Castro Pineiro Jose L. (Harlow GB3) Chambers Mark S. (Watford GB3) Matassa Victor G. (Furneux Pelham GB3)
출원인 / 주소
Merck Sharp & Dohme Ltd. (Hoddesdon GB2 03)
인용정보
피인용 횟수 :
6인용 특허 :
0
초록▼
Compounds of Formula (I), and salts and prodrugs thereof, wherein R1 represents C1-6alkyl or C3-7cycloalkyl; R2 optionally substituted phenyl or R2 represents a group (A) where W is CH2 or NR10, and W1 is CH2, or W and W1 each represent 0; R3 is C1-6alkyl, halo or NR13R14; R4 is H, C1-4alkyl, option
Compounds of Formula (I), and salts and prodrugs thereof, wherein R1 represents C1-6alkyl or C3-7cycloalkyl; R2 optionally substituted phenyl or R2 represents a group (A) where W is CH2 or NR10, and W1 is CH2, or W and W1 each represent 0; R3 is C1-6alkyl, halo or NR13R14; R4 is H, C1-4alkyl, optionally substituted phenyl or optionally substituted benzyl; R5, R6, R7 and R8 are H or C1-4alkyl; or any two of R4, R5, R6, R7 and R8 together form a chain (CH2)t, and any other two of R4, R5, R6, R7 and R8 optionally form a chain (CH2)s where s and t are independently 1, 2 or 3; m is 2, 3, 4, 5, 6, 7, 8 or 9; n is 0, 1, 2, 3 or 4; and x is 0, 1, 2 or 3; are CCK and/or gastrin antagonists useful in therapy. [Figure] (I) [Figure] (A)
대표청구항▼
A compound of Formula (I), or a pharmaceutically acceptable salt or prodrug thereof: [Figure] (I) wherein: R1 represents C1-6alkyl, C3-7cycloalkyl, cyclopropylmethyl, CH2CO2R9 (where R9 is C1-4alkyl) or CH2CONR13R14, (where R13 and R14 each independently represents H or C1-4alkyl, or R13 and R14 tog
A compound of Formula (I), or a pharmaceutically acceptable salt or prodrug thereof: [Figure] (I) wherein: R1 represents C1-6alkyl, C3-7cycloalkyl, cyclopropylmethyl, CH2CO2R9 (where R9 is C1-4alkyl) or CH2CONR13R14, (where R13 and R14 each independently represents H or C1-4alkyl, or R13 and R14 together form a chain (CH2)p where p is 4 or 5); R2 represents a phenyl group optionally substituted by one or more substituents selected from C1-6alkyl, halo, hydroxy, C1-6alkoxy, (CH2)q tetrazolyl optionally substituted in the tetrazole ring by C1-4alkyl, (CH2)q imidazolyl, (CH2)qtriazolyl, (where q is 0, 1, 2 or 3), 5-hydroxy-4-pyrone, NR13R14 (where R13 and R14 are as previously defined), NR10COR9, NR10CONR10′R9, (where R9 is as previously defined and where R10 and R10′are each independently H or C1-6alkyl), CONR13R14 (where R13 and R14 are as previously defined), SO(C1-6alkyl), SO2(C1-6alkyl), trifluoromethyl, CONHSO2R11, SO2NHCOR11, (where R11 is C1-6alkyl, optionally substituted aryl, 2,2-difluorocyclopropane or trifluoromethyl), SO2NHR12 (where R12 is a nitrogen containing heterocycle), B(OH)2, (CH2)qCO2 H or (CH2)qNR10R12 (where q and R10 are as previously defined and R12 represents tetrazolyl optionally substituted by C1-4alkyl); or R2 represents a group [Figure] where W represents CH2 or NR10, where R10 is as previously defined, and W1 represents CH2, or W and W1 each represent 0; R3 represents C1-6alkyl, halo or NR13R14, where R13 and R14 are as previously defined; R4 represents H, C1-4alkyl, optionally substituted phenyl or benzyl optionally substituted in the phenyl ring, where the phenyl substituents are selected from C1-4alkyl, C1-4alkoxy, halo and trifluoromethyl; R5, R6, R7 and R8 each independently represent H or C1-4alkyl; or any two of R4, R5, R6, R7 and R8 together form a chain (CH2)t, and any other two or R4, R5, R6, R7 and R8 optionally form a chain (CH2)s where s and t are independently 1, 2 or 3; m is 2, 3, 4, 5, 6, 7, 8 or 9; n is 0, 1, 2, 3 or 4; and x is 0, 1, 2 or 3.
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이 특허를 인용한 특허 (6)
Kopin, Alan S.; Beinborn, Martin, Assay for and uses of peptide hormone receptor agonists.
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