4-(Phenyl-(piperidin-4-yl)-amino)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders
    2.
    发明申请
    4-(Phenyl-(piperidin-4-yl)-amino)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders 失效
    4-(苯基 - (哌啶-4-基) - 氨基) - 苯甲酰胺衍生物及其用于治疗疼痛,焦虑或胃肠道疾病

    公开(公告)号:US20040235897A1

    公开(公告)日:2004-11-25

    申请号:US10477852

    申请日:2003-11-13

    Abstract: Compounds of general formula I 1 R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1,2 or 3 substituents selected from straight and branched C1-C6alkyl, NO2, CF3, C1-C6alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

    Abstract translation: 通式I R1的化合物选自苯基,吡啶基,吡咯基,噻吩基,呋喃基,咪唑基,三唑基和吡啶N-氧化物中的任一种; 其中每个R 1苯基环和R 1杂芳环可以任选和独立地被1,2或3个选自直链和支链C 1 -C 6烷基,NO 2,CF 3,C 1 -C 6烷氧基,氯,氟,溴和碘的取代基取代。 苯环上和杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护,以及它们的药学上可接受的盐和药物组合物,其包含新化合物及其在治疗中的用途,特别是在治疗疼痛,焦虑和功能性胃肠疾病中的用途。

    4-(phenyl-(piperidin-4yl)-amino)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders
    3.
    发明申请
    4-(phenyl-(piperidin-4yl)-amino)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders 失效
    4-(苯基 - (哌啶-4-基) - 氨基) - 苯甲酰胺衍生物及其用于治疗疼痛,焦虑或胃肠道疾病

    公开(公告)号:US20040142966A1

    公开(公告)日:2004-07-22

    申请号:US10477636

    申请日:2003-11-13

    Abstract: Compounds of general formula InullChemical formula should be inserted here. Please see paper copynull R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6alkyl, NO2, CF3, C1-C6alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

    Abstract translation: 通式Ⅰ化合物[化学式应在此插入。 请参见纸张复制] R1选自苯基,吡啶基,噻吩基,呋喃基,咪唑基,吡咯基,三唑基,噻唑基和吡啶N-氧化物中的任一种; 其中每个R 1苯基环和R 1杂芳环可以任选和独立地被1,2或3个选自直链和支链C 1 -C 6烷基,NO 2,CF 3,C 1 -C 6烷氧基,氯,氟,溴和碘的取代基取代。 苯环上和杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护,以及包含新化合物的盐和药物组合物及其在治疗中的用途,特别是在治疗疼痛,焦虑和功能性胃肠道疾病中的用途。

    4-(phenyl-(piperidin-4yl)-amino)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders
    4.
    发明申请
    4-(phenyl-(piperidin-4yl)-amino)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders 失效
    4-(苯基 - (哌啶-4-基) - 氨基) - 苯甲酰胺衍生物及其用于治疗疼痛,焦虑或胃肠道疾病

    公开(公告)号:US20040142965A1

    公开(公告)日:2004-07-22

    申请号:US10477633

    申请日:2003-11-13

    Abstract: Compounds of general formula I nullChemical formula should be inserted here. Please see paper copynull R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6alkyl, NO2, CF3, C1-C6alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety or functional gastrointestinal disorders.

    Abstract translation: 通式Ⅰ化合物[化学式应在此插入。 R 1选自苯基,吡啶基,噻吩基,呋喃基,咪唑基,吡咯基,三唑基,噻唑基和吡啶N-氧化物中的任一种。 其中每个R 1苯基环和R 1杂芳环可以任选和独立地被1,2或3个选自直链和支链C 1 -C 6烷基,NO 2,CF 3,C 1 -C 6烷氧基,氯,氟,溴和碘的取代基取代。 苯环上和杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护,以及包含新化合物的盐和药物组合物及其在治疗中的用途,特别是在治疗疼痛,焦虑或功能性胃肠道疾病中的用途。

    6-Phenylpyridyl-2-amine derivatives useful as NOS inhibitors
    5.
    发明申请
    6-Phenylpyridyl-2-amine derivatives useful as NOS inhibitors 审中-公开
    用作NOS抑制剂的6-苯基吡啶基-2-胺衍生物

    公开(公告)号:US20040142924A1

    公开(公告)日:2004-07-22

    申请号:US10678369

    申请日:2003-10-03

    Applicant: Pfizer Inc

    Inventor: Jon A. Low III

    Abstract: The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula 1 wherein G, R1 and R2 are defined as in the specification, that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them, and to their use in the treatment and prevention of central nervous system and other disorders.

