Disclosed herein is a method of treating endometrial cancer by administering to the subject a solid pharmaceutical composition comprising 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile or a pharmaceutically-acceptable salt thereof, alone or in combination with a second agent such as letrozole.
A61K 31/573 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone substitués en position 21, p. ex. cortisone, dexaméthasone, prednisone ou aldostérone
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
Disclosed herein is a method of treating ovarian cancer by administering to the subject a solid pharmaceutical composition comprising 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile or a pharmaceutically-acceptable salt thereof, alone or in combination with a second agent such as letrozole.
Disclosed herein is a method of treating a cancer in a subject in need thereof, the method comprising administering to the subject a therapeutically-effective amount of a first compound, or a pharmaceutically-acceptable salt or zwitterion thereof, and a therapeutically-effective amount of a second compound, or a pharmaceutically-acceptable salt thereof.
RAS proteins are frequently mutated in human cancers. Disclosed herein are compounds that disrupt RAS effectors and inhibits Ras/Raf/MEK/ERK pathway signaling. Further disclosed herein are methods of using compounds in combination with MEK inhibitors and/or BRAF inhibitors to treat cancer.
C07C 317/28 - SulfonesSulfoxydes ayant des groupes sulfone ou sulfoxyde et des atomes d'azote, ne faisant pas partie de groupes nitro ou nitroso, liés au même squelette carboné avec des groupes sulfone ou sulfoxyde liés à des atomes de carbone acycliques du squelette carboné
RAS proteins are frequently mutated in human cancers. Disclosed herein are compounds that disrupt RAS effectors and inhibits Ras/Raf/MEK/ERK pathway signaling. Further disclosed herein are methods of using compounds in combination with checkpoint inhibitors to treat cancer.
C07C 235/32 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des atomes d'oxygène ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone acycliques et des atomes d'oxygène, liés par des liaisons simples, liés au même squelette carboné le squelette carboné contenant des cycles aromatiques à six chaînons
A61K 31/136 - Amines, p. ex. amantadine ayant des cycles aromatiques, p. ex. méthadone ayant le groupe amino lié directement au cycle aromatique, p. ex. benzène-amine
Disclosed herein is a method for treating endometrial cancer, e.g., endometroid endometrial cancer, e.g., low grade endometroid endometrial cancer, by administering 8-cyclopenty1-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile or a pharmaceutically-acceptable salt thereof, alone or in combination with a second agent such as an aromatase inhibitor, for example, letrozole, or a pharmaceutically acceptable salt thereof. Also disclosed herein are combinations of 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile or a pharmaceutically-acceptable salt thereof, and second agent such as such an aromatase inhibitor, for example, letrozole, or a pharmaceutically acceptable salt thereof.
A01N 37/06 - Acides carboxyliques non saturés ou leurs thio-analoguesLeurs dérivés
A01N 63/30 - Champignons microscopiquesSubstances produites par des champignons microscopiques ou obtenues à partir de ceux-ci
C12P 1/02 - Préparation de composés ou de compositions, non prévue dans les groupes , utilisant des micro-organismes ou des enzymesProcédés généraux de préparation de composés ou de compositions utilisant des micro-organismes ou des enzymes utilisant des champignons
A01N 37/36 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques comportant un atome de carbone possédant trois liaisons à des hétéro-atomes, avec au plus deux liaisons à un halogène, p. ex. acides carboxyliques contenant au moins un groupe carboxylique ou un thio-analogue, ou d'un de leurs dérivés, et un atome d'oxygène ou de soufre lié par une liaison simple, liés au même squelette carboné, cet atome d'oxygène ou de soufre ne faisant pas partie d'un groupe carboxylique ou d'un thio-analogue, ou d'une de leurs dérivés, p. ex. acides hydroxycarboxyliques
Disclosed herein is a method of treating breast cancer by administering 8-cyclopentyl- 2-((4-(4-methylpiperazin-l-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile, alone or in combination with a second agent such as aromatase inhibitor or a selective estrogen receptor degrader. Also disclosed herein are combinations of 8-cyclopentyl-2-((4-(4-methylpiperazin-l-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile and second agent such as aromatase inhibitor or a selective estrogen receptor degrader.
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
Disclosed herein is a method of treating lymphoma by administering 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile or a pharmaceutically-acceptable salt thereof, alone or in combination with a second agent such a BTK inhibitor, for example ibrutinib, acalabrutinib, or a pharmaceutically-acceptable salt thereof. Also disclosed herein are combinations of 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile or a pharmaceutically-acceptable salt thereof, and second agent such as such a BTK inhibitor, for example ibrutinib or a pharmaceutically-acceptable salt thereof or acalabrutinib or a pharmaceutically-acceptable salt thereof.
