Casagrande Cesare (Arese ITX) Santangelo Francesco (Milan ITX)
출원인 / 주소
Zambon Group S.p.A. (Vicenza ITX 03)
인용정보
피인용 횟수 :
4인용 특허 :
1
초록
Compounds having the formula [Figure] (I) wherein R is 2-[1-oxo-(2H)-phthalazinyl], R1, R2, R3, R4, R5, R6, X, Y, m and n have the meanings shown in the description. The compounds of formula I are pharmaceutically active as anti-vasospastic, anti-aggregating, and anti-proliferative agents.
대표청구항▼
A compound of the formula [Figure] (I) wherein R is a 2-[1-oxo-(2H)-phthalazinyl]group formula [Figure] wherein R4 is hydrogen; R5 and R6, equal to or different from one another, are hydrogen, halogen, nitro, C1-C4 alkyl or C1-C4 alkoxy; R1 and R2, independently, are C1-C4 alkyl or together are -CH2
A compound of the formula [Figure] (I) wherein R is a 2-[1-oxo-(2H)-phthalazinyl]group formula [Figure] wherein R4 is hydrogen; R5 and R6, equal to or different from one another, are hydrogen, halogen, nitro, C1-C4 alkyl or C1-C4 alkoxy; R1 and R2, independently, are C1-C4 alkyl or together are -CH2-CH2-group; X is nitrogen or -CH-; Y is selected from -CO-and -CHOH-. R3 is phenyl optionally substituted by one to three substituents selected from halogen, C1-C4 alkyl and C1-C4 alkoxy; m is an integer from 1 to 4; n is 1; and its salts with pharmaceutically acceptable acids. A compound of the formula [Figure] (1-A) wherein R4 is hydrogen or C1-C4 alkyl; R5 and R6, equal to or different from one another, are hydrogen, halogen, nitro, C1-C4 alkyl or C1-C4 alkoxy; Y is selected from -CH2, -CO-, -CHOH-and -NH-CO-. R3 is phenyl optionally substituted by one to three substituents selected from halogen, C1-C4 alkyl and C1-C4 alkoxy; m is an integer from 1 to 4; n is zero or 1. A compound having the formula [Figure] (I-B) wherein R4 is hydrogen or C1-C4 alkyl; R5 and R6, equal to or different from one another, are hydrogen, halogen, nitro, C1-C4 alkyl or C1-C4 alkoxy; Y is selected from -CH2--CO-, -CHOH-and -NH-CO-. R3 is a phenyl optionally substituted by one to three substituents selected from halogen, C1-C4 alkyl and C1-C4 alkoxy; m is an integer from 1 to 4; n is zero or 1; and its salts with pharmaceutically acceptable acids. A pharmaceutical composition having anti-vasospastic, platelet anti-aggregating and tumor anti-proliterative properties comprising a therapeutically effective amount of a compound according to claim 2, and one or more pharmaceutically acceptable excipients. A compound of the formula [Figure] (I) wherein R is a 2-[1-oxo-(2H)-phthalazinyl]group of formula [Figure] wherein R4 is hydrogen or C1-C4 alkyl, R5 and R6, equal to or different from one another, are hydrogen, halogen, nitro, C1-C4 alkyl or C1-C4 alkoxy; R1 and R2, independently, are C1-C4 alkyl or together are -CH2-CH2-group; X is nitrogen or -CH-; Y is selected from -CH2-, -CO-, -CHOH-and -NH-CO-. R3 is fluorophenyl; m is 2 or 3; n is zero or 1; and its salts with pharmaceutical acceptable acids.
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이 특허에 인용된 특허 (1)
Eberlein Wolfgang (Biberach DEX) Austel Volkhard (Biberach DEX) Heider Joachim (Warthausen DEX) Dammgen Jurgen (Warthausen DEX) Kadatz Rudolf (Biberach DEX) Lillie Christian (Vienna ATX) Kobinger Wal, Phenylalkylamino-alkyl derivatives of quinazolinone and phthalazinone.
Kanter, James; Pandey, Anjali; Robinson, James; Scarborough, Robert M., Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof.
Kanter, James; Pandey, Anjali; Robinson, James; Scarborough, Robert M.; Scarborough, legal representative, Carroll, Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof.
Kanter, James; Robinson, James; Pandey, Anjali; Scarborough, Robert M., Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof.
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