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Class 546/51 - Ring nitrogen is shared by five-membered cyclo and six-membered cyclo (e.g., vincamine, etc.)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the ring nitrogen of the six membered
No. of patents: 119
Last issue date: 10/20/2009


1      
NumberTitleIssue Date
7605262Podophyllotoxin derivatives
4-O esters of podophyllotoxin and 4′-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4′-demethylepipodophyllotoxin. The compounds are useful for treating cancer. ...
10/20/2009
7396837Antitumoral analogs of lamellarins
New lamellarins are provided of the general formula III or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof ...
07/08/2008
7354918Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof
The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR′ wherein A represents a heteroatom and R′ represents a group selected fr...
04/08/2008
7270772Benzopyran colorants, method of manufacture, and method of use
A compound of Formula (I) wherein X is hydrogen or a radical of Formula (II), R1 independently at each occurrence is a C1–C20 aliphatic radical, a C3–C10
09/18/2007
6835807Drug complex and drug delivery system
A drug complex useful as a DDS compound, which is represented by the following formula: A-R—NH—Y—CH2—O—CO-Q, wherein A is a polymer as a drug carrier; R is a spacer, wherein the spacer is an amino acid or an oligopeptide comprising 2 to 8 amino ...
12/28/2004
6811996DDS compounds and method for assaying the same
A drug delivery system compound comprising a carboxy(C1-4)alkyldextran polyalcohol modified with a saccharide compound and a residue of drug compound bound to the carboxy(C1-4)alkyldextran polyalcohol, and a method for measuring a drug delivery...
11/02/2004
6756381Compositions and formulations of 9-nitrocamptothecin polymorphs and methods of use thereof
A polymorphic form of 9-nitrocamptothecin is provided, the polymorph being characterizable as having an IR spectrum with an absorption centered between 3625 cm−1 and 3675 cm−1 and containing more than a trace of water. ...
06/29/2004
6709679Antineoplastic conjugates of transferin, albumin and polyethylene glycol
Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS—, HO— or H2N group and cytostatic compound...
03/23/2004
6699876Camptothecin analogue compounds
Compound of formula (I): ##STR1## wherein: n is 0, 1 or 2, R1 represents (C3 -C11)cycloalkyl or (C3 -C11)cycloalkylalkyl, R2, R3, R4 and R5 are selec...
03/02/2004
6608052Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceut...
08/19/2003
653451520,21-dinor-eburnamenines
A compound selected from the group consisting of all possible isomers or racemates of a compound of the formula ##STR1## wherein the various substituents are as defined in the specification and its non-toxic, pharmaceutically acceptable salts with acids o...
03/18/2003
6509345Camptothecin analogue compounds
Compound of formula (I): ##STR1## wherein: n is 0, 1 or 2, R1, R2, R3, R4 and R5 are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, cycloalkyl, cycloalkylalkyl, hydroxy, hydro...
01/21/2003
6407239Aromatic esters of camptothecins and methods to treat cancers
Aromatic camptothecin ester compounds having the formula: ##STR1## are described as well as formulations containing the compounds. Methods of treating cancer and/or tumors are also disclosed....
06/18/2002
6376617Bioactive derivatives of camptothecin
Water soluble polymeric conjugates of camptothecin consist essentially of N-(2-hydroxypropyl)methacryloylamide units linked via a spacer group to a residue of a camptothecin such as irinotecan or its non-soluble metabolite, 7-ethyl-10-hydroxy-camptothecin...
04/23/2002
6306868Methods for inhibiting the growth of tumors with 7-substituted camptothecin derivatives
Compounds of formula (I), wherein: R1 is --CN, --CH(CN)--R4, --CH.dbd.C(CN)--R4, --CH2 --CH(CN)--R4, --C(.dbd.NOH)--NH2, --C(.dbd.NH)--NH2, --CH.dbd.C(NO2)--R4
10/23/2001
6277992S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof
A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: ##STR1## wherein R0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen ...
08/21/2001
6252079Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof
The present invention provides a short, convergent total synthesis of irinotecan and derivative compounds which comprises of a novel 4+1 radical annulation wherein the precursor ##STR1## is reacted with an aryl isonitrile having the formula ##STR2## ...
06/26/2001
6228855Aromatic esters of camptothecins and methods to treat cancers
Aromatic camptothecin ester compounds having the formula: ##STR1## are described as well as formulations containing the compounds. Methods of treating cancer and/or tumors are also disclosed....
05/08/2001
6187783Phenanthridinium derivatives
A novel phenanthridinium derivative represented by general formula (A): ##STR1## wherein R1 is a substituted or unsubstituted lower aliphatic hydrocarbon group; R is an aliphatic hydrocarbon chain having 2 to 6 carbon atoms which may optionally...
02/13/2001
61302277-Substituted camptothecin derivatives and methods for inhibiting the growth of tumor cells therewith
20S-Camptothecin derivatives in which the 7-position bears as a substituent --CN, --CH(CN)R4, --CH.dbd.C(CN)R4, --C(.dbd.NOH)NH2, --C(.dbd.NH)NH2, --CH.dbd.C(NO2)R4, --CH(CN)R5, ...
10/10/2000
6093720Trans apovincaminic acid ester derivatives
The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), ##STR1## wherein R means hydrogen or a group (a), wherein Z stands for C1-4 alkyl, optionally substituted aryl, aralkyl,...
