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41. 发明申请

US20180258043A1 PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING 审中-公开
公开(公告)号：US20180258043A1
公开(公告)日：2018-09-13
申请号：US15914351
申请日：2018-03-07
申请人： GENENTECH, INC. , CURIS, INC.
发明人： Janet L. GUNZNER-TOSTE , Daniel P. SUTHERLIN , Mark S. STANLEY , Liang BAO , Georgette M. CASTANEDO , Rebecca L. LALONDE , Shumei WANG , Mark E. REYNOLDS , Scott J. SAVAGE , Kimberly MALESKY , Michael S. DINA , Michael F.T. KOEHLER
IPC分类号： C07D213/16 , C07F9/58 , C07D417/04 , C07D413/14 , C07D213/56 , C07D417/14 , C07D213/06 , C07D413/12 , C07D409/12 , C07D405/12 , C07D401/14 , C07D401/12 , C07D417/12
CPC分类号： C07D213/16 , C07D213/06 , C07D213/56 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07F9/58
摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.

42. 发明授权

US09910050B2 Mutant smoothened and methods of using the same 有权
公开(公告)号：US09910050B2
公开(公告)日：2018-03-06
申请号：US15130223
申请日：2016-04-15
申请人： Curis, Inc. , Genentech, Inc.
发明人： Frederic J. de Sauvage , Gerrit J. P. Dijkgraaf , Thomas Januario , Robert L. Yauch
IPC分类号： C07K14/705 , C07K16/28 , G01N33/15 , G01N33/50 , G01N33/74
CPC分类号： G01N33/74 , C07K14/705 , G01N2333/726 , G01N2500/10
摘要： The emergence of mutations in tyrosine kinases following treatment of cancer patients with molecular-targeted therapy represents a major mechanism of acquired drug resistance. Here, we describe a mutation in the serpentine receptor, Smoothened (SMO), which results in resistance to a Hedgehog (Hh) pathway inhibitor in medulloblastoma. A single amino acid substitution in a conserved aspartic acid residue of SMO maintains Hh signaling, but results in the inability of the Hh pathway inhibitor, GDC-0449, to bind SMO and suppress the pathway. This mutation was not only acquired in a GDC-0449-resistant mouse model of medulloblastoma, but was identified in a Medulloblastoma patient following relapse on GDC-0449. The invention provides screening methods to detect SMO mutations and methods to screen for drugs that specifically modulate mutant SMO exhibiting drug resistance.

43. 发明申请

US20180029984A1 PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING 审中-公开
公开(公告)号：US20180029984A1
公开(公告)日：2018-02-01
申请号：US15723805
申请日：2017-10-03
申请人： GENENTECH, INC. , CURIS, INC.
发明人： Janet L. GUNZNER-TOSTE , Daniel SUTHERLIN , Mark S. STANLEY , Liang BAO , Georgette M. CASTANEDO , Rebecca L. LALONDE , Shumei WANG , Mark E. REYNOLDS , Scott J. SAVAGE , Kimberly MALESKY , Michael S. DINA , Michael F.T. KOEHLER
IPC分类号： C07D213/16 , C07D417/04 , C07F9/58 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D213/38 , C07D417/12
CPC分类号： C07D213/16 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/58
摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.

44. 发明申请

US20160058742A1 FUSED AMINO PYRIDINE AS HSP90 INHIBITORS 有权
标题翻译：熔融氨基吡啶作为HSP90抑制剂
公开(公告)号：US20160058742A1
公开(公告)日：2016-03-03
申请号：US14681310
申请日：2015-04-08
申请人： Curis, Inc.
发明人： Xiong Cai , Changgeng Qian , Haixiao Zhai
IPC分类号： A61K31/437 , A61K31/4545
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4545 , Y02A50/411
摘要： The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
摘要翻译：本发明涉及含有融合氨基吡啶核心的HSP90抑制剂，其可用作HSP90的抑制剂及其在治疗HSP90相关疾病和病症如癌症，自身免疫性疾病或神经变性疾病中的用途。

