摘要:
The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I), wherein R1-R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
摘要:
Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
摘要:
The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C(=O)-; -C(=O)-C(=O)-; -NRX-C(=O)-; -Z-C(=O)-; -Z-NRX-C(=O)-; -C(=O)-Z-; -NRX-C(=O)-Z-; -C(=S)-; -NRX-C(=S)-; -Z-C(=S)-; -Z-NRX-C(=S)-; - C(=S)-Z-; -NRX-C(=S)-Z-; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C(=O)-NRX- or -NRX-C(=O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3- dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.
摘要:
The present invention relates to new sulfonamide derivatives of formula (I), wherein R 1 -R 5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
摘要:
Compounds of the formula (I); wherein R 1 is a member selected from the group consisting of C 1 -C 8 alkyl, arylC 0 -C 8 alkyl, C 3 -C 12 cycloalkyl and heterocyclyl, Y 1 is selected from the group consisting of a bond, C(R 5 ) 2 , NR 5 and O; Y 2 is selected from the group consisting of a bond, NR 5 and O; each R 2 , R 3 and R 5 is independently selected from the group consisting of H, alkyl and COR 6 ; A is heterocyclyl, optionally substituted with from 1 to 2 R 7 substituents; L is selected from the group consisting of a direct bond, C 1 -C 12 alkylene, C 1- C 12 heteroalkylene, C 3 -C 6 cycloalkylene, arylene, heteroarylene, -CO-, -SO in - and -Se-; R 4 is selected from the group consisting of H, C 1 C 8 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 ,-C 8 heteroalkyl, arylC 0 -C 8 alkyl, C 3 C, 12 cycloalkyl and heterocyclyl, are claimed. The compounds are inhibitors of the soluble epoxide hydrolase (sEH) and useful for the treatment of hypertension, inflammation, adult respiratory distress syndrome; diabetic complications; end stage renal disease; Raynaud syndrome and arthritis.
摘要:
Compounds of formula (I) : wherein, Z is -N-or>CH; R 1 is -H or -C 1-4 alkyl; Ar 1 is 2-thiazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidinyl, 4-primidinyl, 5-pyrimidinyl, or phenyl, each unsubstituted or substituted at a carbon ring member with one or two R a moieties; Wher each R a moiety is independently selected from the group consisting of -C 1-4 alkyl, -C 2-4 alkenyl, -OH, -OC 1-4 alkyl, halo, -CF 3 , -OCF 3 , -SCF 3 , -SH, -S(O) 0-2 C 1-4 alkyl, -OSO 2 C 1-4 alkyl, -CO 2 C 1-4 alkyl, -CO 2 H, -COC 1-4 alkyl, -N(R b )R c , -SO 2 NR b R c , -NR b SO 2 R c , -C(=O)NR b R c , -NO 2 , and -CN, wherein R b and R c are each independently -H or -C 1-4 alkyl; and Ar 2 is defined in the claims are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
摘要翻译:式(I)化合物:其中Z是-N或> CH; R 1是-H或-C 1-4烷基; Ar 1是在碳环成员上未取代或取代的2-噻唑基,2-吡啶基,3-吡啶基,4-吡啶基,2-嘧啶基,4-环丙基,5-嘧啶基或苯基 具有一个或两个R a a部分; 每个R a a部分独立地选自-C 1-4 - 烷基,-C 2-4二烯基,-OH ,-OC 1-4烷基,卤素,-CF 3,-OCF 3,-SCF 3, -SH,-S(O)0-2个C 1-4烷基,-OSO 2 C 1-4烷基, 烷基,-CO 2 C 1-4烷基,-CO 2 H,-COC 1-4, 烷基,-N(R b)b C c,-SO 2 NR b,C c C(= O)NR B,C(= O)NR b R b, 其中R b和R c各自独立地是-H或者其中R b和R c各自独立地是-H或 -C 1-4 SUB>烷基; 在权利要求中定义的Ar 2用作FAAH抑制剂。 此类化合物可用于治疗由脂肪酰胺水解酶(FAAH)活性介导的疾病状态,病症和病症的药物组合物和方法。 因此,可以施用化合物以治疗例如焦虑,疼痛,炎症,睡眠障碍,进食障碍或运动障碍(例如多发性硬化症)。
摘要:
Compounds represented by general formula (1) or salts thereof and drugs containing the same as the active ingredient. In formula (1), X represents carboxy, etc.; Y represents a single bond, etc.; at least one of A , A and A represents a group represented by the following general formula (2):-R -a -R -a } (wherein R represents divalent C2-12 hydrocarbyl; R represents divalent C2-12 hydrocarbyl, etc.; and a and a represent each a single bond, -N(R )-, etc.); and at least one of Q , Q and Q represents cyclic hydrocarbyl or a heterocycle while the remaining one(s) represent hydrogen, optionally esterified carboxy, hydrocarbyl or a heterocycle. Because of having a potent inhibitory effect on squalene synthase, these compounds are useful as preventives and/or remedies for hypercholesterolemia, hyperlipemia and arteriosclerosis.
摘要翻译:由通式(1)表示的化合物或其盐和与活性成分相同的药物。 在式(1)中,X 1表示羧基等; Y 1表示单键等; A 1,A 2和A 3中的至少一个表示由以下通式(2)表示的基团:-R 2 -a 1 -R 3 -a 2 >其中R 2表示二价C 2- 12烃基; R 3表示二价C 2- 12烃基等;且a 1和a 2各自表示单键,-N(R' 4>) - 等); 并且Q 1,Q 2和Q 3中的至少一个表示环状烃基或杂环,而剩余的一个表示氢,任选酯化的羧基,烃基或杂环。 由于对角鲨烯合酶具有有效的抑制作用,这些化合物可用作高胆固醇血症,高脂血症和动脉硬化症的预防剂和/或治疗药物。