摘要:
The invention provides a process for the production of a compound of formula (I), which comprises reacting a compound of formula (II) with a compound of formula (III), in the presence of a strong base and a palladium(0) catalyst, at an elevated temperature, in a solvent which does not adversely affect the reaction. Compounds of formula (I) may be further processed to compounds of formula (V), which are useful in the treatment of inter alia migraine.
摘要:
The present invention provides the compound having formula (I), wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, -O-, -S-, -NH-, or -CH2-; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
摘要:
L'invention a pour objet des composés ioniques dérivés du malononitrile dans lesquels la charge anionique est délocalisée. Un composé ionique de l'invention comprend une partie anionique associée à au moins une partie cationique M m+ en nombre suffisant pour assurer la neutralité électronique de l'ensemble I1 est caractérisé en ce que M est un hydroxonium, un nitrosonium NO + , un ammonium -NH 4 + , un cation métallique ayant la valence m, un cation organique ayant la valence m ou un cation organométallique ayant la valence m, et que la partie anionique répond à l'une des formules R D -Y-C(C≡N) 2 - ou Z-C(C≡N) 2 - dans lesquelles Z est un groupe électroattracteur, R D est un radical organique et Y est un carbonyle, un thiocarbonyle, un sulfonyle, un sulfinyle ou un phosphonyle. Les composés sont utiles notamment pour les matériaux à conduction ionique, les matériaux à conduction électronique, les colorants et la catalyse de diverses réactions chimiques.
摘要:
The invention regards new brominated compounds containing one or two phenyl rings with favorable physico-chemical properties, good tolerance profile, stability and suitable pharmacokinetic profile as contrast media for X-ray mammography, their pharmaceutical formulations and radiological application. The described new bromine contrast media will increase the sensitivity and specificity of X-ray mammography especially in problematic cases. The new contrast media have a higher X-ray absorption than iodine in the energy range used by mammography, a high hydrophilicity, lower toxicity and better tolerance profile than corresponding iodinated compounds.
摘要:
The present invention provides monofluoroalkyl derivatives of the formula (I) wherein: A represents SO2, CO2 or CONH; Ra represents (1-6C)alkyl, (2-6C)alkenyl, -(1-4C)alkyl(3-8C)cycloalkyl, or (1-4C)alkylaromatic; Rb represents H, (1-6C)alkyl, (2-6C)alkenyl, -(1-4C)alkyl(3-8C)cycloalkyl, or (1-4C)alkylaromatic; or R?a and Rb¿ together with the carbon atoms to which they are attached form a (3-8C) saturated carbocyclic ring, a (3-8C) saturated carbocyclic ring containing a heteroatom selected from the group consisting of sulfur or oxygen, or a (5-8C) carbocyclic ring containing one double bond; R1 represents an unsubstituted or substituted aromatic group, an unsubstituted or substituted heteroaromatic group, or an unsubstituted or substituted (5-8C)cycloalkyl group; R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or when A represents SO¿2?, a group of formula R?3R4¿N in which R?3 and R4¿ each independently represents (1-4C)alkyl or , together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; or a pharmaceutically acceptable salt thereof, useful for potentiating glutamate receptor function in a mammal and thereof, useful for treating a wide variety of condutions, such as psychiatric and neurological disorder.
摘要:
Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formulaR 1 -L-NHSO 2 R 2 in which R1 represents an unsubstituted or substituted aromatic or heteroaromatic group; R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R3R4N in which R3 and R4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; and L represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring; and pharmaceutically acceptable salts thereof. Also disclosed are novel compounds of formula I, processes for preparing them and pharmaceutical compositions containing them.
摘要翻译:可以使用有效量的式R 1 -L-NHSO 2 R 2化合物来增强哺乳动物中的谷氨酸受体功能,其中R 1表示未取代或取代的芳族或杂芳族基团; (1-6C)烷基,(3-6C)环烷基,(1-6C)氟代烷基,(1-6C)氯烷基,(2-6C)烯基,(1-4C)烷氧基(1-4C )烷基,未被取代或被卤素取代的苯基,(1-4C)烷基或(1-4C)烷氧基或式R 3 R 4的基团,其中R 3和R 4, 4“各自独立地表示(1-4C)烷基,或者与它们所连接的氮原子一起形成氮杂环丁烷基,吡咯烷基,哌啶基,吗啉代,哌嗪基,六氢氮杂基或八氢az嗪基; (1-6C)烷基,(2-6C)烷基,(2-6C)链烯基,芳基(2-6C)烷基, 6C)烯基和芳基,或两个与它们所连接的碳原子或碳原子一起形成(3-8C)碳环的取代基; 及其药学上可接受的盐。 还公开了式I的新化合物,其制备方法和含有它们的药物组合物。
摘要:
The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
摘要:
Disclosed is a proton conductor in liquid form, comprised of a mixture of the following components: (a) a salt combined with a nitrogenated base along with an acid, according to formula (I), wherein Z1, Z2, Z3, and Z4, whether identical or different, represent a group -N= or -C(Zi)=, wherein Zi represents a hydrogen atom, a linear or branched alkyl radical with from 1 to 20 carbon atoms, a fluoroalkyl radical with from 1 to 20 carbon atoms, or an oxoalkyl or azaalkyl radical with from 1 to 20 carbon atoms, as long as at least one and at most two of the groups Z1, Z2, Z3, and Z4 represent -N=; two adjacent carbon atoms are possibly hydrogenated; the nitrogenated base possibly forms part of a polymeric matrix; and X- represents an anion derivative of an acid selected from the group formed by the sulphonic acids of the formula R?FSO3H, the sulphonimides of the formula (RFSO2) (R'FSO2)NH and the methylures of the formula (RFSO2) (R'FSO2)CH2 or (RFSO2) (R'FSO2) (R'FSO2)CH, wherein RF, R'F or R'F independently represent a radical F(CF2)n-, n being comprised between 0 and 6, and the acid possibly forming part of a polymeric matrix; and (b) a nitrogenated base according to formula (II), wherein Z1, Z2, Z3, and Z4 have the above-mentioned significance, and the nitrogenated base is possibly part of a polymeric matrix. The components (a) and (b) are present in proportions allowing for the formation of a composition with a melting point of less than 25 °C. The proton conductor disclosed in the invention can be used as a liquid, gel, or polymer electrolyte in various electrochemical systems.
摘要:
The present invention relates to a hydrazine derivative represented by the general formula (I):
(wherein each of Ar¹ and Ar² is a substituted or unsubstituted phenyl group, a substituted or unsubstituted heteroaryl group, or the like, R¹ is an alkyl group or the like, and A is a divalent radical having -C=N-N- or -CH-NH-N- as a fundamental skeleton), which is a useful compound as an agricultural and horticultural insecticide.
摘要翻译:本发明涉及由通式(I)表示的肼衍生物:(其中Ar 1和Ar 2各自为取代或未取代的苯基,取代或未取代的杂芳基,或 类似R 1是烷基等,A是具有-C = N - 或-CH-NH-N-作为基本骨架的二价基团),其作为农业和园艺用途的有用化合物 杀虫剂。