摘要:
A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
摘要:
Novel pesticidal compositions, which are characterized by biodegradability and do not bioaccumulate to an unacceptable level in fats and tissues of animals, fowl and fish, containing active compounds and optionally a carrier suitable for administering said compounds to a pest by contact, ingestion or inhalation, are disclosed. Such compositions comprise in addition to the carrier compounds of the formula ##STR1## where R is H, Cl or other Hal, hydroxyl, lower alkoxyl, lower alkyl, cyano, CONR.sub.2 or NR.sub.2 where R.sub.2 is H or lower alkyl; X and Y may be R, and when taken together may be --O-- or a saturated or unsaturated monocyclic or bicyclic group which may be substituted with R, epoxide, carboxy or carboxymethyl group; and the unsaturated analogs thereof wherein the unsaturation occurs at at least one of the 2 or the 5 positions, and wherein unsaturation may occur optionally in the ring formed by X and Y taken together; with the further proviso that said compound has between 4 and 6 halogens; and a carrier for said compound. Methods of using such pesticides to kill or disable pests are disclosed. Certain novel compounds within the group and novel methods of making said compounds are disclosed.
摘要:
Novel phenanthrene derivatives represented by the general formula (1), ##STR1## wherein the group of the formula ##STR2## is a group of the formula ##STR3## (wherein R.sup.1 is a hydrogen atom or a lower alkyl group), a group of the formula ##STR4## (wherein R.sup.2 is a hydrogen atom or a lower alkanoyl group) or a group of the formula ##STR5## (wherein R.sup.2 is the same as defined above), and salts thereof, and other compounds derived therefrom and salts thereof; processes for preparing the same; and interleukin-1 (IL-1) inhibitors containing the abovementioned novel phenanthrene derivatives as to the active ingredient(s).
摘要:
The present invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 is selected from hydrogen, halo, lower alkyl, lower alkoxy, or thioalkoxy; and R.sub.2 is lower alkoxy; or R.sub.1 and R.sub.2 together form a methylenedioxy or ethylenedioxy ring; R.sub.3 and R.sub.4 are independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, (lower alkyl)amino, (lower alkylsulfonyl)amino, and halo; and R.sub.7 is selected from the group consisting of 2- or 3-thienyl, 2- or 3-furyl, and ##STR2## where R.sub.13 and R.sub.14 are independently selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower alkyl, lower alkoxy, lower alkylthio, methylenedioxy, or ethylenedioxy.The compounds of the present invention selectively inhibit .alpha..sub.2 -adrenergic receptors as well as inhibit the uptake of biogenic amines and are thus useful in the treatment of certain cardiovascular and psychiatric disorders.
摘要:
There is provided a novel and efficient stereoselective total synthesis of epiodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or (lower)-alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower) alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.
摘要:
A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate. The compounds possess antioestrogenic activity and may be used for the treatment of hormone-dependent breast tumors or of anovulatory infertility.
摘要:
There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.
摘要:
Disclosed herein are 1,2,3,3a,8,8a-hexahydro-indeno[1,2-c]pyrroles represented by the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl of 1 to 5 carbon atoms, arylalkyl, loweracyl or benzoalkylenedioxy; R.sub.2 and R.sub.3 may be the same or different and are hydroxy, loweralkoxy, halo, thiomethyl, loweracyl, NR.sub.4 R.sub.5, NHSO.sub.2 R.sub.6 or arylalkoxy or R.sub.2 and R.sub.3 taken together may form a methylenedioxy or ethylenedioxy bridge; R.sub.4 and R.sub.5 may be the same or different and are hydrogen, loweralkyl of 1 to 2 carbon atoms or loweracyl; and R.sub.6 is hydrogen or loweralkyl of 1 to 2 carbon atoms.
摘要翻译:本文公开了由下式表示的1,2,3,3a,8,8a-六氢 - 茚并[1,2-c]吡咯,其中R 1是氢,1至5个碳原子的低级烷基,芳基烷基,低级酰基或 苯并亚二氧基; R2和R3可以相同或不同,是羟基,低级烷氧基,卤素,硫代甲基,低级酰基,NR4R5,NHSO2R6或芳基烷氧基,R2和R3可以一起形成亚甲二氧基或亚乙二氧基桥; R 4和R 5可以相同或不同,为氢,1至2个碳原子的低级烷基或低级酰基; R6为氢或1〜2个碳原子的低级烷基。
摘要:
Racemic endo- and exo-1-methoxybicyclo[2.2.2]oct-5-ene-2-carboxylic acids are starting materials for a novel and efficient synthesis of chiral 3R-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-4R-(3-hydroxypropyl)-1R-cyclohexanol, a compound having valuable central nervous system (CNS) activity, particularly as an analgesic and as an antiemetic.