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公开(公告)号:US12109272B2
公开(公告)日:2024-10-08
申请号:US17902701
申请日:2022-09-02
Applicant: Corcept Therapeutics Incorporated
Inventor: Stacie Shepherd , Joseph K. Belanoff
IPC: A61K47/64 , A61K31/337 , A61K31/4745 , A61P15/00 , A61P35/00
CPC classification number: A61K47/643 , A61K31/337 , A61K31/4745 , A61P15/00 , A61P35/00 , A61K31/4745 , A61K2300/00 , A61K31/337 , A61K2300/00
Abstract: Methods and compositions for treating cancer (e.g., ovarian, fallopian tube, uterine, cervical, vaginal, vulvar, or peritoneal cancer) are disclosed. The methods include intermittent administration of a glucocorticoid receptor modulator (GRM), such as a non-steroidal GRM (e.g., relacorilant), which may be orally administered, along with a cancer chemotherapy agent (such as, e.g., bevacizumab) to the patient. The GRM may be administered: at intervals separated by at least one day without GRM administration; by a schedule linked to the cancer chemotherapy schedule (e.g., a weekly chemotherapy regimen); on the day of, or the day before, or the day after, chemotherapy administration; by combinations thereof; and/or on other days. Ovarian cancer patients receiving intermittent relacorilant administration along with nab-paclitaxel administration had improved overall survival, improved progression free survival, improved duration of response, and other benefits as compared to patients not receiving relacorilant while receiving nab-paclitaxel.
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2.
公开(公告)号:US20240317742A1
公开(公告)日:2024-09-26
申请号:US18584163
申请日:2024-02-22
Applicant: Corcept Therapeutics Incorporated
Inventor: Hazel Joan Hunt , Gary Patrick Reid , Jeffrey Mark Dener , Adam Daisuke Gammack Yamagata , Alexander Fergus Williams , Liam Joseph Badiola , Evangeline Rose Newby
IPC: C07D471/04 , C07D217/26
CPC classification number: C07D471/04 , C07D217/26
Abstract: The present invention provides methods of preparing intermediates of heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators, and compositions having low impurity levels.
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公开(公告)号:US20240245659A1
公开(公告)日:2024-07-25
申请号:US18444342
申请日:2024-02-16
Applicant: Corcept Therapeutics Incorporated
Inventor: Andreas Moraitis
IPC: A61K31/437 , A61K31/4196 , A61K45/06 , A61P5/38
CPC classification number: A61K31/437 , A61K31/4196 , A61K45/06 , A61P5/38
Abstract: Methods and uses are disclosed for treating a subject suffering from a disorder selected from a liver disorder, Cushing's syndrome, or Cushing's Disease, cancer, an infection, an inflammatory condition, a cardiovascular, endocrine, or kidney disease, and combinations thereof, or other disorder for which they may be administered a drug which may cause liver toxicity, without adverse effects on the liver. Such liver disorders include fatty liver diseases are effective for reducing high levels of liver enzymes with a favorable safety profile. The methods and uses comprise administering to the subject an effective amount of a selective nonsteroidal glucocorticoid receptor modulator such as relacorilant, including methods and uses in combination with another drug, without adverse effects on liver enzyme levels, or on liver function. In embodiments, the other drug may be a drug that may cause liver toxicity, such as drugs that inhibit CYP3A enzymes, e.g., itraconazole or ketoconazole.
