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| Number | Title | Issue Date |
| 8063204 | Benzothiazole and benzoxazole linked pyrrolo[2,1-c] [1, 4] benzodiazepine hybrids as novel antitumour agents and process for the preparation thereof The present invention provides a compound of general formula (9), useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4][benzodiazepine g hybrids of general f... | 11/22/2011 |
| 7429658 | Synthesis of protected pyrrolobenzodiazepines A method of synthesis of a N-10 protected PBD compound of formula (I): via an intermediate of formula (II) or formula (V): ... | 09/30/2008 |
| 7407951 | Pyrrolobenzodiazepines Compounds of formula (I): formula (I) and salts, solvates, chemically protected forms, and prodrugs thereof, are disclosed wherein R2 is selected from: an optionally substituted napthyl group; an optionally substituted thiophenyl or furanyl group; and a p... | 08/05/2008 |
| 7312210 | Pyrrolo[2,1-][1,4]benzodiazepine compounds and processes for the preparation thereof The present invention provides novel pyrrolo [2,1-c][1,4]benzodiazepine compounds. This invention also provides a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine compounds. These novel pyrrolo [2,1-c][1,4]benzodiazepine compounds are useful as... | 12/25/2007 |
| 7271164 | Cyclohepta[b][1,4]diazepino[6,7,1,-hi]indoles and derivatives This invention provides compounds of the formula: wherein R1 and R2 are each, independently, H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, ... | 09/18/2007 |
| 7271162 | Cycloocta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives This invention provides compounds of formula I having the structure wherein: R1 and R2 are H, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —S... | 09/18/2007 |
| 7271163 | Cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R | 09/18/2007 |
| 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 |
| 7244724 | Pyrrolobenzodiazepines A compound of formula I: or solvate thereof, wherein n is 1 to 10, and M and M′ are independently selected from monovalent pharmaceutically acceptable cations, or together represent a divalent pharmaceutically ... | 07/17/2007 |
| 7189710 | C2-fluoro pyrrolo [2,1−][1,4]benzodiazepine dimers The present invention relates to novel 2-fluoro-pyrrolo[2,1-c][1,4]benzodiazepine dimers useful as antitumour agents and to a process for the preparation thereof. ... | 03/13/2007 |
| 7186828 | Cyclic urea compounds and preparation thereof A method for preparing cyclic urea compounds from at least an activated carbamic acid derivative containing an unprotected primary or secondary amine function, includes a cyclization step which consists in a reaction between the primary or secondary amine function a... | 03/06/2007 |
| 7173026 | Pyrrolo [2,1-c][1,4]benzodiazepine-anthraquinone conjugates useful as antitumour agents The present invention relates to synthesis of pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone hybrids (V) wherein n=3,4; R=H, OH and to their use as antitumour agents. ... | 02/06/2007 |
| 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 |
| 7064121 | N-acylated lipophilic amino acid derivatives Compounds of structural Formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptabl... | 06/20/2006 |
| 7056913 | C8—linked pyrrolo[2,1-c][1,4]benzodiazepine-acridone/acridine hybrids The present invention provides novel pyrrolo-[2,1-c][1,4]benzodiazepine hybrids useful as anti-tumour agents and a process for the preparation thereof. ... | 06/06/2006 |
| 7049311 | Pyrrolbenzodiazepines Compounds of formula (Ia) and (Ib) wherein A is CH2, or a single bond; R2 is selected from: R, OH, OR, CO2H, CO2R, COH, COR, SO2R, CN; R6, R7 and R9 are independently selected fr... | 05/23/2006 |
| 7015215 | Pyrrolo[2,1-c][1,4] benzodiazepines compounds and process thereof The present invention provides Analogues of 1,1′-{[(bisalkane-1,N-diyl)piperazine]dioxy}bis(11aS)-7-methoxy-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one] of formula (VI) wher... | 03/21/2006 |
| 6979684 | Pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide conjugates linked through piperazine moiety and process for preparation thereof The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide hybrids linked through piperazine moiety as potential antitumour agents. The present invention also relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazep... | 12/27/2005 |
| 6951853 | Process for preparing pyrrolo[2, 1-c] [1,4] benzodiazepine hybrids Novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as well as processes for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids are dislcosed. More particularly, present invention relates to a process for the preparation of novel pyrrolo[2,... | 10/04/2005 |
| 6939869 | Pyrrolo[2,1-c][1,4] benzodiazepine-indole derivatives, their preparation process, and uses of the same Disclosed herein are novel pyrrolo[2,1-c][1,4]benzodiazepine-indole derivatives of formula (I): wherein each of the substituents is given the definition as set forth in the Specification and cl... | 09/06/2005 |
