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1. 发明申请

WO2019209693A1 METHODS OF PREPARING REGIOSELECTIVE N-ALKYL TRIAZOLES 审中-公开
公开(公告)号：WO2019209693A1
公开(公告)日：2019-10-31
申请号：PCT/US2019/028473
申请日：2019-04-22
申请人： CORCEPT THERAPEUTICS, INC.
发明人： HUNT, Hazel , BREMAN, Arjen Christiaan , GRUIJTERS, Bas Wilhelmus Theodorus
IPC分类号： C07D249/04
摘要： Methods of preparing N-2 alkylated triazoles substantially free from N-1 and N-3 alkylated triazoles are disclosed. The methods include one-step alkylation methods and two-step alkylation methods for the preparation of N-alkylated triazoles.

2. 发明申请

WO2018049255A1 GLUCOCORTICOID RECEPTOR MODULATORS TO TREAT PANCREATIC CANCER 审中-公开
标题翻译：糖皮质激素受体调节剂治疗胰腺癌
公开(公告)号：WO2018049255A1
公开(公告)日：2018-03-15
申请号：PCT/US2017/050812
申请日：2017-09-08
申请人： CORCEPT THERAPEUTICS, INC.
发明人： HUNT, Hazel , BLOCK, Thaddeus S.
IPC分类号： A61K31/337 , A61K31/513 , A61K31/7068 , A61K31/4745
摘要： Methods and compositions for treating a subject hosting a non-ACTH-secreting pancreatic tumor are disclosed. The methods include administering to the subject a chemotherapeutic agent and a glucocorticoid receptor modulator (GRM), preferably a selective glucocorticoid receptor modulator (SGRM), to reduce the tumor load in the subject. The GRM may be a nonsteroidal GRM, and may be a nonsteroidal SGRM. The non-ACTH-secreting pancreatic tumor may be an exocrine pancreatic tumor. The nonsteroidal SGRM may be a nonsteroidal compound comprising: a fused azadecalin structure; a heteroaryl ketone fused azadecalin structure; or an octahydro fused azadecalin structure. Pharmaceutical compositions comprising a chemotherapeutic agent and a GRM are disclosed. The GRM in such pharmaceutical compositions may be a nonsteroidal GRM, and may be a SGRM, such as a nonsteroidal SGRM. The nonsteroidal SGRM may comprise: a fused azadecalin structure; a heteroaryl ketone fused azadecalin structure; or an octahydro fused azadecalin structure.
摘要翻译：公开了用于治疗患有非ACTH分泌性胰腺肿瘤的受试者的方法和组合物。该方法包括向受试者施用化疗剂和糖皮质激素受体调节剂（GRM），优选选择性糖皮质激素受体调节剂（SGRM），以降低受试者的肿瘤负荷。 GRM可能是非甾体GRM，可能是非甾体SGRM。非ACTH分泌型胰腺肿瘤可以是外分泌型胰腺肿瘤。非甾体SGRM可以是非甾族化合物，其包含：稠合的氮杂十六烷结构; 杂芳基酮稠合的阿扎德卡因结构; 或八氢稠合的阿扎德卡因结构。公开了包含化学治疗剂和GRM的药物组合物。这种药物组合物中的GRM可以是非甾体GRM，并且可以是SGRM，例如非甾体SGRM。非甾族SGRM可以包含：稠合的氮杂卡因结构; 杂芳基酮稠合的阿扎德卡因结构; 或八氢稠合的氮杂十字结构。

3. 发明申请

WO2017127448A1 DIFFERENTIAL DIAGNOSIS OF ECTOPIC CUSHING'S SYNDROME 审中-公开
标题翻译：异位冲动综合征的差异诊断
公开(公告)号：WO2017127448A1
公开(公告)日：2017-07-27
申请号：PCT/US2017/013974
申请日：2017-01-18
申请人： CORCEPT THERAPEUTICS, INC.
发明人： MORAITIS, Andreas G.
IPC分类号： A61B5/00 , G01N33/74
CPC分类号： G01N33/743 , A61B5/4227 , G01N33/74 , G01N2333/575 , G01N2333/723 , G01N2800/04 , G16H50/30
摘要： Improved methods and systems for differentially diagnosing ACTH-dependent Cushing's syndrome are provided herein. Treatment methods can use glucocorticoid receptor antagonists, which differentially affects the ratio of cortisol to ACTH levels in patients having Cushing's Disease versus patients having Ectopic Cushing's Syndrome. Methods for differentially diagnosing ACTH-dependent Cushing's syndrome can include obtaining baseline cortisol and ACTH levels of a patient, treating the patient with a glucocorticoid receptor antagonist (GRA) according to a protocol that would typically substantially elevate cortisol levels, obtaining post-treatment cortisol and ACTH levels of the patient, determining a differential relationship between baseline cortisol and ACTH levels and post-treatment cortisol and ACTH levels and providing a positive diagnosis based on the differential relationship.
摘要翻译：本文提供了用于区别诊断ACTH依赖性库欣综合征的改进方法和系统。治疗方法可以使用糖皮质激素受体拮抗剂，其差异地影响患有库欣病的患者与具有异位库欣综合征的患者的皮质醇与ACTH水平的比率。用于区别诊断ACTH依赖性库欣综合征的方法可以包括获得患者的基线皮质醇和ACTH水平，根据通常大体上提高皮质醇水平的方案用糖皮质激素受体拮抗剂（GRA）治疗患者，获得治疗后皮质醇和 ACTH水平，确定基线皮质醇和ACTH水平以及治疗后皮质醇和ACTH水平之间的差异关系，并根据差异关系提供阳性诊断。

