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42 results about "Selective progesterone receptor modulator" patented technology
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A selective progesterone receptor modulator (SPRM) is an agent that acts on the progesterone receptor (PR), the biological target of progestogens like progesterone. A characteristic that distinguishes such substances from full receptor agonists (e.g., progesterone, progestins) and full antagonists (e.g., aglepristone) is that their action differs in different tissues, i.e. agonist in some tissues while antagonist in others. This mixed profile of action leads to stimulation or inhibition in tissue-specific manner, which further raises the possibility of dissociating undesirable adverse effects from the development of synthetic PR-modulator drug candidates.
Method for the treatment of a condition remediable by administration of a selective androgen receptor modulator
InactiveUS6960474B2BiocidePeptide/protein ingredientsSelective androgen receptor modulatorHormone dependence
Owner:BRISTOL MYERS SQUIBB CO
Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
InactiveUS6465445B1Reduce riskGood effectBiocideOrganic chemistrySelective progesterone receptor modulatorOsteopetrosis
Novel methods for the medical treatment and / or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure:and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3beta,17beta-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and / or sex steroid precursor is disclosed for the medical treatment and / or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
Owner:ENDORES & DEV
5-cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds
ActiveUS7071205B2Improve fertilityReduced fertilityBiocideOrganic chemistryPR - Progesterone receptorQuinoline
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such compounds and pharmaceutical compositions.
![5-cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/79204447-f7c0-4b00-939d-645ee2a3bb41/US07071205-20060704-C00001.png "5-cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds")
![5-cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/79204447-f7c0-4b00-939d-645ee2a3bb41/US07071205-20060704-C00002.png "5-cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds")
![5-cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/79204447-f7c0-4b00-939d-645ee2a3bb41/US07071205-20060704-C00003.png "5-cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds")
Owner:LIGAND PHARMA INC
Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
InactiveUS6670346B1Reduce riskBiocideOrganic chemistrySelective progesterone receptor modulatorIn vivo
Novel methods for the medical treatment and / or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure:and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3beta,17beta-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and / or sex steroid precursor is disclosed for the medical treatment and / or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
Owner:ENDORES & DEV
5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-5H-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds
ActiveUS7084151B2Improve fertilityReduced fertilityBiocideOrganic chemistryPR - Progesterone receptorQuinoline
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such compounds and pharmaceutical compositions.
![5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-<i>5H</i>-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/c08410d8-05dc-45d9-92b5-f7dcb5b56077/US07084151-20060801-C00001.png "5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-<i>5H</i>-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds")
![5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-<i>5H</i>-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/c08410d8-05dc-45d9-92b5-f7dcb5b56077/US07084151-20060801-C00002.png "5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-<i>5H</i>-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds")
![5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-<i>5H</i>-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/c08410d8-05dc-45d9-92b5-f7dcb5b56077/US07084151-20060801-C00003.png "5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-<i>5H</i>-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds")
Owner:LIGAND PHARMA INC
Method for screening for progesterone receptor isoform-specific ligands and for tissue-selective progesterone receptor ligands
InactiveUS20040121304A1Reduce adverse effectsIncreased riskCompound screeningApoptosis detectionPR - Progesterone receptorProgesterone Receptor Isoform B
The present invention provides a method for screening for progesterone receptor isoform specific ligands as well as a first method for screening for tissue-selective progesterone receptor ligands, both methods comprising selecting progesterone receptor isoform A or progesterone receptor isoform B selective ligands by means of an assay involving cells stably transfected with plasmids expressing the progesterone receptor isoform A or B. Furthermore, the present invention provides a second method for screening for tissue-selective progesterone receptor ligands, comprising in vivo tests in desired target tissues. The present invention further relates to cell lines suitable for this transactivation assay, a respective assay kit and medical uses of the isoform-specific and / or tissue-selective progesterone receptor ligands according to the present invention.
Owner:SCHERING AG
Steroids derivatives as selective progesterone receptor modulators
The present invention is directed to novel steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by at least one progesterone or glucocorticoid receptor.