| 6838455 | Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/... | 01/04/2005 |
| 6800622 | Pyrene-linked pyrrolo[2,1-c][1,4]benzodiazepine hybrids useful as anti-cancer agents The present invention relates to a process for the preparation of novel pyrrolo [2,1-c][1,4]benzodiazepine hybrids useful as antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential... | 10/05/2004 |
| 6774125 | Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/... | 08/10/2004 |
| 6747144 | Collections of compounds A compound of formula (I), wherein: R2 and R3 are independently selected from H, R, OH, OR, ═O, ═CH—R, ═CH2, CH2—CO2R, CH2—CO2H, CH2—SO2R, O—SO2 | 06/08/2004 |
| 6696438 | Cyclic amino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use of such compounds Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid... | 02/24/2004 |
| 6689881 | Method for preparing substituted [1,4]diazepino[6,7,1-hi]indol-4-ones Method for the preparation of enantiomerically pure diazepino-indolone of formula ##STR1## which comprises the intramolecular cyclization of a product of formula ##STR2## where A, B, X1, X2, Z, Z1, Z2 and R are ... | 02/10/2004 |
| 6683075 | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid... | 01/27/2004 |
| 6683073 | Pyrimidine linked pyrrolo[2,1-c][1,4]benzodiazepines as potential antitumour agents The present invention relates to a process for the preparation of novel pyrrolo [2,1-c][1,4]benzodiazepines useful as potential antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepines as po... | 01/27/2004 |
| 6660856 | Synthesis of pyrrolo[2,1-c][1,4]benzodiazepine analogues The present invention provides an efficient process for the preparation of pyrrolo [2,1-c][1,4]benzodiazepines (PBDs) represented by the formula (I): ##STR1## which starts from a subsituted 2-amino benzoic acid compound, and involves a step of an intermed... | 12/09/2003 |
| 6653303 | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use of such compounds Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid... | 11/25/2003 |
| 6624159 | Heterocycle carboxamides as antiviral agents The present invention provides a compound of formula I ##STR1## which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.... | 09/23/2003 |
| 6608192 | Collections of compounds A compound of formula (IV): O is a solid support; L is a linking group or a single bond; X' is selected from CO, NH, S, or O; A is O, S, NH, or a single bond; R2 and R3 are independently selected from: H, R, OH, OR, .dbd.O, .dbd.CH--... | 08/19/2003 |
| 6562806 | Pyrrolobenzodiazepines A compound with formula (I) ##STR1## where R10 is a therapeutically removable nitrogen protecting group; R2 and R3 are independently selected from: H, R, OH, OR, .dbd.O, .dbd.CH--R, .dbd.CH2, CH2 --CO... | 05/13/2003 |
| 6548494 | Tricyclic inhibitors of poly(ADP-ribose) polymerases Compounds of the formula shown below are poly(ADP-ribosyl)transferase inhibitors: ##STR1## Such compounds are useful as therapeutics in treating cancers and in ameliorating the effects of stroke, head trauma, and neurodegenerative disease.... | 04/15/2003 |
| 6525044 | Succinoylamino carbocycles and heterocycles as inhibitors of a-ଲ protein production This invention relates to novel carbocycles and heterocycles having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, ... | 02/25/2003 |
| 6365585 | Phosphodiesterase IV-inhibiting diazepinoindoles Metabolites of the products of formula (I) ##STR1## in which A and R are as defined in the description, which are phosphodiesterase 4 inhibitors.... | 04/02/2002 |
| 6239130 | Phosphodiesterase 4-inhibiting diazepinoindolones ##STR1## The present invention presents compounds that inhibit phosphodiesterase 4 having Formula (I). The present invention also provides methods of using the compounds of Formula (I) to prevent or treat asthma, atopic dermatitis, rheumatoid arthritis, i... | 05/29/2001 |
| 6225306 | Biphenyl derivatives and drug composition A biphenyl derivative represented by the following general formula (1) and a pharmaceutically acceptable salt thereof: ##STR1## [In the formula (1), A represents a single bond, --CH2 --, --CO--, --CS-- or --SO2 --; B represents a sin... | 05/01/2001 |
| 5972927 | Diazepinoindoles as phosphodiesterase 4 inhibitors Diazepinoindoles of formula (I), ##STR1## wherein A is mono- to trisubstituted aryl or heteroaryl, and B is an --OR1 or --NR2 R3 group where R1, R2 and R3 are particularly hydrogen, an... | 10/26/1999 |
| 5962337 | Combinatorial 1,4-benzodiazepin-2,5-dione library A method has now been found of synthesizing a combinatorial library of 1,4-benzodiazepin-2,5-diones on solid supports via an aza-Wittig ring closure, said compounds optionally encoded with tags, and to the use of this library in assays to discover biologi... | 10/05/1999 |