US2005250790A1PendingUtilityA1
Novel sulfonic acid derivatives

Assignee: PFIZERPriority: Jun 20, 2001Filed: Jul 15, 2005Published: Nov 10, 2005
Est. expiryJun 20, 2021(expired)· nominal 20-yr term from priority
A61P 9/00A61P 9/10A61P 37/00A61P 37/08A61P 43/00A61P 37/06A61P 9/04A61P 37/02A61P 3/10A61P 9/08A61P 31/18A61P 31/00A61P 31/22A61P 35/00A61P 29/00A61P 25/00A61P 31/12A61P 33/06A61P 31/16A61P 27/02A61P 31/04A61P 11/00A61P 11/08A61P 19/00A61P 13/12A61P 11/06A61P 21/00A61P 19/02A61P 1/04A61P 1/16A61P 17/06A61P 17/00C07D 295/185C07B 2200/07C07D 213/64C07D 241/04
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Claims
Abstract

A compound of the formula or the pharmaceutically acceptable salt thereof; wherein X, Y, a, b, c, d, R 1 , R 2 , R 3 and R 5 are as defined above useful to treat inflammation and other immune disorders.
Claims

exact text as granted — not AI-modified
1 . A compound of the formula  
     
       
         
         
             
             
         
       
     
     or the pharmaceutically acceptable salts and prodrugs thereof; wherein 
 a=0-5,  
 b=0-2,  
 c=0-2  
 d=0-4  
 X is —O—, —S—, —CH 2 —, —NR 6 — 
 Y is (C 6 -C 10 )aryl, or (C 2 -C 9 )heteroaryl,  
 each R 1  is independently selected from the group consisting of: H—, HO—, halo-, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, NC—, H 2 N—, H 2 N—(C 1 -C 8 )alkyl-, HO—(C═O)—, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 2  and R 3  is independently selected from the group consisting of: H—, oxo, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 6 -C 10 )aryl-(C 1 -C 8 )alkyl-, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 2 -C 9 )heterocyclyl-(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C═O)—NH—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-SO 2 —NH—(C 1 -C 8 )alkyl-, (C 2 -C 9 )heteroaryl-(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 4  is independently selected from the group consisting of: H—, HO—, halo-, NC—, HO—(C═O)—, H 2 N—, (C 1 -C 8 )alkyl-NH—, [(C 1 -C 8 )alkyl] 2 N—, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH-(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 2 -Cg)heteroaryl-, (C 6 -C 10 )aryloxy-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C═O)—, (C 1 -C 8 )alkyl-NH—(C═O)—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C═O)—, [(C 1 -C 8 )alkyl] 2 —N—(C═O)—(C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 1 -C 8 )alkyl-SO 2 —, NC—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—, H 2 N—(C═O)—NH—, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-;  
 R 5  is (C 1 -C 8 )alkyl-.  
 
   
   
       2 - 25 . (canceled)  
   
   
       26 . A pharmaceutical composition for treating or preventing a disorder or condition selected from adult Respiratory Distress Syndrome, asthma, atopic dermatitis, chronic and acute organ transplant rejection, glomerulonephritis, Guillian-Barre, hepatitis, HIV-1, HIV-2, HIV-3, inflammatory bowel disease, influenza, ischemia reperfusion injury, leprosy, multiple sclerosis, optic neuritis, osteoarthritis, polymyalgia rheumatica, psoriasis, psoriatic arthritis, recent onset type I diabetes, Respiratory Distress Syndrome of infancy, rheumatoid arthritis, sarcoidosis, trauma, tuberculosis, uveitis, vasculitis in a mammal, comprising an amount of a compound of the formula  
     
       
         
         
             
             
         
