Alkylidene macrolides having immunosuppressive activity
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/395
C07D-267/00
출원번호
US-0897738
(1992-06-12)
발명자
/ 주소
Rupprecht Kathleen (Cranford NJ) Baker Robert (Cranford NJ)
출원인 / 주소
Merck & Co., Inc. (Rahway NJ 02)
인용정보
피인용 횟수 :
26인용 특허 :
0
초록▼
Alkylidene macrolides of the general structural Formula I: [Figure] I [Figure] have been prepared from suitable precursors by derivitization at C-9 or C-22. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prev
Alkylidene macrolides of the general structural Formula I: [Figure] I [Figure] have been prepared from suitable precursors by derivitization at C-9 or C-22. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia oralopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, inflammatory bowel disease, necrotizing entercolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow\s disease.
대표청구항▼
A compound of formula I: [Figure] I [Figure] or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from: (1) hydrogen; and (2) C1-4 alkanoyl; R2 is selected from: (1) methyl; and (2) hydrogen; R3 is hydrogen, hydroxy, or C1-6alkoxy; R4 is hydrogen, or R3 and R4 taken together form a
A compound of formula I: [Figure] I [Figure] or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from: (1) hydrogen; and (2) C1-4 alkanoyl; R2 is selected from: (1) methyl; and (2) hydrogen; R3 is hydrogen, hydroxy, or C1-6alkoxy; R4 is hydrogen, or R3 and R4 taken together form a double bond; R5 is selected from: (1) methyl, (2) ethyl (3) propyl, and (4) allyl; R6 is hydroxy or hydrogen; R7 is hydrogen, or R6 and R7 taken together from a double bond; R8 is hydrogen, hydroxy, or fluoro; W and X are independently selected from: (1) oxo, (2) (H, OH), (3) (OH, R9), wherein R9 is selected from: (a) C1-6 alkyl, (b) C2-6 alkenyl, (c) -CH2-SOm-C1-6 alkyl, wherein m is 0, 1 or 2, (d) -CH2S(C1-6 alkyl)2+M-, wherein M-is a negative counterion selected from: chloro, bromo, iodo, (e) phenyl, (f) furanyl, (4) 〓CR10R11, wherein R10 and R11 are independently selected from: (a) hydrogen, (b) C1-6 alkyl, (c) C2-6 alkenyl, (d) -SOm-C1-6 alkyl, wherein m is as defined above; with the proviso that W and X are not simultaneously oxo, (H, OH), or combinations thereof; n is 1 or 2.
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