摘要:
The present invention relates to methods for the preparation of benzoxazole sulfonamide compounds of formula (9) as well as novel intermediates of formula (6) for use in said method. More in particular the invention relates to methods for the Preparation of 2-amino-benzoxazole sulfonamide compounds which make use of 2-mercapto-benzoxazole sulfonamide intermediates, more in particular methods employing the intermediate 1-Benzy1-2-hydroxy-3-[isobutyl(2-methylsulfanyl-benzoxazole-6-sulfonyl)-amino)-propyl)-carbamic ester, and to methods amenable to industrial scaling up. Said benzoxazole sulfonamide compounds are particularly useful as HIV protease inhibitors. The substituents are defined in the claims.
摘要:
The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.
摘要:
The invention is directed to physiologically active compounds of general formula (I): wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring; R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; L1 is an -R3-R4- linkage where R3 is alkylene, alkenylene or alkynylene and R4 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, -C(=Z?2)-NR5-, -NR5-C(=Z2)-, -Z2¿-, -C(=O)-, -C(=NOR?5)-, -NR5-, -NR5-C(=Z2)-NR5¿-, -SO¿2?-NR?5-, -NR5-SO¿2-, -O-C(=O)-, -C(=O)-O-, -NR5-C(=O)-O- or -O-C(=O)-NR5-; L2 is optionally substituted alkylene or alkenylene; Y is carboxy or an acid bioisostere; and Z?1 is NR5¿; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).
摘要:
Disclosed are compounds of formula I as modulators of peroxisome proliferator activated receptors (PPARs) for the treatment of metabolic diseases such as obesity: wherein Ar1 is selected from the group consisting of a monocyclic heteroarornatic ring structure and a bicyclic heteroaromatic ring structure; Ar2 is selected from the group consisting of a monocyclic, a bicyclic, and a tricyclic carbocyclic aryl ring structure R1 is selected from the group consisting of alkyl, optionally substituted a five-membered or six-membered heteroarylring or a six-membered aryl ring, optionally substituted R2 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituied cyano; nitro; an amino; an amido; perhaloalkyl; and halogen; R3 is selected from the group consisting of hydrogen; alkyl, optionally substituted and B is a five-membered or six-membered heteroaryl ring, or -(CH2)j-C(O)OR4, wherein j is 0 or I 1 when Ar2 is a bicyclic or tricyclic carbocyclic ring structure and j is 1 when Ar2 is a monocyclic carbocyclic ring structure; and R4 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituted. The obtional substituents are as defined in claim 1.
摘要:
The present invention relates to a method for preparing optically active (R)-aryloxypropionic acid ester derivatives, and more particularly to a method for preparing (R)- aryloxypropionic acid ester derivatives with high optical purity and good yield at low cost from phenol derivatives with various substituted functional groups and (S)-alkyl O-arylsulfonyl lactates.
摘要:
Benzazole compounds of formula (I) wherein R1, R2, R3, R4, X, Y and Z have the significances given in claim 1, may be used as insect-, mite- and tick-repellent compositions and can be produced in known manner.
摘要:
The invention relates to cyclohexenone derivatives of benzazolons of general formula (I), wherein the variables R?1, R2, R3¿, A and Hex have the meaning as cited in claim 1, and the salts thereof, and the use thereof for controlling harmful plants.