摘要:
Novel carbonyl piperazinyl and piperidinyl compounds and pharmaceutical compositions are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel carbonyl piperazinyl or piperidinyl compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
摘要:
Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
摘要:
Novel compounds of Formula are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
摘要:
Novel tricyclic compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
摘要:
Combinatorial libraries are disclosed which are represented by Formula I: (T′—L)q—Ŝ—C(O)—L′—II′ I wherein: Ŝ is a solid support; T′—L— is an identifier residue; and —L′—II′ is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: which interact (i.e., as agonists or antagonists) with &agr; adrenergic receptors, dopamine receptors, &dgr;-opiate receptors, and K+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatement of ocular diseases such as glaucoma.
摘要:
Combinatorial libraries are disclosed which are represented by Formula I: (T'--L).sub.q --S--C(O)--L'--II' I wherein: S is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: ##STR1## which interact (i.e., as agonists or antagonists) with .alpha. adrenergic receptors, dopamine receptors, .sigma.-opiate receptors, and K.sup.+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.
摘要翻译:公开了由式I表示的组合文库:(T'-L)q- + E,crc S + EE -C(O)-L'-II'I其中:+ E,crc S + EE是固体支持物 ; T'-L-是标识符残基; 和-L'-II'是配体/接头残基。 这些文库含有下式的二氢苯并吡喃:其与α-肾上腺素能受体,多巴胺受体,西酞普兰受体和K +通道相互作用(即激动剂或拮抗剂)与碳酸酐酶同功酶的抑制剂相互作用。 它们可用于治疗眼部疾病如青光眼。
摘要:
Combinatorial libraries are disclosed which are represented by Formula I: (T'-L).sub.q -S-C(O)-L'-II' I wherein: S is a solid support; T'-L- is an identifier residue; and -L'-II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: ##STR1## which interact (i.e., as agonists or antagonists) with .alpha. adrenergic receptors, dopamine receptors, .sigma.-opiate receptors, and K.sup.+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.
摘要翻译:公开了由式I表示的组合文库:(T'-L)q- + E,crc S + EE -C(O)-L'-II'I其中:+ E,crc S + EE是固体支持物 ; T'-L-是标识符残基; 和-L'-II'是配体/接头残基。 这些文库含有下式的二氢苯并吡喃:其与α-肾上腺素能受体,多巴胺受体,西酞普兰受体和K +通道相互作用(即激动剂或拮抗剂)与碳酸酐酶同功酶的抑制剂相互作用。 它们可用于治疗眼部疾病如青光眼。
摘要:
Combinatorial libraries are disclosed which are represented by Formula I: ##STR1## wherein: ##STR2## is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula ##STR3## which interact (i.e., as agonists or antagonists) with .alpha. adrenergic receptors, dopamine receptors, .sigma.-opiate receptors, and K.sup.+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.
摘要:
Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
摘要:
Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.