Patent number: 6716840
Abstract: Compounds having the general structure I are provided:
X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of
and L is selected from the group consisting of N, O, S, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r”) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
Type:
Grant
Filed:
April 8, 2002
Date of Patent:
April 6, 2004
Assignee:
Chiron Corporation
Inventors:
Daniel Chu, Rustum S. Boyce, David Duhl, Bryan H. Chang
Patent number: 6653305
Abstract: A compound of formula (I)
wherein:
Ra is a benzyl or 1-phenylethyl group or a phenyl group substituted by the groups R1 and R2, wherein:
R1 is a hydrogen, fluorine, chlorine, or bromine atom, or a methyl, trifluoromethyl, cyano, or ethynyl group, and
R2 is a hydrogen or fluorine atom;
Rb is an R3O—CO—CH2—N—CH2—CH2—OH group optionally substituted at the methylene groups by 1 or 2 methyl or ethyl groups, wherein R3 is a hydrogen atom or a C1-4-alkyl group, a 2-oxomorpholin-4-yl group optionally substituted by 1 or 2 methyl or ethyl groups, or a N-[(1,3-dioxolan-2-yl)methyl]methylamino group;
Rc is a hydrogen atom, or a methoxy, ethoxy, 2-methoxyethoxy, 2-ethoxyethoxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, cyclopropylmethoxy, cyclobutylmethoxy, cyclopentylmethoxy, cyclohexylmethoxy, tetrahydrofuran-3-yloxy, tetrahydropyran-3-yloxy, tetrahydropyran-4-yloxy, tetrahydrofuranylmethoxy, or tetrahydropyranylmethoxy group; and
n is 1, 2, or 3
Type:
Grant
Filed:
August 15, 2001
Date of Patent:
November 25, 2003
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca