摘要:
beta -Aminotetralin derivatives of formula (1): which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a beta -aminotetralins derivative as the active ingredient are described. The beta -aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
摘要:
Styryl sulfone compounds of the invention selectively inhibit proliferation of breast and prostate tumor cells, and induce apoptosis of such tumor cells, while sparing normal cells. The compounds, which are useful in the treatment of breast or prostate cancer, have formula (II) wherein n is zero or one; R1 is selected from the group consisting of hydrogen, chlorine, fluorine and bromine; R2 is selected from the group consisting of hydrogen, chlorine, fluorine, bromine, methyl and methoxy; and R3 is selected from the group consisting of hydrogen, chlorine and fluorine; provided, R2 may not be methyl or methoxy when R1 and R3 are both hydrogen and n is zero or one; and R1, R2 and R3 may not all be hydrogen when n is one, or formula (III) wherein R1 is selected from the group consisting of hydrogen, chlorine, fluorine and bromine or formula (IV) wherein R1 is selected from the group consisting of fluorine and bromine, and R2 is selected from the group consisting of 2-chlorophenyl, 4-chlorophenyl, 4-fluorophenyl and 4-nitro.
摘要:
Battery has an electrolyte comprising a solvent and a salt (I) comprising a hydroxonium, nitrosonium, ammonium, metal, organic or organometallic cation and a 5-membered (hetero)cyclic anion. Battery has an electrolyte comprising a solvent and a salt (I) comprising a hydroxonium, nitrosonium, ammonium, metal, organic or organometallic cation and a 5-membered (hetero)cyclic anion with the following formula: [Image] X1-X5-N=, -N->-, -C(Y)=, -C->(Y)-, -S(O)(Q)=, -S(Q)= or -P(Q')(Q)=, provided that no more than four comprise N, no more than two comprise S (nonadjacent) and no more than one comprises P; Q', Q : 1-8C perhaloalkyl, perhaloalkenyl or optionally substituted 6-12C aryl or aralkyl, each optionally containing O, S or N heteroatoms; Q : an alkyl, alkenyl, aryl, aralkyl, alkylaryl, alkenylaryl, alicyclic or heterocyclic group optionally substituted with halogen and/or ether, thioether, amine, imine, amide, carboxy, carbonyl, isocyanate, isothiocyanate and hydroxy groups; an aromatic group with ring(s) and/or substituent(s) containing heteroatoms; a polymeric group; or a group having one or more cationic and/or anionic ionophore groups; Y : H, F, Cl, Br, CN, SCN, NCS, NCO, NO2, perfluoroalkyl, perfluoroalkoxy, perfluoroalkylmethyl, tetrafluoroethoxy, SCF3, perfluoroalkylthio, tetrafluoroethylthio, trifluorovinyloxy, trifluorovinylthio, SO2F, SO2Q, COOQ, Q-N-SO2- (sic) or COQ; a group comprising one or more aromatic rings that optionally contain N, O, S or P and are optionally substituted with halogen, CN, CO2, SCN, N3, trifluorovinyloxy, (1-12C perfluoroalkyl)methyl, fluoroalkoxy, fluoroalkylthioxy, alkyl, alkenyl, oxaalkyl, oxaalkenyl, azaalkyl, azaalkenyl, thiaalkyl, thiaalkenyl, polymeric groups and groups having one or more cationic and/or anionic ionophore groups; alternatively, two of Y, Q, Q' and Q can form a 4- to 8-membered ring, or one of Y and Q is a multivalent group attached to a second 5-membered (hetero)cyclic anion, or one of Y and Q is a repeat unit of a polymer; provided that at least one Y or Q comprises a dissociating dipole.
摘要:
Aminoguanidine and alkoxyguanidine compounds, including compounds of formula (I) wherein X is O or NR?9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc¿, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula (I). The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.
摘要:
This invention relates to ortho substituted phenyl compounds as inhibitors of prostaglandin synthase, to pharmaceutical compositions comprising such compounds and to methods of using such compounds as antiinflammatory and antipyretic agents. The class of compounds useful in this method of treatment is represented by formula (I).
摘要:
This invention relates to a process for the preparation of 2-nitro-4-(C1-C4 alkylsulfonyl) toluene or 2-nitro-4-(C1-C4 alkylsulfonyl) ethylbenzene by the alkylsulfonylation of 2-nitrotoluene or 2-nitro ethylbenzene.
摘要:
A CCK antagonist compound of formula (I) wherein G is (1) NH2 or (2) substituted amino; R9 is (1) hydrogen, (2) loweralkyl, (3) carboxy-substituted alkyl or (4) carboxyester-substituted alkyl; R10 is (1) hydrogen, (2) loweralkyl, (3) functionalized alkyl or (4) cycloalkyl; D is (1) hydrogen, (2) loweralkyl, (3) functionalized alkyl, (4) cycloalkyl, (5) aryl, (6) functionalized oxyalkyl or (7) heterocyclic; with the proviso that D is other than indolylmethyl, indolinylmethyl or oxindolylmethyl; or R10 taken together with D or R9 taken together with D forms a cyclic group; Z is (1) -C(O)-, (2) -C(S)- or (3) -S(O)2-; B is (1) absent, (2) alkylene, (3) alkenylene, (4) substituted alkenylene, (5) -R26-R27- wherein R26 is absent or -CH2- and R27 is -O-, -S-, -NH- or -N(loweralkyl)- or (6) -R27-CH2- wherein R27 is defined as above; and Ar is (1) aryl or (2) a heterocyclic group.
摘要:
In one aspect, compounds and associated pharmaceutical compositions are described herein for the treatment of various fungal infections and/or other diseases. In some embodiments, for example, compounds of Formula (I) are described herein.