摘要:
The present invention provides wherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5; R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH; R3 is selected from the group consisting of C1-C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl; R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl; m is 0 or an integer from 1 to 3 and n is an integer of from 1 to 4. These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.
摘要翻译:本发明提供其中R 1选自C 1 -C 10烷氧基,OH和NR 4, / SUP> R< 5>; R 2选自C 1 -C 10烷基和(CH 2 N 2)N 2 > n OH; R 3选自C 1 -C 10烷基,杂芳基,例如C 1 -C 6烷基。 噻吩基,呋喃基和吡啶基,苯基,单,二 - ,三取代的苯基和杂芳基; R 4和R 5独立地选自H,C 1 -C 10烷基, C 1 -C 10烷基羟基; C 1 -C 10烷基羟基; m为0或1〜3的整数,n为1〜4的整数。这些化合物可用于降低眼内压和/或治疗青光眼或向人类患者的眼睛提供神经保护作用。
摘要:
The present invention provides the compound having the formula: 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:
The present invention relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
摘要:
The present invention relates to a compound of the formula (I) The compound according to the invention is suitable for the preparation of herbicidal active substances such as sulfonylureas.
摘要:
The invention relates to novel pesticidally active N-bisaryl-and N-aryl-cycloalkylidenyl-null-sulfin-and null-sulfonamino acid amides of the general formula I, including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl; C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR11R12 wherein R11 and R12 are each independently of the other C1-C6alkyl, or together are tetra- or penta-methylene; R2 and R3 ae each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; optionally substituted aryl; optionally substituted heteroaryl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; A is an optionally substituted saturated or unsaturated C3-C8-cycloalkylidene, optionally substituted phenylidene or optionally substituted saturated or unsaturated heterocyclylidene bridge, R4 and R5 are each independently hydrogen or an organic radicak, and R6 is hydrogen; tri-C1C4alkyl-silyl; di-C1-C4alkyl-phenysilyl; C1-C4alkyl-diphenylsilyl; tri-phenylsilyl; optionally subsituted alkyl; optionally substituted alkenyl or optionally substituted alkynyl. The novel compounds possess plant-protecting properties and are suitable for protecting plants against infestation by phytophathogenic microorganisms. 1
摘要:
The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): 1 wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof
摘要:
Compounds of formula (I): wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP.
摘要:
The present invention describes methods for inhibition angiogenesis in tissues using organic peptidomimetic nullvnull3 antagonists, and particularly for inhibiting angiogenesis in inflamed tissues and in tumor tissues and metastases using therapeutic compositions containing nullvnull3 antagonists. The antagonists are organic compounds having a basic group and an acidic group spaced from one another by a distance in the range of about 10 Angstroms to about 100 Angstroms, as described in detail herein.
摘要:
The present invention provides (bis) sulfonamide derivatives of formula (I) useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.