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filingDate 2002-01-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2008-10-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2008-10-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber KR-100861471-B1
titleOfInvention Urea Derivatives as Integrin Alpha 4 Antagonists
abstract Novel antagonists of α4β1 integrin and / or α4β7 integrin of Formula I or pharmaceutically acceptable salts thereof:n n n Formula In n n n n n n n In the above formulan n n R 1 is C 3-10 alkyl, C 3-10 alkenyl, C 3-10 alkynyl, cycloalkyl, cycloalkyl-C 1-10 alkyl, cycloalkyl-C 2-10 alkenyl, cycloalkyl-C 2- 10 alkynyl, heterocyclyl, heterocyclyl-C 2-10 alkyl, heterocyclyl-C 2-10 alkenyl, heterocyclyl-C 2-10 alkynyl, aryl, aryl-C 1-10 alkyl, Aryl-C 2-10 alkenyl, aryl-C 2-10 alkynyl, heteroaryl, heteroaryl-C 1-10 alkyl, heteroaryl-C 2-10 alkenyl, or heteroarylC 2-10 alkynyl ; Wherein said alkyl, alkenyl, and alkynyl group or moiety is unsubstituted or substituted with 1 to 4 substituents, which may be the same or different and independently selected from Ra; Wherein said cycloalkyl, heterocyclyl, aryl and heteroaryl group or moiety is unsubstituted or may be the same or different and is independently substituted with 1 to 4 substituents selected from R b;n n n R2 is hydrogen, C 1-6 alkyl, C 0-2 alkylcycloalkyl, C 0-2 alkylaryl, C 0-2 alkylheteroaryl, cycloalkyl-C 0-2 alkyl, aryl-C 0-2 alkyl or Heteroaryl-C 0-2 alkyl wherein the aryl and heteroaryl groups or moieties are unsubstituted, substituted with 1 to 4 substituents which may be the same or different and are independently selected from Ra;n n n R 3 and R 4 are independently hydrogen or C 1-4 alkyl;n n n R2 and R3, together with the atoms attached to them, may form a 4-8 membered ring;n n n R 5 is C 1-6 alkyl, cycloalkyl, cycloalkyl-C 1-4 alkyl, heterocyclyl, heterocyclyl-C 1-4 alkyl, aryl, aryl-C 1-4 alkyl, heteroaryl, or heteroaryl -C 1-4 alkyl; Wherein said alkyl group or moiety is unsubstituted, may be the same or different and is independently substituted with 1 to 4 substituents selected from Ra; Wherein said cycloalkyl, heterocyclyl, aryl and heteroaryl group or moiety is unsubstituted, substituted with 1 to 4 substituents which may be the same or different and independently selected from R b;n n n L1 is -S-, -S (O)-,-S (0) 2 -,-C (O)-,-C (O) O-,-C (S)-,-N (Rc)-, -CH 2 -, - CH 2 N (Rc) -, -CON (Rc) -, - CSN (Rc) -, - N (Rc) CO -, - N (Rc) CS -, - S (O) 2 N (Rc)-or -N (Rc) S (O) 2- ;n n n L2 is a covalent bond, -O-,-S-,-S (O)-,-S (O) 2 -,-C (O)-,-C (O) O-, -OC (O)-, -C (S),-N (Rc)-,-CON (Rc)-,-OC (O) N (Rc),-CSN (Rc)-,-N (Rc) CO-,-N (Rc) C (O) O-,-N (Rc) CS-,-S (O) 2 N (Rc)-, N (Rc) S (O) 2 -,-N (Rc) CON (Rc)-, or -N (Rc) CSN (Rc)-, wherein if two Rc substituents are present, they may be the same or different;n n n W is O, S, NH, N (Rc), or NCN;n n n X is — (CH 2 ) n aryl- or — (CH 2 ) n heteroaryl-; Wherein the aryl and heteroaryl moieties are unsubstituted, substituted with 1 to 4 substituents which may be the same or different and independently selected from R b;n n n Y is monocyclic aryl, or monocyclic heteroaryl, containing one or two heteroatoms selected from N, O and S, wherein the aryl and heteroaryl moieties are unsubstituted, identical or different and independently from Rb Substituted with 1 to 4 substituents selected;n n n Z is -C (O) ORd, -P (O) 2 ORd, -S (O) 2 ORd, -S (O) 2 N (Rd) (Rd),-C (O) NH 2 , -C ( O) N (Re) S (O) 2 Rd, -S (O) 2 N (Re) C (O) Rd, -5-tetrazolyl, or -C (O) Rd; Wherein if two Rd groups are present they may be the same or different;n n n Ra is -OH, -ORe, -NO 2 , halogen, -S (O) Re, -S (O) 2 Re, -SRe, -S (O) 2 ORe, -S (O) NReRe-S (O ) 2 NReRe, -NReRe, -O (CReRe) mNReRe, -C (O) Re, -CO 2 Re, -CO 2 (CReRe) mCONReRe, -OC (O) Re, -CN, -C (O) NReRe -NReC (O) Re, -OC (O) NReRe, -NReC (O) ORe, -NReC (O) NReRe, -CRe (N-ORe), -CFH 2 , -CF 2 H, or -CF 3 ego ; Wherein if two or more Re groups are present, they may be the same or different;n n n Rb is -OH, -ORe, -NO 2 , halogen, -S (O) Re, -S (O) 2 Re, -SRe, -S (O) ZORe, -S (O) NReRe-S (O) 2NReRe, -NReRe, -O (CReRe) mNReRe, -C (O) Re, -CO 2 Re, -CO 2 (CReRe) mCONReRe, -OC (O) Re, -CN, -C (O) NReRe,- NReC (O) Re, -OC (O) NReRe, -NReC (O) ORe, -NReC (O) NReRe, -CRe (N-ORe),-CFH 2 , -CF 2 H, -CF 3 , C 1 -6 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, cycloalkyl, cycloalkyl-C 1-4 alkyl, heterocyclyl, heterocyclyl-C 1-4 alkyl, aryl, aryl-C 1 -4 alkyl, heteroaryl or heteroaryl-C 1-4 alkyl; Wherein said alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl group or moiety is unsubstituted, may be the same or different, and is independently substituted with 1 to 4 substituents selected from Ra;n n n Rc is hydrogen, C 1-10 alkyl or cycloalkyl; Wherein said alkyl or cycloalkyl group or moiety is unsubstituted, is the same or different and is substituted with 1 to 4 substituents selected from Ra;n n n Rd is hydrogen, C 1-4 alkyl, cycloalkyl, cycloalkyl-C 1-4 alkyl, heterocyclyl, heterocyclyl-C 1-4 alkyl, aryl, aryl-C 1-4 alkyl, heteroaryl, or Heteroaryl-Ci_ 4 alkyl; Wherein said alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl group or moiety is unsubstituted or may be the same or different and is independently substituted with 1 to 4 substituents selected from Ra;n n n Re is hydrogen or C 1-4 alkyl.n n n n is an integer from 0 to 2;n n n m is an integer of 1-6.n n n α4 integrin, α4β1, α4β7, antagonist, urea derivative, cell adhesion, inflammation, immunity, ligand, anti-α4 antibody
priorityDate 2001-01-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 107.