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42 results about "Apoptosis Proteins Inhibitor" patented technology
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Compositions and method for regulating apoptosis
ActiveUS6992063B2Suppress programmed cell deathRelieve suppressionTripeptide ingredientsPeptide preparation methodsInhibitor of apoptosisApoptosis
Peptides and peptidomimetics capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins) are disclosed. The peptides and mimetics are based on the N-terminal tetrapeptide of IAP-binding proteins, such as Smac / DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptides and peptidomimetics for therapeutic purposes and for rational drug design.
Owner:THE TRUSTEES FOR PRINCETON UNIV
Bivalent SMAC mimetics and the uses thereof
ActiveUS20080089896A1Toxic reductionMore tolerableBiocideOrganic chemistrySmac mimeticsSensitized cell
The invention relates to bivalent mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Owner:RGT UNIV OF MICHIGAN
Dimeric IAP inhibitors
ActiveUS20060194741A1Increased cell deathIncreased apoptotic activityBiocideOrganic active ingredientsSmac mimeticsApoptosis
Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac / DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of LAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inbhibitors, NSAIDs, taxanes and platinum containing compounds use broader language
Owner:MEDIVIR AB
Organic compounds
ActiveUS20050234042A1Inhibit bindingUseful in therapyBiocideOrganic chemistryInhibitor of apoptosisOrganic compound
Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I
Owner:NOVARTIS AG
Conformationally Constrained Smac Mimetics and the Uses Thereof
ActiveUS20080269140A1High expressionToxic reductionDipeptide ingredientsTripeptide ingredientsSmac mimeticsSensitized cell
The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Owner:RGT UNIV OF MICHIGAN
Bivalent smac mimetics and the uses thereof
ActiveUS20090123480A1Toxic reductionMore tolerableBiocideOrganic chemistrySmac mimeticsSensitized cell
The invention relates to bivalent mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Owner:RGT UNIV OF MICHIGAN
Conformationally Constrained Smac Mimetics And The Uses Thereof
InactiveUS20080132485A1Toxic reductionMore tolerableBiocideOrganic chemistrySmac mimeticsSensitized cell
The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Owner:RGT UNIV OF MICHIGAN
IAP binding compounds
IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less that 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposes are also disclosed.
Owner:MEDIVIR AB
IAP binding compounds
InactiveUS7718600B2Peptide/protein ingredientsMicrobiological testing/measurementInhibitor of apoptosisTetrapeptide
Compounds that bind cellular IAPs (inhibitor of apoptosis proteins) are disclosed. The compounds are mimetics of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac / DIABOLO, IIid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these compounds for therapeutic, diagnostic and assay purposes.
Owner:THE TRUSTEES FOR PRINCETON UNIV
Conformationally constrained Smac mimetics and the uses thereof
InactiveUS7674787B2Toxic reductionMore tolerableBiocideOrganic chemistrySmac mimeticsSensitized cell
The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Owner:RGT UNIV OF MICHIGAN
Conformationally constrained Smac mimetics and the uses thereof
ActiveUS7932382B2Toxic reductionMore tolerableAntineoplastic agentsHeterocyclic compound active ingredientsSmac mimeticsSensitized cell
The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Owner:RGT UNIV OF MICHIGAN
Bivalent Smac mimetics and the uses thereof
Owner:RGT UNIV OF MICHIGAN
Iap binding compounds
The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, solvates or prodrugs thereof, that bind to Inhibitor of Apoptosis Proteins (IAPs). The compounds of the invention may be used as diagnostic and therapeutic agents in the treatment of proliferative diseases, such as cancer, for promoting apoptosis in proliferating cells, and for sensitizing cells to inducers of apoptosis. The present invention furthermore provides a polymeric compound of formulas (VI) or (VII), comprising either at least two monomeric units of compounds of formula (I), or at least one monomeric unit of a compound of formula (I) and an entity E. The present invention further relates to pharmaceutical compositions comprising said compounds of formulas (I), (VI), and (VII) and the use of said compounds in medicine.
Owner:NUEVOLUTION AS
Heteroaryl-substituted bicyclic smac mimetics and the uses thereof
ActiveUS20110046189A1High expressionMore tolerableBiocideOrganic chemistrySmac mimeticsSensitized cell
The invention relates to heteroaryl-substituted bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Owner:RGT UNIV OF MICHIGAN
Homo- and heterodimeric SMAC mimetic compounds as apoptosis inducers
The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
Owner:BIONTECH AG
Diazo bicyclic smac mimetics and the uses thereof
ActiveUS20100273812A1Toxic reductionMore tolerableBiocideSenses disorderSmac mimeticsSensitized cell
The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Owner:RGT UNIV OF MICHIGAN
Diazo bicyclic Smac mimetics and the uses thereof
The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Owner:RGT UNIV OF MICHIGAN
Method and antisense compound for potentiating anti-cancer agents
InactiveUS20050113328A1Increase lethalityEnhance lethality/doseOrganic active ingredientsBiocideCancer cellAnticarcinogen
A method and compound for enhancing the lethality of an anti-cancer therapy, such as radiation, chemotherapy, or TRAIL protein, are disclosed. The compound is composed of morpholino subunits joined by phosphorodiamidate linkages, and has a targeting sequence that is complementary to an AUG start, IRES, or splice-donor region of the transcript for human X-linked inhibitor of apoptosis protein (XIAP). The method includes exposing cancer cells to the compound.