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公开(公告)号:US20240156806A1
公开(公告)日:2024-05-16
申请号:US18496134
申请日:2023-10-27
Applicant: Corcept Therapeutics Incorporated
Inventor: Grace Mann , Iulia Cristina Tudor , William Guyer , Hazel Hunt , Joseph Custodio
IPC: A61K31/4738 , A61K31/4152 , A61K31/428 , A61P25/28
CPC classification number: A61K31/4738 , A61K31/4152 , A61K31/428 , A61P25/28
Abstract: Applicant discloses methods and compositions for treating a patient suffering from amyotrophic lateral sclerosis (ALS) comprising administration of a heteroaryl ketone fused azadecalin compound. In embodiments, the heteroaryl ketone fused azadecalin compound is dazucorilant: (R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl) sulfonyl)-4, 4a, 5,6,7,8-hexahydro-1-H-pyrazolo[3,4-g]isoquinolin-4a-yl) (pyridin-2-yl)methanone, having the chemical structure illustrated as
Suitable doses include daily administration of 150 milligrams and 300 milligrams of dazucorilant. Suitable doses include daily administration of dazucorilant with food, or with water, or with food and water. Daily administration of dazucorilant is effective to increase dazucorilant exposure up to about 2-fold when continued for seven days or more. Administration of such a heteroaryl ketone fused azadecalin compound may comprise oral administration, enteral administration, or other administration. Pharmaceutical compositions comprising dazucorilant are useful in the treatment of patients suffering from ALS. Suitable pharmaceutical compositions comprising dazucorilant include, e.g., pharmaceutical compositions for oral administration and pharmaceutical compositions for enteral administration.-
公开(公告)号:US20240100052A1
公开(公告)日:2024-03-28
申请号:US18518289
申请日:2023-11-22
Applicant: Corcept Therapeutics Incorporated
Inventor: Ada Lee , Andreas Grauer , Joseph Belanoff
IPC: A61K31/513 , A61P1/16
CPC classification number: A61K31/513 , A61P1/16
Abstract: Applicant discloses methods and compositions for reducing liver fat and for treating fatty liver diseases (e.g., non-alcoholic fatty liver disease (NAFLD) including nonalcoholic steatohepatitis (NASH) and nonalcoholic cirrhosis; alcohol related fatty liver diseases including, alcohol fatty liver disease (AFL), alcoholic steatohepatitis (ASH), and alcoholic cirrhosis; and liver fibrosis). Significant liver fat reductions were obtained in human patients after only between 30 to 44 days of administration of 600 mg/day or 900 mg/day of the cyclohexyl pyrimidine glucocorticoid receptor modulator miricorilant. Liver fat reductions ranged from 38.5% to 73.8% (magnetic resonance imaging measurements in 4 of 5 patients receiving miricorilant, measured between 16-64 days after cessation of miricorilant administration). A further effect of miricorilant was an increase in liver alanine amino transferase (ALT) and aspartate amino transferase (AST). Mouse studies showed that miricorilant reduced measures of NAFLD, body weight, liver weight, and liver collagen and galectin-3 levels.
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6.
公开(公告)号:US11925626B2
公开(公告)日:2024-03-12
申请号:US17950902
申请日:2022-09-22
Applicant: Corcept Therapeutics Incorporated
Inventor: Ian Scott , Travis Lemons , Yip-Fong Chia
IPC: A61K31/4375 , A61K9/00 , A61K9/48 , A61K31/437 , A61K47/10 , A61K47/14 , A61K47/26
CPC classification number: A61K31/437 , A61K9/0053 , A61K9/4808 , A61K9/4866 , A61K47/10 , A61K47/14 , A61K47/26
Abstract: Disclosed herein are novel formulations containing relacorilant ((R)-(1-(4-fluorophenyl)-6-(1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone) that are suitable for administration, including oral administration, to patients suffering from disorders amenable to treatment by glucocorticoid receptor modulators (GRMs). Single unit dosage forms comprise softgel capsules containing these formulations. Such softgel capsules may contain, e.g., relacorilant formulations containing 25 milligrams (mg), 50 mg, 100 mg, 200 mg, 300 mg, 400 mg, 500 mg, or other amounts of relacorilant. These novel formulations and single unit dosage forms may be used to treat diseases and disorders including Cushing's syndrome, Cushing's Disease, and other disorders.
