摘要:
The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.
摘要:
Apparatus in fluid communication with a water leg portion of a hydrocarbon-contaminated water, e.g., a water leg portion of a produced water stream or an offshore drilling or production platform sump tank for conveying water, separated from oil, into contact with non-woven fiber/particulate polymer coalescing media-containing canisters such that the hydrocarbon droplets and other organic material droplets commingled with the sump tank or produced water will be coalesced by passage through the coalescing media. The canisters preferably are provided in a plurality of stacks in each vessel. Solids that do not pass through the canisters are accumulated at the bottom of the vessel and easily drained through a drain port. The water and hydrocarbons will pass through the coalescing media within the canisters and will be separated easily from each vessel, e.g., by gravity separation, sot that the water can be conveyed back to the ocean water without contamination.
摘要:
The present invention relates to a compound represented by formula (I): where the structural variables are as defined herein. The compound is useful for promoting hydration of mucosal surfaces.
摘要:
A windshield assembly for a motorcycle. The windshield assembly includes a flyscreen having one of a grommet and a coupling member and a windscreen having the other of a grommet and a coupling member. The coupling member defines a projection that engages the grommet to couple the windscreen to the flyscreen.
摘要:
N-Phenyl-N-(4-piperdinyl)amide derivatives are disclosed having the general formula (I): ##STR1## wherein X is a member selected from the group consisting of alkoxy-carbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxy-carbonyl-lower alkyl, and (C.sub.1-2)alkoxy-(C.sub.1-2)-alkoxy-carbonyl-lower alkyl, and Ar, R, R.sup.1 and R.sup.2 are defined hereinafter, including isomeric forms thereof and acid addition salts thereof. The compounds exhibit analgesic activity having relatively short durations of analgesic action. The invention embraces the compounds (I), pharmaceutical compositions of (I) and methods of providing analgesia with (I). Also included are certain novel intermediates for making (I).
摘要:
Certain 4-[2-(5-(optionally-substituted-aryl- and heteroaryl)oxazolidin-2-on-3-yl)alkyl]benzoic acids and ester, glycinamide, oxazole and thiazolidinedione derivatives thereof are useful as hypoglycemic agents.
摘要:
Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.4 is CN or COOH or certain esters thereof;R.sub.1 is hydrogen, benzyl or certain acyl groups; R.sub.4 is hydrogen, certain alkyl or certain aralkyl groups; R.sub.5 is hydrogen or certain alkyl groups; Z is (C.sub.1 -C.sub.9)alkylene, optionally interrupted by O, S, SO or SO.sub.2 ; and W is hydrogen, methyl, certain aryl or cycloalkyl groups; useful in mammals as analgesics, tranquilizers, anteimetic agents, diuretics, anticonvulsants, antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.
摘要翻译:式(I')的双环稠合苯并噻唑类化合物及其药学上可接受的阳离子和酸加成盐,其中M为O,CH 2或NR 6; R6是氢,甲酰基,苄氧羰基或某些烷氧基烷基,烷酰基,烷基,芳烷基或芳烷基羰基; A'为:(1)其中A和B之一为氢,使得当A为氢时,B为C(R2R3)(CH2)fQ且f为1或2; 当B为氢时,A为C(R2R3)(CH2)fQ,f为0或1,当A和OR1一起形成内酯或其某些衍生物时; (2)A'是(3)A'是Q3; Q是CO 2 R 7,COR 8,C(OH)R 8 R 9,CN,CONR 12 R 13,CH 2 NR 12 R 13,CH 2 NHCOR 14,CH 2 NHSO 2 R 17或5-四唑基; Q 4是CN或COOH或其某些酯; Q 3是CN,COOH或其某些酯;其中Q 4是CN或COOH或其某些酯; R1是氢,苄基或某些酰基; R4是氢,某些烷基或某些芳烷基; R5是氢或某些烷基; Z是(C1-C9)亚烷基,任选地被O,S,SO或SO 2中断; W是氢,甲基,某些芳基或环烷基; 因此在哺乳动物中作为止痛剂,止痛剂,促炎剂,利尿剂,抗惊厥药,止泻药,镇咳药,治疗青光眼有用。
摘要:
Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.
