摘要:
The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also povided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.
摘要:
Th2 differentiation inhibitors which contain compounds represented by general formula (I), prodrugs thereof, pharmaceutically acceptable salts thereof or solvates of the same, wherein the rings A, B and C are each an aromatic carbon ring, a heterocycle, etc.; X represents a single bond, -O-, -CH2-, -NH-, -SO-, etc.; Y represents hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, etc.; and V and V represent each a single bond, -O-,-NH-, -OCH2-, etc.
摘要:
The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.
摘要:
A method of treating an ocular disorder in a subject associated with aberrant all- trans -retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R 1 is an aliphatic and/or aromatic compound; the primary amine compound upon administration to the subject forming a reversible Schiff-base with theall- trans -retinal or its metabolite including A2E and retinal dimer without adversely affecting normal retinoid cycle performance; the primary amine compound when administered to a Rdh8 -1- Abca4 -1- mouse increasing the optical coherence tomography score of the mouse to at least about 2.5 and increasing 11-ds-retinal amount at least about 30% in comparison to untreated control animal, wherein the primary amine compound is not a local anesthetic, which includes an aromatic amine, that demonstrates sodium channel blockade when administered to the subject.
摘要:
1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.
摘要:
Su Die Erfindung betrifft Verbindungen der Formel (I), worin A 1 , A 2 , R 1 , R 2 , R 3 , R 4 , R 5 und X die in der Beschreibung angebenene Bedeutung haben, Verfahren und Zwischenverbindungen zu deren Herstellung sowie ihre Verwendung zur Bekämpfung von Schädlingen.
摘要:
Compounds of formula (I), wherein: A is a group OCHR4 or N=CR4; Y is O or NH; R1 is C1-C6-alkyl; R2 is C1-C6-alkyl or C1-C6-alkyl substituted by 1 to 5 fluorine atoms; R3 is C1-C6-alkyl, C1-C6-alkoxy, C3-C6-cycloalkyl, C3-C6-cycloalkoxy, C2-C6-alkenyl, C2-C6-alkenyloxy, C2-C6-alkinyl, C2-C6-alkinyloxy, C1-C6-alkoxycarbonyl, CN or halogen, aryl, hetaryl, heterocyclyl, aryloxy, hetaryloxy or heterocyclyloxy, whereby the above-mentioned groups, with the exception of CN and halogen, may be substituted by the same or different substituents; R4 is methyl, ethyl or cyclopropyl; R6 is hydrogen or methyl; have microbicidal, insecticidal and acaricidal activity, and may be used to control plant-pathogenic fungi, acarids and insects in agriculture and in the field of hygiene.
摘要:
Compounds of general formula (I) are excellent bacteriocides exhibiting wide bacteriocidal spectra, wherein R is a heterocyclic group, CHO or CH2OR ; R is alkyl; R is hydrogen, alkyl, alkoxy, halogeno, nitro, cyano or haloalkyl; R is hydrogen, alkyl, cycloalkyl, alkoxyalkyl, alkoxycarbonyl, cyano, haloalkyl, aryl or a heterocyclic group; R is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, alkanoyl, aroyl, alkoxycarbonyl, aryl or a heterocyclic group; A is (1) -CH2ON=C(R )-, (2) -CH2N(R )-N=C(R ), (3) -CH=NOC(R )(R )- or (4) -CH=NN=C(R )-; B is oxygen or NR ; each wavy line refers to the configuration of an E- or Z-isomer or a mixture of both.
摘要翻译:通式(I)的化合物是显示出宽的杀菌光谱的优良杀菌剂,其中R 1是杂环基,CHO或CH2OR 6; R 2是烷基; R 3是氢,烷基,烷氧基,卤代,硝基,氰基或卤代烷基; R 4是氢,烷基,环烷基,烷氧基烷基,烷氧基羰基,氰基,卤代烷基,芳基或杂环基; R 5是氢,烷基,环烷基,烯基,炔基,烷酰基,芳酰基,烷氧基羰基,芳基或杂环基; A是(1)-CH 2 ON = C(R 7) - ,(2)-CH 2 N(R 8)-N = C(R 7),(3)-CH = NOC(R 9) >)(R 10) - 或(4)-CH = NN = C(R 7) - ; B是氧或NR 11; 每个波浪线是指E-或Z-异构体或两者的混合物的构型。
摘要:
Phenyl acetic acid derivatives of formula (I) in which the substituents and index have the following meanings: X is oxygen or sulphur; R is hydrogen and alkyl; R is hydrogen and alkyl; R is cyano, nitro, trifluoromethyl, halogen, alkyl and alkoxy; m is 0, 1 ou 2, in which the radicals R may be different if m is 2; R is hydrogen, cyano, nitro, hydroxy, amino, halogen, alkyl, halogen alkyl, alkoxy, halogen alkoxy, alkylthio, alkylamino or dialkylamino; R is hydrogen, cyano, nitro, hydroxy, amino, halogen, possibly substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, alkenyl, alkenyloxy, alkenylthio, alkenylamino, N-alkenyl-N-alkylamino, alkinyl, alkinyloxy, alkinylthio, alkinylamino, N-alkinyl-N-alkylamino; optionally substituted cycloalkyl, cycloalkyloxy, cycloalkylthio, cycloalkylamino, N-cycloalkyl-N-alkylamino, cycloalkenyl, cycloalkenyloxy, cycloalkenylthio, cycloalkenylamino, N-cycloalkenyl-N-alkylamino, heterocyclyl, heterocyclyloxy, heterocyclylthio, heterocyclylamino, N-heterocylcyl-N-alkylamino, aryl, aryloxy, arylthio, arylamino, n-aryl-n-alkylamino, hetaryl, hetaryloxy, hetarylthio, hetarylamino, N-hetaryl-N-alkylamino; R is hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, alkinyl, alkylcarbonyl, alkenylcarbonyl, alkinylcarbonyl or alkylsulfonyl; optionally substituted aryl, arylcarbonyl, arylsulfonyl, hetaryl, hetarylcarbonyl or hetarylsulphonyl; and their salts, process and intermediate products for their production, and their use.