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Class 544/366 - Five-membered hetero ring having two or more ring hetero atoms of which at least one is nitrogen


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is five-membered
No. of patents: 445
Last issue date: 04/10/2012


1                      
NumberTitleIssue Date
8153793Sulfonamide derivative having PGD2 receptor antagonistic activity
The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound...
04/10/2012
7667037Processes for preparation of ziprasidone
Provided are processes for preparing ziprasidone from CEI and BIPT. ...
02/23/2010
7429659Furan compounds as histamine H modulators
Certain furan compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases. ...
09/30/2008
7427620Azole derivative useful as antifungal agents with reduced interaction with metabolic cytochromes
The present invention relates to novel compounds, of the general formula (I), the N-oxide forms thereof, the salts thereof with pharmaceutically acceptable acids and the stereochemical isomers thereof, which are useful as antifungal agents; to pharmaceutical composi...
09/23/2008
7427612Benzoyl-piperazine derivatives
A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in ...
09/23/2008
7420057Stable polymorph of flibanserin
The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments. ...
09/02/2008
7384945Indole or benzimidazole derivatives as CB1 inverse agonists
Provided are compounds of the formula I: and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compound...
06/10/2008
7381726Polymorphic forms of 1-′4-(5-cyanoindol-3-yl)butyl-4-(2-carbamoylbenzofuran-5-yl)piperazine hydrochloride
The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl...
06/03/2008
7354923Piperazine melanocortin-specific compounds
Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH2 or C═O, R1, R2, a...
04/08/2008
7335660Isochroman compounds for treatment of CNS disorders
This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the tre...
02/26/2008
7323480Substituted triazoles as modulators of PPAR and methods of their preparation
The present invention is directed to certain novel triazole compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and p...
01/29/2008
7320978Oxazole derivatives, preparation and therapeutic use thereof
This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The i...
01/22/2008
7279469Diaminotriazoles useful as inhibitors of protein kinases
The present invention relates to 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 disorders. ...
10/09/2007
7259250C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less th...
08/21/2007
72417644(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders
Compounds of general formula:[Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions includin...
07/10/2007
7238812Tricyclic triazolobenzazepine derivatives, process for producing the same, and antiallergic agents
Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereon. The compounds are useful as antiallerg...
07/03/2007
7238719Process for producing 1,2,3-Triazole compounds
Disclosed is a process for efficiently producing a compound represented by formula (I): wherein R1 represents aryl, amino, alkyl, or alkoxy; R2 represents a protective group of the carboxyli...
07/03/2007
72299944(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain anxiety or gastrointestinal disorders
Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is indepen...
06/12/2007
7193084Polymorphic form of itraconazole
The present invention provides a polymorphic form of itraconazole. ...
03/20/2007
7186827Dipeptide synthesis
Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section: ...
03/06/2007
7183410Stable polymorph of flibanserin
The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments. ...
02/27/2007
7160886Acylated piperazine derivatives as melanocortin-4 receptor agonists
Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of disease...
01/09/2007
7157464Substituted piperazines
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful ...
01/02/2007
7148240Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method for preparing same and compositions containing same
The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular...
12/12/2006
7119203Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metallop...
10/10/2006
7105507Cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R
09/12/2006
RE39265Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compound...
09/05/2006
7098212Piperazine derivatives
The present invention relates to compounds of the formula I and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R1, R2, R3, R4 and R5
08/29/2006
7094778Heterocyclylalkylamines as muscarinic receptor antagonists
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are...
08/22/2006
RE39198Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgesics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amounts of one of the compounds. The compoun...
07/18/2006
7064201Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an in...
06/20/2006
7049308C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less th...
05/23/2006
7045625Asymmetric process for the preparation of diarylethylpiperazines derivatives and novel asymmetric diarylmethylamines as intermediates
An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral su...
05/16/2006
7045520Opioid receptor active compounds
The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also pr...
05/16/2006
7026322Phenylahistin and the phenylahistin analogs, a new class of anti-tumor compounds
Methods of using a compound, its pharmaceutically acceptable salts, and/or its pro-drug esters, in isolated form, to treat cancer, and methods for isolating, for formulating, and for administering the compound, salt, and/or pro-drug ester as an antitumor agent, wher...
04/11/2006
70190332-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives
Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrog...
03/28/2006
6958337Crystalline antifungal polymorph
The crystalline polymorph Form I of (−)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl]methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one represented by the ...
10/25/2005
6951880Aryl and heteroaryl compounds as antibacterial and antifungal agents
This invention provides novel compounds possessing antibacterial and/or antifungal and/or antitumor activity. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided. ...
10/04/2005
6916927Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP-PDE5) for the treatment of sexual dysfunction
Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R1 is C1 to C3 alkyl substituted with C3 t...
07/12/2005
69060742-phenylpiperazine derivatives
A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof: wherein each of X1 and X3 is oxygen or two hydrogen atoms, X...
06/14/2005
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