Disclosed herein is a method of treating breast cancer by administering 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile, alone or in combination with a second agent such as aromatase inhibitor or a selective estrogen receptor degrader. Also disclosed herein are combinations of 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile and second agent such as aromatase inhibitor or a selective estrogen receptor degrader.
Disclosed herein is a method of treating a cancer by administering 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile and an immune checkpoint inhibitor. In some embodiments, the immune checkpoint inhibitor is an anti-PD-1 antibody or an anti-CTLA4 antibody. Also disclosed herein are combinations of 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile and an immune checkpoint inhibitor.
Disclosed herein is a method of treating ovarian cancer, including low grade serous ovarian cancer or high grade serous ovarian cancer, by administering to the subject a solid pharmaceutical composition comprising 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile or a pharmaceutically-acceptable salt thereof, wherein the administering is once daily for at least 4 weeks, alone or in combination with a second agent such as letrozole.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
Disclosed herein is a method of treating endometrial cancer by administering to the subject a solid pharmaceutical composition comprising 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile or a pharmaceutically-acceptable salt thereof, alone or in combination with a second agent such as letrozole.
Disclosed herein is a method of treating a cancer in a subject in need thereof, the method comprising administering to the subject a therapeutically-effective amount of a first compound, or a pharmaceutically-acceptable salt or zwitterion thereof; and a therapeutically-effective amount of a second compound, or a pharmaceutically-acceptable salt thereof.
A61P 35/04 - Agents anticancéreux spécifiques pour le traitement des métastases
C07C 15/44 - Hydrocarbures cycliques ne contenant que des cycles aromatiques à six chaînons en tant que partie cyclique substitués par des radicaux hydrocarbonés non saturés monocycliques le substituant hydrocarboné contenant une liaison double carbone-carbone
Disclosed herein is a method of treating a squamous cell carcinoma (SCC), a SCC associated with a disease, for example, recessive dystrophic epidermolysis bullosa (RDEB). The method of the disclosure describes administering a therapeutically-effective amount of (E)-2-(5-((2,4,6-trimethoxystyrylsulfonyl)methyl)-2-methoxyphenylamino)acetic acid, or a pharmaceutically-acceptable salt or zwitterion thereof, and derivatives thereof.
C07C 317/28 - SulfonesSulfoxydes ayant des groupes sulfone ou sulfoxyde et des atomes d'azote, ne faisant pas partie de groupes nitro ou nitroso, liés au même squelette carboné avec des groupes sulfone ou sulfoxyde liés à des atomes de carbone acycliques du squelette carboné
C07D 295/15 - Composés hétérocycliques contenant des cycles polyméthylène imine d'au moins cinq chaînons, des cycles aza-3 bicyclo [3.2.2] nonane, piperazine, morpholine ou thiomorpholine, ne comportant que des atomes d'hydrogène liés directement aux atomes de carbone du cycle avec des radicaux hydrocarbonés substitués liés aux atomes d'azote du cycle substitués par des atomes de carbone comportant trois liaisons à des hétéro-atomes avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile avec les atomes d'azote du cycle et les atomes de carbone comportant trois liaisons à des hétéro-atomes liés à la même chaîne carbonée, qui n'est pas interrompue par des carbocycles à une chaîne acyclique saturée
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
A61Q 19/00 - Préparations pour les soins de la peau
A61P 17/02 - Médicaments pour le traitement des troubles dermatologiques pour traiter les blessures, les ulcères, les brûlures, les cicatrices, les cheloïdes, ou similaires
RAS proteins are frequently mutated in human cancers. Disclosed herein are compounds that disrupt RAS effectors and inhibits Ras/RafrMEK/ERK pathway signaling. Further disclosed herein are methods of using compounds in combination with checkpoint inhibitors to treat cancer.
C07C 317/10 - SulfonesSulfoxydes ayant des groupes sulfone ou sulfoxyde liés à des atomes de carbone acycliques d'un squelette carboné non saturé contenant des cycles
8-CYCLOPENTYL-7-OXO-2-(4-PIPERAZIN-1-YL-PHENYLAMINO)-7, 8-DIHYDRO-PYRIDO [2,3-D]PYRIMIDINE-6-CARBONITRILE AND USES THEREOF IN TREATING PROLIFERATIVE DISORDERS
Pharmaceutical compositions of (E)-2,4,6-trimethoxystyryl-3-[(carboxymethyl)amino]-4-methoxybenzylsulphone and phamiaceutically acceptable salts thereof are described as well as methods of their use.
