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54 results about "Estrogen receptor activity" patented technology
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Combining with estrogen and transmitting the signal within the cell to trigger a change in cell activity or function. [GOC:signaling, PMID:17615392]
Estriol Therapy for Autoimmune and Neurodegenerative Diseases and Disorders
The present invention discloses administering steroid hormones to mammals to treat autoimmune related diseases, neurodegenerative diseases or disorders, such as Alzheimer's disease, Parkinson's Disease, multiple sclerosis, stroke, ALS Pick's disease, prion disease and Huntington's disease. Most preferably the invention uses estrogens, estranges, estriol or estrogen receptor active agents to prevent or ameliorate clinical symptoms of the diseases and disorders.
Owner:RGT UNIV OF CALIFORNIA
Estriol Therapy for Autoimmune and Neurodegenerative Diseases and Disorders
The present invention discloses administering steroid hormones to mammals to treat autoimmune related diseases, neurodegenerative diseases or disorders, such as Alzheimer's disease, Parkinson's Disease, multiple sclerosis, stroke, ALS Pick's disease, prion disease and Huntington's disease. Most preferably the invention uses estrogens, estranges, estriol or estrogen receptor active agents to prevent or ameliorate clinical symptoms of the diseases and disorders.
Owner:RGT UNIV OF CALIFORNIA
Indole derivatives as estrogen receptor degraders
The present disclosure relates to compounds and a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing the compounds, and processes for their preparation. The disclosure also relates to the use of the compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
Owner:ARVINAS OPERATIONS INC
Anti aromatase compounds pharmaceutical compositions and uses thereof
Compounds of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating estrogen receptor activity in a cell or patient or treating an estrogen receptor-mediated disorder, particularly breast and other cancers, in a patient in need thereof by administering an effective amount of compound of the invention thereto.
Owner:BOEHRINGER INGELHEIM PHARMA INC
Novel compounds
ActiveUS20160136230A1Tetrapeptide ingredientsTripeptide ingredientsDiseaseEstrogen receptor activity
A compound of formula (I):or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
Owner:GLAXOSMITHKLINE INTPROP DEV LTD
Estrogen receptor modulators
InactiveUS6291505B1Unexpected and surprising activity in modulating estrogen receptor activityBiocideOrganic active ingredientsEstrogen receptor activityEstrogen receptor modulator
Estrogen receptor-modulating pyrazole compounds are described in addition to methods and compositions for treating or preventing estrogen receptor-mediated disorders. The compounds described have been found to have unexpected and surprising activity in modulating estrogen receptor activity. Thus, the compounds of the present invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
Owner:CHIRON CORP
Benzothiophene derivatives as estrogen receptor inhibitors
ActiveUS20160368911A1Organic active ingredientsDipeptide ingredientsEstrogen receptor activityBenzothiophene
A compound of formula (I):or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor,
Owner:GLAXOSMITHKLINE INTPROP DEV LTD
Compounds and compositions as selective estrogen receptor degraders
ActiveUS20140235660A1Decreases CMCAvoid fusesBiocideOrganic chemistryEstrogen receptor activityEstrogen
The present invention relates to compounds of formula I:in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
Owner:NOVARTIS AG
Estrogen receptor modulators
InactiveUS6387920B2Unexpected and surprising activity in modulating estrogen receptor activityBiocideNervous disorderDiseaseEstrogen receptor activity
Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
Owner:CHIRON CORP
Method of treating cancer using adenosine and its analogs
The present invention provides methods of treating individuals having malignancies associated with estrogen receptor activity comprising administering to an individual affected with said malignancy, an effective amount of adenosine analog in a pharmaceutical carrier to downregulate or diminish estrogen receptors in the cells. The invention further provides methods of identifying novel adenosine analogues capable of treating malignant cells expressing estrogen receptors. The invention also provides kits comprising adenosine analogs for downregulating estrogen receptors in cells and kits for screening for novel adenosine analogs capable of downregulating estrogen receptors. Further, the invention provides uses of adenosine analogs in downregulation of estrogen receptors, cell growth and cell cycle, as well as pharmaceutical compositions comprising adenosine analogs effective in suppressing cellular growth, cell cycle or downregulating estrogen receptors.