4. 发明申请

WO2016140867A1 USE OF GLUCOCORTICOID RECEPTOR ANTAGONIST AND SOMATOSTATIN ANALOGUES TO TREAT ACTH-SECRETING TUMORS 审中-公开
标题翻译：使用葡萄糖激素受体拮抗剂和SOMATOSTATIN类似物治疗分泌性分泌肿瘤
公开(公告)号：WO2016140867A1
公开(公告)日：2016-09-09
申请号：PCT/US2016/019646
申请日：2016-02-25
申请人： CORCEPT THERAPEUTICS, INC.
发明人： MORAITIS, Andreas G. , BELANOFF, Joseph K.
IPC分类号： A61K45/06 , C07D413/06
CPC分类号： A61K31/567 , A61K31/437 , A61K31/4745 , A61K31/505 , A61K31/513 , A61K38/08 , A61K38/12 , A61K45/06 , A61K51/083 , A61P3/10 , A61P35/00 , A61K2300/00
摘要： Methods, compositions, and pharmaceutical formulations are provided for treatment of ACTH secreting tumors.
摘要翻译：提供方法，组合物和药物制剂用于治疗ACTH分泌性肿瘤。

5. 发明申请

WO2015077537A1 HETEROARYL-ETHER FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS 审中-公开
标题翻译：异氟醚混合阿卡曲林葡萄糖激素受体调节剂
公开(公告)号：WO2015077537A1
公开(公告)日：2015-05-28
申请号：PCT/US2014/066770
申请日：2014-11-21
申请人： CORCEPT THERAPEUTICS, INC.
发明人： HUNT, Hazel , WALTERS, Iain , RAY, Nicholas
IPC分类号： A61K31/437
CPC分类号： C07D471/04
摘要： The present invention provides heteroaryl ether fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
摘要翻译：本发明提供杂芳基醚稠合的十九烷基化合物和使用该化合物作为糖皮质激素受体调节剂的方法。

6. 发明申请

WO2005009382A3 ANTIGLUCOCORTICOID THERAPY FOR THE PREVENTION OF NEUROLOGICAL DAMAGE IN PREMATURE INFANTS 审中-公开
标题翻译：用于预防早产儿神经损伤的抗糖尿病药物治疗
公开(公告)号：WO2005009382A3
公开(公告)日：2005-09-29
申请号：PCT/US2004023592
申请日：2004-07-22
申请人： CORCEPT THERAPEUTICS INC , BELANOFF JOSEPH K
发明人： BELANOFF JOSEPH K
IPC分类号： A61K20060101 , A61K31/235 , A61K31/56 , A61K31/567 , A61K31/569 , A61K31/573 , A61K31/59 , A61K45/06
CPC分类号： A61K31/56 , A61K31/567 , A61K31/569 , A61K31/573 , A61K45/06 , A61K2300/00
摘要： This invention pertains to the discovery that agents which inhibit the binding of cortisol to its receptors can be used in methods for preventing neurological damage associated with glucocorticoid therapy in ventilator-dependent low birth weight preterm infants. Mifepristone, a potent glucocorticoid receptor antagonist, can be used in these methods.
摘要翻译：本发明涉及抑制皮质醇与其受体结合的药剂可用于预防呼吸机依赖性低出生体重早产儿中与糖皮质激素疗法相关的神经损伤的方法。米非司酮是一种有效的糖皮质激素受体拮抗剂，可用于这些方法。

7. 发明申请

WO2004041214A3 METHODS FOR TREATING MIGRAINE 审中-公开
标题翻译：用于处理MIGRAINE的方法
公开(公告)号：WO2004041214A3
公开(公告)日：2004-11-11
申请号：PCT/US0335328
申请日：2003-11-05
申请人： CORCEPT THERAPEUTICS INC , BELANOFF JOSEPH K
发明人： BELANOFF JOSEPH K
IPC分类号： A61K31/00 , A61K31/56 , A61K31/573 , A61K31/59
CPC分类号： A61K31/59 , A61K31/00 , A61K31/56 , A61K31/573
摘要： This invention relates to the discovery that agents capable of inhibiting the biological action of the glucocorticoid receptor can be used in methods for treating migraine in a subject.
摘要翻译：本发明涉及能够抑制糖皮质激素受体的生物学作用的药剂可以用于治疗受试者偏头痛的方法。

