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    Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process
    6.
    发明授权
    Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process 失效

    公开(公告)号：US07381822B2

    公开(公告)日：2008-06-03

    申请号：US10814118

    申请日：2004-03-31

    Applicant: David R. Elmaleh ,  Choi Songwoon ,  Alan J. Fischman

    Inventor： David R. Elmaleh ,  Choi Songwoon ,  Alan J. Fischman

    IPC: C07D401/12 ,  C07D241/10

    CPC classification number: C07D295/205 ,  C07D211/26 ,  C07D211/58 ,  C07D213/74 ,  C07D241/06 ,  C07D241/08 ,  C07D295/088 ,  C07D295/096 ,  C07D295/135 ,  C07D295/192 ,  C07D295/21 ,  C07D295/26

    Abstract: Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The compounds are characterized by the formulae: wherein: n is an integer of 1 to 6; X, Y, Z1 and Z2 can be the same or different and are hydrogen, halo, haloalkyl, alkyl, aryl, (C1-C6) alkoxy, N-alkyl,(C2-C6) acyloxy, N-alkylene, —SH, —SR, wherein R is from the same group as R1 and R2 and can be the same or different than R1 and R2, amino, nitro, cyano, hydroxy, C(═O) OR6, —C(═O) NR5R4, NR3R2, or S(αO)k R1 wherein k is 1 or 2, and R1 to R6 are independently hydrogen or (C1-C6) alkyl; R1, and R2 can be the same or different and are hydrogen, (C1-C6) alkyl, hydroxyalkyl or mercaptoalkyl, —C(═O) OR1, cyano, (C1-C6) alkenyl, (C2-C6) alkynyl, or 1,2,4-oxadiazol-5-yl optionally substituted at the 3-position by Z4 wherein any (C1-C6) alky, (C1-C6) alkanoyl, (C2-C6) alkenyl or (C2-C6) alkynyl can optionally be substituted by 1, 2 or 3 Z; R7 can be hydrogen, O or phenyl R8 can be hydrogen, phenyl, halophenyl, nitrophenyl, pyridyl, piperonyl or sulfoxonitrophenyl Z4 is (C1-C6) alkyl or phenyl, optionally substituted by 1, 2 or 3 Z1 W is O or S T is amino or C1-C6 aminoalkyl A is N or C T is C1-C6 alklyl or sulfonyl and V is alkyl (C0-C6), alkenyl, alkynyl, haloaryl, alkyl phenol, alkyl halophenyl, and R1 or R2 as indicated above and φ is phenyl, naphthyl, thienyl or pyridinyl.

    Piperazinone derivatives
    8.
    发明授权
    Piperazinone derivatives 失效
    哌嗪酮衍生物

    公开(公告)号：US07109259B2

    公开(公告)日：2006-09-19

    申请号：US10138986

    申请日：2002-05-03

    Applicant: Dario Lazzari ,  Mirko Rossi ,  Graziano Zagnoni ,  Alessandro Zedda ,  Stephen Mark Andrews

    Inventor： Dario Lazzari ,  Mirko Rossi ,  Graziano Zagnoni ,  Alessandro Zedda ,  Stephen Mark Andrews

    IPC: C08K5/3452 ,  C08K5/3492 ,  C07D403/14

    CPC classification number: C07D241/06 ,  C07D403/12 ,  C07D403/14 ,  C08K5/34926 ,  G03C1/815 ,  G03C1/8155 ,  G03C7/39244 ,  C08L59/00

    Abstract: A compound of the formula (I) wherein n is preferably 3; G1, G2, G3 and G4 are independently of one another e.g. C1–C4alkyl; A1 is e.g. hydrogen or methyl; A2 is e.g. methylene; A3′ and A3″ are e.g. C1–C4alkyl; A4 is e.g. C1–C8alkyl; Y is e.g. a group of the formula (IV)  wherein R1 is e.g. hydrogen or methyl, R2 is e.g. methylene, R3′ and R3″ are e.g. C1–C4alkyl and R4 is e.g. hydrogen or C1–C8alkyl; and Z is e.g. a group of the formula (VI)  with A10′ and A10″ being independently of one another e.g. hydrogen or C1–C4alkyl and A11′ and A11″ being independently of one another e.g. C2–C6alkylene, is useful for stabilizing an organic material against degradation induced by light, heat or oxidation.

    Abstract translation: 式（I）的化合物，其中n优选为3; G 1，G 2，G 3和G 4各自彼此独立地是例如不同的。 C 1 -C 4烷基; 例如，A 1＆lt; 1＆gt; 氢或甲基; A 是例如。 亚甲基 A 3＆lt; 3＆gt;和＆lt; 3＆gt; C 1 -C 4烷基; A 4是例如。 C 1 -C 8烷基; Y是例如 其中R 1为例如式（Ⅳ）的基团。 氢或甲基，R 2是例如。 亚甲基，R 3'和R 3“是例如。 C 1 -C 4烷基和R 4是例如C 1 -C 4烷基。 氢或C 1 -C 8烷基; Z是例如 具有A 10'和A 10“的式（VI）的基团彼此独立地是例如。 氢或C 1 -C 4烷基，A 11和A 11'彼此独立地为氢或C 1 -C 4烷基。 例如 C 2 -C 6亚烷基可用于稳定有机材料以防止由光，热或氧化引起的降解。

    Melanocortin receptor ligands
    10.
    发明申请
    Melanocortin receptor ligands 失效
    黑皮质素受体配体

    公开(公告)号：US20040224985A1

    公开(公告)日：2004-11-11

    申请号：US10856983

    申请日：2004-05-28

    Applicant: The Procter & Gamble Company

    Inventor： Wieslaw Adam Mazur ,  Xinrong Tian ,  Xiufeng Eric Hu ,  Frank Hallock Ebetino

    IPC: C07D211/54 ,  A61K031/445 ,  A61K031/4015

    CPC classification number: C07D241/08 ,  C07D207/12 ,  C07D211/46 ,  C07D241/06 ,  C07D401/12 ,  C07D403/06 ,  C07K5/06078 ,  C07K5/06191 ,  C07K5/0812 ,  C07K5/0821 ,  C07K5/0827

    Abstract: Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula: 1 wherein A is a conformationally restricted ring system selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprises from 5 to 8 atoms; and W is a unit which preferable comprises D-1-fluorophenyalanine, Y comprises a heteroatom, and Z comprises an aromatic carbocyclic ring. Also disclosed are pharmaceutical compositions comprising the ligands of the invention as well as methods of treating diseases mediated through MC-3/MC-4 receptors.

    Abstract translation: 公开了MC-3 / MC-4受体配体，所述配体具有下式：其中A是选自以下的构象限制性环系：a）非芳族碳环; b）芳族碳环; c）非芳族杂环; d）芳族杂环; 其中所述环包含5至8个原子; W是优选包含D-1-氟苯丙氨酸的单元，Y包含杂原子，Z包括芳族碳环。 还公开了包含本发明配体的药物组合物以及治疗通过MC-3 / MC-4受体介导的疾病的方法。

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