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Class 546/139 - Isoquinolines (including hydrogenated)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system has the following
No. of patents: 354
Last issue date: 02/07/2012


1                  
NumberTitleIssue Date
8110687Bicyclic compounds with kinase inhibitory activity
The present invention provides novel bicyclic compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disea...
02/07/2012
8067600Histone deacetylase inhibitors and methods of use thereof
One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additiona...
11/29/2011
7919624VR1 vanilloid receptor antagonists with a iononic substructure
The invention provides compounds of formula (I), wherein Y, R, n and X are as defined in the description, a process for their preparation and pharmaceutical compositions containing them. The compounds of formula (I) inhibit the Transient Receptor Potential Vanilloid...
04/05/2011
7872136Process for production of 4-fluoroisoquinoline-5-sulfonyl halide or salt thereof
To provide an effective and simple process for producing 4-fluoroisoquinoline-5-sulfonylhalide or a salt thereof, and a simple method for separating for purification of the product from a by-produced position isomer thereof. The process for producing 4-fluoroisoquin...
01/18/2011
7858792Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. Th...
12/28/2010
7507828Histone deacetylase inhibitors and methods of use thereof
One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additiona...
03/24/2009
7501516Quinoline derivatives and their use as tyrosine kinase inhibitors
The invention concerns quinoline derivatives of Formula (I) wherein each of Z, m, R1, n and R3 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in th...
03/10/2009
7452994Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepare...
11/18/2008
RE40558Therapeutic uses of di-aryl acid derivatives
The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as P...
10/28/2008
7442794Rearranged pentanols, a process for their production and their use as anti-inflammatory agents
The invention relates to the compounds of formula I, a process for their production and their use as anti-inflammatory agents. ...
10/28/2008
7439257Aryloxyalkylcarbamate-type derivatives, preparation method thereof and use of same in therapeutics
The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.
10/21/2008
7429586Non-imidazole aryloxyalkylamines
Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...
09/30/2008
7429592Cyanoanthranilamide derivatives and the use thereof as medicaments
Substituted cyanoanthranilamide derivatives, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described. The compounds according to the invention can be used as or in the case of psoriasis, Kap...
09/30/2008
7414063Inhibitors of Akt (protein kinase B)
The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections. ...
08/19/2008
7408065P2Xreceptor antagonists and their use
The invention provides compounds of formula (IA), processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. ...
08/05/2008
7407939Protein kinase inhibitors comprising ATP mimetics conjugated to peptides or peptidomimetics
The present invention provides small molecules having high affinity to the ATP binding site of protein kinases, which are conjugated to apeptide or peptidomimetic moiety which mimics the substrate of PKB. The chimeric compounds according to the present invention pre...
08/05/2008
7405299Compounds as pharmaceutical agents
The current invention relates to compounds of the formula: (Ia) and the pharmaceutically acceptable salts thereof and their use as TGF-beta signal transduction inhibitors for treating cancer and other diseases in a patient in need thereof by administration of said c...
07/29/2008
7402594Sulfated bis-cyclic agents
Sulfated bis-cyclic compounds that are potent anticoagulants and methods for their manufacture are provided. The sulfated compounds are bis-cyclic moieties comprised of an isoquinoline ring joined to a phenyl ring with the general chemical structure formula (I) wher...
07/22/2008
7354931Heterocyclic retinoid compounds
The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders...
04/08/2008
7354944Thiadiazole compounds and methods of use
The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnorm...
04/08/2008
7320992Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods fo...
01/22/2008
7309708Hepatitis C virus inhibitors
Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Compositions comprising the compounds...
12/18/2007
72766075-HTreceptor antagonists
Substituted carbocyclic sulphonamide derivatives of formula (I), in which n is 0 or 1 and the other variables are as defined in the claims, are selective 5-HT7 receptor antagonists and are thereby effective in the treatment of a variety of neurological co...
10/02/2007
7271192Substituted 2-pyrrolidine-2-yl-1H-indole compounds
Novel 2-pyrrolidin-2-yl-1H-indole compounds corresponding to formula (I) wherein R1, R2, R3 and R4 have the meanings given in the description, and pharmaceutical compos...
09/18/2007
7256201Selective estrogen receptor-β ligands
The invention relates to novel compounds having the general formula: (I) and arc useful as selective ER-β ligands in the treatment or prophylaxis of Alzheimer's disease, anxiety disorders, depressive disorders, osteoporosis cardiovascular disease, rheumatoid arthri...
08/14/2007
7253188Aminobenzamide derivative
This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is —S(O)p-A, â...
08/07/2007
7253165Benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as Dantagonists
The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These c...
08/07/2007
7250526Transfer hydrogenation process and catalyst
A catalytic transfer hydrogenation process is provided. The catalyst employed in the process is a metal hydrocarbyl complex which is coordinated to defined bidentate ligands substituted with at least one group selected from an optionally substituted sulphonated hydr...
07/31/2007
7244725Acetyl 2-hydroxy-1, 3-diaminoalkanes
Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and RC are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase en...
07/17/2007
7241774Substituted tetrahydroisoquinoline compounds, methods of making, and their use
The present invention relates to novel substituted tetrahydroisoquinoline compounds, pharmaceutical compositions containing the compounds, methods of making the compounds, and methods of using the compounds to destroy a target cell, such as a cancer cell, and to tre...
07/10/2007
7241775Composition, process of making, and medical use of substituted 4-phenyltetrahydroisoquinolines
Substituted 4-phenyltetrahydroisoquinolines of formula I, process for their preparation, their use as a medicament and medicaments containing them. The compounds of formula I can be used, among other uses, in the e...
07/10/2007
7235547Pharmaceutical composition comprising an AChE inhibitor and a mGluR2 antagonist
The present invention relates to a pharmaceutical composition comprising an inhibitor of acetylcholinesterase (AChE inhibitor) and a metabotropic glutamate receptor 2 antagonist (mGluR2 antagonist) and a pharmaceutically acceptable excipient. The invention also rela...
06/26/2007
7230104Fungicidal 5-phenyl substituted 2-(cyanoamino) pyrimidines
Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered h...
06/12/2007
7217722Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
An objective of the present invention is to provide compounds having Rho kinase inhibitory activity. The compounds according to the present invention are those represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: Het—X—Z...
05/15/2007
7217706Propanolamine derivatives
This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympatho...
05/15/2007
7217714CCR5 modulators
Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ]   (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/15/2007
7214689Isoquinoline compounds
The invention relatests compound of formula (I): wherein: n is 1, 2 or 3, A represents a group
05/08/2007
72115855-HTreceptor antagonists
The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions compr...
05/01/2007
72115845-HT7 receptor ligands
The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline propyl sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising...
05/01/2007
7205312N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydrox...
04/17/2007
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