|
Match
|
Document |
Document Title |
|
|
7498334 |
Pyrrolopyrimidines as phosphodiesterase VII inhibitors
Pyrrolopyrimidine derivatives of the formula I
in which R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1 , act as phosphodiesterase VII inhibitors and can be employed for the treatment...
|
|
|
7420052 |
Intermediates 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, R 1 , R 2 , R 3 and R 4 are the group selected independently from the group...
|
|
|
7285533 |
Apo-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...
|
|
|
7238704 |
Vinca 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...
|
|
|
7235564 |
Vinorelbine 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...
|
|
|
7060290 |
Phosphocholine 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...
|
|
|
6365735 |
Vinca-alkaloid derivatives and preparation method
The invention concerns a novel method for preparing vinca-alkaloids by reacting a catharantine-type product and a vindoline-type product, characterized in that it consists in selecting the reaction...
|
|
|
RE37449 |
Process of synthesis of 3',4'-anhydrovinblastine, 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...
|
|
|
6127377 |
Vinca 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...
|
|
|
6011041 |
Use 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...
|
|
|
5948750 |
Conjugates 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...
|
|
|
5882881 |
Inhibition 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...
|
|
|
5744607 |
Basic 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 R 1 is selected from the group consisting of unsubstituted, mono- or...
|
|
|
5667764 |
Compounds, 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...
|
|
|
5665358 |
Antibody drug-conjugates
Immunoconjugates of antibodies or antigen-recognizing fragments of antibodies and monovalent cytotoxic drug derivatives make use of β-alanine derived linkers wherein the antibody or fragment...
|
|
|
5620985 |
Antimitotic 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...
|
|
|
5547667 |
Linker for bioactive agents
Conjugates of general formula 1: [A--O--W--Z] a --T 1 wherein the moiety A--O-- is the residue of drug of formula A--O--H in which --O--H is a primary or...
|
|
|
5432279 |
Process 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.,...
|
|
|
5334385 |
New 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...
|
|
|
5220016 |
Synthesis 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...
|
|
|
5100881 |
N-(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: R 1 represents a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or...
|
|
|
5095109 |
Novel alkaloids
Cycloalkyl and aromatic vinblastine and vincristine derivatives useful as anti-tumor agents.
|
|
|
5055449 |
Vincristine-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...
|
|
|
5047528 |
Process 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...
|
|
|
5043340 |
Derivatives 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.
|
|
|
5043336 |
Cyclic imide derivatives of 4-desacetyl VLB c-3 carboxhydrazide
Cyclic imide derivatives of 4-desacetyl VLB C-3 carboxydrazide, active anti-tumor agents.
|
|
|
5037977 |
Method 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 Fe 3 + and (1) removing or inactivating the...
|
|
|
5030620 |
Vinblastine 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 R 1 denotes a...
|
|
|
5006652 |
Intermediates 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...
|
|
|
4959367 |
4-oxo-1,2,3-benzotriazines
Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is N or CH; R 1 and R 2 are the same or different and are hydrogen, halogen, CF 3 , C 1 -6 alkyl, C 1...
|
|
|
4946833 |
N-(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: R 1 denotes a hydrogen atom, a linear or branched alkyl radical...
|
|
|
4897477 |
Synthesis 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...
|
|
|
4895854 |
Antitumor 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...
|
|
|
4831038 |
Vinblastine derivatives and pharmaceutical composition containing them
The invention relates to vinca (indole-dihydroindole) alkaloid derivatives, in which a fatty chain containing at least 7 aliphatic carbon atoms is present at least at the C 3 /C 4 -position. The...
|
|
|
4831133 |
Extraction of alkaloids of Catharanthus roseus tissue
Alkaloids present in Catharanthus roseus tissue are selectively concentrated by aqueous extraction of ground tissue followed by extraction with organic solvent e.g. ethyl acetate. The resultant...
