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Class 514/262.1 - Exactly four ring nitrogens in the bicyclo ring system


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the bicyclo ring system has exactly
No. of patents: 337
Last issue date: 05/29/2012


1                  
NumberTitleIssue Date
8188098GPR119 receptor agonists
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...
05/29/2012
8183247Boron compounds useful in BNCT
The present invention relates to novel boron comprising compounds, to pharmaceutical compositions comprising said compounds, to the therapeutic use of said compounds, and to a process for preparation of said compounds. The compounds are useful in boron neutron captu...
05/22/2012
8173662Fused pyrimidines as inhibitors of nucleoside phosphorylases and nucleosidases
The present invention relates to compounds of the general formula (I) which are inhibitors of purine muclioside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5′-methylthioadenosine phosphorylases (MTAP), 5′-methylthioadenosine mucliosidases (MT...
05/08/2012
8158633Phenyl-substituted pyrazolopyrimidines
The invention relates to novel phenyl-substituted pyrazolopyrimidines, process for their preparation, and their use for producing medicaments for improving perception, concentration, learning and/or memory. ...
04/17/2012
8158634Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
The invention provides compounds having Formula Ia, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and Y are as defined in the specification; as well as pha...
04/17/2012
8148386Agent for the prevention and treatment of prostatic hyperplasia comprising pyrazolopyrimidinone compound
The present invention relates to an agent for preventing and treating benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) associated with BPH and a relaxant for relaxing urethral smooth muscle or prostatic smooth muscle comprising a pyrazolopy...
04/03/2012
8148387AKT and P70 S6 kinase inhibitors
The present invention provides AKT and p70 S6 kinase inhibitors of the formula: The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and methods of ...
04/03/2012
81432627-(3′,4′-Dialkoxyphenyl)[1,2,4]-triazolo[1,5-A]pyrimidine compounds, process for preparing thereof, and pharmaceutical composition for treating or preventing asthma, chronic obstructive pulmonary disease, arthritis, atopic dermatitis, tumor and degenerative brain diseases comprising the same
The present invention relates to novel {7-(3′,4′-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compounds or pharmaceutically acceptable salts thereof, a process for preparing the same, and pharmaceutical compositions for treating or preventing inflammatory d...
03/27/2012
8143263Therapeutic agents
A compound of Formula (I): is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion. ...
03/27/2012
8088781Inhibitors of brutons 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 th...
01/03/2012
8071608Therapeutic agents
(2S)-2-[1-(2-Chloro-6-cyano-phenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-[(1R)-2-hydroxy-1-methyl-ethoxy]-N-(5-methylpyrazin-2-yl)propanamide or a pharmaceutically acceptable salt thereof is useful in the treatment or prevention of a disease or medical condition media...
12/06/2011
8071607Mnk1 or Mnk2 inhibitors
The present invention relates to the use of pyrazolopyrimidine compounds for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a...
12/06/2011
80440606-cyclylmethyl- and 6-alkylmethyl pyrazolo[3,4-D]pyrimidines, methods for their preparation and methods for their use to treat impairments of perception, concentration learning and/or memory
Described are 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolo[3,4-d]pyrimidines of the formula (I): as defined herein, processes for their preparation and their use for producing medicaments for treating impairment o...
10/25/2011
8039477Substituted pyrazolo[3,4-d]pyrimidin-4-one compounds as phosphodiesterase inhibitors
The invention relates to novel alkyl-substituted pyrazolopyrimidines, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory with compounds of formula (I):
10/18/2011
8008309Inhibitors 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 th...
08/30/2011
7973046Use of allopurinol for the treatment of palmar plantar erythrodysesthesia
Allopurinol or a pharmaceutically acceptable salt thereof can be used for the treatment or prevention of palmar plantar erythrodysesthesia induced by chemotherapy. The allopurinol or its salt may be administered topically to the affected areas, palms and soles, pref...
07/05/2011
7968554Pyrazolo[3,4-d]pyrimidine derivatives
Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as so...
06/28/2011
7964607Pyrazolo[3,4-d]pyrimidine compounds
The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3 are as defined herein. Pharmaceutical compositions co...
06/21/2011
7960396Inhibitors 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 th...
