摘要:
Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.
摘要翻译:式的新型化合物或其药学上可接受的盐或溶剂合物,其中:虚线表示任选的双键; X 1为任选取代的烷基,环烷基,芳基,杂芳基或杂环烷基; X 2为-CHO, - CN,任选取代的氨基,烷基或芳基;或X 1是任选取代的苯并稠合的杂环基,X 2是氢;或X 1和X 2一起形成任选的苯并稠合的螺杂环基R 1, R 2,R 3和R 4独立地为H和烷基,或(R 1和R 4)或(R 2和R 3)或(R 1) >和R 3)或(R 2和R 4)可以一起形成1至3个碳原子的亚烷基桥; Z 1是任选取代的烷基,芳基,杂芳基,环烷基或杂环烷基,或 -CO 2(烷基或取代的氨基)或CN; Z 2是H或Z 1; Z 3是H或烷基; 或Z 1,Z 2和Z 3与它们所连接的碳一起形成双环饱和或不饱和环; 因此,公开了用于治疗疼痛,焦虑,咳嗽,哮喘,抑郁和酒精滥用的所述化合物作为伤害感受肽受体抑制剂的用途。
摘要:
The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activity. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.
摘要:
Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.
摘要翻译:新型式的化合物或其药学上可接受的盐或溶剂合物,其中:虚线表示任选的双键; X 1是任选取代的烷基,环烷基,芳基,杂芳基或杂环烷基; X 2是-CHO,-CN,任选取代的氨基,烷基或芳基; 或X 1是任选取代的苯并稠合的杂环基,X 2是氢; 或X 1和X 2一起形成任选的苯并稠合的螺杂环基R 1,R 2,R 2, 或者R 4和R 4独立地是H和烷基,或者(R 1和R 4)和(R 0) 或者R 2和R 3)或(R 1和R 3)或(R 2) 和R 4)可以形成1至3个碳原子的亚烷基桥; Z 1是任选取代的烷基,芳基,杂芳基,环烷基或杂环烷基或-CO 2(烷基或取代的氨基)或CN; Z 2是H或Z 1; Z 3是H或烷基; 或Z 1,Z 2和Z 3与它们所连接的碳一起形成双环饱和或不饱和环; 因此,公开了用于治疗疼痛,焦虑,咳嗽,哮喘,抑郁和酒精滥用的所述化合物作为伤害感受肽受体抑制剂的用途。
摘要:
Relief from the symptoms of rhinitis is obtained by treatment with: (a) an antihistaminic effective amount of a histamine H.sub.1 receptor antagonist; together with (b) a sufficient amount of a histamine H.sub.3 receptor antagonist to provide a nasal decongestant effect. The components may be administered together in a single dosage form, or separately in the same or different dosage forms to maintain therapeutic systemic levels of both components.
摘要:
This invention relates to a method of treating cognition deficit disorders comprising administering to a mammal in need of such treatment an effective amount of a dual histamine H3 receptor antagonist/m2 muscarinic antagonist, or a combination of a histamine H3 receptor antagonist and a m2 muscarinic antagonist.
摘要翻译:本发明涉及一种治疗认知缺陷障碍的方法,包括对需要这种治疗的哺乳动物施用有效量的双重组胺H 3受体拮抗剂/ m 2毒蕈碱 拮抗剂,或组胺H 3受体拮抗剂和am2S毒蕈碱拮抗剂的组合。
摘要:
The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
摘要:
The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
摘要:
Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.
摘要翻译:式的新型化合物或其药学上可接受的盐或溶剂化物,其中:虚线表示任选的双键; X 1为任选取代的烷基,环烷基,芳基,杂芳基或杂环烷基; X 2为-CHO,-CN,任选取代的氨基, 烷基或芳基;或X 1是任选取代的苯并稠合的杂环基,并且X 2是氢;或者X 1和X 2一起形成任选的苯并稠合的螺杂环基R1,R2,R3和R4独立地是H和烷基,或(R1和R4)或 和(R 3和R 3)或(R 1和R 3)或(R 2和R 4)在一起可以形成1至3个碳原子的亚烷基桥; Z 1是任选取代的烷基,芳基,杂芳基,环烷基或杂环烷基,或-CO 2(烷基或取代的氨基 )或CN; Z2是H或Z1; Z 3是H或烷基; 或Z 1,Z 2和Z 3与它们所连接的碳一起形成双环饱和或不饱和环;因此,药物组合物以及所述化合物用作疼痛,焦虑,咳嗽,哮喘的伤害感受肽受体抑制剂的用途 ,公开抑郁症和酗酒。
摘要:
Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused Spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.
摘要翻译:式的新型化合物或其药学上可接受的盐或溶剂化物,其中:虚线表示任选的双键; X 1为任选取代的烷基,环烷基,芳基,杂芳基或杂环烷基; X 2为-CHO,-CN,任选取代的氨基, 烷基或芳基;或X 1为任选取代的苯并稠合的杂环基,且X 2为氢;或X 1和X 2一起形成任选的苯并稠合的螺杂环基R1,R2,R3和R4独立地为H和烷基,或(R1和R4)或 和(R 3和R 3)或(R 1和R 3)或(R 2和R 4)在一起可以形成1至3个碳原子的亚烷基桥; Z 1是任选取代的烷基,芳基,杂芳基,环烷基或杂环烷基,或-CO 2(烷基或取代的氨基 )或CN; Z2是H或Z1; Z 3是H或烷基; 或Z 1,Z 2和Z 3与它们所连接的碳一起形成双环饱和或不饱和环; 因此,公开了用于治疗疼痛,焦虑,咳嗽,哮喘,抑郁和酒精滥用的所述化合物作为伤害感受肽受体抑制剂的用途。