Abstract:
The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation (I).
Abstract:
The present invention is directed to pyrrolidine compounds of formula (I) wherein R , R , R , R , R , R and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
Abstract:
The oxygen concentration of a sample is determined utilizing a water-soluble metal ligand complex which is brought into interactive proximity with the sample to form a mixture. The mixture is irradiated with electromagnetic light energy so as to cause emission of light indicative of oxygen. The emitted light is measured, and the measurement utilized so as to determine oxygen concentration of the sample.
Abstract:
The present invention pertains to the field of medicine and more precisely relates to a novel immuno-modulator of formula (I) which exhibits anti-microbial and anti-mycobacterial activities. This modulator is produced by reacting equimolecular amounts of 6-methyluracyl-5-sulphochloride and isoniazide in acetonitrile at a high temperature. The preparation is practically not toxic (LD50 in severe conditions exceeding 7000 mg/kg) and can be used according to given clinical tests for expressing the immuno-modulating and anti-mycobacterial activity. This preparation can be used for correcting various immuno-deficiencies including in HIV-infected patients as well as for treating mycobacterioses such as leprosy, tuberculosis, etc. This preparation can be administered internally or parenterally. The compound described in the present invention represents the active substance of this pharmaceutical preparation, wherein said preparation can be used against secondary immuno-deficiencies or mycobacterioses.
Abstract:
Disclosed herein are methods for treating or limiting development of cardiovascular disease-related neurological disorders by administering a compound of general formula (I), as defined herein.
Abstract:
The present invention relates to compounds of general formula (I-1) or (I-2) wherein R 1 is hydrogen, lower alkyl, lower alkoxy, halogen, O(CH 2 ) 2 -lower akoxy, O(CH 2 ) 2 N(CH 3 ) 2 , or O(CH 2 )-morpholinyl; R 1' is hydrogen, lower alkyl, lower alkoxy, halogen, O(CH 2 ) 2 -lower akoxy, O(CH 2 ) 2 N(CH 3 ) 2 , or O(CH 2 )-morpholinyl; with the proviso that both R 1 and R 1' may be simultaneously hydrogen, but only one of R 1 and R 1' is lower alkyl, lower alkoxy, halogen, O(CH 2 ) 2 -lower akoxy, O(CH 2 ) 2 N(CH 3 ) 2 , or O(CH 2 )-morpholinyl; Het is a 5-or 6 membered heteroaryl group, wherein the heteroatom is selected from N, O or S; X is -CRR'-, -CRR'-NR'-, -C(O)-, -CH 2 -S-, -CH 2 -S(O) 2 -, CH 2 -O- or -CH 2 -CRR'-; R/R' are independently from each other hydrogen, lower alkyl, hydroxy or phenyl, or R and R' may form together with the carbon atom to which they are attached a cyclopropyl ring; R 2 is lower alkyl, -C(O)O-lower alkyl, C 3-6 -cycloalkyl optionally substituted by lower alkyl or =O, bridged cyclohexyl or C 3-6 -cycloalkenyl, or is a 5-membered heteroaryl group, wherein the heteroatom is selected from N, O or S and which is optionally substituted by one or more lower alkyl, or is pyridinyl, optionally substituted by halogen or lower alkoxy; or is phenyl, optionally substituted by one or more R 2' , selected from halogen, cyano, S(O) 2 -lower alkyl, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or amino, or is benzo[1,3]dioxolyl, naphthyl, indolyl, benzo-isoxazolyl, 2,3-dihydro-1H-indenyl, optionally substituted by lower alkoxy or by an oxo group, or is 3,4-dihydro-2H- [1,4]oxazinyl, optionally substituted by an oxo group, or is a five or six membered heterocycloalkyl group; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
Abstract:
The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X 1 , X 2 , Z, R 3 , R 4 , and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
Abstract:
Novel oxime O-ether compounds represented by general formula [I]; and fungicides for agricultural and horticultural use, containing the compounds as the active ingredient [I] wherein R is C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, or the like; m is an integer of 1 to 4; R is hydrogen, C1-6 alkyl, or the like; R and R are each hydrogen or C1-6 alkyl; R is hydrogen, C1-6 alkyl, or the like; R is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, halogeno, or the like; and n is an integer of 1 to 4.
Abstract translation:由通式[I]表示的新型肟O-醚化合物; 和用于农业和园艺用途的杀真菌剂,其含有化合物作为活性成分[I],其中R 1为C 1-6烷基,C 3-6环烷基,C 1-6烷氧基等; m为1〜4的整数。 R 2是氢,C 1-6烷基等; R 3和R 4各自为氢或C 1-6烷基; R 5是氢,C 1-6烷基等; R 6是C 1-6烷基,C 2-6烯基,C 2-6炔基,C 1-6烷氧基,卤代等; n为1〜4的整数。
Abstract:
Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants at very low concentrations of these biologically active compounds.
Abstract:
Novel chemical compounds having herbicidal activity, agricultural compositions, process for their manufacture and their use in crop protection are provided.