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Attorney: Thies; J. Eric, Rose; David L.


Number of patents: 159
Last date: June 18, 2002

1        
NumberTitleIssue Date
6407255Chemical synthesis of 1,2,4-triazolinone derivative
The present invention relates to a process for the preparation of morpholine derivatives of formula (I) which are useful as a therapeutic agents. ##STR1##...
06/18/2002
6387388Pesticidal formulation
The present invention is directed to a pesticidal composition of a water-soluble pesticide and processes for its manufacture. More specifically, the invention relates to a soluble granule (SG) pesticidal formulation comprising a water-soluble pesticide an...
05/14/2002
6372764Pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: ##STR1## (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine ...
04/16/2002
6372754Spirocyclic ketones and their use as tachykinin antagonists
The present invention relates compounds of the formula (I): ##STR1## wherein R1, R2, R3, R4 and R5 represent a variety of substituents; R6 represents hydrogen, CORa, CO2 R
04/16/2002
6350915Process for the synthesis of 1-(3,5-bis(trifluoromethyl)-phenyl)ethan-1-one
The present invention is concerned with a novel process for the preparation of 1-(3,5-bis(trifluromethyl)phenyl)ethan-1-one (CAS 30071-93-3). This compound is useful as an intermediate in the synthesis of therapeutic agents....
02/26/2002
6348330Method for measuring human neurokinin-3 receptor ligand binding
A recombinant human neurokinin-3 receptor (hereinafter identified as human NK3R) is disclosed which has been prepared by polymerase chain reaction techniques. Also disclosed is the complete sequence of human NK3R complementary DNA; expression systems, inc...
02/19/2002
6329401Enhancement of sleep with a tachykinin antagonist
A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep....
12/11/2001
6319953Treatment of depression and anxiety with fluoxetine and an NK-1 receptor antagonist
The present invention relates to the treatment or prevention of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and fluoxetine....
11/20/2001
63035933-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: ##STR1## (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine ...
10/16/2001
6297376Chemical synthesis of morpholine derivatives
##STR1## The present invention relates to a process for the preparation of mopholine derivatives of formula (I) which are useful as a therapeutic agents....
10/02/2001
6274604Alteration of circadian rhythmicity with a tachykinin antagonist
A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep....
08/14/2001
6271230Use of NK-1 receptor antagonists for treating cognitive disorders
The present invention provides methods for the treatment or prevention of cognitive disorders which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK...
08/07/2001
6271347Eosinophil eotaxin receptor
The eosinophil eotaxin receptor has been isolated, cloned and sequenced. This receptor is a human ଲ-chemokine receptor and has been designated "CC CKR3". The eosinophil eotaxin receptor may be used to screen and identify compounds that bind to the e...
08/07/2001
6258943Human neurokinin-3 receptor
A recombinant human neurokinin-3 receptor (hereinafter identified as human NK3R) is disclosed which has been prepared by polymerase chain reaction techniques. Also disclosed is the complete sequence of human NK3R complementary DNA; expression systems, inc...
07/10/2001
6255545Process for the synthesis of 3,5-bis(trifluoromethyl)-bromobenzene
The present invention is concerned with a novel process for the preparation of 3,5-bis(trifluoromethyl)bromobenzene (CAS 328-70-1). This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity....
07/03/2001
6255550Stabilization of the reagent dimethyl titanocene
The present invention is directed to organic solutions of the reagent dimethyl titanocene which further comprise a sterically hindered ester and optionally titanocene dichloride. Stability of the reagent dimethyl titanocene is enhanced by the presence of ...
07/03/2001
6235735Morpholine and thiomorpholine tachykinin receptor antagonists
Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiov...
05/22/2001
6232311Method for treating or preventing psychosomatic and psychoimmunologic disorders
A tachykinin receptor antagonist is useful for treating or preventing a psychosomatic disorder in a patient....
05/15/2001
6229010Polymorphic form of a tachykinin receptor antagonist
This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in t...
05/08/2001
6225320Spiro-azacyclic derivatives and their use as therapeutic agents
Substituted spiro-azacyclic derivatives of structural formula I are tachykinin receptor antagonists of use, for example, in the treatment of pain, inflammation, migraine, emesis and posttherpetic neuralgia ##STR1## Wherein A is a pyridyl, X is --CH2--, Y ...
