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Class 540/478 - Containing additional heterocyclic polycyclo ring system having plural ring nitrogens (e.g., vinblastine, vincristine, etc.)


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain an additional polycyclo ring system
No. of patents: 107
Last issue date: 09/02/2008


1      
NumberTitleIssue Date
7420052Intermediates for synthesis of vinblastine, process for preparation of the intermediates and process for synthesis of vinblastines
An intermediate for vinblastine synthesis represented by general formula A. general formula A. (in the formula, R1, R2, R3 and R4 are the group selected independently fr...
09/02/2008
7285533Apo-2 ligand
A novel cytokine, designated Apo-2 ligand, which induces mammalian cell apoptosis is provided. The Apo-2 ligand is believed to be a member of the TNF cytokine family. Compositions including Apo-2 ligand chimeras, nucleic acid encoding Apo-2 ligand, and antibodies to...
10/23/2007
7238704Vinca derivatives
The present invention relates to derivatives of vinca alkaloids. Pharmaceutical compositions containing these compounds as well as processes of preparation and treatment of various conditions are also disclosed. ...
07/03/2007
7235564Vinorelbine derivatives
The present invention relates to novel vinorelbine derivatives. Pharmaceutical compositions containing these compounds as well as processes of preparation and processes of use for treatment of various conditions are also disclosed. ...
06/26/2007
7060290Phosphocholine linked prodrug derivatives
Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substitute...
06/13/2006
6746668Apo-2 ligand
A novel cytokine, designated Apo-2 ligand, which induces mammalian cell apoptosis is provided. The Apo-2 ligand is believed to be a member of the TNF cytokine family. Compositions including Apo-2 ligand chimeras, nucleic acid encoding Apo-2 ligand, and antibodies to...
06/08/2004
6482825Growth-hormone secretagogues
This invention provides compounds of formula I ##STR1## and pharmaceutically-acceptable salts thereof, where the substituents are defined in the specification, which are growth hormone secretogogues useful for treatment and prevention of osteoporosis, con...
11/19/2002
6177444Allosteric adenosine receptor modulators
The present invention relates to compounds of formulas (IA), (IB), and (IC): ##STR1## the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection ag...
01/23/2001
6127377Vinca alkaloid antimitotic halogenated derivatives
The invention concerns novel halogenated derivatives of the vinblastine and vinorelbine family, corresponding to general formula (I) and their therapeutically acceptable salts. The invention also concerns the application of these compounds in therapy and ...
10/03/2000
6127333Conjugates useful in the treatment of prostate cancer
Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. The conjugates of the invention are characterized ...
10/03/2000
6011041Use of anhydrovinblastine
The present invention is particularly directed to the use of a derivative of vinblastine, 3',4'-anhydrovinblastine (AHVB), which differs from vinblastine in that it possesses a double bond at the 3',4' position of the caranthine nucleus rather than the hy...
01/04/2000
5948750Conjugates useful in the treatment of prostate cancer
Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of pro...
09/07/1999
5882881Inhibition of cyst formation by cytoskeletal specific drugs
The invention provides a method of producing a culture of polycystic kidney cells which form cysts in vitro. A cell culture of polycystic kidney cells is also provided. A method for screening an agent in vitro to determine the effectiveness of the agent i...
03/16/1999
5789189Inhibition of cyst formation by cytoskeletal specific drugs
The invention provides a method of producing a culture of polycystic kidney cells which form cysts in vitro. A cell culture of polycystic kidney cells is also provided. A method for screening an agent in vitro to determine the effectiveness of the agent i...
08/04/1998
5744607Basic derivatives of glutamic acid and aspartic acid as gastrin or cholecystokinin antagonists
The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or...
04/28/1998
5667764Compounds, compositions and methods for binding bio-affecting substances to surface membranes of bio-particles
Compounds are provided having the capability of binding therapeutically active substances to lipid containing bio-compatible particles, such as cells or viruses. These compounds include a bio-affecting moiety, comprising a therapeutically active substance...
09/16/1997
5665358Antibody drug-conjugates
Immunoconjugates of antibodies or antigen-recognizing fragments of antibodies and monovalent cytotoxic drug derivatives make use of ଲ-alanine derived linkers wherein the antibody or fragment thereof is attached to the linker's carboxy group via an e...
09/09/1997
5620985Antimitotic binary alkaloid derivatives from catharanthus roseus
Novel fluorinated derivatives of the vinblastine and vinorelbine family of general formula (1), ##STR1## wherein the symbols have the meanings indicated in the Specification and Claims, and the therapeutically-acceptable salts of these molecules, as ...
