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47 results about "Ubiquitin ligase binding" patented technology
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Imide-based modulators of proteolysis and associated methods of use
The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation / inhibition of targeted polypeptides of nearly any type.
Owner:ARVINAS OPERATIONS INC
Compounds and methods for the enhanced degradation of targeted proteins
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation / inhibition of targeted polypeptides.
Owner:YALE UNIV +1
Compounds and methods for the targeted degradation of androgen receptor
ActiveUS20160214972A1Organic active ingredientsNervous disorderAndrogen Receptor GeneUbiquitin ligase
The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation / inhibition of Androgen Receptor.
Owner:ARVINAS OPERATIONS INC
Cereblon ligands and bifunctional compounds comprising the same
The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation / inhibition of targeted polypeptides of nearly any type.
Owner:ARVINAS OPERATIONS INC
Cereblon ligands and bifunctional compounds comprising the same
The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation / inhibition of targeted polypeptides of nearly any type.
Owner:ARVINAS OPERATIONS INC
Compounds and methods for the targeted degradation of androgen receptor
PendingUS20170327469A1Organic chemistryPharmaceutical non-active ingredientsAndrogen Receptor GeneUbiquitin ligase
The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation / inhibition of Androgen Receptor.
Owner:ARVINAS OPERATIONS INC
TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE
InactiveUS20180147202A1Easy to useOrganic active ingredientsPeptidesTANK-binding kinase 1Ubiquitin ligase
The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK 1. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds TBK1 such that TBK1 is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of TBK1. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation / inhibition of TBK1.
Owner:ARVINAS OPERATIONS INC
Proteolysis targeting chimera compounds and methods of preparing and using same
InactiveCN108366992AOrganic active ingredientsPharmaceutical non-active ingredientsMedicineTyrosine-kinase inhibitor
Owner:YALE UNIV
ALK (anaplastic lymphoma kinase) protein degradation agent and anti-tumor application thereof
ActiveCN109912655AGroup 5/15 element organic compoundsPharmaceutical non-active ingredientsProtein DegradationsAbnormal tissue growth
The invention discloses a compound in a formula (I) and an anti-tumor application thereof. The compound in the formula (I) has degradation and inhabitation functions on ALK target protein and mainly comprises four parts, the first part ALK-TKIs is a compound with ALK tyrosine kinase inhabitation activity; the second part LIN is different linkers; the third part ULM (ubiquitin ligase binding moiety) of VHL, CRBN or other protease micromolecular ligand with a ubiquitination function; the fourth part group A is carboxyl or deficiency and covalently binds ALK-TKIs with LIN and covalently binds LINwith ULM. A series of designed and synthesized compounds have wide pharmacological activity, have functions of degrading ALK protein and inhibiting ALK activity and can be applied to related tumor therapy.
Owner:SHANGHAI TECH UNIV
Protein degradation target compound, antitumor applications and intermediates thereof, and applications of intermediates
ActiveCN110357889AOrganic chemistryPharmaceutical non-active ingredientsProtein targetProtein degradation
The present invention relates to a compound represented by a formula (I), antitumor applications and intermediates thereof, and applications of the intermediates, wherein the intermediates are compounds represented by a formula (III) and a formula (IV), the compound represented by the formula (I) has degradation effects on specific target proteins, and mainly comprises three parts, the first partis small molecules binding protein (SMBP), the second part is a link unit (Linker), the third part ubiquitin ligase binding moiety (ULM) is a ligand with ubiquitination function, SMBP and LIN are covalently bound, and LIN is covalently bound to ULM. According to the present invention, a series of the designed and synthesized compounds of the present disclosure have wide pharmacological activities,have function of degradation of specific proteins and / or inhibition of activities, and can be used for related tumor treatment.
Owner:SHANGHAI TECH UNIV
Tau-protein targeting protacs and associated methods of use
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain onone end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase toeffect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation / inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
Owner:ARVINAS
Compounds & Methods for the Enhanced Degradation of Targeted Proteins & Other Polypeptides by an E3 Ubiquitin Ligase
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation / inhibition of targeted polypeptides.
Owner:YALE UNIV +2
Compounds and methods for the targeted degradation of androgen receptor
ActiveUS10584101B2Halogenated hydrocarbon active ingredientsNervous disorderAndrogen Receptor GeneUbiquitin ligase
Owner:ARVINAS OPERATIONS INC
Modulators of estrogen receptor proteolysis and associated methods of use
The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation / inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Owner:ARVINAS OPERATIONS INC
Compounds and methods for the targeted degradation of androgen receptor
InactiveUS20180346461A1Organic active ingredientsNervous disorderAndrogen Receptor GeneUbiquitin ligase
Owner:ARVINAS OPERATIONS INC
TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE
ActiveUS20190192514A1Easy to useOrganic active ingredientsPeptidesTANK-binding kinase 1Ubiquitin ligase
Owner:ARVINAS OPERATIONS INC
Compounds and methods for the enhanced degradation of targeted proteins
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation / inhibition of targeted polypeptides.
Owner:YALE UNIV +1
Compounds and methods for the targeted degradation of bromodomain-containing proteins
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation / inhibition of targeted polypeptides.
