摘要:
Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.
摘要:
Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.
摘要:
An object of the present invention is to provide an amino composition which provides, when used as a curing agent for epoxy resin, a long pot life and an excellent appearance of a coating film to an epoxy resin composition without deteriorating the reactivity of the composition. The amino composition is obtained by addition reaction of diamine such as metaxylylenediamine and 1,3-bis (aminomethyl) cyclohexane and styrene, wherein the content of the diamine is less than 15% by weight based upon the total weight of the amino composition and the content of 1-addition product of having one phenethyl group is 50 to 100% by weight based upon the total weight of amino compound(s) obtained by the addition reaction.
摘要:
Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.
摘要:
Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
摘要:
This invention relates to an improved process for the preparation of cyclohexylamines wherein an aromatic amine is contacted with hydrogen in the presence of a hydrogenation catalyst. The improvement resides in utilizing a hydrogenation catalyst comprised of rhodium metal, utilizing a dialkyl ether solvent, and effecting delay addition of the aromatic diamine to the reaction medium.
摘要:
Compounds of Formula I:E-NH-D-NH-B-A-B-NH-D-NH-E (I)wherein A is C.sub.2 -C.sub.6 alkene, C.sub.3 -C.sub.6 cycloalkyl, cycloalkenyl, or cycloaryl; B is independently a single bond, C.sub.1 -C.sub.6 alkyl alkenyl; D is independently C.sub.1 -C.sub.6 alkyl or alkenyl, or C.sub.3 -C.sub.6 cycloalkyl, cycloalkenyl, or cycloaryl; and E is independently H, C.sub.1 -C.sub.6 alkyl or alkenyl; and pharmaceutically-suitable salts thereof; a synthetic method therefor, pharmaceutical dosage forms containing one of more of these compounds, and use of these compounds in the treatment of neoplastic cell growth, are disclosed.
摘要:
Use of a compound having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which may be the same or different represent hydrogen atoms or alkyl groups of 1-6 carbon atoms, or NR.sup.1 R.sup.2 and/or NR.sup.3 R.sup.4 together represent a heterocyclic group having 5 or 6 ring atoms, x is 0 or 1 and when x is 0, the dashed line represents a double bond, W represents a saturated or ethylenically unsaturated divalent hydrocarbyl group required to complete a cycloalkane, cycloalkene or cycloalkadiene ring of 3 to 6 ring atoms and from 0 to 2 double bonds, in the form of the free base or an acid addition salt tolerable to plants, as a plant fungicide, as a fungicide, especially as a mildewicide.Some of the compounds of formula (1) are new and are claimed per se.
摘要:
THE ISOMER RATIO IN A NON-EQUILIBRATED MIXTURE OF THE CIS AND TRANS ISOMERS OF A C6-C14 CYCLOALKYLANEBIS(METHYLAMINE9 SUCH AS 1,4-CYCLOHEXNEBIS(METHYLAMINE) CAN BE CONVENIENTLY ALTERED BY CONTACTING THE MIXTURE AT 175*290*C. WITH HYDROGEN IN THE PRESENCE OF A HYDROGENATION CATALYST AND AMMONIA. A HIGH YEILD OF ONE OF SUCH ISOMERS CAN BE OBTAINED BY SIMILARLY CONTACTING A MIXTURE OF SUCH ISOMERS WHEREIN THE RATIO OF SAID ONE ISOMER TO THE OTHER OF SAID ISOMERS IS LOWER THAN THE CORRESPONDING EQUILBRIUM RATIO OF SUCH ISOMERS, SELECTIVELY SEPARATING SAID ONE ISOMER FROM THE CONTACTED MIXTURE AND RECYCLING THE RESIDUAL MIXTURE FOR MORE OF SUCH CONTACTING.
摘要:
The method for producing trans-rich-1,4-bis(aminomethyl)cyclohexane includes blending 1,4-bis(aminomethyl)cyclohexane with an alkali metal compound and XDA and heating the mixture to isomerize 1,4-bis(aminomethyl)cyclohexane so that the trans isomer content relative to the cis/trans isomers in total is more than 70 mass %, and purifying the isomerized 1,4-bis(aminomethyl)cyclohexane by distillation after the isomerization step. The alkali metal compound is at least one compound selected from the group consisting of alkali metal hydride, alkali metal amide, and alkyl alkali metal. In the isomerization step, 0.01 mol or more and less than 4 mol of XDA is blended relative to 100 mol of 1,4-bis(aminomethyl)cyclohexane, a dimer produced from one molecular of 1,4-bis(aminomethyl)cyclohexane and one molecular of XDA, and a trimer produced from two molecules of 1,4-bis(aminomethyl)cyclohexane and one molecular of XDA are produced, and the dimer content is 5 mass % or more and less than 75 mass % relative to the dimer and trimer in total.