04/15/1997
5432279Process for the preparation of binary indole alkaloids
The present invention relates to a process for the preparation, from e.g. anhydrovinblastine, of binary indole alkaloids effective as an anti-cancer drug, such as vinblastine, leurosidine, etc., wherein a trivalent iron source and hydride source are added...
07/11/1995
5391549Cinnoline-3-carboxylic acid derivatives
A novel cinnoline derivative having an antagonistic activity against serotonin 5-HT3 receptor, its pharmaceutically acceptable salts, its N-oxide derivatives or solvates thereof, and pharmaceutical formulations containing the same for the preve...
02/21/1995
5387578New linker for bioactive agents
Conjugate of general formula 1: [A--O--W-Z]a -T 1 wherein the moity A--O--is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is...
02/07/1995
5334385New alkaloid derivatives, their use and pharmaceutical formulations containing them
Salts of a pharmacologically active, naturally occurring or synthetic alkaloids, or alkaloid derivatives and a phosphatidic acid are provided, which preferably have the formula [Alk]x [PA]y wherein Alk represents a cation derived from sai...
08/02/1994
5294611Angiotensin II receptor blocking 2,3,6 substituted quinazolinones
The invention provides novel 2,3,6 substituted quinazolinones having the formula: ##STR1## wherein R6, R and X are as described in the specification, which have activity as angiotensin II (AII) antagonists....
03/15/1994
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
5114919Adjuncts in cancer chemotherapy
Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compound...
05/19/1992
5100881N-(23-vincristinoyl) and N-(5'-noranhydro-23-vinblastinoyl) compounds of 1-aminomethylphosphonic acid useful for the treatment of neoplastic diseases
The invention relates to the compounds of general formula I: ##STR1## in which: R1 represents a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or branched alkenyl radical containing from 2 t...
03/31/1992
5095109Novel alkaloids
Cycloalkyl and aromatic vinblastine and vincristine derivatives useful as anti-tumor agents....
03/10/1992
5055449Vincristine-containing product
The present invention provides a pharmaceutical product for combating cancer with vincristine as active constituent, the neuropathic complications being prevented by a peptide. The product according to the invention contains: (a) vincristine or a salt the...
10/08/1991
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
5043340Derivatives of 4-desacetyl VLB C-3 carboxhydrazide
Derivatives of 4-desacetyl VLB C-3 carboxhydrazide, active anti-tumor agents and useful as intermediates for active anti-tumor conjugates....
08/27/1991
5043336Cyclic imide derivatives of 4-desacetyl VLB c-3 carboxhydrazide
Cyclic imide derivatives of 4-desacetyl VLB C-3 carboxydrazide, active anti-tumor agents....
08/27/1991
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
5030620Vinblastine derivatives, and pharmaceutical compositions containing them
A description is given of conjugates of vinca alkaloid of the indole-dihydroindole type with a protein or a protein fragment, corresponding to the general formula ##STR1## in which R1 denotes a protein or a protein fragment; R2 ...
07/09/1991
5006652Intermediates for antibody-vinca drug conjugates
A seris of antibody-vinca drug conjugates comprise antibodies which target antigens associated with undesirable cells, so that the cells are controlled or killed by the cytotoxic vinca drug. The drug is linked to the antibody through an organic group comp...
04/09/1991
49593674-oxo-1,2,3-benzotriazines
Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is N or CH; R1 and R2 are the same or different and are hydrogen, halogen, CF3, C1-6 alkyl, C1-7 acyl, C...
09/25/1990
4946833N-(23-vinblastinoyl)compounds of 1-aminomethylphosphonic acid useful for treating neoplastic diseases
The invention relates to N-(23-vinblastinoyl)compounds of 1-aminomethylphosphonic acid of general formula I ##STR1## in which: R1 denotes a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or ...
08/07/1990
4935509Novel alkaloids
Cycloalkyl and aromatic vinblastine and vincristine derivatives useful as anti-tumor agents....
06/19/1990
4897477Synthesis of vinblastine and vincristine type compounds
A new process for the stereospecific synthesis of alkaloids of the vinblastine and vincristine type including the synthesis of vinblastine and vincristine as well novel alkaloids which are active as anti-tumor agents....
01/30/1990
4895853Antitumor alkaloids
This invention relates to antitumor alkaloid compositions, a process of producing the compositions and a method for inhibiting tumors utilizing the compositions. More particularly, the compositions are antitumor alkaloids which are derived from marine org...
01/23/1990
4895854Antitumor alkaloids
This invention relates to antitumor alkaloid compositions, a process of producing the compositions and a method for inhibiting tumors utilizing the compositions. More particularly, the compositions are antitumor alkaloids which are derived from marine org...
01/23/1990
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