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Class 544/262 - The other cyclo in the bicyclo ring system is five-membered


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein a five-membered ring is the other cyclo
No. of applications: 263
Last issue date: 05/24/2012


1              
Application No.Application TitleIssue Date
20120129852AZAINDAZOLES AS KINASE INHIBITORS AND USE THEREOF
Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, (I) are useful as kinase modulators, including Btk modulation, wherein A1, A2, A3, R4 are as defined herein.

...
05/24/2012
20120129873INHIBITORS OF BRUTON'S TYROSINE KINASE
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the co...
05/24/2012
20120108612INHIBITORS OF BRUTON'S TYROSINE KINASE
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the co...
05/03/2012
20120108604PROCESSES FOR PREPARING AMINE SALTS OF SILDENAFIL-ANALOGUES AND USE THEREOF
A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R1, Ra and RX are as defined in the specification. The amine complex salts disclosed in the present invention are character...
05/03/2012
20120083502HETEROCYCLIC COMPOUNDS AND THEIR USES
Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, ...
04/05/2012
20120071490P70 S6 KINASE INHIBITORS
The present invention provides p70 S6 kinase inhibitors of the formula:

pharmaceutical formulations comprising them, and methods for their use....

03/22/2012
20120053189BTK INHIBITORS FOR THE TREATMENT OF IMMUNE MEDIATED CONDITIONS
Disclosed herein are pharmaceutical dosage forms of Brutons tyrosine kinase (Btk) inhibitors. Methods for the preparation of the compounds are disclosed. Methods of using the pharmaceutical dosage forms are disclosed for the treatment of immune mediated conditions and i...
03/01/2012
20120041004FUSED PYRIMIDINE-DIONE DERIVATIVES AS TRPAI MODULATORS
The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions a...
02/16/2012
20120015963NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
The present disclosure is directed to novel compounds of Formula (I)

pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are ...

01/19/2012
201200102246-CYCLYLMETHYL-AND 6-ALKYLMETHYL-SUBSTITUTED PYRAZOLEPYRIMIDINES
The invention relates to novel 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines, process for their preparation and their use for producing medicaments for improving perception, concentration, learning and/or memory....
01/12/2012
20120009152NITRIC OXIDE DONORS FOR TREATMENT OF DISEASE AND INJURY
A method of promoting neurogenesis by administering a therapeutic amount of a phosphodiesterase inhibitor compound to a patient in need of neurogenesis promotion. A compound for providing neurogenesis having an effective amount of a phosphodiesterase inhibitor sufficien...
01/12/2012
20110312908SMALL MOLECULE MYRISTATE INHIBITORS OF BCR-ABL AND METHODS OF USE
The present invention provides novel heteroaryl compounds that are linked to an aryl group via an amine linker. Such compounds are useful for the treatment of cancers....
12/22/2011
20110306762ACID ADDITION SALT OF UDENAFIL, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
The present invention provides an acid addition salt of Udenafil, a preparation method thereof and a pharmaceutical composition comprising the same. The acid addition salt of Udenafil in which Udenafil is bonded to an organic acid selected from the group consisting of o...
12/15/2011
20110301144Kinase Antagonists
The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tyrosine kinase, PI3 kinase and mTOR, or PI33 kinase, mTOR and tyrosine kinase....
12/08/2011
20110281821Modulators of Mitotic Kinases
The invention relates to compounds of Formula (I), a polymorph, an enantiomer, a stereoisomer, a solvate, an N-oxide derivative, or a pharmaceutically acceptable salt thereof: Formula (I), which have inhibitory effect on one or more protein kinases that are involved in ...
11/17/2011
20110281832ORGANIC COMPOUNDS
Optionally substituted (5- or 7-amino)-3,4-dihydro-(optionally 4-oxo, 4-thioxo or 4-imino)-1H-pyrrolo[3,4-d]pyrimidin-2(6H)-ones, Compounds of Formula I, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them....
11/17/2011
20110281866HETEROCYCLIC KINASE INHIBITORS
The present invention provides heterocyclic compounds for use as kinase inhibitors and in other applications. Also provided are pharmaceutical compositions and methods of treatments of diseases and conditions associated with P13 kinase activity....
11/17/2011
20110275651FUSED RING HETEROARYL KINASE INHIBITORS
Provided herein are fused ring heteroaryl compounds useful in a variety of methods, including reducing the activity of certain kinases and treating certain disease states....
11/10/2011
20110263559INDAZOLE COMPOUNDS USEFUL AS KETOHEXOKINASE INHIBITORS
The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated...
10/27/2011
20110257203INHIBITORS OF BRUTON'S TYROSINE KINASE
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the co...
10/20/2011
20110230476PI3 KINASE INHIBITORS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same....
09/22/2011
20110212960NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDER
The invention relates to novel pyrazolopyrimidinones according to formula (I).

The new compounds shall be used for the manufacture of medicaments, in particular medicaments for the treatment of conditions con...

09/01/2011
201101840001-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D] PYRIMIDIN-4-ONE DERIVATES AND THEIR USE AS PDE9A MODULATORS
The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, Formula (I) with is a mono-, bi- or tri-cyclic heterocyclyl group, the ring members of which are carbon atoms and at least 1, preferably 1, 2 or 3, heteroatom(s), which are selected from the group o...
07/28/2011
20110184001INHIBITORS OF BRUTON'S TYROSINE KINASE
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the co...
07/28/2011
20110172216PYRAZOLOPYRIMIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders su...
07/14/2011
20110172228KINASE INHIBITORS AND METHODS OF USE
The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention a...
07/14/2011
20110166165BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a c...
07/07/2011
201101651183-HETEROCYCLIC SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF
The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral i...
07/07/2011
20110160222MODULATORS OF GLUCOSE HOMEOSTASIS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS
Aryl 119 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control....
06/30/2011
20110152277HETEROCYCLIC COMPOUNDS AND THEIR USES
Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, ...
06/23/2011
20110144134Anti-Inflammatory Pyrazolopyrimndines
The present invention provides anti-inflammatory compounds useful in the treatment of diseases and conditions in which inflammation is involved in disease progression or the manifestation of symptoms of the disease or condition....
06/16/2011
20110135668COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibiti...
06/09/2011
20110130397PYRROLINONE COMPOUNDS AS INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF
Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods...
06/02/2011
20110124641BENZOTHIAZOLE KINASE INHIBITORS AND METHODS OF USE
The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PI3 kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of ...
05/26/2011
20110118286BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS GPCR MODULATORS
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, ...
05/19/2011
20110112077Quinolizidinone m1 Receptor Positive Allosteric Modulators
The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders....
05/12/2011
20110086866INHIBITORS OF BRUTON'S TYROSINE KINASE
Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein,...
04/14/2011
20110082137NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS
The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I),

in which Hc is a tetrahydropyranyl-group and R1 is the group V—W−*, whereby V and W independently of each ...

04/07/2011
20110065918NEW PHENYLALANINE DERIVATIVES
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.

...

03/17/2011
201100657306-CYCLYLMETHYL-AND 6-ALKYLMETHYL-SUBSTITUTED PYRAZOLEPYRIMIDINES
The invention relates to novel 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines, process for their preparation and their use for producing medicaments for improving perception, concentration, learning and/or memory....
03/17/2011
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