摘要:
The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
摘要:
The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
摘要:
This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
摘要:
In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
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:
The present invention relates to novel bicyclic heterocycle derivatives, pharmaceutical compositions comprising the bicyclic heterocycle derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is: I, Ia, Ib ou Ic. R2 is alkyl, alkenyl, aryl, cycloalkyl. heterocycloalkyl or heteroaryl, any of which can be optionally substituted with R3; Y is —C(O)—, —S—, —S(O)—, —S(O)2—, —CH2— or —O—, such that if Y is —O— or —S—, then M is other than N and R1 is (Ib);
摘要翻译:本发明涉及新的双环杂环衍生物,包含双环杂环衍生物的药物组合物和这些化合物用于治疗或预防过敏,过敏诱发的气道反应,充血,心血管疾病,炎性疾病,胃肠道疾病, 糖尿病,糖尿病并发症,葡萄糖耐量降低或空腹血糖受损。 R 1是:I,Ia,Ib o Ic。 R2是烷基,烯基,芳基,环烷基。 杂环烷基或杂芳基,其中任何一个可以任选被R 3取代; Y是-C(O) - , - S - , - S(O) - , - S(O)2 - , - CH 2 - 或-O-,如果Y是-O-或-S-, M不是N,R1是(Ib);
摘要:
In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要:
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.
摘要:
Disclosed are novel compounds of the formula wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally substituted aryl or heteroaryl, and the remaining variables are as defined in the specification, and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.
摘要:
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H. receptor antagonist.