摘要:
There is provided a method for producing an epoxy compound having an epoxy ring bonded to a triazinetrione ring via a long chain alkylene group, an olefin compound having a specific structure is used to efficiently obtain an epoxy compound of which an olefin moiety is epoxidized in high yield. A method for producing an epoxy compound of Formula (2): comprising reacting a triolefin compound of the following Formula (1): (In the above-mentioned Formulae, R 1 to R 9 are each independently a hydrogen atom or a methyl group; and n1 to n3 are each independently an integer of 1 to 4) with hydrogen peroxide, a nitrile compound, and an alkaline substance in a solvent. The nitrile compound is an aliphatic nitrile compound or an aromatic nitrile compound. The alkaline substance is phosphate, carbonate, or an alkaline metal hydroxide.
摘要:
Primarily, the present invention relates to compounds of the formula (I) defined below and to the use thereof as herbicides, in particular for controlling broad-leaved weeds and/or weed grasses in crops of useful plants and/or as plant growth regulators for influencing the growth of crops of useful plants. The present invention further relates to herbicidal or crop growth-regulating compositions comprising one or more of the compounds of the formula (I). Moreover, the present invention relates to processes for preparing the compounds of the formula (I).
摘要:
The present invention provides analogs of formula (I) of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF. The compounds (II) are used to treat diabetes, inflammatory and autoimmune conditions. wherein R1 is hydrogen or a group having the formula -C(=O)R3, wherein R is lower alkyl, and R2 is selected from the group consisting of.
摘要:
The present invention relates to C ompounds having the structure of Formula I: wherein n is an integer from 1 to 5; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; R2 is alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR4R5, -NHC(=Y)R4, - NHC(=Y)NR5Rχ, -NHC(=O)OR4, -NHSO2R4, C(=Y)NR4R5, C(=O)OR6 [wherein Y is oxygen or sulphur], OR5, -O(C=O)NR4R5, O-acyl, S(O)mR4, -SO2N(R4)2, cyano, amidino or guanidino [wherein R4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; R5 is hydrogen or R4; Rx is R4 or -SO2N(R4)2 and R6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; R3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR4, -OC(=O)NR4R5, O-acyl, NH2, NR4R5, -NHC(=Y)R4, -NHC(=Y)NR5Rx, - NHC(=O)OR4, -NHSO2R4, and to processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by over-expression and over-activation of an matrix metalloproteinase, using the compounds.
摘要:
The invention relates to novel substituted benzoyl ketones of formula (I), wherein n represents 0, 1, 2 or 3; A represents a simple bond or alkanediyl (alkylene); R1 represents hydrogen or optionally substituted alkyl or cycloalkyl; R2 represents hydrogen, cyano, carbamoyl, halogen, or optionally substituted alkyl, alkoxy, alkoxycarbonyl, alkylthio, alkylsulfinyl or alkylsulfonyl; R3 represents hydrogen, nitro, cyano, carboxy, carbamoyl, thiocarbamoyl, halogen or optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl; R4 represents nitro, cyano, carboxy, carbamoyl, thiocarbamoyl, halogen or optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl; and Z represents an optionally substituted 4 to 12-membered, saturated or unsaturated, monocyclic or bicyclic, heterocyclic grouping containing 1 to 4 hetero atoms (up to 4 nitrogen atoms and optionally, - alternatively or additionally - an oxygen atom or a sulphur atom, or an SO¿2? grouping), which also contains one to three oxo-groups (C=O) and/or thioxo-groups (C=S) as constituents of the heterocycle. The invention also relates to methods for producing the inventive substituted benzoyl ketones and to their use as herbicides.
摘要:
Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have generalized formula (1) wherein r is 0-2, T is selected from (a) and (b) and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis of degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要:
The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.
摘要:
The present invention provides analogs of formula (I) of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF. The compounds (II) are used to treat diabetes, inflammatory and autoimmune conditions. wherein R1 is hydrogen or a group having the formula -C(=O)R3, wherein R is lower alkyl, and R2 is selected from the group consisting of.
摘要:
Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have generalized formula (I) wherein R1 represents C¿6?-C12 alkyl; C5-C12 alkoxy; C5-C12 alkylthio; a polyether of formula R?2O(C¿2H4O)a- in which a is 1 or 2 and R2 is C1-C5 alkyl, phenyl, or benzyl; and substituted alkynyl of formula R3(CH2)b-C C-; in which b is 1-10 and R3 is H-, HO-, or R4O- in which R4 is C1-C3 alkyl, phenyl, or benzyl. The alkyl, phenyl, and benzyl portions of R1 may bear at least one pharmaceutically-acceptable substituent. The subscript n is 2-4. R5 represents phenyl; imidoyl of 4-12 carbon atoms; (3H)-benzo-1,2,3-triazin-4-on-3-yl; N-saccharinyl; (2H)-phthalazin-1-on-2-yl; 2-benzoxazolin-2-on-3-yl; 5,5-dimethyloxazolidine-2,4-dion-3-yl; and thiazolidine-2,4-dion-3-yl; with the phenyl and benzo portions of R5 permissibly bearing at least one pharmaceutically-acceptable substituent. Pharmaceutically acceptable salts of these materials are also included.