摘要:
A spiro compound represented by the following formula (I) wherein R1 and R2 are the same or different and each is a hydrogen atom, a chlorine atom and the like, n is 1, 2 or 3, a bond containing a broken line is a single bond or a double bond, A is —X—(CH2)q—N(R3)(R4); a group represented by the following formula (a) and the like, wherein X is an oxygen atom or a sulfur atom, q is 2 or 3, R3 and R4 are the same or different and each is a C1-6 alkyl group and the like, or R3 and R4 optionally form, together with the adjacent nitrogen atom, a piperidine ring and the like optionally substituted by one or two C1-6 alkyl and the like, R5 is a C1-6 alkyl group and the like, R6 is a hydrogen atom and the like, and r and t are each independently one or two, or a pharmaceutically acceptable acid addition salt thereof. The compound is useful as a selective estrogen receptor modulator having a climacteric syndrome-ameliorating effect, and can be expected to be a drug for the prophylaxis and/or treatment of osteoporosis, climacteric syndrome and breast cancer.
摘要:
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
摘要:
The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
摘要:
The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of the general formula I wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of the general formula II wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group—with an acrylic acid C1-4ester, cyclizing the resulting compound of the general formula IV wherein R1, R2 and A are as defined above, R3 stands for C1-4 alkyl group—, eliminating the —COOR3 group and the A protective group of the keto-ester of general formula V wherein R1, R2, R3 and A are as defined above, optionally without isolation of the compounds of the general formulae IV
摘要:
The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate products for their preparation and their use as pest control agents and herbicides.
摘要:
This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
摘要:
A process for preparing intermediate compound (VII), compound (VIII) and compound (XIV) which will be raw materials for the synthesis of a synthetic antibactrial compound, via compound (I) or compound (X) and then, compound (II), the compounds each being shown below; and novel compounds useful for the preparation. 1
摘要:
The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) 1 in which A, B, G, X, Y, Z and W are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.
摘要:
A heat development image forming process comprises steps of: imagewise exposing to light a heat developable light-sensitive material comprising a support, a light-sensitive layer and a non-light-sensitive layer, and then heating the light-sensitive material. The light-sensitive layer or the non-light-sensitive layer contains a heptamethine cyanine dye represented by the formula (I): in which Z.sup.1 is --CR.sup.11 R.sup.12 --, --O--, --S-- or --NR.sup.13 --; Z.sup.2 is --CR.sup.21 R.sup.22 --, --O--, --S-- or --NR.sup.23 --; each of R.sup.1 and R.sup.2 independently is an alkyl group, a substituted alkyl group, an alkenyl group, a substituted alkenyl group, an aralkyl group or a substituted aralkyl group; R.sup.3 is hydrogen, a halogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, a substituted cycloalkyl group, an aryl group, a substituted aryl group, a heterocyclic group, a substituted heterocyclic group, cyano, --SO.sub.2 R.sup.31, --OR.sup.32, --SR.sup.33 or --NR.sup.34 R.sup.35 ; X is an anion; and n is 0 or 1.
摘要翻译:热显影图像形成方法包括以下步骤:将包含支撑体,感光层和非感光层的可热显影的感光材料成像曝光,然后加热感光材料。 感光层或非感光层含有由式(I)表示的七甲基氰花青染料:其中Z 1为-CR 11 R 12 - , - O - , - S-或-NR 13 - 。 Z2为-CR 21 R 22 - , - O - , - S-或-NR 23 - ; R 1和R 2各自独立地为烷基,取代的烷基,烯基,取代的烯基,芳烷基或取代的芳烷基; R 3是氢,卤素原子,烷基,取代的烷基,环烷基,取代的环烷基,芳基,取代的芳基,杂环基,取代的杂环基,氰基,-SO 2 R 31, OR32,-SR33或-NR34R35; X是阴离子; n为0或1。
摘要:
The present application describes novel lactams and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.