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Attorney: Eck; Steven R.


Number of patents: 128
Last date: November 15, 2011

1        
NumberTitleIssue Date
8058278Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes
The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium channel blocker as defined herein and an osmolyte to a subject to a ...
11/15/2011
7981898Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes
The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium channel blocker as defined herein and an osmolyte to a subject to a ...
07/19/2011
7423054Therapeutic pyrazolo[3,4-b]pyridines and indazoles
The present invention provides for compounds of Formula I: wherein R2, R3, R4, R5, R6, R7, X, and L have any of the values defined in the specification, and ...
09/09/2008
7411001Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids
The present invention relates to oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof. The present invention also relates to crystalline forms of oxygenated esters of 4-iodophenylamino benzhyd...
08/12/2008
7407956Benzamide inhibitors of the P2Xreceptor
The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment of IL...
08/05/2008
7235549Benzamide, heteroarylamide and reverse amides
The present invention relates to novel to P2X7 inhibitors of formula I and to processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them, an...
06/26/2007
7235657Methods for preparing P2X inhibitors
The present invention relates to the methods for preparing compounds of the formula I: or the pharmaceutically acceptable salts thereof, wherein R1, R2, R4, R10, and R
06/26/2007
7232915Process for the synthesis of 1,3-diols
An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane spe...
06/19/2007
7232930Compounds and methods for preparing methanesulfonamides
A process for preparing (S)-(−)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4-[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide(IIa) with fluoroamine (III) in the pre...
06/19/2007
7196208Processes for preparing 7-carboxy substituted steroids
This invention relates to processes for the preparation of 7-carboxy substituted steroid compounds of Formula I, wherein R1 is selected from H or COR4; R4 is C
03/27/2007
7132437Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension
Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component...
11/07/2006
7119094Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a varie...
10/10/2006
70227112-(4-Pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones
This invention provides antiangiogenic compounds of the Formula (I), which are useful for treating diseases, resulting from uncontrolled cellular proliferation such as cancer, atherosclerosis, rheumatoid arthritis, and psoriasis. ...
04/04/2006
70020285-androsten-3β-ol steroid intermediates and processes for their preparation
The present invention provides 5-androsten-3β-ol steroid intermediates and processes for their preparation. ...
02/21/2006
6974813N-[(substituted five-membered di-or triaza diunsaturated ring) carbonyl] guanidine derivatives for the treatment of ischemia
NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia. ...
12/13/2005
6974812Benzamide inhibitors of the P2X7 Ereceptor
The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment ...
12/13/2005
6960662Process for preparing 2-(4-pyridyl)amino-6-dialkyloxyphenyl-pyrido[2,3-d]pyrimidin-7-ones
The present invention relates to a process for preparing 2-(pyridin-4-ylamino-pyrido [2,3-d]pyrimidine of Formula II by reacting a 4-aminopyridine of the formula with a 2...
11/01/2005
6942876Analgesic compositions comprising anti-epileptic compounds and methods of using same
The present invention is directed to novel combinations of anti-epileptic compounds that demonstrate pain alleviating properties, with compounds selected from the group consisting of analgesics, NMDA receptor antagonists, and NSAIDs and pharmaceutical compositions c...
09/13/2005
6927219N-alkyl-adamantyl triazinyl benzamide derivatives
The present invention relates to novel to N-alkyl adamantyl triazinyl benzylamide derivatives of formmula I: and to processs for their preparation, intermediates useful in their preparation, pharmaceutical compositions...
08/09/2005
6916807Triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as ...
07/12/2005
6841671Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said “A” is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutica...
01/11/2005
68219634-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors
Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical,...
11/23/2004
6395762Phenyl amino squarate and thiadiazole dioxide beta-3 adrenergic receptor agonists
This invention provides compounds of Formula I having the structure ##STR1## wherein, ##STR2## R1, R2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting ...
05/28/2002
6391897Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides substituted compounds of the general formulae: ##STR1## wherein B and E are C or N; D, G and W are O, S, or N; or salt forms thereof, and methods and pharmaceutical compositions for their use in treating disorders related to insuli...
