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Class 546/268.7 - Thiadiazoles (including hydrogenated)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the five-membered hetero ring consists
No. of patents: 357
Last issue date: 12/13/2011


1                  
NumberTitleIssue Date
8076486Heteroaryl-substituted arylaminopyridine derivatives as MEK inhibitors
The invention provides novel heteroaryl-substituted arylaminopyridine derivative MEK inhibitors of Formula (Ia) Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as canc...
12/13/2011
7910743Compounds, compositions and methods
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. ...
03/22/2011
7414055Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this inven...
08/19/2008
7390907Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu...
06/24/2008
7297797Pyrrolines
The invention relates to novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R
11/20/2007
7253192Phenyl derivatives comprising an acetylene group
This invention is concerned with compounds of the formula I: wherein one of R5, R6 and R7 is and X1, X2
08/07/2007
7241895Polymorphic forms of 5-[4-[2-[n-methyl-n-(2-pyridyl)amino[ethoxy]benzyl] thiazolidine-2,4-dione maleate and process for their preparation
This invention relates to novel polymorphic/pseudopolymorphic forms of 5-[4-[2[N-methyl-N-(2-pyridyl)amino]ethoxy]benzyl]thiazolidine-2,4-dione maleate having formula (I). The invention also relates to a pharmaceutical composition comprising the novel polymorphic fo...
07/10/2007
7217714CCR5 modulators
Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ]   (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/15/2007
7183303Gamma-secretase inhibitors
Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease. ...
02/27/2007
7163951N-biarylmethyl aminocycloalkanecarboxamide derivatives
N-Biarylmethylaminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. ...
01/16/2007
7153878Peroxisome proliferator activated receptor modulators
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I. (Formula I); wherein: (a) R5 is selected from the group consisting of (C1–C6)alkyl, (C
12/26/2006
7144899Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)—N(R25)CH(R30)— wherein the nitrogen atom is attached to R1
12/05/2006
7141672Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. ...
11/28/2006
71354723-Heterocyclic benzylamide derivatives as potassium channel openers
The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6
11/14/2006
71324255-substituted-six-membered heteroaromatic glucokinase activators
The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are ...
11/07/2006
7105556Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2
09/12/2006
7105533Fused heterobicyclo substituted phenyl metabotropic glutamate-5 modulators
Phenyl compounds substituted with a fused-heterobicyclo moiety, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other disease...
09/12/2006
7099772Route determination method and device
A route calculation method allowing an optimized route to be drawn up by means of a calculator between a point α and a point β, consisting in using digitized data from at least a first and a second source, and consisting of (i) determining a plurality of alpha nod...
08/29/2006
7037880Ethylene derivatives and pesticides containing said derivatives
Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent su...
05/02/2006
70226504-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines
A description is given of 4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines of formula (I) and of their use as herbicides. In this formula (I) R1, R2, R3 and R4
04/04/2006
6987189Short synthesis of pyridine-based pharmaceutical intermediates
A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1–C4 alkyl, C1–C4 alkoxy,...
01/17/2006
6953798β-alanine derivates
Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra′)R  (1) Ar1 is an optionally substituted aromatic or...
10/11/2005
69169334-pyridinyl-n-acyl-l-phenylalanines
Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4. ...
07/12/2005
6906089Triarylimidazole derivatives as cytokine inhibitors
Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2 and R3 are various substituent groups; and one of X...
06/14/2005
6855825Short synthesis of pyridine-based pharmaceutical intermediates
A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1-C4 alkyl, C1-C4 alkoxy, ar...
02/15/2005
6844295Benzoxazole compound, process for producing the same, and herbicide
The present invention relates to benzoxazole compounds represented by the following formula (I): wherein R1 to R4 may be the same or different from each other, and each re...
01/18/2005
6699896Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides compounds having the structure ##STR1## wherein A is OR5, or ##STR2## R1 is alkyl, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, pyridyl, ##STR3## R2 is H, alkyl, or aryl; R3
03/02/2004
6667326Pesticidal aminoheterocyclamide compounds
The invention relates to compounds of the general formula ##STR1## wherein R1, R2, R3, R4, R5, X1, X2, X3, m and n have the significances given in claim 1, and optionally ...
12/23/2003
6656910Serine protease inhibitors
The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, s...
12/02/2003
6656911Serine protease inhibitors
The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, s...
12/02/2003
6645990Thiazolyl urea compounds and methods of uses
Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, p...
11/11/2003
6596724Oxadiazole and thiadiazole derivatives of dihydropyridine NPY antagonists
A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of oxadiazole, thiadiazole and thiadiazole oxide derivatives of dihydropyridines of Formula I. ##STR1## wherein B is ##STR2## with X being O, S or ##STR3## an...
07/22/2003
6515132Process for the preparation of rosiglitazone maleate
The invention discloses a process for the preparation of a pyridine derivative namely 5-{4-2(N-methyl-N(2-pyridyl)amino ethoxy]benzyl]thiazolidine-2,4-dione maleate comprising the steps of: (a) reacting 2-chloropyridine with 2-(N-methyl amino)ethanol; (b) coup...
02/04/2003
6458950Compounds and pharmaceutical compositions containing the same
A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen,...
10/01/2002
6407123Diaminopyridine-containing thiourea inhibitors of herpes viruses
Compounds of the formula ##STR1## wherein R1 -R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl ...
06/18/2002
6391327Pesticidal composition
A pesticidal composition comprising prallethrin and a neonicotinoid compound given in the following formula (1), (2) or (3), as an active ingredient ##STR1## wherein, A represents a 6-chloro-3-pyridyl, 2-chloro-5-thiazolyl, tetrahydrofuran-2-yl, tetr...
05/21/2002
63766712-sulfamoylbenzoic acid derivatives
2-Sulfamoylbenzoic acid derivatives of general formula (I): ##STR1## which have both an antagonistic effect on the leukotriene D4 receptor and an antagonistic effect on the thromboxane A2 receptor and salts thereof, pharmaceuticals, ...
04/23/2002
6376675Muscarinic receptor agonists
A compound of Formula (III): ##STR1## wherein X is a linkage independently selected from (CH2)12 or (CH2 CH2)4 O3 and wherein R3 is independently selected from H, CH2 ...
04/23/2002
63690832-methoxyimino-2 (pyrinyloxymethyl) phenyl acetamides with polyether derivatives on the pyridine ring
The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of ...
04/09/2002
6362204Phenylalanine derivatives
Phenylalanine derivatives of formula (1) are described: ##STR1## wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; and R5 is a group --L2 (CH2)t R6 in which L...
03/26/2002
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