Owner:TRUSTEES OF BOSTON UNIV
3-substituted acrylic acid compound as well as preparation method and application thereof
ActiveCN107814798AInhibit receptor activityOrganic active ingredientsNervous disorderDiseaseEstrogen receptor activity
The invention provides a 3-substituted acrylic acid compound as well as a preparation method and application thereof and in particular relates to a 3-substituted acrylic acid compound, a stereoisomer,a pro-drug, a hydrate or pharmaceutically acceptable salt or ester thereof, and a pharmaceutical composition thereof as well as a preparation method and application thereof. The compound provided bythe invention can inhibit activity of an estrogen receptor, regulate expression level of the estrogen receptor down or induce degradation of the estrogen receptor and can be used for preventing or treating diseases related to overactivity of the estrogen receptor, especially estrogen receptor positive (ER+) drug-resistant diseases (such as breast cancer producing drug resistance to anti-estrogen therapy).
Owner:SICHUAN KELUN BIOTECH BIOPHARMACEUTICAL CO LTD
Estriol therapy for autoimmune and neurodegenerative disease and disorders
The present invention discloses administering steroid hormones to mammals to treat autoimmune related diseases, including post-partum auto immune diseases) and more particularly. Most preferably the invention uses estrogens, estranges, estriol or estrogen receptor active agents to prevent or ameliorate clinical symptoms of these Th1-mediated (cell-mediated) autoimmune diseases known to either have an initial onset following the birth of a child or which are exacerbated in patients in the post-partum period.
Owner:RGT UNIV OF CALIFORNIA
Pharmaceutical compositions and uses for androst-5-ene-3β, 17β-diol
InactiveUS6884795B2Reduce riskBetter respondBiocideOrganic active ingredientsDiseaseEstrogen receptor activity
Androst-5-ene-3β,17β diol is used to treat or reduce the likelihood of acquiring osteoporosis or menopausal symptoms, or other diseases affected by estrogen receptor activity, and for conditions which respond well to DHEA treatment, but where a higher ratio of estrogenic to androgenic effects is desired. Combination therapies are included, as are kits and pharmaceutical compositions for providing the active ingredients of claimed methods and combinations.
Owner:ENDORES & DEV
Use of estriol and other estranes, estrogens and estrogen receptor active compositions in the treatment of psoriasis and other autoimmune disorders
Methods, compositions and kits for treating psoriasis and other autoimmune diseases in human or animal subjects. The disclosed methods generally comprise administering to the subject a therapeutically effective amount of a naturally occurring or synthetic agent comprising estriol or another estrane, estrogen or estrogen receptor-effective composition. The disclosed compositions and kits generally comprise topical preparations and / or combination preparations wherein 2 or more agents are combined for either simultaneous administration or administration at different times and by the same or different route(s) of administration.
Owner:RGT UNIV OF CALIFORNIA
Pharmaceutical compositions and uses for androst-5-ene-3β, 17β-diol
InactiveUS6964955B2Treating and preventing imbalances or reductions in the levelsImprove the level ofBiocideOrganic active ingredientsDiseaseEstrogen receptor activity
Androst-5-ene-3β,17βdiol is used to treat or reduce the likelihood of acquiring osteoporosis or menopausal symptoms, or other diseases affected by estrogen receptor activity, and for conditions which respond well to DHEA treatment, but where a higher ratio of estrogenic to androgenic effects is desired. Combination therapies are included, as are kits and pharmaceutical compositions for providing the active ingredients of claimed methods and combinations.