       
     
     or the pharmaceutically acceptable salts thereof; wherein 
 a=0-5,  
 b=0-2,  
 c=0-2  
 d=0-4  
 X is —O— 
 Y is (C 6 -C 10 )aryl, or (C 2 -C 9 )heteroaryl,  
 each R 1  is independently selected from the group consisting of: H—, HO—, halo-, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, NC—, H 2 N—, H 2 N—(C 1 -C 8 )alkyl-, HO—(C═O)—, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 2  and R 3  is independently selected from the group consisting of: H—, oxo, (C 1 -C 8 )alkyl- substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 3 -C 8 )cycloalkyl-(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 6 -C 10 )aryl-(C 1 -C 8 )alkyl-, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 2 -C 9 )heterocyclyl-(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C═O)—NH—(C I—C 8 )alkyl-, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-SO 2 —NH—(C 1 -C 8 )alkyl-, (C 2 -Cg)heteroaryl-(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 4  is independently selected from the group consisting of: H—, HO—, halo-, NC—, HO—(C═O)—, H 2 N—, (C 1 -C 8 )alkyl-NH—, [(C 1 -C 8 )alkyl] 2 N—, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH-(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 2 -C 9 )heteroaryl-, (C 6 -C 10 )aryloxy-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C═O)—, (C 1 -C 8 )alkyl-NH—(C═O)—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C═O)—, [(C 1 -C 8 )alkyl] 2 —N—(C═O)—(C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 1 -C 8 )alkyl-SO 2 —, NC—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—, H 2 N—(C═O)—NH—, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-;  
 R 5  is (C 1 -C 8 )alkyl-,  
 that is effective in treating or preventing such disorders or conditions and a pharmaceutically acceptable carrier.  
 
   
   
       27 . A method for treating or preventing a disorder or condition selected from adult Respiratory Distress Syndrome, asthma, atopic dermatitis, chronic and acute organ transplant rejection, glomerulonephritis, Guillian-Barre, hepatitis, HIV-1, HIV-2, HIV-3, inflammatory bowel disease, influenza, ischemia reperfusion injury, leprosy, multiple sclerosis, optic neuritis, osteoarthritis, polymyalgia rheumatica, psoriasis, psoriatic arthritis, recent onset type I diabetes, Respiratory Distress Syndrome of infancy, rheumatoid arthritis, sarcoidosis, trauma, tuberculosis, uveitis, vasculitis in a mammal, comprising administering to a mammal an amount of a compound of the formula  
     
       
         
         
             
             
         
       
     
     or the pharmaceutically acceptable salts thereof; wherein 
 a=0-5,  
 b=0-2,  
 c=0-2  
 d=0-4  
 X is —O— 
 Y is (C 6 -C 10 )aryl, or (C 2 -C 9 )heteroaryl,  
 each R 1  is independently selected from the group consisting of: H—, HO—, halo-, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, NC—, H 2 N—, H 2 N—(C 1 -C 8 )alkyl-, HO—(C═O)—, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 2  and R 3  is independently selected from the group consisting of: H—, oxo, (C 1 -C 8 )alkyl- substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 3 -C 8 )cycloalkyl-(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 6 -C 10 )aryl-(C 1 -C 8 )alkyl-, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 2 -C 9 )heterocyclyl-(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C═O)—NH—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-SO 2 —NH—(C 1 -C 8 )alkyl-, (C 2 -Cg)heteroaryl-(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 4  is independently selected from the group consisting of: H—, HO—, halo-, NC—, HO—(C═O)—, H 2 N—, (C 1 -C 8 )alkyl-NH—, [(C 1 -C 8 )alkyl] 2 N—, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH-(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 2 -Cg)heteroaryl-, (C 6 -C 10 )aryloxy-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C═O)—, (C 1 -C 8 )alkyl-NH—(C═O)—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C═O)—, [(C 1 -C 8 )alkyl] 2 —N—(C═O)—(C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 1 -C 8 )alkyl-SO 2 —, NC—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—, H 2 N—(C═O)—NH—, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-;  
 R 5  is (C 1 -C 8 )alkyl-,  
 that is effective in treating or preventing such disorders or conditions.  
 
