Patent classifications
C07C62/38
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds having the general formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables R.sup.AA, n, ring A, X.sup.1, L, m, X.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, and R.sup.6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
COMPOUNDS FOR THE TREATMENT OF OBESITY AND METHODS OF USE THEREOF
Pentacyclic triterpene compounds are provided herein. Also provided are pharmaceutical formulations containing a therapeutically effective amount of one or more of the compounds, or pharmaceutically acceptable salts or prodrugs thereof, in combination with one or more pharmaceutically acceptable excipients. The pharmaceutical formulations can be administered to a pre-obese, obese, or morbidly obese patient to induce weight loss, reduce body fat, reduce food intake, improve glucose homeostasis, prevent obesity, or a combination thereof. The compounds can also be co-administered with leptin or a leptin analog.
COMPOUNDS FOR THE TREATMENT OF OBESITY AND METHODS OF USE THEREOF
Pentacyclic triterpene compounds are provided herein. Also provided are pharmaceutical formulations containing a therapeutically effective amount of one or more of the compounds, or pharmaceutically acceptable salts or prodrugs thereof, in combination with one or more pharmaceutically acceptable excipients. The pharmaceutical formulations can be administered to a pre-obese, obese, or morbidly obese patient to induce weight loss, reduce body fat, reduce food intake, improve glucose homeostasis, prevent obesity, or a combination thereof. The compounds can also be co-administered with leptin or a leptin analog.
PLANT GROWTH PROMOTERS AND METHODS OF USING THEM
New plant growth regulators, including compounds and compositions, and methods of use including for promoting root growth. The compounds are carotenoid oxidation products, and a preferred example is 3-OH--apo-13-Carotenone. A method comprising promoting the growth of at least one plant with use of an effective amount of at least one composition comprising an effective amount of at least one compound which is represented by A-B-C, wherein B is a bivalent polyene moiety, A is a monovalent moiety linked to B by a six-membered carbon ring, wherein the ring has at least one substituent linked to the ring by an oxygen atom, and C is a monovalent moiety linked to B by a carbonyl group. Synergistic effects can be used with combinations of compounds.
PLANT GROWTH PROMOTERS AND METHODS OF USING THEM
New plant growth regulators, including compounds and compositions, and methods of use including for promoting root growth. The compounds are carotenoid oxidation products, and a preferred example is 3-OH--apo-13-Carotenone. A method comprising promoting the growth of at least one plant with use of an effective amount of at least one composition comprising an effective amount of at least one compound which is represented by A-B-C, wherein B is a bivalent polyene moiety, A is a monovalent moiety linked to B by a six-membered carbon ring, wherein the ring has at least one substituent linked to the ring by an oxygen atom, and C is a monovalent moiety linked to B by a carbonyl group. Synergistic effects can be used with combinations of compounds.
Compounds for the treatment of obesity and methods of use thereof
Pentacyclic triterpene weight loss agents are provided herein. Also provided are pharmaceutical formulations containing a therapeutically effective amount of one or more of the weight loss agents, or pharmaceutically acceptable salts or prodrugs thereof, in combination with one or more pharmaceutically acceptable excipients. The pharmaceutical formulations can be administered to a pre-obese, obese, or morbidly obese patient to induce weight loss, reduce body fat, reduce food intake, improve glucose homeostasis, prevent obesity, or a combination thereof. The weight loss agents can also be co-administered with leptin or a leptin analog.
PHOTOSENSITIVE RESIN COMPOSITION, POLYAMIDE RESIN, METHOD FOR PRODUCING POLYAMIDE RESIN, COMPOUND, METHOD FOR PRODUCING COMPOUND, METHOD FOR PRODUCING CURED FILM, AND CURED FILM
A photosensitive resin composition capable of forming a cured film with satisfactory adhesion to substrates and excellent transparency, a polyamide resin which is used in the photosensitive resin composition, a method for producing the polyamide resin, a compound which is used as a raw material of the polyamide resin, a method for producing the compound, a method for producing a cured film using the photosensitive resin composition, and a cured film which is obtained by curing the photosensitive resin composition. The photosensitive resin composition including a resin and a photopolymerization initiator. The resin is a polyamide resin including a structural unit, which includes a specific saturated alicyclic skeleton, and at least one carboxy group esterified by a unit containing a polymerizable group of a predetermined structure.
