摘要:
The present invention relates to cyclobenzaprine analogs and amitriptyline analogs, including deuterated forms useful for treatment or prevention of symptoms associated with post-traumatic stress disorder.
摘要:
This invention relates to novel derivatives of 5H-dibenzo (a,d)cycloheptenes, to the processes for their preparation, to their muscarinic receptor antagonist properties and to their end-use application for treating Parkinson's Disease, tardive dyskinesia, and motion sickness.
摘要:
10-(2-substituted-aminoethyl)-10,11-dihydro-5-methyl-2 or 3, 7 or 8-substituted or unsubstituted-5H-dibenzo[a,d]cycloheptenes, e.g., 10-(2-dimethylaminoethyl)-10,11-dihydro-5-methyl-5H-dibenzo[a,d]cycloheptene, are prepared by hydrogenating a corresponding 10-(2-dimethyl-aminoethyl)-10,11-dihydro-5-methylene-2 or 3, 7 or 8-substituted or unsubstituted-5H-dibenzo[a,d]cycloheptenes and are useful as anti-depressants.
摘要:
Compounds of the class of 1,1a,6,10b-tetrahydro-1,6methanodibenzo(a,e)cyclopropa(c)cycloheptene derivatives and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an antidepressive and stimulating action. Specific embodiments are N-methyl-1,1a,6,10b-tetrahydro -1,6methanodibenzo(a,e)cyclopropa(c)cycloheptene-11-aminehydrochloride, N,N-dimethyl-1,1a,6,10b-tetrahydro-1,6 -methanodibenzo(a,e)cyclopropa(c)cycloheptene-11-amine-fumarate, Nmethyl-1,1a,6,10b-tetrahydro-1,6-methano-dibenzo(a, e)cyclopropa(c)cycloheptene-11-methylamine-maleate, N,N-dimethyl1,1a,6,10b-tetrahydro-1,6-methano-dibenzo(a,e)cyclopropa(c) cycloheptene-11-methylamine-hydrochloride,N,N-dimethyl-11hydroxy-1,1a,6,10b -tetrahydro-1,6-methano-dibenzo(a, e)cyclopropa(c)cycloheptene-11-methylamine-fumarate and N,Ndimethyl-11-hydroxy-1,1a,6,10b-tetrahydro-1,6-methano-dibenzo(a, e)cyclopropa(c)cycloheptene-11-ethylamine-hydrochloride.
摘要:
Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH. Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.
摘要:
Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.4 is alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha., and methods for treating septic shock, inflammation, or allergic disease.
摘要:
The dihydrodibenzocycloheptyliden-ethylpiperazine derivative has the formula: ##STR1## wherein R represents a substituent selected from the group consisting of --CH.dbd.CH.sub.2 ; --CO.sub.2 C.sub.2 H.sub.5 ; --CH.dbd.CH--CO.sub.2 CH.sub.3 ; ##STR2## and
摘要:
A dihydrodibenzocycloheptyliden-ethyl-piperazine derivative of the general formula: ##STR1## in which, R=--CH.dbd.CH.sub.2 ; --CH.sub.2 OH; --COOH; --CO.sub.2 C.sub.2 H.sub.5 ; --CH.dbd.CH--CO.sub.2 CH.sub.3 ; --CH.dbd.CH--CO.sub.2 CH.sub.3, --C.sub.6 H.sub.5, ##STR2## or pharmaceutically acceptable salts thereof, are disclosed. The compounds of the invention are useful in pharmaceutical compositions for the treatment of pathologies responsive to vasodilatory agents.
摘要:
The present invention provides methods of inducing proliferation of and/or differentiating cells comprising contacting cells with compounds within the methods of the invention. The present invention further provides cells obtainable by the methods of the invention. Liver disease affects more than 500 million people worldwide. Organ transplantation is the gold standard for treatment of liver failure, but organ shortages are acute.
摘要:
A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumour cells.
摘要翻译:描述了可用于治疗或预防癌症的药物组合物和方法中的一类化合物。 化合物抑制RET激酶的能力被定量,即它们各自的RET IC 50和EC 50值被描述。 已知一种这样的化合物,称为环苯扎林,本文称为SW-01,已被鉴定为RET特异性,IC 50为300nM。 SW-01抑制RET自身磷酸化并阻断甲状腺癌细胞系的生长和转化。 已在胰腺癌,乳腺癌和SCLC细胞系中进一步检测。 该化合物显示用于抑制肿瘤细胞的存活和增殖。