摘要:
This invention relates to a method of treating or preventing cardic arrhythmias by administering to the affected patient a safe but effective amount of a dibenzocycloheptene compound having an aminomethyl and a 5-hydroxy substituent at the 5position. These compounds are prepared by treatment of dibenzocyclohepten-5-ones with dimethylsulfonium methylide or dimethylsulfoxonium methylide to produce an intermediate spiroepoxide compound which is subsequently reacted with ammonia or a lower aliphatic primary or secondary amine to produce a 5hydroxy-5-aminomethyl-5H-dibenzo(a,d)cycloheptene or an N-alkyl derivative of such a compound. These 5-hydroxy-5-aminomethyl-5Hdibenzo(a,d)cycloheptenes have antiarrhythmic activity and can be used to overcome or prevent cardiac irregularities.
摘要:
The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.
摘要:
Analogues of dieldrin containing a reduced number of chlorine atoms are described, notably 2,10-syn-bisdechlorodieldrin and 2,3,10-syn-trisdechlorodieldrin. These have varying toxicities towards various insect species but offer the advantage of improved biodegradability.
摘要:
The invention comprises an insecticidal composition comprising endrin and tribenzylamine as stabilizing agent. The composition preferably contains tribenzylamine in an amount of at least 0.01, preferably 0.01 to 0.25, weight percent based on the amount of endrin present. The compositions may be in the form of emulsifiable concentrates wettable powders, granulars, dusts and solutions.
摘要:
The disclosure herein generally relates to methods of treating an overweight or obese condition, and overweight or obesity-related conditions. In one embodiment, the disclosure provides a method of treating an overweight or obese condition involving administering to the subject in need thereof, an amount of a pharmaceutical composition including a MetAp-2 inhibitory compound, or a salt, ester, or prodrug thereof, effective to result in weight loss in the subject.
摘要:
A polymerizable liquid crystal compound represented by formula (1): wherein Al and A2 are each a cyclic-structure group; Z1 is a bonding group; m is an integer from 0 to 5; P1 is a polymerizable group represented by formula (2-1); Q1 is alkylene having 1 to 20 carbons; P2 is a polymerizable group represented by any one of formula (2-1) to formula (2-4), hydrogen, fluorine, chlorine, —CN, —CF3, —OCF3, alkyl having 1 to 20 carbons or alkoxy having 1 to 20 carbons; Q2 is a group defined in Q1 when P2 is a polymerizable group and, and Q2 is a single bond when P2 is not a polymerizable group; and in formula (2-2) to formula (2-4), Ra is hydrogen, halogen or alkyl having 1 to 5 carbons.
摘要:
The invention relates to borneol derivatives of general formula I ##STR1## in which R.sup.1 means C(O)--CH(OR.sup.6)--CH(NHR.sup.7)--R.sup.8, R.sup.2 means hydrogen, --OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9a, --OSO.sub.2 R.sup.9a, --OP(O)(OH).sub.2, NHR.sup.9a, NR.sup.9a R.sup.9b, R.sup.3 means hydrogen, --OH, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9b, --OSO.sub.2 R.sup.9b, --OP(O)(OH).sub.2, or R.sup.2, R.sup.3 together mean an oxygen atom, R.sup.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.n --OR.sup.11a, R.sup.5 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.p --OR.sup.11b, or R.sup.4, R.sup.5 together mean an oxygen atom, a=CHR.sup.10 group, n means 0 to 8, p means 1 to 8, R.sup.7 means --C(O)R.sup.12, --SO.sub.2 R.sup.12, --C(O)OR.sup.12, --C(O)NHR.sup.9d, --C(O)NR.sup.9d R.sup.9e, ##STR2## R.sup.8 means aryl, R.sup.9a-e, R.sup.12 are the same or different and mean C.sub.1 -C.sub.10 alkyl, C.sub.4 -C.sub.8 cycloalkyl, aryl, C.sub.7 -C.sub.16 aralkyl, R.sup.10 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.s --OR.sup.14, s means 1 to 8, R.sup.6, R.sup.11a,b, R.sup.14 are the same or different and mean hydrogen, C.sub.1 -C.sub.10 alkyl, aryl, C.sub.7 -C.sub.16 aralkyl, --SO.sub.2 R.sup.9c, --P(O)(OH).sub.2, R.sup.13, R.sup.15a,b are the same or different and mean hydrogen, C.sub.1 -C.sub.10 alkyl, aryl, C.sub.7 -C.sub.16 aralkyl, X.sup.1, X.sup.2 are the same or different and mean X, X can be hydrogen, halogen, --OH, --NO.sub.2, --N.sub.3, --CN, --NR.sup.15a R.sup.15b, --NHSO.sub.2 R.sup.15a, --CO.sub.2 R.sup.15, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 acyloxy, C.sub.1 -C.sub.10 acyl, and, if R.sup.15 means hydrogen, their salts with physiologically compatible bases, as well as the .alpha.-, .beta.-or .gamma.-cyclodextrin clathrates, as well as the compounds of formula I that are encapsulated with liposomes.