Owner:JANSSEN PHARMA NV
Selective androgen receptor modulators and methods of use thereof
InactiveCN1471508AHas oral bioavailabilityProlong biological half-lifeOrganic active ingredientsBiocideHormone Receptor ModulatorsSpermatogenesis
This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of nonsteroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.
Owner:UNIV OF TENNESSEE RES FOUND
Selective androgen receptor modulators and methods of use thereof
InactiveUS7919647B2Reduce incidenceDecreasing regressionBiocideOrganic chemistrySelective androgen receptor modulatorSelective progesterone receptor modulator
Owner:UNIV OF TENNESSEE RES FOUND
Sequential SPRM/ progestin treatment
InactiveUS20050215536A1BiocideOrganic active ingredientsGynecologySelective progesterone receptor modulator
The methods provided herein comprise administering a selective progesterone receptor modulator (SPRM) during a first dosing period and at least one progestogen during a second dosing period. The dosing periods can run concomitantly or sequentially with or without a period where neither the SPRM nor the progestogen is administered.
Owner:ABBOTT ENDOCRINE INC
Compositions and methods for treating dysfunctional uterine bleeding
InactiveUS20090118253A1Treating and preventing anemiaPrevent anemiaOrganic active ingredientsSexual disorderSubject matterProgesterones
The subject matter of the instant invention is pertinent to the field of hormone therapy. More specifically, the subject matter of the instant invention concerns methods of treating dysfunctional uterine bleeding. The instant invention is also relevant to the treatment and / or prevention of anemia in patients with dysfunctional uterine bleeding. Compositions for practicing the methods, comprising progesterone antagonists are also disclosed. Embodiments of the instant invention also disclose methods for identifying new selective progesterone receptor modulators for practicing disclosed methods of treatment.
Owner:APTALIS PHARMA
Solid dispersion of a selective modulator of the progesterone receptor
InactiveCN105120899AOrganic active ingredientsPowder deliveryMetaboliteProgesterone receptor modulators
The subject matter of the present invention is a solid dispersion comprising an active ingredient chosen from the group consisting of selective modulators of the progesterone receptor, metabolites thereof and mixtures thereof, and a pharmaceutically acceptable polymeric excipient. The invention also relates to a pharmaceutical composition comprising said solid dispersion and to the therapeutic uses thereof.
Owner:LAB HRA PHARMA SA
Mutagenesis of plants for overproduction of selective estrogen receptor modulators
ActiveUS9758788B2Mutant preparationVector-based foreign material introductionPlant cellSelective Progesterone Receptor Modulators
Owner:NAPROGENIX
Solid dispersion of a selective modulator of the progesterone receptor
InactiveUS20160213684A1Powder deliveryOrganic active ingredientsMetabolitePR - Progesterone receptor
The subject of the present invention is a solid dispersion comprising an active ingredient selected from the group consisting of selective progesterone receptor modulators, metabolites thereof and mixtures thereof, and a pharmaceutically acceptable polymeric excipient. The invention also relates to a pharmaceutical composition comprising said solid dispersion and to the therapeutic uses thereof.
Owner:LAB HRA PHARMA SA
Ethylene derivative serving as selective estrogen receptor modulators (SERMs)
InactiveCN102532073ANervous disorderOrganic chemistryDiseaseSelective Progesterone Receptor Modulators
The invention provides an ethylene derivative represented by a formula I. Serving as selective estrogen receptor modulators (SERMs), the ethylene derivative can be used for preventing and / or treating diseases or disease symptoms influenced by selective estrogen receptor modulation. The formula I is shown in the specifications.
Owner:CENTAURUS BIOPHARMA
Co-micronisation product comprising a selective progesterone-receptor modulator
The subject of the present invention is a co-micronization product comprising: an active ingredient selected from the group consisting of selective progesterone receptor modulators, metabolites thereof and mixtures thereof, and an N-vinyl-2-pyrrolidone-based polymeric excipient. The invention also relates to a pharmaceutical composition comprising said co-micronization product and to the therapeutic uses thereof.
