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Class 544/368 - The five-membered hetero ring is one of the cyclos in a polycyclo ring system


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the five-membered hetero ring is one of
No. of patents: 460
Last issue date: 05/15/2012


1                      
NumberTitleIssue Date
8178674Process for the preparation of ziprasidone
The invention relates to processes for the preparation of substantially pure ziprasidone. The invention also relates to the preparation of acid addition salts of ziprasidone. More particularly, it relates to the preparation of substantially pure hydrochloride salt o...
05/15/2012
8163908Sirtuin modulating compounds
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, dis...
04/24/2012
7939662Amorphous ziprasidone hydrochloride (5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride) and processes to produce the same
The present invention relates to a new and useful amorphous form of ziprasidone hydrochloride (5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride) and preparations thereof. ...
05/10/2011
7790886Polymorphic forms of ziprasidone and its hydrochloride salt and process for preparation thereof
The present invention is related to crystalline forms of ziprasidone and its hydrochloride salt and an amorphous form of ziprasidone hydrochloride and the process for the preparation thereof. The crystalline forms and amorphous form of the invention are suitable for...
09/07/2010
7777037Ziprasidone process
A process for preparing ziprasidone having low levels of keto ziprasidone and hydroxy ziprasidone impurities. ...
08/17/2010
7728136Method for the preparation of aryl piperazinyl-heterocyclic compounds
A novel method for preparing a compound of formula I which comprises of coupling the piperazine derivative of formula II with alkyl halide containing compound of the formula III
06/01/2010
7714130Processes for preparing gonadotropin releasing hormone receptor antagonists
Methods of making Gonadotropin Releasing Hormone (“GnRH”) (also known as Leutinizing Hormone Releasing Hormone) receptor antagonists, comprising reacting a compound having Formula I: with a compound having formula L
05/11/2010
7678799Crystalline ziprasidone HCl and processes for preparation thereof
Provided is crystalline ziprasidone HCl and processes for preparation thereof. ...
03/16/2010
7608711Process for the preparation of ziprasidone
A process for the preparation of ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the des...
10/27/2009
7462717C6-and C9-substituted chromeno[4,3-c]isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one...
12/09/2008
7435738Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate)
The invention relates to a stable polymorphic form of the compound 7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2 (3H)-benzoxazolone monomethanesulfonate (INNM bifeprunox mesylate), a method for the preparation of said polymorphic form and its use in pharmaceu...
10/14/2008
7423040Stable crystalline form of bifeprunox mesylate, dosage forms thereof and methods for using same
The present disclosure provides novel pharmaceutical compounds and methods for making the same, novel pharmaceutical dosage forms and methods for making the same, and methods for using said compounds and dosage forms to treat and prevent diseases and/or disorders.
09/09/2008
7420056Substituted bicyclic imidazo-3-ylamine compounds
Substituted bicyclic imidazo-3-yl-amine compounds are provided, as well as processes for the production thereof and pharmaceutical formulations containing these compounds. The use of these compounds for the production of pharmaceutical formulations and related metho...
09/02/2008
7417046Substituted pyrazoles
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S. ...
08/26/2008
7407960Substituted heterocyclic compounds
Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent cl...
08/05/2008
7405216Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate)
The invention relates to a stable polymorphic form of the compound 7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate (INNM bifeprunox mesylate), a method for the preparation of said polymorphic form and its use in pharmaceut...
07/29/2008
7405217N-aroyl piperazine derivatives as orexin receptor antagonists
This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals. ...
07/29/2008
7393850Substituted pyrazoles
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S. ...
07/01/2008
7348347Substituted 4,5,6,7-tetrahydrobenzthiazol-2-ylamine compounds
Substituted 4,5,6,7-tetrahydrobenzothiazol-2-ylamine compounds, a method for their production; pharmaceutical compositions comprising them, and methods of use for modulating biological functions and/or treating or inhibiting various medical conditions such as, e.g.,...
03/25/2008
7335653Bis-aryl sulfonamides
Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls i...
02/26/2008
7329749Piperazinylcarbonylquinolines and -isoquinolines
Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkins...
02/12/2008
7309703Substituted pyrazoles
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described. ...
12/18/2007
7301037Charged compounds comprising a nucleic acid binding moiety and uses therefor
Charged compounds are provided that comprise one or more regions of localized positive charge, compositions comprising such compounds, methods of synthesizing such compounds, methods of screening such compounds to identify those having anti-infective activity, and m...
11/27/2007
7297699Piperazine and piperidine compounds
The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or h...
11/20/2007
7271168Piperazine derivatives having SST1 antagonistic activity
The invention provides compounds of formula (1) wherein X, R1 and R2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety an...
09/18/2007
7271169Substituted heterocyclic compounds
Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, inte...
09/18/2007
7265103Substituted amino isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart o...
09/04/2007
7262198Substituted heterocyclic compounds
Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atri...
08/28/2007
7253172Dipeptidyl peptidase inhibitors for the treatment of diabetes
Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent d...
08/07/2007
7241761Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups
The present invention relates to compounds of the general formula I wherein R1 is the group and R2, R′, R″, R3...
07/10/2007
7235661Fused bicyclic aromatic compounds that are useful in treating sexual dysfunction
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherei...
06/26/2007
7214679Piperidine/piperazine-type inhibitors of p38 kinase
Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase. ...
05/08/2007
7214796Process for production of 1-[2-(benzimidazol-2-yl-thio)ethyl]piperazine or salts thereof
This invention relates to a method for producing 1-[2-(benzimidazol-2-ylthio)ethyl]piperazine (5) or its salt by the following reaction scheme: This invention enables efficient production of 1-[2-(benzimidazol-2-yl...
05/08/2007
7208496Substituted heterocyclic compounds
Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, inte...
04/24/2007
7186724Heterocyclic substituted carbonyl derivatives and their use as dopamine Dreceptor ligands
The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine...
03/06/2007
7179896Method of making PNA oligomers
This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers:
02/20/2007
7169786Isoxazoline derivatives as anti-depressants
The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piper...
01/30/2007
7163944Cyclic diamine compound and pharmaceutical containing the same
The present invention relates to 2-[4-[2-(7-trifluoromethylbenzoxazol-2-ylthio)ethyl]piperazin-1-yl]-N-[4-hydroxy-2,6-bis(trifluoromethyl)phenyl]acetamide or salt thereof, and an intermediate for the preparation thereof. The above-described compound has both ...
01/16/2007
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
7144883Bicyclic sulfonamide compounds
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obe...
12/05/2006
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