05/01/2001
6214846Substituted 3-(benzylamino)piperidine derivatives and their use as therapeutic agents
The present invention relates to compounds of formula (I), wherein R1 represents a fluoroC1-2 alkoxy group; and R2 represents a hydrogen or halogen atom or a C1-4 alkyl, C1-4 alkoxy, fluoroC1-4
04/10/2001
6211174Naphtho-fused lactams promote release of growth hormone
The present invention is directed to certain naphtho-fused lactams of the general structural formula: ##STR1## wherein and R1, R1a, R1b, R2a, R2b, R3a, R4, R5, R6...
04/03/2001
6180624Tachykinin antagonist and an opioid analgesic effective at treating pain or nociception
This invention relates to methods and compositions for treating pain and nociception in a patient by administering a combination of a morpholine or thiomorpholine tachykinin antagonist and an opioid analgesic....
01/30/2001
6177564Process for the synthesis of N-benzyl-3-(4-fluorophenyl)-1-4-oxazin-2-one
The present invention is concerned with a novel process for the preparation of N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one of the formula: ##STR1## This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological act...
01/23/2001
6172077Spiro-azacyclic derivatives and their use as therapeutic agents
The present invention is directed to substituted spiro-azacyclic derivatives of the formula (I): ##STR1## (wherein R1, R2, R3, R4, R5, R6, R9, R10, X, Y, p and q are d...
01/09/2001
6166037Pyrrolidine and piperidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R1, R2, R3, R4a, R4b, R4c, R4d, R4e, R4f,...
12/26/2000
6162805Use of an NK-1 receptor antagonist and an SSRI for treating obesity
The present invention relates to the use of an NK-1 receptor antagonist and a selective serotonin reuptake inhibitor for the treatment or prevention of obesity....
12/19/2000
6156749Use of NK-1 receptor antagonists for treating movement disorders
The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 antagonist for the manufacture of a medicament for oral administration for the treatment or prevention of movement disorders, methods of treatment using such a NK-...
12/05/2000
6140349Cyclic amine modulators of chemokine receptor activity
The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R1, R2, R3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compou...
10/31/2000
6140324Use of a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine to treat motion sickness
The present invention relates to the use of a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine for the treatment or prevention of motion sickness. There is also provided pharmaceutical compositions and products comprising a tachyk...
10/31/2000
6136827Cyclic amine modulations of chemokine receptor activity
The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R1, R2, R3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compou...
10/24/2000
61368241-piperidinyl-propan-2-derivatives and their use as therapeutic agents
The present invention relates compounds of the formula (I): ##STR1## wherein R1 and R2 each independently represents a phenyl group optionally substituted by a variety of substituents; R3 represents a variety of substituen...
10/24/2000
6130331Chemical synthesis of a chiral 1,4-oxazin-2-one
The present invention relates to a process for the preparation of substantially pure N-((S)-(-)-଱-methylbenzyl)-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one hydrochloride, which comprises selectively crystallising the (S,S)-diastereomer as the hydro...
10/10/2000
6127365Spiro-ketal derivatives and their use as therapeutic agents
The present invention is directed to compounds of the formula (I): ##STR1## (wherein R1, R2, R3, R4, R5, R6, R9a, R9b, m and n are as defined herein) which are tachyki...
10/03/2000
6123964Wet granulation formulation of a growth hormone secretagogue
The present invention relates to a pharmaceutical composition and a process for the preparation of a tablet containing a growth hormone secretagogue as the active ingredient. The tablet is prepared by forming a powder blend of the active ingredient N...
09/26/2000
61243193,3-disubstituted piperidines as modulators of chemokine receptor activity
The present invention is directed to 3,3-disubstituted piperidines of the formula I: ##STR1## (wherein X, Y, Z, Ar, R, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are ...
09/26/2000
6121325Naphthyl compounds promote release of growth hormone
The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R1, R1a, R2a, R3, R3a, R4, R5, R6, A, W, and n are as d...
09/19/2000
6121261Method for treating attention deficit disorder
A tachykinin receptor antagonist is useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity, in a patient....
09/19/2000
6117855Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent
The present invention relates to the treatment or prevention of depression and/or anxiety by the administration of a combination of CNS-penetrant NK-1 receptor antagonists and an antidepressant or anti-anxiety agent....
09/12/2000
6114315Use of NK-1 receptor antagonists for treating major depressive disorders with anxiety
The present invention provides methods for the treatment or prevention of major depressive disorder with anxiety without concomitant therapy with other anti-depressant or anti-anxiety agents which comprises oral administration of an orally active, long ac...
09/05/2000
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