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Class 546/164 - Fully saturated quinolines


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the quinoline ring system is fully saturated,
No. of patents: 169
Last issue date: 10/07/2008


1          
NumberTitleIssue Date
7432282Pyridinalkyl-aminoalkyl-IH-indole derivatives having an inhibitory action on 5-HT and serotonin reuptake as antidepressants and anxiolytics
Novel indole derivatives of the formula (I), in which X, Y, R1, R1′, m and n have the meanings indicated in Patent Claim 1, have a strong affinity to the 5-HT1A and in some cases to the 5-HT1D receptors. The compounds in...
10/07/2008
7335677Inhibitors of dipeptidyl peptidase IV
Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3
02/26/2008
7312222Heterocyclic piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases. ...
12/25/2007
7273936Oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors
Novel oxazole and thiazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of tran...
09/25/2007
721471420-hydroxyeicosatetraenoic acid production inhibitors
A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a...
05/08/2007
7189758Glucocorticoid mimetics, methods of making them, pharmaceutical formulations, and uses thereof
A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutic...
03/13/2007
7145021Analogs of terpene trilactones from and related compounds and uses thereof
The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable ...
12/05/2006
7084155Chemokine receptor binding heterocyclic compounds
Novel compounds that are useful for targeting chemokine receptors are disclosed. These compounds are complex tertiary amines. ...
08/01/2006
7053057Caspase inhibitors and uses thereof
This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2
05/30/2006
7049325Quinoline derivatives as anti-inflammatory agents
This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a CH2, CH(OH), C(O), C═NOR4, NR
05/23/2006
7041829Antagonists of the magnesium binding defect as therapeutic agents and methods for treatment of abnormal physiological states
This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of m...
05/09/2006
6992092Anti-diabetic agents
The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2
01/31/2006
6951870Coumarin derivatives with COMT inhibiting activity
Compounds of formula I′ wherein the two —OH substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R...
10/04/2005
6936610Heterocyclic derivatives
The invention relates to heterocyclic derivatives of formula (I) A—B—X1—T1(R2)—L1—T2(R3)—X2—Q  (I) or pharmaceutically-acceptable salts thereof, which ...
08/30/2005
6916813(1-phenyl-2-heteoaryl)ethyl-guanidine compounds as inhibitors of mitochondrial F1F0 ATP hydrolase
Compounds having the formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F1F0 ATPase activity and treating ischemic conditions including myocardial ...
07/12/2005
6900319Thrombin inhibitors
The invention relates to a compound of the formula I: or a salt thereof with a physiologically tolerated acid, or stereoisomers thereof, wherein R1, R2, A, B, C and D have the meanings described i...
05/31/2005
6777427Tetrahydroquinoline compounds
Tetrahydroquinoline compounds of general formula (I) or pharmacologically acceptable salts thereof, which have a specific and strong binding affinity for AR, exhibit AR agonism or antagonism, have therapeutic effects on AR-mediated diseases, particularly by not acti...
08/17/2004
6734191Chemokine receptor binding heterocyclic compounds
Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole. ...
05/11/2004
6620824Process for the synthesis of gonadotropin releasing hormone antagonists
The present invention relates to a process for preparing a compound of gonadotropin releasing hormone antagonists having a Formula I, ##STR1## in an efficient way, which involves preparation of key intermediates: 2-arylindole core; a chiral aziridine, in ...
09/16/2003
6610702Ammonium salts of inositol hexaphosphate, and uses thereof
The present invention comprises compounds, compositions thereof, and methods capable of delivering inositol hexaphospahte (IHP) to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, ...
08/26/2003
6608084Aza-bicycles which modulate the inhibition of cell adhesion
##STR1## The invention is directed to physiologically active compounds of formula (I) wherein R1 represents R3 --Z3 --, R3 --L2 --R4 --Z3 --, R3 --L3 --Ar1
08/19/2003
6525068Hydronaphtalene compounds, prepared by a rhodium catalyzed ring opening reaction in the presence of phosphine ligand
The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the p...
02/25/2003
64762324-(2-amino-1-hydroxyethyl)oxazoline derivative and method for producing same
A 4-(2-amino-1-hydroxyethyl)oxazoline derivative of the formula [XIII] ##STR1## and a method for producing the same, in which R4 is an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an option...
11/05/2002
6387992Substituted 5-heteroaryl-2-(2-hydroxyphenyl)-2h-benzotriazole UV absorbers, a process for preparation thereof and compositions stabilized therewith
Compounds of formula I or II ##STR1## where R is a heteroaryl moiety, such as 3-pyridyl, or T is a heteroaryl moiety, such as thien-2,5-diyl, and E1 and E2 are independently hydrogen, alkyl, aralkyl and the like, are prepared by reac...
05/14/2002
63690765-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists
Novel 5-benzyl-octahydroindoles and 6-benzyl-decahydroquinolines substituted in the 1-position are effective as NMDA NR2B antagonists useful for relieving pain....
04/09/2002
6362212Oxime derivative and bactericide containing the same as active ingredient
A compound represented by general formula (I) or a salt thereof, a process for producing the same, an intermediate for the production thereof, and a bactericide (fungicide) containing the same as the active ingredient wherein R1 represent optio...
03/26/2002
63232283-substituted indole angiogenesis inhibitors
3-Substituted indole carbohydrazides having the formula ##STR1## are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting angiogenesis in a mammal....
11/27/2001
6310080Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, rela...
10/30/2001
62620744-Hetaroylpyrazol derivatives and the use thereof as herbicides
Hetaroyl derivatives of the formula I ##STR1## where: R1 and R2 are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C1 -C6 -alkyl, C1 -C6 -alkoxy, C1 -C
07/17/2001
6211176଱- and ଲ-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
଱- and ଲ-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease....
04/03/2001
61660412-heteroaryl and 2-heterocyclic benzoxazoles as PDE IV inhibitors for the treatment of asthma
Novel compounds which are effective PDE IV inhibitors are disclosed. The present invention is directed to compounds having the general formula I ##STR1## wherein: X is a halogen; Q is --CH2 --CH2 --, --CH2 --, a single or ...
12/26/2000
6156766Benzamide compounds and pharmaceutical use thereof
Benzamide compounds of the formula ##STR1## wherein each symbol is defined in the specification, isomers thereof and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions comprising a therapeutically effective amount of...
12/05/2000
61302383-(cyclohexanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors
The present invention relates to novel 3-(cyclohexanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in t...
10/10/2000
6124502Mercaptoketones and mercaptoalcohols and a process for their preparation
This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R1 is C1 -C12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C1 -C
09/26/2000
6110933Amino acid derivatives and their use as phospholipase A2 inhibitor
The present invention relates to a novel fatty acid derivative of the following formula: ##STR1## wherein R1 is acyl group, etc.; R2 is acyl(lower)alkyl; R3 is lower alkyl, etc.; R4 is hydrogen, etc.; and X is -...
08/29/2000
6090787Antithrombotic agents
This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors....
07/18/2000
6087346Sigma receptor ligands and the use thereof
The invention relates to methods for the treatment of central nervous system disorders, neurological disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising ...
07/11/2000
6004933Cysteine protease inhibitors
The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and R1 is optionally substituted alkyl or ...
12/21/1999
5972989Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, mor...
10/26/1999
5968970Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
Described herein is a retroviral protease inhibiting compound of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof....
10/19/1999
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