NZ505887A - Multi-binding compounds; useful as beta2-adrenergic receptor agonists - Google Patents

Multi-binding compounds; useful as beta2-adrenergic receptor agonists

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Publication number
NZ505887A
NZ505887A NZ505887A NZ50588799A NZ505887A NZ 505887 A NZ505887 A NZ 505887A NZ 505887 A NZ505887 A NZ 505887A NZ 50588799 A NZ50588799 A NZ 50588799A NZ 505887 A NZ505887 A NZ 505887A
Authority
NZ
New Zealand
Prior art keywords
binding compounds
adrenergic receptor
attached
ligands
receptor agonists
Prior art date
Application number
NZ505887A
Inventor
Edmund J Moran
Seok-Ki Choi
Original Assignee
Theravance Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Theravance Inc filed Critical Theravance Inc
Priority to NZ505887A priority Critical patent/NZ505887A/en
Priority claimed from PCT/US1999/011804 external-priority patent/WO1999064035A1/en
Publication of NZ505887A publication Critical patent/NZ505887A/en

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Abstract

A â2-adrenergic receptor agonist compound of formula II and its salts, wherein: Ar1 and Ar3 are aryl, heteroaryl or heterocyclyl; Ar2 is (a) phenylene, wherein W and X are attached at the 1,2-, 1,3- or 1,4-position of the ring; (b) cyclohexylene optionally substituted with methyl, wherein W and X are attached at the 1,3- or 1,4-position of the cyclohexylene ring; and (c) piperazinylene, wherein W and X are attached at the 1,4-positions of the piperazinylene ring; Q is -NHCH2CH(OH)-; W is alkylene or substituted alkylene; and X is a covalent bond. â2-adrenergic receptor agonists are multi-binding compounds of formula II that bind endothelin receptors are used to treat disorders affecting the cardiovascular, renal, endocrine and nervous systems in mammals that are mediated by the endothelin receptors, such as congestive heart failure, pulmonary hypertension, cerebral vasospasm following subarachnoid hemorrhage, essential hypertension, myocardial infarction, myocardial ischemia, unstable angina, restenosis, renal failure of ischemic origin, portal hypertension, cardiac hypertrophy, atherosclerosis, eclampsia, cerebrovascular disease, vascular disease, migraines, and auto-immune diseases, such as Morbus Wegener and Morbus Raynaud, to name a few. These multi-binding compounds (â2-adrenergic receptor agonists) comprise a plurality of ligands each of which can bind to such receptors thereby modulating the biological processes/functions thereof. Each of the ligands, which may be the same or different, is covalently attached to a linker or linkers which may be the same or different to provide for the multi-binding compound. The linker is selected such that the multi-binding compound so constructed demonstrates increased modulation of the biological processes mediated by the endothelin receptor than that provided by the ligands in monomeric form. The specification also discloses pharmaceutical compositions comprising the multi-binding compounds, methods of inhibiting and treating the disorders mediated by endothelin receptors, and methods of preparing these multi-binding compounds.
NZ505887A 1999-06-07 1999-06-07 Multi-binding compounds; useful as beta2-adrenergic receptor agonists NZ505887A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
NZ505887A NZ505887A (en) 1999-06-07 1999-06-07 Multi-binding compounds; useful as beta2-adrenergic receptor agonists

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
NZ505887A NZ505887A (en) 1999-06-07 1999-06-07 Multi-binding compounds; useful as beta2-adrenergic receptor agonists
PCT/US1999/011804 WO1999064035A1 (en) 1998-06-08 1999-06-07 β2-ADRENERGIC RECEPTOR AGONISTS

Publications (1)

Publication Number Publication Date
NZ505887A true NZ505887A (en) 2003-01-31

Family

ID=19928010

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ505887A NZ505887A (en) 1999-06-07 1999-06-07 Multi-binding compounds; useful as beta2-adrenergic receptor agonists

Country Status (1)

Country Link
NZ (1) NZ505887A (en)

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