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Class 546/284.1 - Polycyclo ring system having the additional hetero ring as one of the cyclos


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is one of the
No. of patents: 339
Last issue date: 06/28/2011


1                  
NumberTitleIssue Date
7968724Ester derivatives as phosphodiesterase inhibitors
The invention provides inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are new ester derivatives, methods of preparing such compounds, compositions containing them, and therapeutic uses thereof. ...
06/28/2011
7687631Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following ...
03/30/2010
7563900Process for the preparation N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methane sulfonamido-dibenzo[b,d]furan-1-carboxamide
The present invention relates to a method of preparing N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof, such as its sodium salt, and novel intermediate compounds useful i...
07/21/2009
7541471Synthesis of himbacine analogs
The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improv...
06/02/2009
7511150Synthesis of heterocyclic compounds
Methods for the synthesis of heterocyclic compounds including N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide and pharmaceutically acceptable salts thereof. ...
03/31/2009
7442712Constrained himbacine analogs as thrombin receptor antagonists
A compound represented by the structural formula and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line
10/28/2008
7439368Process for producing 3-acylaminobenzofuran-2-carboxylic acid derivative
The present invention provides a process of preparing a compound of the formula [I]: wherein X is a group of the formula: —N═ or —CH═; R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower a...
10/21/2008
7419986Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, pre...
09/02/2008
7368476Hydroxamates as therapeutic agents
The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparin...
05/06/2008
7368477Benzofuranyl alkanamine derivatives and uses thereof
Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R1′, R2, R3, R4, n, and Ar are as defined, and described in clas...
05/06/2008
7335666Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, pre...
02/26/2008
7304078Thrombin receptor antagonists
Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond;
12/04/2007
72915806-(1,1-difluoroalkyl)-4-aminopicolinates and their use as herbicides
4-Aminopicolinic acids having (1,1-difluoroalkyl) substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control. ...
11/06/2007
7250518Nicotinamide acids, amides, and their mimetics active as inhibitors of PDE4 isozymes
Compounds of the formula: useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils. ...
07/31/2007
7241795Synthesis and antimicrobial activity of novel dicationic “reversed amidines”
The present invention relates to novel 2,5-bis{[alkyl (or aryl) imino]aminophenyl}furans and thiophenes of the general formula in which R1, R2, R3 and R4 are each indep...
07/10/2007
72355683-(cyclopenten-1-yl)-benzyl-or 3-(cyclopenten-1-yl)-heteroarylmethyl-amine derivatives and use thereof as medicines for treating schizophrenia
The invention provides compounds of the formula: wherein (a) is a single or double bond; W is CH, CH2, CHCH3, C(CH3)2, C(CH2)2 or C(CH2...
06/26/2007
7205305Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
04/17/2007
7189758Glucocorticoid mimetics, methods of making them, pharmaceutical formulations, and uses thereof
A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutic...
03/13/2007
7183293Ether derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t i...
02/27/2007
7153871Phosphodiesterase 4 inhibitors, including aminoindazole and aminobenzofuran analogs
PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs. The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3
12/26/2006
7144885Fused tricyclic heterocycles useful for treating hyper-proliferative disorders
This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disorders ...
12/05/2006
7145021Analogs of terpene trilactones from and related compounds and uses thereof
The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable ...
12/05/2006
7135479Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress di...
11/14/2006
7126003Method for producing 2-azetidinone derivative
A process for producing a compound represented by the following formula (II) which comprises treating a compound represented by the following formula (I) (wherein R1, R2 and R3 represent each a specific substituent) with an enzyme ca...
10/24/2006
7045545Aminoalkylbenzofurans as serotonin (5-HT(2c)) agonists
The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R1, R2, R3, R4, R4′, R5, R5′, and R12 are as described in the specification.
05/16/2006
7037920Substituted tricyclic himbacine derivatives that are useful as thrombin receptor antagonists
Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salts thereof, wherein: n1 and n2 are independently 0-2; Het...
05/02/2006
7022718Pyridine and pyrimidine derivatives
The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The co...
04/04/2006
6989398Benzanilides as potassium channel openers
Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided. ...
01/24/2006
6943182Cyclopentabenzofuran derivatives and their use
The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-κB-dependent diseases and medicaments which contain the cyclopentabenzofur...
09/13/2005
6894065Thrombin receptor antagonists
Heterocyclic-substituted compounds of the formula or a pharmaceutically acceptable salt thereof, are disclosed, wherein: Z is —(CH2)n—;
05/17/2005
6881733Serotonergic benzofurans
The present invention provides serotonergic benzofurans of Formula (I): where A, R, R1, R2, R3, and R4 are as described in the specification. ...
04/19/2005
6881743Pyridine matrix metalloproteinase inhibitors
Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independen...
04/19/2005
6858632Derivatives of isosorbide mononitrate and its use as vasodilating agents with reduced tolerance
Novel derivatives of isosorbide mononitrate and its pharmaceutically acceptable salts, which have vasodilating activity with a reduced effect of tolerance, of the general formula (I) in which A and B independently repr...
02/22/2005
6855822Benzo[b]furan dimers
Benzo[b]furan dimers and processes for their preparation are provided. The invention provides a synthetic process for the preparation of benzo[b]furan dimer using mild reaction conditions, which provides a high substituent tolerance and is appropriate for use in sol...
02/15/2005
6846819Fab I inhibitors
Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections. ...
01/25/2005
6846817Nicotine receptor ligands
The invention provides nicotine receptor agonists of formula I: wherein R1, x, y, and n have any of the values given in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceut...
01/25/2005
6828333Ether derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t is 0, 1...
12/07/2004
6794392Cell differentiation inducer
The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune...
09/21/2004
6720423Dihydrobenzofuran and dihydrobenzothiophene 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
Compounds of the formula where the variables have the meaning defined in the specification, are specific or selective agonists of RXR retinoid receptors. ...
04/13/2004
6706882Process for the preparation of (pyridinylidene)-phthalides
A process for the preparation of (pyridinylidene)-phthalides starting from 3-oxo-1,3-dihydro-isobenzofuran-1-carboxylic acids and pyridinecarbaldehydes, is described. ...
03/16/2004
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