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Home   •   Spotlight  •  rlist3q03p  •  Most Requested Patent Families 3Q03-Chemistry and Related Science (9)
Most Requested Patent Families 3Q03-Chemistry and Related Science
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Following is one of the patent documents most requested by researchers using CAS electronic products.



CAS indexed 102 chemical substances from this document.
CAS subject entries for this document include: Combinatorial library; Cyclophanes; Macrocyclic compounds.

CAPLUS COPYRIGHT 2003 ACS on STN

TITLE: Methods for cyclophane-like compounds and macrocyclic compounds having reactive functional groups
INVENTOR(S): Cook, Phillip Dan
PATENT ASSIGNEE(S): Isis Pharmaceuticals, Inc., USA; Cook, Phillip Dan
SOURCE: PCT Int. Appl., 167 pp. CODEN: PIXXD2
LANGUAGE: English
PATENT INFORMATION:
PATENT NO.       KIND  DATE           APPLICATION NO.  DATE
---------------  ----  --------       ---------------  --------
WO 9810286 A1 19980312 WO 1997-US15493 19970904 W: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW, AM, AZ, BY, KG, KZ, MD, RU, TJ, TM RW: GH, KE, LS, MW, SD, SZ, UG, ZW, AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE, BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG AU 713740 B2 19991209 AU 1997-26244 19970624 AU 9726244 A1 19971106 AU 9742480 A1 19980326 AU 1997-42480 19970904 US 6232463 B1 20010515 US 1998-128508 19980804 US 6559303 B1 20030506 US 1999-254219 19990409

ABSTRACT:
Novel macrocyclic compds. are constructed to include large cyclic structures that are interrupted by at least one ring system. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chem. functional groups. Libraries of such macrocyclic compds. are prepd. utilizing permutations and combinations of the chem. functional groups and the nitrogenous moieties to build complexity into the library. E.g., reaction of N1-(tosyl-O-aminopropanol-3-yl)diaminoethane and 2,6-pyridinedicarbonyl dichloride in presence of proton sponge gave 48% of an isomeric mixt. of 1,11,18,28-tetracarboxy-2,10,19,27-tetraaza-7,22-bistosylaza-3,26-dioxa[11.1 1]pyridinophane and 1,11,18,28-tetracarboxy-2,10,19,27-tetraaza-7,24-bistosylaza-3,20-dioxa[11.1 1]pyridinophane. These compds. showed inhibitory activity in a E. coli PLA2 assay. Prepn. of the libraries included the following steps: prepn. of compds. with a first functional group and a second functional group, blocking the first functional group, reacting the second functional group with a reagent pool of at least four compds., deblocking the first functional group, and reacting the deblocked compds. with a reagent.

 

Updated 5/9/2007 1:02:44 PM
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