Pharmaceutical compositions of (E)-2,4,6-trimethoxystyryl-3-[(carboxymethyl)amino]-4- methoxybenzylsulphone and pharmaceutically acceptable salts thereof are described as well as methods of their use, and a dose regimen of (E)-2,4,6-trimethoxystyryl-3- [(carboxymethyl)amino]-4-methoxybenzylsulphone, sodium salt to reduce the incidence of urothelial toxicity.
The invention discloses a method of treating cancer refractory to an anticancer agent comprising administering to a cancer patient a pharmaceutical composition comprising at least one compound of Formula 1
2 or a pharmaceutically acceptable salt of such a compound, and an anticancer agent.
A61K 31/198 - Alpha-amino-acides, p. ex. alanine ou acide édétique [EDTA]
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 31/706 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle
A61K 31/454 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pimozide, dompéridone
A61K 31/428 - Thiazoles condensés avec des carbocycles
An aqueous pharmaceutical solution composition comprising between about 20 mg/ml to about 100 mg/ml of a radioprotective α,β-unsaturated aryl sulfone, a cosolvent comprising polyethylene glycol (PEG), polypropylene glycol, polyglycerol, DMA, propylene glycol, glycerol, ethanol, sorbitol, isopropyl alcohol, or a combination thereof in an amount between about 25% and about 90% w/v, and a water soluble Vitamin E derivative, wherein the composition has a pH within the range of about 7.0 to about 9.5.
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK (USA)
Inventeur(s)
Tycko, Benjamin
Raza, Azra
Wilhelm, Francois
Abrégé
The invention discloses a diagnostic method for predicting the therapeutic efficacy of a broad specificity kinase inhibitor in a subject with refractory cancer comprising determining the locus-specific DNA methylation profile of the subject, wherein the locus-specific DNA methylation profile predicts the therapeutic efficacy of a broad specificity kinase inhibitor for treatment of a subject with refractory cancer.
C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK (USA)
Inventeur(s)
Maniar, Manoj
Raza, Azra
Wilhelm, Francois
Abrégé
The invention discloses a method of treating cancer refractory to an anticancer agent comprising administering to a cancer patient a pharmaceutical composition comprising at least one compound of Formula (1) Where R1 is selected from the group consisting of -NH2, -NH-CH2-COOH, -NH- CH(CH3)-COOH, -NH-C(CH3)2-COOH, -NH-CH2-CH2-OH and -N-(CH2CH2OH)2 or a pharmaceutically acceptable salt of such a compound, and an anticancer agent.
An aqueous pharmaceutical solution composition comprising between about 20 mg/ml to about 100 mg/ml of a radioprotective α,β-unsaturated aryl sulfone, a cosolvent comprising polyethylene glycol (PEG), polypropylene glycol, polyglycerol, DMA, propylene glycol, glycerol, ethanol, sorbitol, isopropyl alcohol, or a combination thereof in an amount between about 25% and about 90% w/v, and a water soluble Vitamin E derivative, wherein the composition has a pH within the range of about 7.0 to about 9.5.
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
The present invention provides compositions and methods for promoting rapid healing and/or regeneration of damaged tissue resulting from a wound comprising administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising a compound of (E)-4-carboxystyryl-4-chlorobenzylsulfone, or a functional derivative thereof, and a pharmaceutically acceptable excipient.
An aqueous pharmaceutical solution composition comprising between about 20 mg/ml to about 100 mg/ml of a radioprotective α,β-unsaturated aryl sulfone, a cosolvent comprising polyethylene glycol (PEG), polypropylene glycol, polyglycerol, DMA, propylene glycol, glycerol, ethanol, sorbitol, isopropyl alcohol, or a combination thereof in an amount between about 25% and about 90% w/v, and a water soluble Vitamin E derivative, wherein the composition has a pH within the range of about 7.0 to about 9.5.
