Class 540/569 - 1,4-benzodiazepines (including hydrogenated)

Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system has the following
No. of patents: 43
Last issue date: 02/15/2011

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Number	Title	Issue Date
7888503	Benzodiazepine derivatives that inhibit rock The present invention relates to dihydrobenzodiazepine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dihydrobenzodiazepine derivatives are useful ...	02/15/2011
7358239	Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is...	04/15/2008
7265105	Pyrrolobenzodiazepines A compound of the formula II: wherein: R′2 is CHR″2, where R″2 is H. R6 and R9 are H and R7	09/04/2007
7220739	Therapeutic application of pro-apoptotic benzodiazepines Benzodiazepine compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1,4-benzodiazepine-2,5-dione compounds of the following structures:	05/22/2007
7074921	Process for the preparation of 3,7-disubstituted-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine compounds Methods for the synthesis of benzodiazepine compounds having farnesyl protein transferase inhibitory activity. ...	07/11/2006
7067511	Pyrrolobenzodiazepines Compounds of the formulae Ia and Ib: wherein: A is CH2, or a single bond; R2 is selected from: R, OH, OR, CO2H, CO2R, COH,...	06/27/2006
7056910	1,4,5.6-tetrahydroimidazo[4,5-d]diazepine derivatives or salts thereof To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof. ...	06/06/2006
7008938	Benzene-fused heteroring derivatives and pharmaceutical agents comprising the same as active ingredient A benzene-fused heteroring derivative 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 activity against cyst...	03/07/2006
6995154	Heterocyclic topoisomerase poisons The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical co...	02/07/2006
6949642	Production of tertiary amines by reductive amination A process for the production of tertiary amines by reductive amination of carbonyl compounds with secondary amines in the presence of a water scavenger, preferably trifluoroacetic acid anhydride, is disclosed. This process has applications in the preparation of imid...	09/27/2005
6858599	Tricyclic compound having spiro union This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which e...	02/22/2005
6821977	Antidiabetic agents A compound of the formula whereon R1 is: R5 is: and n, m,...	11/23/2004
6703387	Inhibitors of HPV E1 helicase enzyme The invention is concerned with novel benzodiazepine derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are inhibitors of the human papillomavirus E1 helicase e...	03/09/2004
6699849	Cyclodextrin complexes of benzodiazepines Methods for enhancing the complexation efficiency of a drug with cyclodextrin and for enhancing the availability of a drug following administration of a cyclodextrin-drug complex....	03/02/2004
6696435	Substituted N,N-disubstituted fused-heterocyclo amino compounds useful for inhibiting cholesteryl ester transfer protein activity The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating...	02/24/2004
6667302	Heterocyclic topoisomerase poisons The invention provides compounds of formula I: ##STR1## wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the c...	12/23/2003
6455519	Use of substituted N, N-disubstituted fused-heterocyclo amino compounds for inhibiting cholesteryl ester transfer protein activity The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for t...	09/24/2002
6362178	2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP...	03/26/2002
6201119	Antiretroviral tetrahydroimidazo[1,4]benzodiazepin-2(thi) ones The compounds are of the class 1,4-benzodiazepines of the formula: ##STR1## An illustrative compound is (S)-6-chloro-2,3,4,5-tetrahydro-3-methyl-4-(3-methyl-2-butenyl)-1H-1,4-ben zodiazepin-9-amine. The compounds are useful as intermediates in the pre...	03/13/2001
6171578	Benzodiazepine derivatives for imaging thrombi The invention provides compounds comprising glycoprotein IIb/IIIa receptor-binding benzodiazepine derivatives covalently linked to metal ion chelators. The compounds of the invention may be labeled with a radionuclide such as 99m Tc and used to...	01/09/2001
6140322	Amidine and isothiourea derivatives as inhibitors of nitric oxide synthase There are provided novel compounds of formula (I) ##STR1## wherein X, R1, R2, R3, R4 and R5 are as defined in the specification and optical isomers and racemates thereof and pharmaceutically acce...	10/31/2000
6121258	1,5-heterocyclic metalloprotease inhibitors The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibito...	09/19/2000