   
   
       28 . A pharmaceutical composition for treating or preventing a disorder or condition that can be treated or prevented by antagonizing the CCR1 receptor in a mammal selected from adult Respiratory Distress Syndrome, asthma, atopic dermatitis, chronic and acute organ transplant rejection, glomerulonephritis, Guillian-Barre, hepatitis, HIV-1, HIV-2, HIV-3, inflammatory bowel disease, influenza, ischemia reperfusion injury, leprosy, multiple sclerosis, optic neuritis, osteoarthritis, polymyalgia rheumatica, psoriasis, psoriatic arthritis, recent onset type I diabetes, Respiratory Distress Syndrome of infancy, rheumatoid arthritis, sarcoidosis, trauma, tuberculosis, uveitis, vasculitis in a mammal, comprising a CCR1 receptor antagonizing effective amount of a compound of the formula  
     
       
         
         
             
             
         
       
     
     or the pharmaceutically acceptable salts thereof; wherein 
 a=0-5,  
 b=0-2,  
 c=0-2  
 d=0-4  
 X is —O— 
 Y is (C 6 -C 10 )aryl, or (C 2 -C 9 )heteroaryl,  
 each R 1  is independently selected from the group consisting of: H—, HO—, halo-, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, NC—, H 2 N—, H 2 N—(C 1 -C 8 )alkyl-, HO—(C═O)—, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 2  and R 3  is independently selected from the group consisting of: H—, oxo, (C 1 -C 8 )alkyl- substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 3 -C 8 )cycloalkyl-(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 6 -C 10 )aryl-(C 1 -C 8 )alkyl-, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 2 -C 9 )heterocyclyl-(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C═O)—NH—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-SO 2 —NH—(C I—C 8 )alkyl-, (C 2 -C 9 )heteroaryl-(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 4  is independently selected from the group consisting of: H—, HO—, halo-, NC—, HO—(C═O)—, H 2 N—, (C 1 -C 8 )alkyl-NH—, [(C 1 -C 8 )alkyl] 2 N—, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 2 -Cg)heteroaryl-, (C 6 -C 10 )aryloxy-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C═O)—, (C 1 -C 8 )alkyl-NH—(C═O)—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C═O)—, [(C 1 -C 8 )alkyl] 2 —N—(C═O)—(C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 1 -C 8 )alkyl-SO 2 —, NC—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—, H 2 N—(C═O)—NH—, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-;  
 R 5  is (C 1 -C 8 )alkyl-,  
 and a pharmaceutically acceptable carrier.  
 
   
   
       29 . A method for treating or preventing a disorder or condition selected from adult Respiratory Distress Syndrome, asthma, atopic dermatitis, chronic and acute organ transplant rejection, glomerulonephritis, Guillian-Barre, hepatitis, HIV-1, HIV-2, HIV-3, inflammatory bowel disease, influenza, ischemia reperfusion injury, leprosy, multiple sclerosis, optic neuritis, osteoarthritis, polymyalgia rheumatica, psoriasis, psoriatic arthritis, recent onset type I diabetes, Respiratory Distress Syndrome of infancy, rheumatoid arthritis, sarcoidosis, trauma, tuberculosis, uveitis, vasculitis in a mammal, comprising administering to a mammal in need of such treatment or prevention a CCR1 receptor antagonizing effective amount of a compound of the formula  
     
       
         
         
             
             
         
       
     