45. 发明申请

US20140155606A1 QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY 审中-公开
标题翻译：基于喹喔啉的含有抑制锌结合蛋白的EGFR抑制剂
公开(公告)号：US20140155606A1
公开(公告)日：2014-06-05
申请号：US13894542
申请日：2013-05-15
申请人： Curis, Inc.
发明人： Changgeng Qian , Xiong Cai , Stephen Gould
IPC分类号： C07D239/94
CPC分类号： C07D239/94
摘要： The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (I) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.
摘要翻译：本发明涉及含有下述式（I）的锌结合部分的衍生物的喹唑啉。这些化合物具有作为表皮生长因子受体酪氨酸激酶（EGFR-TK）抑制剂的增强和意想不到的性质，并且可用于治疗EGFR-TK相关疾病和疾病如癌症。这些化合物还可以作为HDAC抑制剂。

46. 发明申请

US20130190350A1 Mediators of Hedgehog Signaling Pathways, Compositions and Uses Related Thereto 失效
公开(公告)号：US20130190350A1
公开(公告)日：2013-07-25
申请号：US13712525
申请日：2012-12-12
申请人： Curis, Inc.
发明人： Lee L. RUBIN , Oivin GUICHERIT , Stephen PRICE , Edward Andrew BOYD
IPC分类号： C07D263/57 , C07D235/18 , C07D401/12 , C07D405/12 , C07D471/04 , C07D413/12
CPC分类号： C07D263/57 , A61K31/395 , A61K31/4184 , A61K31/423 , A61K31/428 , C07D235/18 , C07D401/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.

47. 发明申请

US20040127474A1 Regulators of the hedgehog pathway, compositions and uses related thereto 审中-公开
标题翻译：刺猬路径的调节剂，与之相关的组合物和用途
公开(公告)号：US20040127474A1
公开(公告)日：2004-07-01
申请号：US10735116
申请日：2003-12-12
申请人： Curis, Inc.
发明人： Henryk Dudek , Benxiu Ji
IPC分类号： A61K031/56 , A61K031/13
CPC分类号： A61K31/585 , A61K31/35 , A61K31/56 , A61K31/58 , A61K31/70 , Y10S514/863
摘要： The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.
摘要翻译：本发明提供用于抑制由刺猬获得功能，功能丧失功能或平滑增益功能引起的异常生长状态的可用方法和试剂，包括使细胞与化合物如多肽或小分子接触其量足以控制异常生长状态，例如，激发正常的ptc途径或拮抗平滑或刺猬活性。本发明进一步提供了用于改善hedgehog功能丧失功能，ptc功能增益或平滑功能丧失的后果的可用方法和试剂，包括使细胞与化合物如多肽或小分子接触，其量足以改善。在某些实施方案中，主题化合物，例如cAMP类似物，腺苷酸环化酶激动剂或cAMP磷酸二酯酶抑制剂调节cAMP水平，其依次调节刺猬蛋白通路的活性。

48. 发明授权

US11643401B2 Crystal forms of immunomodulators 有权
公开(公告)号：US11643401B2
公开(公告)日：2023-05-09
申请号：US17350445
申请日：2021-06-17
申请人： Curis, Inc.
发明人： Shu Yu
IPC分类号： C07D271/06
CPC分类号： C07D271/06 , C07B2200/13
摘要： The invention relates to crystalline forms of a 3-substituted 1,2,4-oxadiazole compound, including an anhydrous crystalline form, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for pharmaceutical, veterinary, and agriculturally-relevant uses.

49. 发明授权

US11597732B2 Phosphoinositide 3-kinase inhibitors with a zinc binding moiety 有权
公开(公告)号：US11597732B2
公开(公告)日：2023-03-07
申请号：US17585701
申请日：2022-01-27
申请人： Curis, Inc.
发明人： Xiong Cai , Haixiao Zhai , Chengjung Lai , Changgeng Qian
IPC分类号： C07D495/04 , C07D491/04 , C07D413/14 , A61K31/535
摘要： The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

50. 发明申请

US20220370422A1 COMPOUNDS AND COMPOSITIONS FOR TREATING HEMATOLOGICAL DISORDERS 有权
公开(公告)号：US20220370422A1
公开(公告)日：2022-11-24
申请号：US17566371
申请日：2021-12-30
申请人： Curis, Inc.
发明人： Robert Booher
IPC分类号： A61K31/437 , A61K31/5377 , A61P35/02 , A61K45/06 , A61K31/4545 , A61K31/496
摘要： The present invention provides methods of treating hematological disorders and solid malignant tumors, using substituted indazole compounds and pharmaceutically acceptable salts thereof. The compounds inhibit IRAK4 and BCL-2 kinases.

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