Owner:ENDORES & DEV
Benzothiophene derivatives as estrogen receptor inhibitors
A compound of formula (I):or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
Owner:GLAXOSMITHKLINE INTPROP DEV LTD
Compounds
A compound of formula (I):or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
Owner:GLAXOSMITHKLINE INTPROP DEV LTD
Compounds with activity at estrogen receptors
InactiveUS20090131510A1Reduce inflammationImprove the level ofBiocideSenses disorderEstrogen receptor activityEphA Receptors
Owner:ACADIA PHARMA INC
Novel Estrogen Receptor Ligands
Owner:OASMIA PHARMA AB
Novel estrogen receptor ligands
The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt: wherein R3 is selected from the group consisting of ORA; —CHO; —C(O)C1-4alkyl; —C(O)phenyl; —O—C(O)RA; and N(RB)2; R6 is selected from certain cyclic groups defined in the specification; and the remaining groups are defined in the specification; together with a pharmaceutically acceptable carrier. Most of the compounds are novel. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
Owner:KARO BIO AB
Compounds and compositions as selective estrogen receptor degraders
ActiveUS8877801B2Improve throughputLimit deliveryBiocideOrganic chemistryDiseaseEstrogen receptor activity
The present invention relates to compounds of formula I:in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
Owner:NOVARTIS AG
Novel estrogen receptor ligands
The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification.
Owner:KARO BIO AB
Estrogen receptor modulators
InactiveUS20040077701A1Unexpected and surprising activity in modulating estrogen receptor activityOrganic active ingredientsBiocideEstrogen receptor activityEstrogen receptor modulator
Estrogen receptor-modulating pyrazole compounds are described in addition to methods and compositions for treating or preventing estrogen receptor-mediated disorders. The compounds described have been found to have unexpected and surprising activity in modulating estrogen receptor activity. Thus, the compounds of the present invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
Owner:CHIRON CORP
Substituted pyrazoles as estrogen receptor ligands
The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
Owner:KARO BIO AB
Estriol Therapy for Autoimmune and Neurodegenerative Disease and Disorders
The present invention discloses administering steroid hormones to mammals to treat autoimmune related diseases, including post-partum auto immune diseases) and more particularly. Most preferably the invention uses estrogens, estranges, estriol or estrogen receptor active agents to prevent or ameliorate clinical symptoms of these ThI-mediated (cell-mediated) autoimmune diseases known to either have an initial onset following the birth of a child or which are exacerbated in patients in the postpartum period.
Owner:RGT UNIV OF CALIFORNIA
Compounds with activity at estrogen receptors
Owner:ACADIA PHARMA INC
Aptamer modulators of estrogen receptors
The present invention relates to a nucleic acid aptamer molecule that includes a domain that binds to an estrogen receptor, molecular complexes that include the nucleic acid aptamer molecule and an estrogen receptor, and constructed DMA molecules and expression systems, as well as host cells, that the contain an RNA aptamer molecule of the invention. Use of these aptamers and encoding constructs to inhibiting estrogen receptor activity in a cell and to treat estrogen receptor-positive cancers is also described.
Owner:THE RES FOUND OF STATE UNIV OF NEW YORK
Novel estrogen receptor ligands
The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
Owner:KARO BIO AB
Cucurbitane-Triterpenoid Compounds, Pharmaceutical Composition, Use and Preparation Method Thereof
InactiveUS20120252772A1Inhibitory activityActivate transactivationOrganic active ingredientsSteroidsEstrogen receptor activityDouble bond
Disclosed is a cucurbitane-triterpenoid compound for activating estrogen receptor activity, and a pharmaceutical composition, use and preparation method thereof. The cucurbitane-triterpenoid compound is presented as formula (I):wherein a single bond or a double bond is formed between C5 and C10, and a single bond or a double bond is fromed between C8 and C9; when a single bond is formed between C5 and C10, the R1 is oxygen; while a single bond is formed between C8 and C9, R2 is carbonyl group (—C═O), methyl hydroxyl group (—CH(OH)), methyl ketone or methyl dimethoxy group (—CH(OCH3)2); and wherein while R1 is oxygen (—O—) and R2 is carbonyl group (—C═O) or methyl hydroxyl group (—CH(OH)), a single bond is formed between R1 (—O—) and C19 of R2 such that R1 and R2 are formed tetrahydro-2H-pyran-2-one or hemiacetal ring.
Owner:NAT TAIWAN UNIV
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