07/25/2000
5965566High molecular weight polymer-based prodrugs
The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of biologically active moiety; X is an electron withdrawing group; Y and Y' are independently O or S; (n) is zero (0) or a positive integer, preferably from 1 to ab...
10/12/1999
5880131High molecular weight polymer-based prodrugs
High molecular weight, water-soluble prodrugs of the formula: ##STR1## wherein: D is a biologically active moiety; M is X or Q; X is an electron withdrawing group; Q is a moiety containing a free electron pair positioned five or six atoms from Y'; Y and Y...
03/09/1999
5840900High molecular weight polymer-based prodrugs
The present invention is directed compositions of the formula: ##STR1## wherein: D is a biologically active moiety; X is an electron withdrawing group; Y and Y' are independently O or S; R1 is selected from the group consisting of H, C1-6...
11/24/1998
5622957Benzopyrrolizinoquinolizinones
A compound selected from those of general formula (I): ##STR1## wherein A represents a bivalent radical ##STR2## and R1, R2, R3, R4, R6, R7, R8, R9 and Z are...
04/22/1997
5614549High molecular weight polymer-based prodrugs
Water-soluble prodrugs of the formula: ##STR1## wherein: D is a biologically active nucleophile; M is X or Q; x is an electron withdrawing group; Q is a moiety containing a free electron pair positioned five or six atoms from Y'; Y and Y' are oxygen or su...
03/25/1997
5602131EburnanE analogues
A compound selected from those of general formula (I): ##STR1## wherein A represents a bivalent radical selected from ##STR2## and R1, R2, R3, R4, R5, R6, R7, R8
02/11/1997
5514794Antibody-drug conjugates
Derivatized drugs are prepared with a linker consisting of a malonate, wherein the drug is linked through a methylene to the 2-position carbon of the malonate....
05/07/1996
542431420,21-dinoreburnamenines
A compound in all racemic or optionally active forms selected from the group consisting of a compound of the formula ##STR1## where the substituents are defined as in the specification and their non-toxic, pharmaceutically acceptable acid addition sa...
06/13/1995
5332748Substituted derivatives of 20,21-dinoreburnamenine, their preparation process and the new intermediates thus obtained, their use as medicaments and the pharmaceutical compositions containing them
A compound and all possible racemic or optically active isomer forms, selected from the group consisting of compound of the formula ##STR1## wherein the substituents are defined as set forth in the application as filed. Useful for treating cerebral i...
07/26/1994
5220016Synthesis of navelbine analogs
The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-prot...
06/15/1993
520435515-nitro-2ଲ, 3ଲ-dihydro- and 15-nitro-2ଲ,3ଲ,6,7-tetrahydrotabersonine derivatives, pharmaceutical compositions containing them and process for preparing same
The invention relates to novel 15-nitro-2ଲ,3ଲ-dihydro- and 15-nitro-2ଲ,3ଲ,6,7-tetrahydrotabersonine derivatives of the formula (I), ##STR1## wherein R1 stands for hydrogen; R2 stands for hydrogen or a C
04/20/1993
5122607Racemic and optically active octahydro-indolo(2,3-a) tetrahydropyranyl (2,3-c) quinolizine diester derivatives and process for preparing the same
New intermediate compounds are disclosed of the formula I, ##STR1## wherein R1 and R2 are independently alkyl having 1 to 4 carbon atoms, or acid-addition salts thereof of formula Ib, ##STR2## wherein X represents an acid r...
06/16/1992
5093337Substituted derivatives of 20,21-dinoreburnamenine, their use as medicaments and the pharmaceutical compositions containing them
The invention concerns compounds of formula (I); ##STR1## in which R1, R2 and R3, identical or different, stand for hydrogen, halogen, alkyl or alkoxy (C1-5), hydroxy, trifluoromethyl, nitro, amino, alkylam...
03/03/1992
50811202-,21-Dinoreburnamenines containing a 15-aminated group
A compound selected from the group consisting of a compound of the formula (I): ##STR1## in which R1 and R2 are individually selected from the group consisting of hydrogen, an alkyl of 1 to 5 carbon atoms, --(CH2...
01/14/1992
5047528Process of synthesis of vinblastine and vincristine
The present invention relates to the synthesis of dimer alkaloid compounds, particularly those of the Catharantus (Vinca) family, from an indole unit, such as cantharanthine, and a dihydroindole unit, such as vindoline. A multi-step process is disclosed i...
09/10/1991
5037977Method for production of dimeric alkaloids
This invention concerns a method for the production of dimeric alkaloids, characterized by reacting of catharanthine with vindoline in the presence of Fe3+ and (1) removing or inactivating the Fe3+ and allowing the reaction product...
08/06/1991
5034396Method of treating depression with optically active isomers of 20,21-dinoreburnamenines
A compound selected from the group consisting of optically active isomers of a racemic compound of the formula ##STR1## wherein the 3-hydrogen and 16-hydrogen are trans and ##STR2## is selected from the group consisting of ##STR3## wit...
07/23/1991
4980474Apovincaminic acid derivatives
An apovincaminic acid derivative represented by the formula ##STR1## wherein n is an integer of from 2 to 11, and a pharmaceutically acceptable salt thereof are disclosed. These compounds are useful for therapy of cerebrovascular injuries, peripheral...
12/25/1990
4939255Hexa-cyclic camptothecin derivatives
A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound through Friedlaender reaction. It has an excellent antitumor activ...
07/03/1990
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