Use of benzotropolone derivatives as UV absorbers and antioxidants and their use in sunscreens and/or cosmetic compositions
Described is the use of benzotropolone and their derivatives, especially the compounds of formula (1); wherein R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 independently of one another are hydrogen; OH; C.sub.1-C.sub.30alkyl, C.sub.2-C.sub.30al-kenyl, C.sub.1-C.sub.30alkoxy, C.sub.3-C.sub.12cycloalkyl or C.sub.1C.sub.30hydroxyalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C.sub.6-C.sub.20aryl, which may be substituted by one or more G; C.sub.4-C.sub.20heteroaryl, which may be substituted by one or more G, C.sub.2-C.sub.18alkenyl, C.sub.2-C.sub.18alkynyl, C.sub.7-C.sub.25aralkyl, CN, or COR.sub.17; C.sub.1-C.sub.30mono- or dialkylamino; COR.sub.9; COOR.sub.9; CONR.sub.9R.sub.10; CN; SO.sub.2R.sub.9; OCOOR.sub.9; OCOR.sub.9; NHCOOR.sub.9; NR.sub.9COR.sub.10; NH.sub.2; *(CO)NH(CH.sub.2).sub.n1(PO)(OR.sub.11).sub.2; (CO)O(CH.sub.2).sub.n1(PO)(OR.sub.11).sub.2; sulphate; sulphonate; phosphate; phosphonate; (CH.sub.2).sub.n2[O(SO.sub.2)].sub.n3OR.sub.11; O(CH.sub.2).sub.n4(CO).sub.n5R.sub.11; (O).sub.n6(CH.sub.2).sub.n7(PO)(OR.sub.9).sub.2; (O).sub.n6(CH.sub.2).sub.n7SO.sub.2OR.sub.9; halogen; organosilanyl; organo-siloxanyl; or a sugar residue linked directly in an - or -mode via the anomeric oxygen to the benzotropolone system or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar-(CH.sub.2).sub.n(X.sub.1).sub.1 or 0-benzotropolone system, wherein n=1-10 and X.sub.1O; (CO); OCO; COO, NH; S; SO.sub.2); R.sub.1, R.sub.7 and R.sub.8 independently of one another are hydrogen; C.sub.1C.sub.12alkyl or C.sub.3-C.sub.12-cycloalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C.sub.6-C.sub.20aryl, which may be substituted by one or more G; C.sub.4-C.sub.20heteroaryl, which may be substituted by one or more G, C.sub.2-C.sub.18alkenyl, C.sub.2-C.sub.18alkynyl, C.sub.7-C.sub.25aralkyl, or COOR.sub.9; COR.sub.9; CONR.sub.9R.sub.10; SO.sub.3R.sub.9; SO.sub.2R.sub.9; PO.sub.3(R.sub.9).sub.2; PO.sub.2(R.sub.9).sub.2; organosilanyl; organosiloxanyl; or a sugar residue linked directly in an - or -mode via the anomeric oxygen to the benzotropolone system or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar-(CH.sub.2).sub.n(X.sub.2).sub.1 or 0*, wherein n=1-10 and X.sub.2C(O); OCO*); R.sub.9 and R.sub.10 independently from each other are hydrogen; C.sub.1C.sub.18alkyl or C.sub.3-C.sub.12-cycloalkyl which may be substituted by one or more E and/or interrupted by one or more D; C.sub.6-C.sub.20aryl, which may be substituted by one or more G; C.sub.4-C.sub.20heteroaryl, which may be substituted by one or more G; organosilanyl; organosiloxany