093743A1

    公开(公告)日：2010-04-15

    申请号：US12636949

    申请日：2009-12-14

    申请人： Paul W. FINN ,  Ivars Kalvinsh ,  Einars Loza ,  Victor Andrianov ,  Olga Habarova ,  Daina Lolya ,  Irina Piskunova

    发明人： Paul W. FINN ,  Ivars Kalvinsh ,  Einars Loza ,  Victor Andrianov ,  Olga Habarova ,  Daina Lolya ,  Irina Piskunova

    IPC分类号： A61K31/498 ,  C07D215/12 ,  C07D263/56 ,  C07D241/36 ,  A61K31/47 ,  A61K31/423 ,  A61P35/00

    CPC分类号： C07D263/56 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D241/42 ,  C07D241/44 ,  C07D277/64

    摘要： This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated C1 7alkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the α-position; and with the proviso that A is not benzimidazol-2-yl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

    摘要翻译： 本发明涉及抑制HDAC（组蛋白脱乙酰酶）活性的某些下式的氨基甲酸化合物，其中：A独立地是未取代或取代的双环C 9-10杂芳基（例如喹啉基;喹喔啉基;苯并恶唑基;苯并噻唑基）; Q是酸性引导基团，独立地是主链长度为4以下的未取代或取代的饱和或不饱和的C 1-7亚烷基; 条件是如果A是未取代的苯并噻唑-2-基，则Q是不饱和基团; 并且条件是如果A是未取代的喹啉-6-基，那么Q在α-位是未取代的; 并且条件是A不是苯并咪唑-2-基; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。 本发明还涉及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体外和体内的用途，以抑制HDAC，以及治疗由HDAC，癌症，增殖性病症，牛皮癣等介导的病症 。