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1. 发明申请

WO2006094934A8 SUBSTITUTED OXA-DIAZA-SPIRO-[5.5]-UNDECANONE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的OXA-DIAZA-SPIRO- [5.5] - 十一酮衍生物及其作为神经激肽原拮抗剂的用途
公开(公告)号：WO2006094934A8
公开(公告)日：2006-12-07
申请号：PCT/EP2006060419
申请日：2006-03-03
申请人： JANSSEN PHARMACEUTICA NV , JANSSENS FRANS EDUARD , COUPA SOPHIE , PONCELET ALAIN PHILIPPE , SCHOENTJES BRUNO
发明人： JANSSENS FRANS EDUARD , COUPA SOPHIE , PONCELET ALAIN PHILIPPE , SCHOENTJES BRUNO
IPC分类号： C07D498/10 , A61K31/537 , A61P25/18 , A61P25/24
CPC分类号： C07D498/10 , B82Y5/00
摘要： This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK 1 antagonistic activity, an NK 3 antagonistic activity, a combined NK 1 /NK 2 antagonistic activity and a combined NK 1 /NK 2 /NK 3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incont inence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
摘要翻译：本发明涉及具有神经激肽拮抗活性，特别是NK 1拮抗活性，NK 3拮抗活性，联合NK _{1 / NK _{2 拮抗活性和组合的NK _{1 / NK _{2 / NK _{3 拮抗活性，它们的制备，包含它们的组合物以及它们作为药物的用途，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁，肠易激综合征（IBS），昼夜节律紊乱， - 惊厥，疼痛，尤其是内脏和神经性疼痛，胰腺炎，神经原性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿障碍如尿失禁。根据本发明的化合物可以由通式（I）表示并且还包含其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为在权利要求1中。}}}}}

2. 发明申请

WO2010089327A2 INDOLE DERIVATIVES AS ANTICANCER AGENTS 审中-公开
标题翻译：吲哚衍生物作为抗癌剂
公开(公告)号：WO2010089327A2
公开(公告)日：2010-08-12
申请号：PCT/EP2010051316
申请日：2010-02-03
申请人： JANSSEN PHARMACEUTICA NV , SCHOENTJES BRUNO , DESCAMPS SOPHIE , AMBLARD NATHALIE CLAUDIE ISABELLE
发明人： SCHOENTJES BRUNO , DESCAMPS SOPHIE , AMBLARD NATHALIE CLAUDIE ISABELLE
IPC分类号： C07D401/12 , A61K31/435 , A61K31/44 , A61P35/00
CPC分类号： C07D401/12
摘要： The present invention provides compounds of formula (I), their use for the treatment of cancer as well as pharmaceutical compositions comprising said compounds of formula (I).
摘要翻译：本发明提供了式（I）化合物，它们用于治疗癌症的用途以及包含所述式（I）化合物的药物组合物。

3. 发明申请

WO2008132155A2 INHIBITORS OF THE BINDING BETWEEN HDM2 AND THE PROTEASOME 审中-公开
标题翻译： HDM2与抗生素之间的结合的抑制剂
公开(公告)号：WO2008132155A2
公开(公告)日：2008-11-06
申请号：PCT/EP2008055051
申请日：2008-04-25
申请人： JANSSEN PHARMACEUTICA NV , ARTS JANINE , BLATTNER CHRISTINE , KULIKOV ROMAN NIKOLAEVICH , VALCKX ANNEMIE FRANCINE , DESCAMPS SOPHIE , JANSSEN CORNELUS GERARDUS MARIA , SCHOENTJES BRUNO
发明人： ARTS JANINE , BLATTNER CHRISTINE , KULIKOV ROMAN NIKOLAEVICH , VALCKX ANNEMIE FRANCINE , DESCAMPS SOPHIE , JANSSEN CORNELUS GERARDUS MARIA , SCHOENTJES BRUNO
IPC分类号： C12Q1/25 , A61K31/4427 , A61K31/4439 , A61K38/10 , G06F19/00
CPC分类号： C07K14/82 , A61K31/4427 , A61K31/4439 , A61K38/00 , C12Q1/37 , G01N2333/9015 , G01N2500/02 , Y02A90/24 , Y02A90/26
摘要： This invention provides methods for determining whether a test compound interacts with the binding between HDM2 and the proteasome. It further provides compounds, pharmaceutical compositions comprising said test compound, and the use of said compounds and compositions, in particular as anti-cancer agent, even more particular for treating cell proliferative disorders in a subject.
摘要翻译：本发明提供了用于确定测试化合物是否与HDM2与蛋白酶体之间的结合相互作用的方法。它还提供化合物，包含所述测试化合物的药物组合物，以及所述化合物和组合物，特别是抗癌剂的用途，甚至更具体地用于治疗受试者的细胞增殖性疾病。