05/21/2002
63727452,3,4,4A-tetrahydro-1H-pyrazino[1,2-A]quinoxalin-5(6H)one derivatives
This invention provides compounds of formula I, ##STR1## wherein R is hydrogen or alkyl of 1-6 carbon atoms; R' is hydrogen, alkyl of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each,...
04/16/2002
6369072Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides substituted compounds of the general formulae: ##STR1## wherein B and E are C or N; D, G and W are O, S, or N; or salt forms thereof, and methods and pharmaceutical compositions for their use in treating disorders related to insuli...
04/09/2002
6352718Vasopressin antagonist formulation and process
This invention provides novel formulations for N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)ylcarbonyl)-3-chloropheny l]-5-fluoro-2-methyl-benzamide, or a pharmaceutically acceptable salt thereof, and processes for making them, the formulations compris...
03/05/2002
6350773Therapeutic combinations of (S)-2-(benzylamino-methyl)-2,3,8,9,-tetrahydro 7H-1,4-dioxino{2,3-e}indol-8-one and neuroleptics for the treatment or prevention of psychotic disorders
Therapeutic combinations useful in the treatment or prevention of psychotic disorders, to pharmaceutical compositions containing said combinations, and to their use in the treatment or prophylaxis of prevention disorders are provided....
02/26/2002
6348486Methods for modulating bladder function
This invention provides methods and pharmaceutical compositions for maintaining bladder control or treating urinary incontinence in a mammal utilizing agonists of KCNQ potassium channels, including KCNQ2, KCNQ3, KCNQ4 and KCNQ5 potassium channels, alone o...
02/19/2002
6344451Pyrrolobenzodiazepine carboxyamide vasopressin agonists
The present invention provides compounds of the formula: ##STR1## wherein: X, Y and Z are independently selected from O, S, CH, CH2, N, or NR4 ; W is moiety selected from (CH2)n ; n=1-2; R1, R2 ...
02/05/2002
63406764-aryl-1-oxa-9-thia-cyclopenta (b) fluorenes
This invention provides compounds of Formula I having the structure ##STR1## wherein B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atom...
01/22/2002
63263672-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures...
12/04/2001
6310081Biphenyl sulfonyl aryl carboxylic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides compounds of Formula I having the structure ##STR1## wherein A, Q, R3, and R4 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to i...
10/30/2001
6297234Arylthiophene vasopressin agonists
The present invention provides compounds of the general formula: ##STR1## wherein Y is a moiety selected independently, from NH or --(CH2)n -- wherein n is 1; m is an integer from 1 to 2; and the moiety ##STR2## represents: (1) a 5-m...
10/02/2001
6288100Benzimidazole derivatives
Disclosed herein are compounds of formula I or II: ##STR1## wherein R is alkyl phenyl or substituted phenyl; R2 is hydrogen, halogen, alkoxy or alkyl; R1 is hydrogen, alkyl, aryl, arylalkyl, or substituted benzyl; or a pharmaceutically accepta...
09/11/2001
62812384-aryl-1-oxa-9-thia-cylopenta[B]fluorenes
This invention provides compounds of Formula I having the structure ##STR1## wherein B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atom...
08/28/2001
6268504Aryloxy-alkyl-dialkylamines
The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: ##STR1## wherein: R1 and R2 are, independently, selected from H;...
07/31/2001
62683601H-pyrido[2,3-b][1,5]benzodiazipine vasopressin agonists
The present invention provides compounds of the general formula: ##STR1## wherein Y is a moiety selected independently, from NH or --(CH2)n -- wherein n is 1; m is an integer from 1 to 2; and the moiety ##STR2## represents: (1) a 5-m...
07/31/2001
6242605Aryloxy-alkyl-dialkylamines
The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: ##STR1## wherein: R1 and R2 are, independently, selected from H;...
06/05/2001
6235900Tricyclic pyridine N-oxides vasopressin agonists
The present invention provides compounds of the general formula: ##STR1## as well as methods and pharmaceutical compositions utilizing these compounds for the inducement of temporary delay of urination or the treatment of disorders which may be remedied o...
05/22/2001
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