摘要:
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein Y, R1, R2, R3, R4, R5, R6, R7 R7′ are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are therefore useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis, and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要:
Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要:
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
摘要翻译:公开了下式的化合物或其药学上可接受的无毒盐,其中A,B,C,D,X,R 1,R 2, R 3,R 4,R 5和R 6是本文定义的变量,这些化合物是高度选择性的激动剂 ,GABAa脑受体的拮抗剂或反向激动剂或GABAa脑受体的激动剂,拮抗剂或反向激动剂的前药,因此可用于诊断和治疗焦虑症,唐氏综合征,睡眠,认知和癫痫发作障碍,抑郁症,苯并二氮卓过量 药物,提高记忆力和警觉性。
摘要:
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
摘要翻译:公开了下式的化合物或其药学上可接受的无毒盐,其中A,B,C,D,X,R 1,R 2, R 3,R 4,R 5和R 6是本文定义的变量,这些化合物是高度选择性的激动剂 ,GABAa脑受体的拮抗剂或反向激动剂或GABAa脑受体的激动剂,拮抗剂或反向激动剂的前药,因此可用于诊断和治疗焦虑症,唐氏综合征,睡眠,认知和癫痫发作障碍,抑郁症,苯并二氮卓过量 药物,提高记忆力和警觉性。
摘要:
Provided are compounds (and pharmaceutically acceptable non-toxic salt of such compounds) of the formula: in which A and B are C1-C3 alkylene; R1 is C1-C6 alkyl; R2 and R3 are hydrogen or C1-C6 alkyl; U and V are C1-C6 alkyl or halogen; X, Y and Z are hydrogen, C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, trifluoromethoxy, halogen, or cyano; and W represents up to three substituents which are C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, trifluoromethoxy, halogen, hydroxy, amino, or cyano. These compounds act as modulators of blood glucose levels and are useful for the treatment of diabetes, eating disorders, and obesity. Pharmaceutical compositions and methods of use of the compounds as pharmaceutical agents are also provided.
摘要:
Amido, amino and sulfonamide substituted benzylamine derivatives useful in treating eating disorders have the formula ##STR1## where X.sub.1, X.sub.2, and X.sub.3, independently represent substituents of formula ##STR2## D=H, lower straight or branched chain alkyl having 1-6 carbon atoms, a methylene unit incorporated into a ring connected with G as in the cases of pyrrolidine, pyrrolidone, piperidine, and piperidone;E=O or H.sub.2 ;O=0 or 1;G=straight or branched chain lower alkyl having 1-6 carbon atoms, aryl, aryl substituted with halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, heteroaryl--selected from the group consisting of 2-, 3-, or 4-pyridyl, 2-pyrazyl, 2-, or 3-thienyl, 2-pyrazinyl, 2-, 3-, or 4-quinolyl, 1-, 3-, or 4-isoquinolyl, 2-quinoxalyl, 3-, or 4-cinnolyl, said heteroaryl substituted with halogen, hydroxy, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms;and A, T and R.sub.1 -R.sub.4 are hydrogen or organic substituents.
摘要翻译:可用于治疗进食障碍的酰氨基,氨基和磺酰胺取代的苄基胺衍生物具有下式,其中X1,X2和X3独立地表示式D = H的取代基,具有1-6个碳原子的低级直链或支链烷基, 如吡咯烷,吡咯烷酮,哌啶和哌啶酮的情况下与G连接的环; E = O或H2; O = 0或1; G =具有1-6个碳原子的直链或支链低级烷基,芳基,被卤素取代的芳基,具有1-6个碳原子的直链或支链低级烷基,杂芳基 - 选自2-,3-或 4-吡啶基,2-吡嗪基,2-或3-噻吩基,2-吡嗪基,2-,3-或4-喹啉基,1-,3-或4-异喹啉基,2-喹喔啉基,3-或 所述杂芳基被卤素取代,羟基,具有1-6个碳原子的直链或支链低级烷基,具有1-6个碳原子的直链或支链低级烷氧基; 并且A,T和R 1 -R 4是氢或有机取代基。
摘要:
This invention encompasses compounds of the formula where X1, X2, and X3, independently represent substituents of formula and the pharmaceutically acceptable salts thereof wherein the remaining variables are as defined herein and wherein said compounds are useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.
摘要:
At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, and prodrugs thereof. Methods of treating or preventing disorders in which aberrant kinase activity is implicated, pharmaceutically compositions, and methods for detecting the presence kinases in cells or biological preparations and for identifying kinases of therapeutic interest.
摘要:
Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
摘要:
This invention pertains to compounds of Formula I: and the pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to Hsp90 complex modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including chronic myeloid leukemia, melanoma, breast, ovarian, brain, thyroid, colorectal, prostate, and bladder cancer, heart disease, stroke, autoimmune/inflammatory diseases, and neurodegenerative diseases. Thus methods of treatment include administering a sufficient amount of a compound of Formula I or form thereof to decrease the symptoms or slow the progression of these diseases or disorders. The invention also encompasses methods of treating non-human patients, including livestock and domesticated companion animals, suffering from a disease or disorder responsive to Hsp90 complex modulation. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agent. The invention also includes a method for determining the presence of certain kinases or Hsp90 complex in a sample, comprising contacting the sample with a compound of Formula I or form thereof, and detecting Hsp9O complex activity in the sample.