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Class 544/132 - 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 in which the additional hetero ring is five-membered
No. of patents: 275
Last issue date: 12/20/2011


1              
NumberTitleIssue Date
8080656Process for the preparation of aprepitant
The present invention relates to a highly pure (2R,3S)-4-benzyl-3-(4-fluorophenyl)morpholin-2-yl 3,5-bis(trifluoromethyl)benzoate of Formula II, and a process for its preparation. The present invention further provides a process for preparation of Aprepitant of Form...
12/20/2011
7915407Process for {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid
The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl) -morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically ...
03/29/2011
7847095Process for 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1.,2,4-triazol-3-one
The present invention is concerned with a novel process for the preparation of the compound 5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4 -tria-zol-3-one. This compound is useful as a substanc...
12/07/2010
7807829Process for {3-[2()-[(1)-1-[3,5-bis(trifluoromethyl) phenyl]ethoxy]-3()-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid
The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(tri-fluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically ...
10/05/2010
74427162-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to t...
10/28/2008
7425555Heteroaryl substituted biphenyl derivatives as p38 kinase inhibitors
Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38. ...
09/16/2008
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
7317007Benzothiazole derivatives with activity as adenosine receptor ligands
The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor. ...
01/08/2008
7304062Peroxisome proliferator activated receptor alpha agonists
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C
12/04/2007
7288541Propylcarbamate derivatives as inhibitors of serine and cysteine proteases
The present invention includes ketone derivatives (I) and (II), which are useful as cathepsin K inhibitors. The described invention also includes methods of making such ketone derivatives as well as methods of using the same in the treatment of disorders, including ...
10/30/2007
7285548Urea substituted benzothiazoles
The present invention relates to compounds of formula I wherein R1 and R2 are described herein, and their pharmaceutically acceptable salts thereof for the...
10/23/2007
7282499Sigma receptor inhibitors
The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to some pyrazole derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy...
10/16/2007
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
7279476Pyrazole-derived kinase inhibitors and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formula: where B, R1, n, R3, Q, and R4 are described in the specification. The compounds are...
10/09/2007
7226920Aminotriazole compounds 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, processes for preparing the compounds and methods of using the compositions in the treatment of various...
06/05/2007
7208504Bicyclic inhibitors of hormone sensitive lipase
Benzotriazoles of formula I in which R1 to R8 have the abovementioned meanings and process for their preparation are described. The compounds show an inhibitory effect on hormone-sensitive lipase. ...
04/24/2007
7196082Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the us...
03/27/2007
7160912Heterocyclic compounds having antibacterial activity: process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them. The present invention also relates to a process for t...
01/09/2007
7138420Substituted benzimidazole compounds
Disclosed are substituted benzimidazole compounds of formula (I): wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit It...
11/21/2006
7102001Process for preparing pyrrolotriazine
The present invention provides a process for preparing compounds of formula (I) or a pharmaceutically acceptable salt thereof. The compounds prepared by the process of the invention inhibit tyrosine kinas...
09/05/2006
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
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
6982264Substituted alcohols useful in treatment of Alzheimer's disease
The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are u...
01/03/2006
6972292Certain substituted polyketides, pharmaceutical compositions containing them and their use in treating tumors
The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds ...
12/06/2005
6969697Substituted benzoylcyclohexenones
The invention relates to novel substituted benzoylcyclohexenones of the formula (I), in which n, A, R1, R2, R3, R4, Y and Z are each as defined in the descriptio...
11/29/2005
69560366-hydroxy-indazole derivatives for treating glaucoma
Substituted 1-(α-alkyl-ethylamino)-1H-indazol-6-ols useful for lowering and controlling IOP and treating glaucoma are disclosed ...
10/18/2005
69272335ht2 agonists for controlling IOP and treating glaucoma
Compositions and methods for controlling intraocular pressure and treating glaucoma using 1-(2-aminopropyl)-indazol-6-ol are disclosed. ...
08/09/2005
6914058Antibacterial compounds: process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotammers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceuti...
07/05/2005
6900207N-containing five-membered ring compounds and pharmaceutical agents comprising the same as active ingredient
An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activit...
05/31/2005
68283151-Amino triazoloc4,3-a! quinazoline-5-ones and/or -5-thiones inhibiting phosphodiesterase IV
The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutical...
12/07/2004
6787543Benzhydryl derivatives
A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the present in...
09/07/2004
6723742Substituted 3,5-diphenyl-1,2,4-triazoles and their use as pharmaceutical metal chelators
The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly activ...
04/20/2004
6673939Process for the preparation of 1,2,4-triazolin-5-one derivatives
The present invention relates to a process for the preparation of a compound of formula (I) wherein R represents hydrogen, C1-10 alkyl, haloC1-10 alkyl or aryl; which are useful intermediates in the preparation of morpholine derivati...
01/06/2004
6638930Morpholine and thiomorpholine tachykinin receptor antagonists
Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiov...
10/28/2003
6630468Disubstituted pyrazolines and triazolines as factor Xa inhibitors
The present application describes disubstituted pyrazolines and triazolines of formulae I and II: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing gro...
10/07/2003
6608059Fatty acid synthase inhibitors
This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH....
08/19/2003
6583142Polymorphic form of a tachykinin receptor antagonist
This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in t...
06/24/2003
6544990Substituted quinolinecarboxamides as antiviral agents
The present invention discloses disubstiuted 4-oxo-1,4-dihydro-3-quinolinecarboxamide derivatives. The compounds are useful as antiviral agents, in particular, as agents against viruses of the herpes family....
04/08/2003
6506747Substituted 1-(4-aminophenyl)pyrazoles and their use as anti-inflammatory agents
1-(4-aminophenyl)pyrazoles optionally substituted on the 3- and 5-positions of the pyrazole ring and on the amino group at the 4-position of the phenyl ring are disclosed and described, which pyrazoles inhibit IL-2 production in T-lymphocytes....
01/14/2003
6495697Silver halide color photographic lightsensitive material and novel pyrrolotriazole compound
A silver halide color photographic lightsensitive material contains a coupler represented by formula (I) below in at least one layer on a support (in this formula, X represents a hydrogen atom or a group which can split off by a coupling reaction with an ...
12/17/2002
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