摘要:
This invention relates to compounds of formulas 1 and 2 ##STR1## and to pharmaceutically acceptable salts and solvates thereof, wherein X, X.sup.1, R.sup.1, R.sup.2, R.sup.7, R.sup.17 and R.sup.19 are as defined herein. The compounds of formulas 1 and 2 may be useful in the treatment of bacterial, parasitic and protozoal infections, as well as disorders related to bacterial, parasitic and protozoal infections, in mammals, fish and birds. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and 2 and to methods of treating bacterial, parasitic and protozoal infections by administering the compounds of formula 1 and 2.
摘要:
This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is (C1-C4)alkyl optionally substituted with halo, amino or an alkyl amino; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
摘要翻译:本发明涉及下式的化合物或其药学上可接受的盐,其中A和R 1各自为任选取代的5至6元杂芳基,其中杂芳基任选地稠合于碳环或5至6个 杂芳基 R 2是任选被卤素,氨基或烷基氨基取代的(C 1 -C 4)烷基; R 3和R 4各自为氢,卤素,任选被卤素取代的(C 1 -C 4)烷基等; X 1至X 4各自为氢,卤素,羟基,任选被卤素取代的(C 1 -C 4)烷基等。 这些化合物具有COX-2抑制活性,因此可用于治疗或预防炎症或其他COX-2相关疾病。
摘要:
The present invention relates to compounds of the formula wherein R2, R3, R6 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).
摘要:
An efficient synthesis of sulfonyl pyrazoles of formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, R1 through R9 are as defined in the specification, comprising reacting a compound of formula II: wherein the ring of the formula (R5)-A-(SOmR4), m R1 through R9 are as defined above and wherein R10 is halo, (C1-C6)alkyl-SO3—, (C6-C10)aryl-SO3—, (C1-C6)alkyl-SO2—, or (C6-C10)aryl-SO2—; wherein each of said (C1-C6)alkyl component of said (C1-C6)alkyl-SO3— and (C1-C6)alkyl-SO2— radicals may optionally be substituted on any carbon atom by one to six fluoro substituents per (C1-C6)alkyl component; with a compound of formula R3—H, wherein R3 is as defined above, in the presence of a fluoride containing salt and in the presence of a solvent.
摘要:
The present invention relates to 5-heterocyclo-pyrazoles of the formula I: wherein ring W, m, n, and R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.
摘要:
The present invention relates to 5-heteroatom-substituted pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.
摘要:
The present invention relates to heterocyclo alkylsulfonyl pyrazoles of the formula I: wherein the ring of the formula (R5)—A—(SOmR4), m, X, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.