4. 发明授权

EP3126365B1 MACROCYLIC PYRIDINE DERIVATIVES 有权
公开(公告)号：EP3126365B1
公开(公告)日：2018-01-10
申请号：EP15713523
申请日：2015-04-02
申请人： JANSSEN PHARMACEUTICA NV
发明人： DIELS GASTON STANISLAS MARCELLA , SCHOENTJES BRUNO , VERSELE MATTHIAS LUC AIMÉ , BERTHELOT DIDIER JEAN-CLAUDE , WILLEMS MARC , VIELLEVOYE MARCEL , SOMMEN FRANÇOIS MARIA , WROBLOWSKI BERTHOLD , MEERPOEL LIEVEN
IPC分类号： C07D471/22 , A61K31/505 , A61P35/00 , C07D498/22
CPC分类号： C07D471/22 , C07D491/22 , C07D498/22 , C07D513/22 , Y02P20/582
摘要： wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

5. 发明专利

AU2015239098B2 Macrocylic pyrimidine derivatives 未知
公开(公告)号：AU2015239098B2
公开(公告)日：2019-08-01
申请号：AU2015239098
申请日：2015-04-02
申请人： JANSSEN PHARMACEUTICA NV
发明人： MEERPOEL LIEVEN , DIELS GASTON STANISLAS MARCELLA , SCHOENTJES BRUNO , VERSELE MATTHIAS LUC AIME , BERTHELOT DIDIER JEAN-CLAUDE , WILLEMS MARC , VIELLEVOYE MARCEL , EMBRECHTS WERNER CONSTANT JOHAN , WROBLOWSKI BERTHOLD
IPC分类号： C07D471/22 , A61K31/505 , A61P35/00 , C07D498/22
摘要： The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

6. 发明专利

AU2015239100B2 Macrocylic pyridine derivatives 未知
公开(公告)号：AU2015239100B2
公开(公告)日：2019-06-27
申请号：AU2015239100
申请日：2015-04-02
申请人： JANSSEN PHARMACEUTICA NV
发明人： DIELS GASTON STANISLAS MARCELLA , SCHOENTJES BRUNO , VERSELE MATTHIAS LUC AIME , BERTHELOT DIDIER JEAN-CLAUDE , WILLEMS MARC , VIELLEVOYE MARCEL , SOMMEN FRANCOIS MARIA , WROBLOWSKI BERTHOLD , MEERPOEL LIEVEN
IPC分类号： C07D471/22 , A61K31/505 , A61P35/00 , C07D498/22
摘要： The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