     or the pharmaceutically acceptable salts thereof; wherein 
 a=0-5,  
 b=0-2,  
 c=0-2  
 d=0-4  
 X is —O— 
 Y is (C 6 -C 10 )aryl, or (C 2 -C 9 )heteroaryl,  
 each R 1  is independently selected from the group consisting of: H—, HO—, halo-, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, NC—, H 2 N—, H 2 N—(C 1 -C 8 )alkyl-, HO—(C═O)—, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 2  and R 3  is independently selected from the group consisting of: H—, oxo, (C 1 -C 8 )alkyl- substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-, (C 3 -Cg)cycloalkyl-, (C 3 -C 8 )cycloalkyl-(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 6 -C 10 )aryl-(C 1 -C 8 )alkyl-, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 2 -C 9 )heterocyclyl-(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C═O)—NH—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-SO 2 —NH—(C 1 -C 8 )alkyl-, (C 2 -C 9 )heteroaryl-(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 4  is independently selected from the group consisting of: H—, HO—, halo-, NC—, HO—(C═O)—, H 2 N—, (C 1 -C 8 )alkyl-NH—, [(C 1 -C 8 )alkyl] 2 N—, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH-(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 2 -C 9 )heteroaryl-, (C 6 -C 10 )aryloxy-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C═O)—, (C 1 -C 8 )alkyl-NH—(C═O)—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C═O)—, [(C 1 -C 8 )alkyl] 2 —N—(C═O)—(C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 1 -C 8 )alkyl-SO 2 —, NC—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—, H 2 N—(C═O)—NH—, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-;  
 R 5  is (C 1 -C 8 )alkyl-.  
 
   
   
       30 . A method for treating or preventing a disorder or condition selected from autoimmune diseases, lupus, acute and chronic inflammatory conditions, allergic conditions, infection associated with inflammation, viral, chronic bronchitis, xeno-transplantation, transplantation tissue rejection, atherosclerosis, restenosis, HIV infectivity, and granulomatous in a mammal, comprising administering to a mammal in need of such treatment or prevention a CCR1 receptor antagonizing effective amount of a compound of the formula  
     
       
         
         
             
             
         
       
     
     or the pharmaceutically acceptable salts thereof; wherein 
 a=0-5,  
 b=0-2,  
 c=0-2  
 d=0-4  
 X is —O— 
 Y is (C 6 -C 10 )aryl, or (C 2 -C 9 )heteroaryl,  
 each R 1  is independently selected from the group consisting of: H—, HO—, halo-, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, NC—, H 2 N—, H 2 N—(C 1 -C 8 )alkyl-, HO—(C═O)—, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 2  and R 3  is independently selected from the group consisting of: H—, oxo, (C 1 -C 8 )alkyl- substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 3 -C 8 )cycloalkyl-(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 6 -C 10 )aryl-(C 1 -C 8 )alkyl-, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 2 -C 9 )heterocyclyl-(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C═O)—NH—(C 1 -C 8 )alkyl-, H 2 N—(C═O)—NH—(C—C 8 )alkyl-, (C—C 8 )alkyl-SO 2 —NH—(C 1 -C 8 )alkyl-, (C 2 -C 9 )heteroaryl-(C 1 -C 8 )alkyl-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-;  
 each R 4  is independently selected from the group consisting of: H—, HO—, halo-, NC—, HO—(C═O)—, H 2 N—, (C 1 -C 8 )alkyl-NH—, [(C 1 -C 8 )alkyl] 2 N—, (C 1 -C 8 )alkyl- optionally substituted with 1-3 fluorine atoms, (C 1 -C 8 )alkyl-O— wherein the alkyl group is optionally substituted with 1-3 fluorine atoms, HO—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-O—(C 1 -C 8 )alkyl-, H 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH-(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—, (C 1 -C 8 )alkyl-(C═O)—(C 1 -C 8 )alkyl-, (C 6 -C 10 )aryl-, (C 2 -Cg)heteroaryl-, (C 6 -C 10 )aryloxy-, H 2 N—(C═O)—, H 2 N—(C═O)—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-NH—(C═O)—, (C 1 -C 8 )alkyl-NH—(C═O)—(C 1 -C 8 )alkyl-, [(C 1 -C 8 )alkyl] 2 N—(C═O)—, [(C 1 -C 8 )alkyl] 2 —N—(C═O)—(C 1 -C 8 )alkyl-, (C 3 -C 8 )cycloalkyl-, (C 1 -C 8 )alkyl-SO 2 —, NC—(C 1 -C 8 )alkyl-, (C 1 -C 8 )alkyl-(C═O)—NH—, H 2 N—(C═O)—NH—, H 2 N—(C═O)—NH—(C 1 -C 8 )alkyl-;  
 R 5  is (C 1 -C 8 )alkyl-.
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