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公开(公告)号:US11827608B2
公开(公告)日:2023-11-28
申请号:US17556786
申请日:2021-12-20
Applicant: Corcept Therapeutics Incorporated
Inventor: Jeffrey Mark Dener , Hazel Joan Hunt , Nicholas David Tyrrell
IPC: C07D239/10 , C07D239/36 , C07D239/54
CPC classification number: C07D239/10 , C07D239/36 , C07D239/54
Abstract: The present invention provides methods of preparing 2-amino-6-((1r,4r)-4-phenylcyclohexyl)-5-(3-(trifluoromethyl)benzyl)pyrimidin-4(3H)-one, and 2-amino-6-((1r,4r)-4-phenylcyclohexyl)-5-(3-(trifluoromethyl)benzyl)pyrimidin-4(3H)-one monohydrate, as well as new intermediate compounds.
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8.
公开(公告)号:US20230346774A1
公开(公告)日:2023-11-02
申请号:US17793271
申请日:2021-02-10
Applicant: Corcept Therapeutics Incorporated
Inventor: Andrew E. Greenstein , Andreas Grauer , Stacie Peacock Shepherd
IPC: A61P35/00 , A61K39/395 , A61K31/4745 , A61K31/337
CPC classification number: A61K31/4745 , A61K31/337 , A61K39/3955 , A61P35/00 , A61K2039/505
Abstract: Methods of improving immune function in a cancer patient having a solid tumor are disclosed. The improvement in immune function may slow or stop tumor growth, and may reduce tumor load. Methods include administering effective amounts of a cancer treatment and a nonsteroidal glucocorticoid receptor modulator (GRM) or selective GRM (SGRM). The cancer treatment may include administration of a checkpoint inhibitor. GRM or SGRM administration may induce checkpoint-inhibitor sensitivity in the cancer. Improved immune function may include increased CD8+ T-cell activation, increased pro-inflammatory cytokine secretion, increased TNFα secretion, increased IFNy secretion, and other changes as compared to such activation and secretion prior to GRM administration. In embodiments, immune function is improved after 1, 2, 3, or more days of GRM administration. Other patient characteristics may also be improved by the methods disclosed herein. GRMs include heteroaryl-ketone fused azadecalin and octahydro fused azadecalin GRMs. GRM administration includes oral GRM administration.
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公开(公告)号:US20230212128A1
公开(公告)日:2023-07-06
申请号:US18061745
申请日:2022-12-05
Applicant: Corcept Therapeutics Incorporated
Inventor: Hazel Joan Hunt , Lorraine Donaghy , Keith Lorimer , Nathan Jay Dixon , Jeffrey Mark Dener
IPC: C07D239/54
CPC classification number: C07D239/54 , C07B2200/13
Abstract: The present invention provides crystalline forms of (E)-6-(4-Phenylcyclohexyl)-5-(3-trifluoromethylbenzyl)-1H-pyrimidine-2,4-dione, and methods of making and using the same.
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10.
公开(公告)号:US11684612B2
公开(公告)日:2023-06-27
申请号:US18084866
申请日:2022-12-20
Applicant: Corcept Therapeutics Incorporated
Inventor: Andreas Moraitis
IPC: A61K31/437 , A61P5/44
CPC classification number: A61K31/437 , A61P5/44
Abstract: Methods and compositions are disclosed for diagnosing a patient suspected of suffering from, and for treating a patient suffering from, a disorder such as hypercortisolemia, metabolic syndrome, pre-diabetes, diabetes, Cushing's syndrome, Cushing's Disease, hyperglycemia secondary to hypercortisolemia, a liver disease, a cardiac disorder, high blood pressure, a blood clotting disorder, a cancer, a psychological disorder, weight gain, a disorder of glucose control, a bone disorder (e.g., osteoporosis), hypogonadism, pseudoacromegaly, pituitary tumors, functional hypercortisolism, ACTH secreting tumors, peripheral neuropathy, dyslipidemia and other disorders.
The methods and compositions include administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (GRM). The preferred heteroaryl-ketone fused azadecalin GRM is relacorilant ((R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone). In some cases, the GRM (e.g., relacorilant) is orally administered. In some cases, the GRM (e.g., relacorilant) is orally administered without food.
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