7. 发明专利

EA029758B1 МАКРОЦИКЛИЧЕСКИЕ ПРОИЗВОДНЫЕ ПИРИДИНА 未知
公开(公告)号：EA029758B1
公开(公告)日：2018-05-31
申请号：EA201692000
申请日：2015-04-02
申请人： JANSSEN PHARMACEUTICA NV
发明人： DIELS GASTON STANISLAS MARCELLA , SCHOENTJES BRUNO , VERSELE MATTHIAS LUC AIME , BERTHELOT DIDIER JEAN-CLAUDE , WILLEMS MARC , VIELLEVOYE MARCEL , SOMMEN FRANCOIS MARIA , WROBLOWSKI BERTHOLD , MEERPOEL LIEVEN
IPC分类号： C07D471/22 , A61K31/505 , A61P35/00 , C07D498/22
摘要： Изобретениеотноситсяк замещенныммакроциклическимпроизводнымпиримидинаформулы (I)гдепеременныеимеютзначения, определенныев формулеизобретения. Соединенияв соответствиис изобретениемобладают EF2K-ингибирующейактивностьюи необязательнотакже Vps34-ингибирующейактивностью. Изобретение, крометого, относитсяк способамполучениятакихновыхсоединений, кфармацевтическимкомпозициям, содержащимуказанныесоединенияв качествеактивногоингредиента, атакжек применениюуказанныхсоединенийв качествелекарственногопрепарата.

9. 发明专利

PE20161365A1 DERIVADOS MACROCICLICOS DE PIRIDINA 未知
公开(公告)号：PE20161365A1
公开(公告)日：2016-12-17
申请号：PE2016001843
申请日：2015-04-02
申请人： JANSSEN PHARMACEUTICA NV
发明人： BERTHELOT DIDIER JEAN-CLAUDE , DIELS GASTON STANISLAS MARCELLA , MEERPOEL LIEVEN , SCHOENTJES BRUNO , WROBLOWSKI BERTHOLD , VERSELE MATTHIAS LUC AIME , VIELLEVOYE MARCEL , WILLEMS MARC , SOMMEN FRANÇOIS MARIA
IPC分类号： A61K31/505 , A61P35/00 , C07D471/22 , C07D498/22
摘要： Se refiere a compuestos de formula I, donde: Xa, Xb y Xc son independientemente CH o N; X1 es -(CHR12)s-NR1-Xe-alcanodiil C1-C4- (SO2)p3- o (CH2)s-O-Xe-alcanodiil C1-C4-(SO2)p3-; Xe es C(=O)-, entre otros; a es NR4-C(=O)-[C(R5b)2]r, NR4-C(R5b)2-C(=O)- o C(=O)- NR4-C(R5b)2; b es i), donde Xd1 es CH o N, Xd2 es CH2 o NH; el anillo A es fenilo o piridilo; R1 es hidrogeno, alquilo C1-C4, entre otros; R12 es hidrogeno o alquilo C1-C4; o R1 y R12 se unen para formar alcanodiilo C1-C4, entre otros; s es 0, 1 o 2; p3 es es 0 o 1; R3 es hidrogeno, oxo, entre otros; R4 es hidrogeno, alquilo C1-C4 o alquiloxi C1-C4-alquilo C1-C4; R5b es hidrogeno, alquilo C1-C4, entre otros; p2 y r son 0, 1 o 2; R6 es hidrogeno, halo, entre otros; n es 1 o 2. Dichos compuestos son inhibidores de EF2K y opcionalmente tienen actividad inhibidora de Vps34, siendo utiles en el tratamiento de neoplasias malignas hematologicas y de tumores solidos como glioblastoma, meduloblastoma, entre otros

10. 发明专利

SG11201608241UA MACROCYLIC PYRIDINE DERIVATIVES 未知
公开(公告)号：SG11201608241UA
公开(公告)日：2016-10-28
申请号：SG11201608241U
申请日：2015-04-02
申请人： JANSSEN PHARMACEUTICA NV
发明人： DIELS GASTON STANISLAS MARCELLA , SCHOENTJES BRUNO , VERSELE MATTHIAS LUC AIMÉ , BERTHELOT DIDIER JEAN-CLAUDE , WILLEMS MARC , VIELLEVOYE MARCEL , SOMMEN FRANÇOIS MARIA , WROBLOWSKI BERTHOLD , MEERPOEL LIEVEN
IPC分类号： C07D471/22 , A61K31/505 , A61P35/00 , C07D498/22
摘要： wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

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