Abstract
A series of 10 closely related patent applications define Theravance’s approach to the development of long-acting M3 selective antagonists for the treatment of chronic obstructive pulmonary disease. The applications illustrate a modular approach to the design of such agents, comprising a muscarinic pharmacophore attached to a second, less functionalised moiety via a variable length spacer incorporating heteroatoms. Eight of the applications utilise a a 4-piperidinylester of biphenylcarbamic acid as the muscarinic pharmacophore and two utilise 2,2-diphenyl-2-(S)-pyrrolidin-3-ylacetamide. The first group of eight applications encompasses the use of two tail groups and four different sets of linking groups, whereas the second uses two very different tail groups and different spacers.
Patent Details
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Mu Y, Malathong V.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203083
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Mu Y, Stangeland EL, Kushner A, Husfeld C.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203131
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Mu Y.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203132
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Mu Y, Husfeld C, Li L.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203133
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Mu Y.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203134
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Husfeld C.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203137
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Mu Y, Husfeld C, Li L.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203138
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Mu Y, Mischki T, Malathong V.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203139
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Dunham S, Li L.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203161
Title Long-acting muscarinic M3 receptor antagonists
Assignee Theravance Inc.
Inventors Mammen M, Ji Y-H, Chen Y, Husfeld C.
Priority date 11/03/04
Filing date 10/03/05
Publication date 15/09/05
Publication no. US20050203167