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Patent No. 5076029

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Attorney: Johnston; George W.


Number of patents: 919
Last date: May 22, 2012

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NumberTitleIssue Date
81833802-aminoquinolines
The present invention is concerned with 2-aminoquinoline derivatives of formula I where R1, R2, R3, R4, R5, R6, A, and n are as defined in the specification ...
05/22/2012
8183262Pyridine derivatives as mGluR2 antagonists
The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R1, R
05/22/2012
8183254Inhibitors of JNK
The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I:
05/22/2012
8178689Tricyclic compounds
The present invention provides novel compounds of formula I, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the tre...
05/15/2012
8178583Compounds
The invention is concerned with compounds of formula I: wherein R, R2, and Q are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are useful as...
05/15/2012
8178538Pyridazinones
The present invention is concerned with novel pyridazinones of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologicall...
05/15/2012
8173652Isoxazole-isoxazoles and isoxazole-isothiazoles
The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for ...
05/08/2012
8163906Dihydroquinone and dihydronaphthridine inhibitors of JNK
Compounds of formula I are effective modulators of JNK: wherein X is CR11 or N; Y is —C(O)R3, 5-membered heteroaryl, or 5-membered heterocyclyl;
04/24/2012
8163793Proline derivatives
The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament. ...
04/24/2012
8163781Bi-aryl aminotetralines
The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1-R5, A, B, Q, W, and X are defined in the detailed description and claims...
04/24/2012
8163778Pyridines as FBPase inhibitors for treatment of diabetes
Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.
04/24/2012
81637406-substituted benzoxazines
The present invention is concerned with 6-substituted benzoxazine derivatives of formula (I) wherein X, Y, R1 and R2 are as described herein, their manufacture, and pharmaceutical compositions containi...
04/24/2012
8163728Pyrazoles
The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present inven...
04/24/2012
8158668Methods for treating CNS disorders with 4-imidazole derivatives
The present invention relates to methods for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, n...
04/17/2012
8158655Sulfonamide derivatives
The invention is concerned with the novel sulfonamide derivatives of formula (I) wherein A, R1 to R2″, X and Y are as defined in the description and in the claims, as well as physiologically acceptab...
04/17/2012
8153815Pseudoproline dipeptides
Disclosed is a process for the manufacture of pseudo proline dipeptides of the formula wherein R1 is a side chain of an alpha amino acid, R2 is an amino protecting group and R3 and R4
04/10/2012
8153805Biaryl derivatives
The invention is concerned with novel biaryl derivatives of formula (I), wherein m, R1, R2, R3, X1, X2 and X3 are...
04/10/2012
8153679Radiolabelled inhibitors of the glycine 1 transporter
The present invention relates to novel radiolabelled inhibitors of formula I for the Glycine 1 transporter (GlyT1), useful for the labelling and diagnostic imaging of the glycine 1 transporter functionality. wherein ...
04/10/2012
81536633-amino-indazole or 3-amino-4,5,6,7-tetrahydro-indazole derivatives
This invention relates to novel indazole derivatives of formula I: wherein R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compo...
04/10/2012
8153653Amido-tropane derivatives
The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by...
04/10/2012
8143442Preparation for a cyclohexanecarboxylic acid derivative and intermediates
A process for the preparation of a compound of formula (Ia): which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds. ...
03/27/2012
8143422Benzimidazole derivatives
The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and este...
03/27/2012
8143281Indoles
The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of ...
03/27/2012
8143280Glucocorticoid receptor antagonists
The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts t...
03/27/2012
8143273Quinolizidine and indolizidine derivatives
The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid add...
03/27/2012
8138208Aminotetrahydroindazoloacetic acids
The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, W, X, R1-R5 and n are defined in the detailed description and claims. In...
03/20/2012
8138189Substituted benzene compounds as modulators of the glucocorticoid receptor
The present invention relates to compounds of formula I wherein R.sup.1a to R.sup.1e and R.sup.2 to R.sup.5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are gluc...
03/20/2012
8138175Heterocyclyl compounds
The invention is concerned with novel heterocyclyl compounds of formula (I): wherein A, X, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p ...
03/20/2012
8134001Spiroindolinone derivatives
There are provided compounds of the formula and pharmaceutically acceptable salts and esters thereof wherein W, V, X, Y, A, R and R′ are as described herein. The compounds are useful as ant...
03/13/2012
8133979Antibodies against human angiopoietin 2
The present invention relates to antibodies against human Angiopoietin 2 (anti-ANG-2 antibodies), methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof. ...
03/13/2012
8133909Heteroaromatic monoamides as orexinin receptor antagonists
The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3, R4, R5, Ar, Ar1, Ar2, n, o and p are as described in the...
03/13/2012
8129423Imidazolone and imidazoloidinone derivatives as 11b-HSD1 inhibitors
Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositio...
03/06/2012
8124641Aminotetrahydroindazoloacetic acids
The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, R1-R3 and n are defined in the detailed description and claims. In addition, the present inven...
02/28/2012
8124636Imidazolidinone derivatives as 11B-HSD1 inhibitors
Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein A and R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical composition...
02/28/2012
8124629Naphthylacetic acids
The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 are defined in the detailed description and claims. In addi...
02/28/2012
8124604Inhibitors of bruton's tyrosine kinase
This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2′, Y3, Y
02/28/2012
8119636Pyrrolopyrazine kinase inhibitors
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-i...
02/21/2012
8097637Benzoyl-piperidine derivatives as dual modulators of the 5-HT2A and D3 receptors
The present invention relates to compounds of formula (I) wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their man...
01/17/2012
8097634Azacyclic derivatives
The invention provides novel compounds having the general formula (I) wherein R1, R2 and A are as described herein, compositions including the compounds and methods of using the compounds. The compound...
01/17/2012
8093385Leukotriene Binhibitors
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi...
01/10/2012
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