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Class 546/135 - Additional hetero ring containing


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain an additional hetero ring.
No. of patents: 128
Last issue date: 04/21/2009


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NumberTitleIssue Date
7521558Crystalline form of a biphenyl compound
The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof...
04/21/2009
7439256(Arylamidoaryl) cyanoguanidine compounds
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R5 and J are defined herein, are useful in the treatment of cancer. ...
10/21/2008
7378421Chromenone derivatives
Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for...
05/27/2008
7375219Substituted indole compounds having NOS inhibitory activity
The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other p...
05/20/2008
7355046Biphenyl derivatives
This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defin...
04/08/2008
7345058Pyrazoles
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi...
03/18/2008
7326786Thiazolinone unsubstituted quinolines
Thiazolinone quinoline derivatives having no substitution on the quinoline ring active as CDK1 inhibitors which are useful as anti-proliferation agents such as for treating solid tumors. ...
02/05/2008
7312231Quinuclidine carbamate derivatives and their use as M3 antagonists
A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl ...
12/25/2007
7312335Asymmetric Michael and Aldol additions using bifunctional cinchona-alkaloid-based catalysts
One aspect of the present invention relates to quinine-based and quinidine-based catalysts. Another aspect of the invention relates to a method of preparing a derivatized quinine-based or quinidine-based catalyst comprising 1) reacting quinine or quinidine with base...
12/25/2007
7253285Thiazolinone 4-monosubstituted quinolines
Thiazolinone monosubstituted quinoline derivatives where the quinoline ring is mono-substituted at the 4 positions which derivatives demonstrates CDK1 antiproliferative activity and are useful as anti-cancer agents. ...
08/07/2007
7250515Thiazolinone 3,4-disubstituted quinolines
Thiazolinone disubstituted quinoline derivatives where the quinoline ring is disubstituted at the 3, 4 positions which derivatives demonstrate CDK1 antiproliferative activity and are useful as anti-cancer agents. ...
07/31/2007
72417733-quinuclidinyl heteroatom bridged biaryl derivatives
Compounds of formula: or pharmaceutically acceptable salts, esters, amides, or prodrugs thereof, wherein: A and G are each independently N or N+—O−; m and n are each independently 0, 1, ...
07/10/2007
7208501Quinuclidine carbamate derivatives and their use as M3 antagonists
A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl ...
04/24/2007
7205318Lactam-containing cyclic diamines and derivatives as a factor Xa inhibitors
The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P4-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Com...
04/17/2007
7179818Substituted aminoquinuclidine compounds
This invention is directed towards substituted aminoquinuclidine compounds useful as delta-opioid receptor modulators, delta-opioid receptor agonists useful as analgesics and delta-opioid receptor antagonists useful as immunosuppressants, antiinflammatory agents, ag...
02/20/2007
7176217Azabicyclo compound matrix metalloprotease inhibitor and skin preparation
An azabicyclo compound (I) or a salt thereof in accordance with the present invention has an excellent inhibiting action on matrix metalloproteases (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions.
02/13/2007
7132432Hydantoin derivatives as inhibitors of tumor necrosis factor-alpha converting enzyme (TACE)
The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables L, Z0, R1, R4, R5, an...
11/07/2006
7129261Cytotoxic agents
The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as ot...
10/31/2006
7115654Caspase-1 inhibitors and methods for their use
The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions:
10/03/2006
7115629Carbamates derived from arylalkylamines
The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C1–C4)-alkylthio, (C1–C4)-alkoxyl, (C1–C4)-alkoxyl substituted by one o...
10/03/2006
71055382-pyrrolidin-2-yl-[1,3,4]-oxadiazole compounds and their use as anti-depressants
Substituted 2-pyrrolidin-2-yl compounds corresponding to formula I a method for their production, pharmaceutical compositions containing them, and methods of using them, especially for treating pain and/or depres...
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
7091217Chemokine receptor binding heterocyclic compounds
Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole. ...
08/15/2006
7041685Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present i...
05/09/2006
7041693Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein L, Z0, R1, R4, R5, a...
05/09/2006
7022259Liquid crystal compounds, preparation thereof, and composition containing the same
A liquid crystal compound with high helical twisting power, a method for preparing the same, and a liquid crystal composition containing the same. The liquid crystal compounds include cyclic group chain structures similar to the liquid crystal to serve as the core s...
04/04/2006
7001900Azabicyclic compounds for the treatment of disease
The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1–2 nitrogen atoms or a 10-membered bicyclic-six-...
02/21/2006
6984648Cyclic β-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-α
The present application describes novel cyclic β-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms s...
01/10/2006
69583483-glyoxylamideindoles for treating cancer
Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceuticall...
10/25/2005
69538553-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof
The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The ar...
10/11/2005
6927293Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...
08/09/2005
6916828Carbamates derivatived from arylakylamines
The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C1-C4)-alkylthio, (C1-C4)-alkoxyl, (C1-C4)-alkoxyl substituted by one or seve...
07/12/2005
68848073-substituted quinuclidines and their use as nicotinic agonists
This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the com...
04/26/2005
6864265Chemokine receptor binding heterocyclic compounds
Compounds that bind to chemokine receptors such as CXCR4 and CCR5 demonstrate protective effects against infection of cells by human immunodeficiency virus are disclosed. These compounds contain a tertiary amine[[s]] linked to a core nitrogen via an ar...
03/08/2005
6858613Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease
The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to trea...
02/22/2005
6825181Aminoisoquinoline derivatives
Aminoisoquinoline derivatives of the following formulae or analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an excellent effect of inhibiting activated blood-coagulation factor X, and they are useful as anticoagulants ...
11/30/2004
6821962Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and /or p56lck tyrosine kinases
This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a pati...
11/23/2004
68154511,2,3,4-Tetrahydroisoquinolines derivatives as urotensin II receptor antagonists
The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for ...
11/09/2004
6762200Oxa(thia)zolidine derivative and anti-inflammatory drug
The present invention provides medicinal compositions characterized by containing as the active ingredient either a compound represented by a general formula (1) or a pharmaceutically acceptable composite thereof, [where...
07/13/2004
6756384Imidazole compounds
A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatm...
06/29/2004
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