Owner:ARVINAS OPERATIONS INC +1
Proteolytic targeting chimera, and preparation method and application thereof
ActiveCN110642849AGrowth inhibitionTo achieve the purpose of treatmentOrganic active ingredientsOrganic chemistryProtein targetPharmaceutical Substances
The invention relates to a proteolytic targeting chimera, and a preparation method and application thereof. The structure of the proteolytic targeting chimera is as in the description, wherein L is aconnecting group containing at least one heteroatom of N and O, and can be used to connect a pseudolaric acid part capable of being specifically combined with a target CD147 protein and a thalidomidepart capable of being connected with E3 ubiquitin ligase. Through simultaneous action on the target protein and the E3 ubiquitin ligase, activated ubiquitin is transferred to the target protein, so that selective ubiquitination on the target protein is realized, and finally the ubiquitinated target protein is recognized and degraded by a proteasome. The preparation method of the compound is simpleand is easy to realize, and the proteolytic targeting chimera can obviously reduce the level of the CD147 protein, and has high application value in preparation of medicaments for treating or preventing cancers, in particular in preparation of antitumor medicaments taking CD147 as a target point.
Owner:XIANGYA HOSPITAL CENT SOUTH UNIV
Compounds and methods for the targeted degradation of androgen receptor
ActiveUS20200095205A1Halogenated hydrocarbon active ingredientsNervous disorderAndrogen Receptor GeneUbiquitin ligase
The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation / inhibition of Androgen Receptor.
Owner:ARVINAS OPERATIONS INC
Bifunctional compound, and preparation method and application thereof
The invention relates to a bifunctional compound, and a preparation method and application thereof. The bifunctional compound comprises: a binding moiety which binds to E3 ubiquitin ligase; a target protein binding moiety that binds to an androgen receptor; and a linking moiety linking the E3 ubiquitin ligase binding moiety and the target protein binding moiety. The bifunctional compound locates an androgen receptor adjacent to the ubiquitin ligase to achieve degradation or inhibition of the androgen receptor.
Owner:SUZHOU KINTOR PHARMA
Cereblon ligands and bifunctional compounds comprising the same
Owner:ARVINAS OPERATIONS INC
Cereblon ligands and bifunctional compounds comprising the same
Owner:ARVINAS OPERATIONS INC
Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
The present disclosure relates to bifunctional compounds, ULM- L-PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and / or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation / inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
Owner:ARVINAS OPERATIONS INC +1
Alk protein degradation agent and Anti-tumor application thereof
PendingUS20200306273A1Group 5/15 element organic compoundsPharmaceutical non-active ingredientsProtein targetTyrosine
A compound of formula (I) and its antitumor application are disclosed. The compounds of formula (I) have degradation and inhibitory effects on ALK target proteins. They are mainly composed of four parts: the first part, ALK-TKI, being compounds with ALK tyrosine kinase inhibitory activity; the second part, LIN, being different kinds of linker (Linker); the third part, the ULM, being a small molecule ligand (ULM, ubiquitin ligase binding moiety) with ubiquitination of VHL, CRBN or other proteases; and the fourth part, the group A, being a carbonyl group or absent, which covalently bond ALK-TKI to LIN, wherein LIN and ULM are covalently bonded. A series of compounds designed and synthesized by the present disclosure have wide pharmacological activities, have functions of degrading ALK protein and inhibiting ALK activity, and can be used for related tumor treatment.
Owner:SHANGHAI TECH UNIV
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
Imide-based modulators of proteolysis and associated methods of use
The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and / or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation / inhibition of targeted polypeptides of nearly any type.
Owner:ARVINAS OPERATIONS INC
Allosteric bcr-abl proteolysis targeting chimeric compounds
The present invention includes novel compounds and methods for preventing or treating diseases associated with and / or caused by overexpression and / or uncontrolled activation of a tyrosine kinase in a subject in need thereof. In certain embodiments, the compounds of the present invention include an allosteric tyrosine kinase inhibitor, a linker, and a ubiquitin ligase binder. The methods of the present invention include administering to the subject an pharmaceutically effective amount of at least one compound of the invention.
Owner:YALE UNIV
Bifunctional organic compound and preparation method and application thereof
The invention relates to a bifunctional organic compound as well as a preparation method and application thereof. The bifunctional organic compound has a structure as shown in a formula (I), wherein Ris selected from at least one of alkenyl, alkynyl, substituted or unsubstituted alkyl or alkoxy; the golden larch bark acetic acid part can be specifically combined with CD147 protein, and the structure of the hydrochloride part of the protein degradation agent 1 can be combined with E3 ubiquitin ligase. The bifunctional organic compound is a small molecular protein degradation targeting chimericbody. When used for degrading the target CD147 protein, the compound can form a target protein-proteolysis targeting chimerate-E3 ubiquitinase ternary complex, then activated ubiquitin is transferredto the target protein, and finally the ubiquitinated target CD147 protein is recognized and degraded by proteasome, so that tumor cell growth is effectively inhibited.
Owner:XIANGYA HOSPITAL CENT SOUTH UNIV
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