Owner:LAB HRA PHARMA SA
Selective progesterone receptor modulators (SPRM) and stabilized estrogen level in patient
ActiveUS20180369257A1Peptide/protein ingredientsSulfur/selenium/tellurium active ingredientsDiseasePhysiology
The present invention is related to Selective Progesterone Receptor Modulators (SPRM) as described and defined herein, and covers the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of sexual hormone dependent diseases and gynaecological diseases in particular Endometriosis or Uterine Fibroids (UF), as a sole agent or in combination with other active ingredients wherein circulating endogenous estradiol concentration of treated women is maintained to a level in a range of 40 pg / mL to 85 pg / mL.
Owner:BAYER PHARMA AG
Therapeutic combinations comprising selective estrofen receptor modulator and parathyroid hormone
InactiveCN1305373AImprove bone qualityReduce the chance of fracturePeptide/protein ingredientsSkeletal disorderOsteoporotic boneSelective progesterone receptor modulator
This invention is directed to pharmaceutical combination compositions and methods comprising (-)-cis-6-phenyl-5-(4-(2-pyrrolidin-1-yl-ethoxy)-phenyl)-5,6,7,8-tetrahydronaphthalene-2-ol or a pharmaceutically acceptable salt thereof and parathyroid hormone or a biologically active fragment thereof, methods of using such compositions and kits containing such compositions. The compositions are useful for treating musculoskeletal frailty, including osteoporosis, osteoporotic fracture, low bone mass and frailty.
Owner:PFIZER PRODS ETAT DE CONNECTICUT
Sequential sprm/ progestin treatment
InactiveUS20100004214A1BiocideOrganic active ingredientsGynecologySelective progesterone receptor modulator
Owner:CHWALISZ KRISTOF
Copper intrauterine device
InactiveUS20150320766A1Inhibits motilityInhibits viabilityBiocideOrganic active ingredientsSide effectGynecology
The invention relates to a copper contraceptive intrauterine system (IUS) with a flexible frame, which system is further capable of releasing a selective progesterone receptor modulator (SPRM), such as ulipristal acetate, for reducing or preventing bleeding side effects.
Owner:LAB HRA PHARMA SA
Compositions and methods for suppressing endometrial proliferation
InactiveCN104997789AOrganic active ingredientsAntipyreticProgesteronesSelective progesterone receptor modulator
The subject matter of the instant invention is pertinent to the field of hormone therapy. More specifically, the subject matter of the instant invention concerns methods of treating estrogen-dependent conditions such as endometrial hyperplasia and endometrial cancer in a female undergoing estrogen and / or selective estrogen receptor modulator (SERM) therapy. The instant invention is also relevant to the suppression of endometrial proliferation. The instant invention is also relevant to the treatment of pain associated with endometriosis. The compositions for practicing the methods, comprising progesterone antagonists are also disclosed. Embodiments of the instant invention also disclose methods for identifying new selective progesterone receptor modulators for practicing disclosed methods of treatment.
Owner:APTALIS PHARMA
5-Cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds
The present invention relates to methods for modulating processes mediated by progesterone receptor using nonsteroidal compounds and compositions which may be high affinity, high specificity agonists, partial agonists (i.e., partial activators and / or tissue-specific activators) and / or antagonists for progesterone receptors.
![5-Cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/3f230340-4b76-41e4-abdd-2a85e0f53309/US20060194827A1-20060831-C00001.png "5-Cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds")
![5-Cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/3f230340-4b76-41e4-abdd-2a85e0f53309/US20060194827A1-20060831-C00002.png "5-Cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds")
![5-Cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/3f230340-4b76-41e4-abdd-2a85e0f53309/US20060194827A1-20060831-C00003.png "5-Cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds")
Owner:LIGAND PHARMA INC
Copper intrauterine device
InactiveUS20190008763A1Inhibits motilityInhibits viabilityOrganic active ingredientsInorganic active ingredientsSide effectGynecology
The invention relates to a copper contraceptive intrauterine system (IUS) with a flexible frame, which system is further capable of releasing a selective progesterone receptor modulator (SPRM), such as ulipristal acetate, for reducing or preventing bleeding side effects.
