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Attorney: Magatti; Anita W.


Number of patents: 119
Last date: June 22, 2010

1      
NumberTitleIssue Date
7741318Pyrazolo [1,5-A]pyrimidine adenosine Areceptor antagonists
Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S...
06/22/2010
7709492Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A receptor antagonists
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or...
05/04/2010
7511062Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl...
03/31/2009
7300941Non-imidazole compounds
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such ...
11/27/2007
7220735Benzimidazolone histamine Hantagonists
Disclosed are novel compounds of the formula wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally s...
05/22/2007
7098213CCR5 antagonists useful for treating AIDS
Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13...
08/29/2006
7094784High affinity ligands for nociceptin receptor ORL-1
Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1
08/22/2006
7078408[1,2,4]-Triazole bicyclic adenosine A2a receptor antagonists
Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1–C6)-alkyl, halo,...
07/18/2006
7067655Adenosine A2a receptor antagonists
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2
06/27/2006
7060701CCR5 antagonists useful for treating AIDS
Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13...
06/13/2006
7049320NKantagonists
A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R...
05/23/2006
7041666Adenosine A2a receptor antagonists
Disclosed are compounds having the structural formula or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted ...
05/09/2006
7008946CCR5 antagonists useful for treating AIDS
Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13 ...
03/07/2006
6951871Indole derivatives useful as histamine H3 antagonists
Disclosed are novel compounds of the formula wherein M1 is CH or N and M2 is C(R3) or N; R1 is optionally substituted indolyl or an aza derivative thereof; R2 is o...
10/04/2005
6916811Adenosine A2a receptor antagonists
Disclosed herein are compounds having the structural formula A including pharmaceutically acceptable salts or solvates of said compound, wherein X, Y, Q and R are as defined in the specification; pharmaceutical composi...
07/12/2005
6906081Use of dual H3/M2 antagonists in the treatment of cognition deficit disorders
This invention relates to a method of treating cognition deficit disorders comprising administering to a mammal in need of such treatment an effective amount of a dual histamine H3 receptor antagonist/m2 muscarinic antagonist, or a combination ...
06/14/2005
6903123Azetidinyl diamines useful as ligands of the nociceptin receptor ORL-1
Disclosed are nociceptin ORL-1 receptor agonists of the formula wherein: (a) R1 is optionally substituted alkyl, fluorenyl, pyrimidinyl or optionally substituted piperidinyl;
06/07/2005
6900211CCR5 antagonists useful for treating aids
Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4-R7 and R13 a...
05/31/2005
6897216Adenosine A2a receptor antagonists
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is...
05/24/2005
68972172-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2
05/24/2005
6875772[1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists
Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1
04/05/2005
6849621Piperidine compounds
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, fo...
02/01/2005
6727254Heteroaryl tropane derivatives as superior ligands for nociceptin receptor ORL-1
Novel compounds of the formula wherein R is optionally substituted heteroaryl or R1 is H or C1-C6 alkyl; and R2 and ...
04/27/2004
6720325CCR5 antagonists useful for treating aids
Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4—R7 and R13 are H or alkyl; R1 is...
04/13/2004
6720328Non-imidazole compounds
Disclosed are novel compounds of the formula In Formula I, M1 is carbon, M2, M3 and M4 are carbon or nitrogen and the remaining variables are as defined in the specification. A...
04/13/2004
6689765Piperazine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted hete...
02/10/2004
6653315Adenosine A2a receptor antagonists
Compounds having the structural formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl or heteroaryl, cycloalkenyl, --C(.dbd.CH2)CH3, --C.ident.C--CH3, --CH.dbd.C(C...
11/25/2003
6645987Nor-seco himbacine derivatives useful as thrombin receptor antagonists
Heterocyclic-substituted compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, are disclosed....
11/11/2003
6635630Selective neurokinin antagonists
Compound represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is --O--, --S--, --SO--, ...
10/21/2003
6632828Substituted imidazole neuropeptide Y Y5 receptor antagonists
Compounds of the formula I ##STR1## or a pharmaceutically acceptable salt, solvate or N-oxide thereof, wherein X is .dbd.CH-- or .dbd.N--; Y is H, halogen, trihaloalkyl, alkyl, alkenyl, cycloalkyl, cycloalkyl, SH, --S-alkyl, or --CN. R is alkyl, --...
10/14/2003
6630475Adenosine A2a receptor antagonists
Compounds having the structural formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or --C(O)CH2 --; Y is --N(R2)CH2 CH...
10/07/2003
6602885Piperidine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein ##STR2## R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substitut...
08/05/2003
6534502Substituted oximes and hydrazones as neurokinin antagonists
Compound represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or --OR6 ; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, --C(O...
03/18/2003
6498168Muscarinic antagonists
Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R1, R2, R3, R4, R21, R...
12/24/2002
6472394MCH antagonists and their use in the treatment of obesity
Disclosed are compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt, ester or solvate thereof, wherein W is R1 --CR3 R12 NR4 C(O)-- or R11 C(O)NR4 --; the...
10/29/2002
6458812Muscarinic antagonists
Amide derivatives of 1,4 di-substituted piperidine compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, ester or solvate thereof, wherein R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroar...
10/01/2002
6455527High affinity ligands for nociceptin receptor ORL-1
Novel compounds of the formula ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X
09/24/2002
6451797Muscarinic antagonists
Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts and solvates) ##STR1## wherein wherein one of Y and Z is --N-- and the other is --N-- or --CH--; ...
09/17/2002
6444687Substituted imidazole neuropeptide Y Y5 receptor antagonists
Compounds of the formula I ##STR1## or a pharmaceutically acceptable salt, solvate or N-oxide thereof, wherein X is .dbd.CH-- or .dbd.N--; Y is H, halogen, trihaloalkyl, alkyl, alkenyl, cycloalkyl, cycloalkyl, SH, --S-alkyl, or --CN. R is alkyl, --CF3
09/03/2002
6436928Selective neurokinin antagonists
A compound represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is --O--, --SO0-2
08/20/2002
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