The invention provides drug screening methods and methods for determining efficacy of a therapeutic regimen in humans. In particular, the invention provides screening methods to determine efficacy of a therapeutic regimen to protect human subjects from deleterious effects of cytotoxic agents. The inventive method comprises i) extracting target cells from the human subject prior to exposure to a cytotoxic agent, ii) treating the subject with a cytotoxic protective drug; iii) extracting the target cells from the subject after treatment with the cytotoxic protective drug of step ii); iv) exposing the target cells of steps i) and iii) to the cytotoxic agent; and v) analyzing and comparing one or more parameters indicative of viability and growth conditions in target cells of step i) and step iii), wherein a favorable viability and growth condition of the target cells of step iii) as compared to target cells of step i) is indicative of the efficacy of the therapeutic regimen in the human subject.
Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation.
Composition for parenteral administration are provided which comprise an effective amount of a compound of formula I
or a compound of formula IIa
and at least about 50% by weight of at least one water soluble polymer selected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.
Activated cytotoxic compounds are described for attachment to targeting molecules for the treatment of a mammalian disease condition which comprise, an activator, a spacer linker, a linker (e.g., self-immolative), and a cytotoxic drug selected from the group consisting of AMINO-SUBSTITUTED (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES, AMINO-AND-HYDROXY SUBSTITUTED STYRYLSULFONANILIDES, and SUBSTITUTED PHENOXY- AND PHENYLTHIO-STYRYLSULFONE DERIVATIVES. Activated cytotoxic compound attached to a targeting molecule are described wherein the targeting molecule is selected from the group consisting essentially of an antibody, a receptor, a ligand, a cytokine, a hormone, and a signal transduction molecule. The invention is further directed to a method of treatment of disease conditions.
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
C07D 207/46 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec les hétéro-atomes liés directement à l'atome d'azote du cycle
C07K 16/00 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux
29.
Treatment of proliferative disorders with amino-substituted (E)-2,6- dialkoxystyryl 4-substituted benzylsulfones
A01N 57/00 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques du phosphore
A01N 37/18 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques comportant un atome de carbone possédant trois liaisons à des hétéro-atomes, avec au plus deux liaisons à un halogène, p. ex. acides carboxyliques contenant le groupe —CO—N, p. ex. amides ou imides d'acide carboxyliqueLeurs thio-analogues
Temple University—Of The Commonwealth System of Higher Education (USA)
Onconova Therapeutics, Inc. (USA)
Inventeur(s)
Reddy, M. V. Ramana
Reddy, E. Premkumar
Bell, Stanley C.
Abrégé
α,β-Unsaturated sulfides, sulfones, sulfoxides and sulfonamides according to Formula I:
2, X, n, * and R are as defined herein, are prepared by dehydration of β-hydroxy sulfides, sulfones, sulfoxides or sulfonamides.
Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation. Composition for parenteral administration are provided which comprise an effective amount of compound of formula I
or a compound of formula IIa
and at least about 50% by weight of at least one water soluble polymer selected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.
Solution and suspension formulations are provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject which comprises an effective amount of at least one radioprotective α, β unsaturated aryl sulfone wherein the composition has a pH within the range of about 8 to about 9.
A01N 57/00 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques du phosphore
Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation. Composition for parenteral administration are provided which comprise an effective amount of a compound of formula (I) or a compound of formula (IIa) and at least about 50% by weight of at least one water soluble polymerselected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.
A01N 57/00 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques du phosphore
Activated cytotoxic compounds are described for attachment to targeting molecules for the treatment of a mammalian disease condition which comprise, an activator, a spacer linker, a linker (e.g., self-immolative), and a cytotoxic drug selected from the group consisting of AMINO-SUBSTITUTED (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES, AMINO-AND- HYDROXY SUBSTITUTED STYRYLSULFONANILIDES, and SUBSTITUTED PHENOXY- AND PHENYLTHIO-STYRYLSULFONE DERIVATIVES. Activated cytotoxic compound attached to a targeting molecule are described wherein the targeting molecule is selected from the group consisting essentially of an antibody, a receptor, a ligand, a cytokine, a hormone, and a signal transduction molecule. The invention is further directed to a method of treatment of disease conditions.
A61K 31/4015 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil ayant des groupes oxo liés directement à l'hétérocycle, p. ex. piracétam, éthosuximide
35.
Substituted phenoxy-and phenylthio-derivatives for treating proliferative disorders
Temple University - Of The Commonwealth System of Higher Education (USA)
Onconova Therapeutics Inc. (USA)
Inventeur(s)
Reddy, E. Premkumar
Reddy, M. V. Ramana
Bell, Stanley C.
Abrégé
Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
A01N 57/00 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques du phosphore
A01N 57/00 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques du phosphore
brevets