    Abstract translation: 本发明涉及下式的6-苯基 - 吡啶-2-基胺衍生物,其中G,R 1和R 2如说明书中所定义,其表现出作为一氧化氮合酶(NOS)抑制剂的活性, 含有它们的药物组合物,以及它们在治疗和预防中枢神经系统和其它疾病中的用途。

    Piperidine derivatives useful as CCR5 antagonists

    公开(公告)号:US20040092551A1

    公开(公告)日:2004-05-13

    申请号:US10629466

    申请日:2003-07-29

    CPC classification number: C07D401/14

    Abstract: The present invention provides a compound of the formula 1 or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R9, R10, A and B are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.

    N-(4-aryloxypiperidin-1-ylalkyl) cinnamic amides as ccr33 receptor antagonists
    10.
    发明申请
    N-(4-aryloxypiperidin-1-ylalkyl) cinnamic amides as ccr33 receptor antagonists 失效
    N-(4-芳氧基哌啶-1-基烷基)肉桂酰胺,为ccr33受体拮抗剂

    公开(公告)号:US20040087621A1

    公开(公告)日:2004-05-06

    申请号:US10398533

    申请日:2003-04-08

    CPC classification number: C07D211/46

    Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C1-C8-alkyl optionally substituted by cyano or halogen, Ar2 is phenyl optionally which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is C1-C8-alkyl substituted by hydroxy, C1-C8-alkoxy, acyloxy, nullN(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, phenyl-C1-C8-alkoxycarbonyl, -CON(R4)R5 or by a monovalent cyclic organic group, R2 and Rnull3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen, C1-C8-alkyl optionally substituted by hydroxy or phenyl, or phenyl optionally substituted by C1-C8-alkyl, halogen, cyano or C1-C8-alkoxy, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, Rnull6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1, 2, 3 or 4. The compounds are useful as pharmaceuticals.

    Abstract translation: Ar 1是被一个或多个选自卤素,氰基,硝基和任选被氰基或卤素取代的C 1 -C 8烷基的取代基取代的苯基,Ar 2是游离或盐形式的式(I)化合物, 是任选未取代或被一个或多个选自卤素,氰基,羟基,硝基,C 1 -C 8 - 烷基,C 1 -C 8 - 卤代烷基,C 1 -C 8 - 烷氧基或C 1 -C 8 - 烷氧基羰基的取代基取代的苯基,R 1 是被羟基,C 1 -C 8 - 烷氧基,酰氧基,-N(R 2)R 3,卤素,羧基,C 1 -C 8 - 烷氧基羰基,苯基-C 1 -C 8 - 烷氧基羰基, -CON(R 4)R 5或单价环状有机基团R 2和R 3定义字符文件=“US20040087621A1-20040506-P00900.TIF”wi =“20”he = “20”id =“custom-character-00001”/>各自独立地为氢或C 1 -C 8 - 烷基,或R 2为氢,R 3为酰基或SO 2 R 6,或R 2为 和R 3与它们所连接的氮原子一起表示5-或6-元杂环基,R 4和R 5各自独立地为氢 任选被羟基或苯基取代的C 1 -C 8 - 烷基或任选被C 1 -C 8 - 烷基,卤素,氰基或C 1 -C 8 - 烷氧基取代的苯基,或R 4和R 5与氮原子一起 它们所连接的表示5-或6-元杂环基,R 6 是C 1 -C 8 - 烷基,C 1 -C 8 - 卤代烷基或任选被C 1 -C 8 - 烷基取代的苯基,n是1,2,3或4.这些化合物可用作药物。

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