摘要:
Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
摘要:
This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility.
摘要:
Disclosed is a compound of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R is selected from the group consisting of: H, Cl, Br, F, and I; T represents C or N with the dotted line attached to T representing a double bond when T is C and being absent when T is N; and X represents O or S with the proviso that T is N when X is O.Also disclosed is a pharmaceutical composition comprising a compound of Formula I and a pharmaceutically acceptable carrier.Further disclosed is a method of treating asthma, allergy and/or inflammation comprising administering to a mammal in need of such treatment an anti-asthmatic, anti-allergic and/or an anti-inflammatory, respectively, effective amount of a compound of Formula I.
摘要:
Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
摘要:
Disclosed is a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: AR.sup.1 represents ##STR2## AR.sup.2 represents ##STR3## or a five-membered heterocyclic aromatic group selected from the group consisting of Formulas I to XII, wherein the substitutable carbon atoms of the five-membered heterocyclic group can optionally be substituted with a group R.sup.1. Also disclosed are pharmaceutical compositions containing compounds of Formula 1.0. Further disclosed is a method for treating asthma, allergy and inflammation by administering an anti-asthmatic, anti-allergic or anti-inflammatory, respectively, effective amount of a compound of Formula 1.0.
摘要:
Novel compounds and compositions which inhibit SRS--A in mammals are disclosed. Methods for preparing said compounds and compositions and methods for their use for treating allergic reactions, inflammation and for reducing the severity of myocardial infarction resulting from heart attack are disclosed.Useful intermediates for preparing said compounds are also disclosed.
摘要:
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要:
Disclosed is a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: AR.sup.1 represents ##STR2## AR.sup.2 represents ##STR3## or a five-membered heterocyclic aromatic group selected from the group consisting of Formulas I to XII, wherein the substitutable carbon atoms of the five-membered heterocyclic group can optionally be substituted with a group R.sup.1.Also disclosed are pharmaceutical compositions containing compounds of Formula 1.0.Further disclosed is a method for treating asthma, allergy and inflammation by administering an anti-asthmatic, anti-allergic or anti-inflammatory, respectively, effective amount of a compound of Formula 1.0.
摘要翻译:公开了式1.0的化合物:其中:AR1表示SEQ ID NO:表示选自下式的五元杂环芳族基团:式(1.0)或其药学上可接受的盐或溶剂合物, I至XII,其中五元杂环基的可取代的碳原子可任选地被基团R 1取代。 还公开了含有式1.0化合物的药物组合物。 还公开了一种通过分别施用抗哮喘,抗过敏或抗炎的有效量的式1.0化合物来治疗哮喘,过敏和炎症的方法。
摘要:
The invention is drawn to bridged bis-aryl carbinol compounds of formula (I): ##STR1## wherein, a, b, c, d, Q, Z, L and R.sup.1 -R.sup.9 are as defined in the specification, their pharmaceutical composition and method of using them in treating asthma, allergy and inflammation.
摘要:
Benzopyrido piperidylidene compounds of the formula ##STR1## wherein R is H, Cl, Br, F or I, which are useful in treating asthma, allergy and/or inflammation.