http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-035318-A1
Outgoing Links
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| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-00 |
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| filingDate | 2000-05-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b9841e65fbb71a59d04aeba57dc88c88 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bdd7bc4f4f02a383707f8d0d4d350fe7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6aa678214f7481ad9936bb0619d67ba7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_45db182bfd301bb78f7cb5e65b3f6a2f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7590373ad11b14eee103994ac0ad65c1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_092a5947bb4726cb3ad5e924c2bdb2fe http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cd37aff467097e11d9084408fa0f96a0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_78c3f3ee6da4a88eda545b527d2a2281 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a781f18b839413aa51d6865dbe5c5707 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_939424f7dcec0cd1e43dd2ebff40a278 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c811132cfc8a51bf94072af68c439cb0 |
| publicationDate | 2004-05-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-035318-A1 |
| titleOfInvention | ALFA-AMINO-BETA-SULFONIL HYDROXAMIC ACID COMPOUNDS AND THEIR USE IN THE MANUFACTURE OF MEDICINES |
| abstract | A family of molecules is described that inhibits the activity of matrix metalloproteases (MMP) and, in particular, inhibits the activity of one or more among MMP-2, MMP-9 or MMP-13, while they generally exhibit little activity against MMP-1. The contemplated compound also exhibits little inhibition of TNF production. The compound contemplated is an a-amino-b-sulfonyl carbocycle, heterocycle, aryl or heteroarylhydroxamic acid corresponding to the structure of Formula (1) or a salt acceptable for pharmaceutical use thereof; where R2 is selected from the group consisting of a hydride group, C1-4-hydrocarbyl, hydroxy-C1-4-hydrocarbyl, C1-4-hydrocarbyloxy, halo-C1-4-hydrocarbyl, C1-4-hydrocarbyloxymethyl, aryl, aryl- C1-4-hydrocarbyl, aminomethyl, (N-C1-3-hydrocarbyl) aminomethyl, (N, N-di-C1-3-hydrocarbyl) aminomethyl, (N-morpholin) methyl, (N-pyrrolidin) methyl and (N -thiomorpholin) methyl; R1 is a substituent containing an optionally substituted carbocycle, heterocycle, aryl or heteroaryl radical, directly attached to the represented SO2 group having a length greater than that of an extended pentyl group and less than approximately that of an eicosyl group extended, where R1 defines a three-dimensional volume after rotation around an axis plotted through position 1 attached to SO2 and position 4 of a radical of a 6-member ring or plotted through position 1 attached to SO2 and the center of a link in the 3 or 4 position of a 5-membered ring radical, where the largest dimension of said volume in a direction transverse to the axis of rotation is approximately that of a furanyl ring to approximately that of two phenyl rings; R6 and R7 are independently selected from the group formed by a hydride group, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, aralkyl, carboxyalkyl, carboxyalkylcarbonyl, alcoxicarbonilaminoalquilcarbonilo, heterocyclecarbonyl, heterocycloalkylcarbonyl, ariloxicarbonilaminoalquilcarbonilo, aralquiloxicarbonilaminoalquilcarbonilo, perfluoro, trifluorometilalquilcarbonilo, alquiltioalquilcarbonilo, ariltioalquilcarbonilo, aralquiltioalquilcarbonilo, heteroaralquiltioalquilcarbonilo or a sulfoxide or a sulfone of any such substituents thio, alkylsulfonyl, arylsulfonyl and an aminocarbonylalkyl or aminocarbonylalkylcarbonyl group where the aminocarbonylalkyl or aminocarbonylalkylcarbonyl nitrogen (i) is not substituted, or (ii) is the reactive amine of an amino acid or (iii) it is substituted with one or two radicals selected from the group consisting of a hydroxyalkyl, hydroxyheteroaralkyl, cycloalkyl group uyl, aralkyl, trifluoromethyl alkyl, heterocycloalkyl, benzofused heterocycloalkyl, benzofused cycloalkyl and an N, N-alkylaminoalkyl substituted with a dialkyl group or (iv) said carboxamide nitrogen and two substituents attached thereto together form a heterocycle, heteroalkyl or heteroalkyl ring 5 to 8 members, which in turn is substituted or unsubstituted with one or two radicals independently selected from the group alkyl, alkoxycarbonyl, nitro, heterocycloalkyl, hydroxy, hydroxycarbonyl, aryl, aralkyl, heteroaralkyl and amine, or R6 and R7 together with the Nitrogen atom represented forms a cyclic, saturated or unsaturated imide substituent in which the ring contains five to eight atoms; and R20 is (a) -O-R21, where R21 is selected from the group consisting of a hydride group, C1-6-alkyl, aryl, ar-C1-6-alkyl and a cation acceptable for pharmaceutical use, (b) - NR13-O-R22, where R22 is a selectively removable protective group and R13 is a hydride, C1-6-alkyl or benzyl group or (c) -NR13-O-R14, where R14 is a hydride, a cation acceptable for use pharmaceutical or a C (W) R15 group, where W is O or S and R15 is selected from the group consisting of a C1-6-alkyl, aryl, C1-6-alkoxy, heteroaryl-C1-6-alkyl, C3- group 8-cycloalkyl-C1-6-alkyl, aryloxy, ar-C1-6-alkoxy, ar-C1-6-alkyl, heteroaryl and amino-C1-6-alkyl, where the aminoalkyl nitrogen (i) is not substituted or (ii) is substituted with one or two substituents independently selected from the group consisting of a C1-6-alkyl, aryl, ar-C1-6-alkyl, C3-8-cyclooalkyl-C1-6-alkyl, ar-C1- radical 6-alkoxycarbonyl, C1-6-alkoxycarbonyl and C1-6-alkanoyl or (iii) where the amino-C1-6-alkyl nitrogen and two substituents attached thereto form a 5- to 8-membered heterocycle or heteroaryl ring. The use of said compounds in the manufacture of medicaments for the treatment of a mammal that has a condition associated with a pathological activity of matrix metalloproteases is also described. |
| priorityDate | 1999-05-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 119.