6069114	2-amino-4-bicycloamino-1,3,5-Triazines, their preparation, and their use as herbicide and plant growth regulators Compounds of the formula (I) and their salts ##STR1## in which R1 to R6, Y1, to Y2, Y3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepa...	05/30/2000
6011029	Inhibitors of farnesyl protein transferase The present invention comprises benzodiazepine compounds having farnesyl transferase inhibitory activity....	01/04/2000
5985869	Benzoheterocyclic compounds Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy,...	11/16/1999
5580979	Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions The present invention makes available novel compounds represented by the general formula ##STR1## wherein Y represents a phosphate analog. Which compounds are useful for inhibiting an interaction between a protein containing an SH2 domain and a ...	12/03/1996
5559230	Benzoheterocyclic compounds Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R2 is H, halogen, alkoxy, phenyialkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy,...	09/24/1996
5532232	Guanidine derivatives Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The co...	07/02/1996
5466799	Synthesis of benzodiazepines A general method is provided for the synthesis of substituted 2,3-dihydro-5-phenyl-1H-1,4-benzodiazepines by the reaction of bis-trifiated-2,5-dihydroxy benzophenones with 1,2-bisaminoethanes, followed by displacement of the 7-trifloxy group....	11/14/1995
5416083	Benzodiazepinyl-terminated non-peptidyl ଱-succinamidoacyl aminodiols as anti-hypertensive agents Non-peptidyl compounds characterized generally as ଱-succinamidoacyl aminodiols having a benzodiazepinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension....	05/16/1995
5175159	3-substituted-1,4-benzodiazepines as oxytocin antagonists Compounds of Formula I are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarean delivery. ##STR1##...	12/29/1992
5142048	Intermediate for preparation of amino acid derivatives The invention relates to novel intermediate compounds for preparation of novel amino acid derivatives having renin inhibiting activity....	08/25/1992
5036153	Preparation of 2,5-diazabicyclo[2.2.1]heptanes and intermediates (R,R)-2,5-Diazabicyclo[ 2.2.1]heptanes are prepared from a compound of the formula ##STR1## wherein X and R2 are as defined herein, by heating with tosylchloride in pyridine, reacting the formed compound of the formula ##STR2## w...	07/30/1991
4594436	Isomeric 2-chloromethyl-1,4-benzodiazepine or 3-chloro-1,5-benzodiazocine compound [1,2]-fused 1,4-benzodiazepine compounds are disclosed corresponding to the general formula I ##STR1## wherein X is an oxygen or sulfur atom or an optionally substituted imino group, R1 is a hydrogen or halogen atom, lower alkyl radical, a...	06/10/1986
4479901	Fluorination of carbanions with N-fluoro-N-alkylsulfonamides Process for fluorinating an organic carbanion, which process comprises contacting and reacting, in a dry inert atmosphere, the compound of the formula selected from ##STR1## wherein ##STR2## is the carbanion, M is a counter ion, and X is a ...	10/30/1984
4280957	Imidazodiazepines and processes therefor Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of o...	07/28/1981
4261924	4-Nitro-2-trichloromethylphenylsulfenamides New 4-nitro-2-trichloromethylphenylsulfenamides having a fungicidal and bactericidal action, processes for their manufacture, fungicides containing these compounds as active ingredients, and a process for combating fungi with these compounds....	04/14/1981
4208327	5-Aryl-1-(2-oxazolin-2-yl)-1H-1,4-benzodiazepines and related compounds 5-Aryl-1-(2-oxazolin-2-yl)-1H-1,4-benzodiazepines and related compounds having the formula ##STR1## wherein A is methylene or carbonyl; Z is oxygen, imino or thio; R1, R2, and R3 independently are hydrogen, halogen, t...	06/17/1980
4044003	Process for preparing 1,4-benzodiazepines 1,4-Benzodiazepine derivatives of the formula, ##STR1## wherein R1 is hydrogen, a lower alkyl, a haloalkyl, a cycloalkylalkyl, an alkoxyalkyl, an acyloxyalkyl, an alkylthioalkyl, an alkylaminoalkyl, a dialkylaminoalkyl, a hydroxyalkyl, car...	08/23/1977
4008223	6-Aza-3H-1,4-benzodiazepines There are produced 6-aza-3H-1, 4-benzodiazepines and 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula ##STR1## where R1 is a halogen, R2 and R3 are hydrogen, halogen, trifluoromethyl, nitro, nitrile, hydroxy, l...	02/15/1977

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Class 540/569 - 1,4-benzodiazepines (including hydrogenated)