8. 发明申请

WO2003020216A1 METHODS FOR INHIBITING COGNITIVE DETERIORATION IN ADULTS WITH DOWN'S SYNDROME 审中-公开
标题翻译：用于抑制患者的综合征的认知检测方法
公开(公告)号：WO2003020216A1
公开(公告)日：2003-03-13
申请号：PCT/US2002/027576
申请日：2002-08-27
申请人： CORCEPT THERAPEUTICS, INC. , BELANOFF, Joseph, K.
发明人： BELANOFF, Joseph, K.
IPC分类号： A61K
CPC分类号： A61K31/573 , A61K31/56 , A61K31/567 , A61K31/575
摘要： This invention generally pertains to the field of psychiatry. In particular, this invention pertains to the discovery that agents capable of inhibiting the binding of cortisol to its receptors can be used in methods for preventing or reversing cognitive deterioration in adults with Down's syndrome. Mifepristone, a potent specific glucocorticoid receptor antagonist, can be used in these methods. The invention also provides a kit for preventing or reversing cognitive deterioration in a DS patient including a glucocorticoid receptor antagonist and instructional material teaching the indications, dosage and schedule of administration of the glucocorticoid receptor antagonist.
摘要翻译：本发明一般涉及精神病学领域。特别地，本发明涉及以下发现：能够抑制皮质醇与其受体结合的药剂可用于预防或逆转唐氏综合症患者的认知衰退的方法。米非司酮是一种有效的特异性糖皮质激素受体拮抗剂，可用于这些方法。本发明还提供了用于预防或逆转DS患者的认知恶化的试剂盒，其包括糖皮质激素受体拮抗剂和教导糖皮质激素受体拮抗剂施用的适应症，剂量和时间表的说明材料。

9. 发明申请

WO2013177559A3 HETEROARYL-KETONE FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS 审中-公开
标题翻译：异氟烷酮融合的阿卡曲林葡萄糖激素受体调节剂
公开(公告)号：WO2013177559A3
公开(公告)日：2014-01-16
申请号：PCT/US2013042732
申请日：2013-05-24
申请人： CORCEPT THERAPEUTICS INC
发明人： HUNT HAZEL , JOHNSON TONY , RAY NICHOLAS , WALTERS IAIN
IPC分类号： A61K31/5377 , C07D471/02
CPC分类号： C07D471/04
摘要： The present Invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. In some embodiments, the present invention provides a pharmaceutical cmnposition including a pharmaceutically acceptable excipient and the compound of formula I. In some embodiments, the present invention provides a method of modulating a glucocorticoid receptor, the method including contacting a glucocorticoid receptor with a compound of formula I, thereby modulating the glucocorticoid receptor, as well as a method of treating a disorder through modulating a glucocorticoid receptor, the method including administering to a subject in need of such treatment, a therapeutically eftective amount of a compound of formula (I), thereby treating the disorder.
摘要翻译：本发明提供杂芳基酮稠合的十九烷基化合物和使用该化合物作为糖皮质激素受体调节剂的方法。在一些实施方案中，本发明提供包含药学上可接受的赋形剂和式I化合物的药物定位。在一些实施方案中，本发明提供调节糖皮质激素受体的方法，所述方法包括将糖皮质激素受体与式I，从而调节糖皮质激素受体，以及通过调节糖皮质激素受体来治疗疾病的方法，所述方法包括向需要这种治疗的受试者施用治疗有效量的式（I）化合物，从而治疗病症。

10. 发明申请

WO2012094618A1 COMBINATION STEROID AND GLUCOCORTICOID RECEPTOR ANTAGONIST THERAPY 审中-公开
标题翻译：联合甾体和葡萄糖激素受体拮抗剂治疗
公开(公告)号：WO2012094618A1
公开(公告)日：2012-07-12
申请号：PCT/US2012/020521
申请日：2012-01-06
申请人： CORCEPT THERAPEUTICS, INC. , BELANOFF, Joe , LOCKEY, Peter
发明人： BELANOFF, Joe , LOCKEY, Peter
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： A61K31/437 , A61K31/573 , A61K45/06 , A61K2300/00
摘要： The present invention provides compositions of an anti-inflammatory glucocorticosteroid and a glucocorticoid receptor (GR) modulator useful for inhibiting glucocorticoid receptor induced transactivation without substantially inhibiting glucocorticoid receptor induced transrepression. Also provided are methods of treating a disorder or condition and reducing the side effects of glucocorticosteroid treatment, using the compositions of the present invention.
摘要翻译：本发明提供抗炎糖皮质激素和糖皮质激素受体（GR）调节剂的组合物，其可用于抑制糖皮质激素受体诱导的反式激活而基本上不抑制糖皮质激素受体诱导的转录抑制。还提供了使用本发明的组合物治疗疾病或病症并减少糖皮质激素治疗的副作用的方法。

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