摘要:
The present invention comprises novel compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein: G is hydroxymethylene or carbonyl;R.sub.a and R.sub.b are each methyl or hydrogen;R.sub.1 is hydrogen or alkanoyl having one to five carbon atoms;R.sub.2 is hydrogen, bromo, chloro or fluoro;R.sub.3 is hydrogen, bromo, chloro, fluoro, alkyl having one to six carbon atoms, (CH.sub.2).sub.p COOR.sub.4 wherein p is an integer from 0-6 and R.sub.4 is hydrogen, methyl or ethyl, or (CH.sub.2).sub.q OH wherein q is an integer from 1-6; with the proviso that when R.sub.3 is hydrogen or alkyl, R.sub.2 is bromo, chloro or fluoro;Z is (--alk.sub.1).sub.m --X--(alk.sub.2).sub.n --wherein each of (alk.sub.1) and (alk.sub.2) has from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each zero or 1;X is oxygen or methylene; andW is methyl, pyridyl, piperidyl or ##STR2## wherein W.sub.1 is hydrogen, fluoro, chloro or methoxy. An analgesically producing quantity of the compound when administered to a mammal produces analgesia therein.
摘要:
9-Amino-1-hydroxyoctahydrobenzo[c]quinoline derivatives of formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein R is hydrogen, COR.sub.7 or SO.sub.2 R.sub.8 where R.sub.7 is hydrogen, alkyl, having from one to five carbon atoms; alkenyl and alkynyl each having from two to six carbon atoms; trifluoromethyl, benzyl, furyl, thienyl, pyridyl or R.sub.9 C.sub.6 H.sub.4 where R.sub.9 is H, NH.sub.2, F, Cl, Br, Ch.sub.3 or OCH.sub.3 ; R.sub.8 is alkyl having from one to five carbon atoms or R.sub.9 C.sub.6 H.sub.4 ; R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl having from one to five carbon atoms or --CO--(CH.sub.2).sub.p --NR.sub.2 R.sub.3 wherein p is 0 or an integer from 1 to 4; each of R.sub.2 and R.sub.3 when taken individually is hydrogen or alkyl having from one to four carbon atoms; R.sub.2 and R.sub.3 when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino or N-alkylpiperazino having from one to four carbon atoms in the alkyl group;R.sub.4 is hydrogen, alkyl having from 1 to 6 carbon atoms or --(CH.sub.2).sub.z --C.sub.6 H.sub.5 wherein z is an integer from 1 to 4;R.sub.5 is hydrogen, methyl or ethyl;R.sub.6 is hydrogen, --(CH.sub.2).sub.y --carbalkoxy having from one to four carbon atoms in the alkoxy group and wherein y is 0 or an integer from 1 to 4, carbobenzyloxy, formyl, alkanoyl having from two to five carbon atoms, alkyl having from one to six carbon atoms; --(CH.sub.2).sub.x --C.sub.6 H.sub.5 wherein x is an integer from 1 to 4; or --CO(CH.sub.2).sub.x-1 --C.sub.6 H.sub.5 ;Z is (a) alkylene having from one to nine carbon atoms; (b) -(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from one to nine carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than nine; each of m and n is 0 or 1; X is O, S, SO and SO.sub.2 ; andW is hydrogen, methyl, pyridyl, piperidyl, ##STR2## wherein W.sub.1 is selected from the group consisting of hydrogen, fluoro and chloro; and ##STR3## wherein W.sub.2 is hydrogen or ##STR4## a is an integer from 1 to 5 and b is 0 or an integer from 1 to 5; with the proviso that the sum of a and b is not greater than 5; useful in mammals as analgesics, tranquilizers, anti-emetic agents, diuretics, anticonvulsants, antidiarrheals, antitussives, in treatment of glaucoma, and intermediates therefore.