Owner:LAB HRA PHARMA SA
Oxa-steroids derivatives as selective progesterone receptor modulators
The present invention is directed to 7 oxa-estra-4,9-diene-3,17-dione derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by at least one progesterone or glucocorticoid receptor.
Owner:JANSSEN PHARMA NV
Sequential SPRM/progestin treatment
InactiveUS20050215535A1BiocideOrganic active ingredientsGynecologySelective progesterone receptor modulator
The methods provided herein comprise administering a selective progesterone receptor modulator (SPRM) during a first dosing period and at least one progestogen during a second dosing period. The dosing periods can run concomitantly or sequentially with or without a period where neither the SPRM nor the progestogen is administered.
Owner:ABBOTT ENDOCRINE INC
Selective androgen receptor modulators and methods of use thereof
InactiveCN1736371AHas oral bioavailabilityProlong biological half-lifeOrganic active ingredientsOrganic chemistryHormone Receptor ModulatorsSelective progesterone receptor modulator
This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of non-steroidal agonist compounds. The invention further provides compositions containing the selective androgen modulator compounds or the non-steroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.
Owner:UNIV OF TENNESSEE RES FOUND
Selective androgen receptor modulators and methods of use thereof
InactiveCN1736981AHas oral bioavailabilityProlong biological half-lifeOrganic active ingredientsOrganic chemistryHormone Receptor ModulatorsSpermatogenesis
This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of non-steroidal agonist compounds. The invention further provides compositions containing the selective androgen modulator compounds or the non-steroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.
Owner:UNIV OF TENNESSEE RES FOUND
Compositions and methods for suppressing endometrial proliferation
ActiveUS20100216756A1Prevent proliferationWeak affinityOrganic active ingredientsNervous disorderSelective progesterone receptor modulatorEndometrial cancer
The subject matter of the instant invention is pertinent to the field of hormone therapy. More specifically, the subject matter of the instant invention concerns methods of treating estrogen-dependent conditions such as endometrial hyperplasia and endometrial cancer in a female undergoing estrogen and / or selective estrogen receptor modulator (SERM) therapy. The instant invention is also relevant to the suppression of endometrial proliferation. The instant invention is also relevant to the treatment of pain associated with endometriosis. The compositions for practicing the methods, comprising progesterone antagonists are also disclosed. Embodiments of the instant invention also disclose methods for identifying new selective progesterone receptor modulators for practicing disclosed methods of treatment.
Owner:APTALIS PHARMA
Oxa-steroids derivatives as selective progesterone receptor modulators
The present invention is directed to novel 7-oxa-estra-4,9-diene-3,17-dione derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by at least one progesterone or glucocorticoid receptor.
Owner:JANSSEN PHARMA NV
5-substituted 7,9-difluoro-5H-chromeno[3,4-f]quinoline compounds as selective progesterone receptor modulator compounds
InactiveUS7163946B2Improve fertilityReduced fertilityBiocideOrganic chemistryPR - Progesterone receptorQuinoline
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by progesterone receptor. Also provided are methods of making such compounds and pharmaceutical compositions.
![5-substituted 7,9-difluoro-5H-chromeno[3,4-f]quinoline compounds as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/3ffa70df-13a6-462b-b19c-4c6e0afc2346/US07163946-20070116-C00001.png "5-substituted 7,9-difluoro-5H-chromeno[3,4-f]quinoline compounds as selective progesterone receptor modulator compounds")
![5-substituted 7,9-difluoro-5H-chromeno[3,4-f]quinoline compounds as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/3ffa70df-13a6-462b-b19c-4c6e0afc2346/US07163946-20070116-C00002.png "5-substituted 7,9-difluoro-5H-chromeno[3,4-f]quinoline compounds as selective progesterone receptor modulator compounds")
![5-substituted 7,9-difluoro-5H-chromeno[3,4-f]quinoline compounds as selective progesterone receptor modulator compounds](https://images-eureka.patsnap.com/patent_img/3ffa70df-13a6-462b-b19c-4c6e0afc2346/US07163946-20070116-C00003.png "5-substituted 7,9-difluoro-5H-chromeno[3,4-f]quinoline compounds as selective progesterone receptor modulator compounds")
Owner:LIGAND PHARMA INC
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