|
|
|
4798829 |
1-Azabicyclo[3,2,2]nonane derivatives having 5-HT receptor antagonist activity
Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 1, 2, or 3; and m and p are independently 1 or 2 such that m+n+p≥4; X is NH; or O when Ar is of...
|
|
|
4778885 |
Production of alkaloid dimers using ferric ion
Alkaloid dimers are formed by coupling vindoline and catharanthine in the presence of ferric ion. The predominant products are 3',4'-anhydrovinblastine and vinblastine when reaction conditions are...
|
|
|
4769453 |
Bis-indolic compounds
The present invention relates to a process for the preparation of bis-indolic compounds, and the bis-indolic compounds produced by the process.
|
|
|
4767855 |
Process for the preparation of vincristine
The present invention relates to a process for the preparation of vincristine. The process for the semisynthesis of vincristine according to the present invention comprises oxidizing vinblastine or...
|
|
|
4765972 |
Vinca alkaloid photoactive analogs and their uses
Pharmacologically active, radioactive, and photoactive vinblastine analogs are provided which can be used to bind covalently to cellular polypeptides which have high affinity for Vinca alkaloids....
|
|
|
4757077 |
Bis-indole derivatives and pharmaceutical compositions containing them
The invention relates to novel bis-indole derivatives of the general formula (I) ##STR1## wherein R 1 stands for a hydrogen atom or an acetyl group; R 2 stands for a hydrogen atom; R 3 ...
|
|
|
4753948 |
Furfuryl derivatives of vinblastine-type bis-indoles, and pharmaceutical compositions containing them
The invention relates to novel furfuryl derivatives of the general formula (I), ##STR1## wherein R 1 stands for a hydrogen atom or an acetyl group, R 2 stands for a hydroxyl or ethyl group of ...
|
|
|
4749787 |
Process of isolating vinblastine from the plant catharanthis roseus
This invention relates to a chemical process of producing an antitumor alkaloid. More particularly, it relates to a method of isolation of vinblastine from Catharanthus roseus, comprising the steps...
|
|
|
4746665 |
Nitro derivatives of vinblastine-type bisindoles, and pharmaceutical compositions containing them
The invention relates to novel nitro derivatives of the general formula (I) ##STR1## wherein R 1 stands for a methyl or a formyl group; R 2 stands for a hydroxy or ethyl group of β-position; ...
|
|
|
4737586 |
Process for the preparation of bis-indolic compounds
The present invention relates to a process for the preparation of bis-indolic compounds, and the bis-indolic compounds produced by the process.
|
|
|
4684638 |
Metal complexes of bis-indole compounds and aqueous pharmaceutical compositions containing them
The invention relates to new aqueous pharmaceutical compositions containing as active ingredient a pharmaceutically acceptable complex of a bis-indole compound with a bi- or multivalent metal ion...
|
|
|
4675400 |
Bifunctional derivatives of 4-desacetyl indole-dihydroindole alkaloids
Bifunctional derivatives of a 3-carboxhydrazide of an antineoplastic dimeric indole-dihydroindole alkaloids, useful both in forming conjugates with immunoglobulins and as anti-tumor agents.
|
|
|
4667030 |
Hydrazide succinimide derivatives of antineoplastic indole-dihydroindole alkaloids
An antineoplastic dimeric indole-dihydroindole (vinca) alkaloid carrying a hydrazine succinimide group at C-3, capable of forming conjugates with a diacid at C-4.
|
|
|
4659816 |
Process for the preparation of dimeric alkaloids
A process is disclosed for the preparation of dimeric alkaloids of formula (II) ##STR1## wherein R stands for methyl or formyl, as well as acid addition salts thereof which comprises oxidizing the...
|
|
|
4639456 |
Vinblastin-23-oyl amino acid derivatives
Vinblastine derivatives of the formula ##STR1## wherein R 1 is an ester of a α-aminoacid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine,...
|