06/14/2011
7956062Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof
A reactive oxygen generating enzyme inhibitor with NO donor bioactivity, e.g., nitrated allopurinol, is useful to treat heart failure, stable angina, ischemic disorder, ischemic reperfusion injury, atherosclerosis, sickle cell disease, diabetes, Alzheimer's disease,...
06/07/2011
79476955-membered annelated heterocyclic pyrimidines as kinase inhibitors
This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, Q1, Q2, X1, X2, Y and...
05/24/2011
7947694Substituted pyrazolo[3,4-D]pyrimidines as cell cycle kinase inhibitors
This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cel...
05/24/2011
7943624Pyridinylpyrazolopyrimidinone derivatives as PDE 7 inhibitors
To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyrid...
05/17/2011
7935708Dihydropyrazolopyrimidinone derivatives
The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alk...
05/03/2011
7932257Substituted pyrazolo[4,3-d]pyrimidines as aurora kinase inhibitors
The present invention provides compounds having the formula: wherein A-B together represent one of the following structures: ...
04/26/2011
7919498Substituted pyrazolo[3,4-d]pyrimidines as PI3K inhibitors
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, psorias...
04/05/2011
7910594Vitamin-mitomycin conjugates
This invention relates to vitamin-mitomycin conjugates, to a method of using the conjugates to selectively eliminate a population of pathogenic cells in a host animal harboring the pathogenic cells, and to a method of preparation of the conjugates. The conjugate is ...
03/22/2011
7829571Cyclic derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma. ...
11/09/2010
7799794Treatment for cardiovascular disease
This invention relates to a method for treating and preventing hypertension by administering a therapeutically effective amount of an agent capable of reducing uric acid levels in a patient in need of such treatment. Additionally, the scope of the invention includes...
09/21/2010
7786131Pyrimido[5,4-d]pyrimidines derivatives as irreversible inhibitors of tyrosine kinases
The present invention relates to pyrimido [5,4-d] pyrimidine compounds of Formula II or a pharmaceutically acceptable salt thereof, wherein Q is and X, E1, E2
08/31/2010
7763624Substituted pyrazolo[3,4-d]pyrimidines as ACK-1 and LCK inhibitors
The present invention relates to compounds of Formula I or a stereomer, a tautomer, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof, pharmaceutical formulations containing the compounds, methods of treat...
07/27/2010
7745450Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy
The invention relates to 3-, 5-, 7-trisubstituted pyrazolo[4,3-d]pyrimidines represented by the general formula I and pharmaceutically acceptable salts thereof, wherein R3 is an optionally substituted alkyl, cyclo...
06/29/2010
7741330Pyrazolo-pyrimidine inhibitors 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 prot...
06/22/2010
7737156Selective phosphodiesterase 9A inhibitors as medicaments for improving cognitive processes
The invention relates to the use of selective phosphodiesterase 9A (PDE9A) inhibitors for producing medicaments for improving perception, concentration, cognitive processes, learning and/or memory. ...
06/15/2010
7732454Inhibitors of Bruton's tyrosine kinase
Disclosed herein are imidazo[1,5-f][1,2,4]triazine compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). The imidazo[1,5-f][1,2,4]triazine compounds described are irreversible inhibitors of Btk. Methods for the preparation of the imidazo[1,5-f][1,2...
06/08/2010
7718662Pyrazolo-pyrimidine inhibitors 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 prot...
05/18/2010
7642267Benzimidazole and pyridylimidazole derivatives
This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I. The invention is particularly related to such compounds that bind with high selectivity and high affinity to the ben...
01/05/2010
7629349Pyrazolo [3,4-d] pyrimidine derivatives and their use as purinergic receptor antagonists
Pharmaceutical compositions and their uses comprising compounds of formula (I): wherein: R1 is selected from: alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR6R7, NR5
12/08/2009
7625906Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of ...
12/01/2009
7625907Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof
A reactive oxygen generating enzyme inhibitor with NO donor bioactivity, e.g., nitrated allopurinol, is useful to treat heart failure, stable angina, ischemic disorder, ischemic reperfusion injury, atherosclerosis, sickle cell disease, diabetes, Alzheimer's disease,...
12/01/2009
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