Owner:AVI BIOPHARMA
Novel artemisinin derivatives as well as synthetic method and application thereof
InactiveCN110143974AOrganic active ingredientsOrganic chemistryInhibitory effectApoptosis Proteins Inhibitor
The invention discloses novel artemisinin derivatives as well as a synthetic method and application thereof. The derivatives have a structure represented by a general formula I shown in the description, and each substituent is as defined in the description and claims. The derivatives provided by the invention can be used as an anti-apoptotic protein inhibitor and have better inhibitory effects onBcl-2.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Bivalent SMAC mimetics and the uses thereof
Owner:RGT UNIV OF MICHIGAN
Bivalent diazo bicyclic Smac mimetics and the uses thereof
The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.
Owner:RGT UNIV OF MICHIGAN
Compound as apoptosis protein inhibitor, and application thereof
ActiveCN108440507AImprove complianceLittle side effectsOrganic active ingredientsOrganic chemistryDiseaseApoptosis protein
The present invention belongs to the field of medical chemistry, relates to a class of compounds of apoptosis protein inhibitors, and applications thereof, and particularly provides a compound represented by a formula I, or an isomer thereof, a pharmaceutically acceptable salt, a solvate, a crystal or a prodrug thereof, preparation methods of the compounds, pharmaceutical compositions containing the compounds, and uses of the compounds or the compositions in treatment and / or prevention of IAPs overexpression related diseases such as viral infections, cancer, hyperblastosis diseases or inflammatory diseases. According to the present invention, the compound has good inhibitory activity against IAPs, and is highly expected to be used as the treatment drug for viral infection, cancer, hyperblastosis diseases or inflammatory diseases. The formula I is defined in the specification.
Owner:NANJING SANHOME PHARM RES & DEV CO LTD
Bivalent diazo bicyclic smac
The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.
Owner:RGT UNIV OF MICHIGAN
Use of apotosis inhibiting compounds in degenerative neurological disorders
ActiveUS8017385B2Avoid deathImprove biological activityBiocideNervous disorderDiseaseAdeno associate virus
The invention provides methods and compositions for localized delivery of a vector comprising a therapeutic agent to a specific region of the brain associated with a neurodegenerative diseases that is characterized by an excess buildup of buildup of intracellular protein aggregates. In particular, the invention provides methods and compositions used to deliver an adeno-associated virus vector (AAV) comprising a nucleotide sequence encoding an inhibitor of apoptosis protein (IAP) to cells in the region.
Owner:MEIRAGTX UK II LTD
Heteroaryl-substituted bicyclic Smac mimetics and the uses thereof
Owner:RGT UNIV OF MICHIGAN
Modulators of btk proteolysis and methods of use
The present disclosure relates to bifunctional compounds, which find utility as modulators of Burton's Tyrosine Kinase (BTK). In particular, the present disclosure is directed to bifunctional compounds. One end of a bifunctional compound includes a Von Hippel-Lindau, Cereblon, Inhibitors of Apotosis Proteins, or Mouse Double-Minute Homolog 2 ligand that binds to the respective E3 ubiquitin ligase. The other end of a bifunctional compound includes a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Diseases or disorders that result from aggregation, accumulation, and / or overactivation of the target protein can be treated or prevented with compounds and compositions of the present disclosure.
Owner:YALE UNIV
Iap binding compounds
Compounds that bind cellular IAPs (inhibitor of apoptosis proteins) are disclosed. The compounds are mimetics of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac / DIABOLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these compounds for therapeutic, diagnostic and assay purposes.
Owner:THE TRUSTEES OF PRINCETON UNIV
Anti-tumor diazo dicyclic apoptosis protein inhibitor
ActiveCN110028508AEnhanced inhibitory effectReduce inhibitionOrganic active ingredientsOrganic chemistryApoptosisMda mb 231
The invention provides a novel apoptosis protein inhibitor or pharmaceutically acceptable salts and isomers as well as preparation methods thereof and a pharmaceutical composition. The definition of each group is shown in the description. The invention further provides application of the compound and pharmaceutically acceptable salts and isomers thereof to preparation of medicines for treating IAP(Immimmunosuppressive Acidic Protein) related diseases. The compound disclosed by the invention has high binding affinity to XIAP, cIAP1 and cIAP2 proteins, has an excellent inhibiting effect on cellgrowth in MDA-MB-231 breast cancer and PC-3 pancreatic cancer cell lines, and also has high medicinal value and wide market prospects.
Owner:NANJING HUAWE MEDICINE TECH DEV
Method of treating hearing loss using xiap
InactiveUS20110171202A1Preventing hearing lossPrevent the hearing lossSenses disorderVirusesInhibitor of apoptosisImpaired Balance
Disclosed is a method of treating or preventing hearing loss in a subject. The method comprises administering to the subject in need thereof, an adeno-associated viral expression vector encoding X-linked inhibitor of apoptosis protein (XIAP). The XIAP is positioned in the vector for expression in an inner ear organ, or associated neural structures, of the subject so as to treat or prevent the hearing loss. Also disclosed is a method of treating or preventing impaired balance.
Owner:AUDIGEN
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