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1.发明授权Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢异喹啉及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取公开(公告)号：US09499531B2
公开(公告)日：2016-11-22
申请号：US14737897
申请日：2015-06-12
发明人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
IPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D217/00 , C07D217/20 , C07D407/04
CPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/00 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.
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2.发明申请ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN 有权ARYL-和HETEROARYL取代的四氢喹啉和其用于阻断肾上腺素，多巴胺和丝氨酸蛋白酶的重复使用公开(公告)号：US20140243524A1
公开(公告)日：2014-08-28
申请号：US14268753
申请日：2014-05-02
发明人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
IPC分类号： C07D217/00 , C07D405/04 , C07D401/04 , C07D413/14 , C07D217/04 , C07D217/20 , C07D409/14 , C07D409/04 , C07D417/04
CPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/00 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.
摘要翻译： 本发明的化合物由式（I）中所示的化学结构表示：其中：指定为*的碳原子为R或S构型; 并且X是选自苯并呋喃基，苯并[b]噻吩基，苯并异噻唑基，苯并异恶唑基，吲唑基，吲哚基，异吲哚基，吲嗪基，苯并咪唑基，苯并恶唑基，苯并噻唑基，苯并三唑基，咪唑并[1,2-a 吡啶并[1,5-a]吡啶基，[1,2,4]三唑并[4,3-a]吡啶基，噻吩并[2,3-b]吡啶基，噻吩并[3,2-b] 二氢苯并噻吩基，二氢苯并呋喃基，二氢苯并噻吩基，四氢萘基，喹啉基，异喹啉基，4H-喹啉基，9H-喹啉基，喹唑啉基，噌啉基，酞嗪基，喹喔啉基， 苯并[1,2,3]三嗪基，苯并[1,2,4]三嗪基，2H-色烯基，4H-色烯基和稠合的双环碳环或稠合双环杂环，其任选被如所定义的取代基（数目为1至4） 在R14; 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。
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3.发明授权Aryl- and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢苯并氮杂及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取公开(公告)号：US09403776B2
公开(公告)日：2016-08-02
申请号：US14304833
申请日：2014-06-13
发明人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Ryan , Wenge Cui , Richard E. Olson
IPC分类号： C07D403/04 , C07D223/16 , C07D401/04 , C07D401/12 , C07D409/04 , C07D409/14 , C07D413/04 , C07D471/04 , C07D487/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
CPC分类号： C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
摘要翻译： 本发明的化合物由以下芳基 - 和杂芳基取代的四氢苯并吖庚因和具有式I（AE）和式（II）的二氢苯并氮杂衍生物表示：其中指定为*的碳原子为R或S构型， X和R 1 -R 9如本文所定义。
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4.发明授权Ligand-therapeutic agent conjugates, silicon-based linkers, and methods for making and using them 有权配体治疗剂缀合物，硅基接头，以及制造和使用它们的方法公开(公告)号：US09352049B2
公开(公告)日：2016-05-31
申请号：US14209460
申请日：2014-03-13
发明人： Peter R. Guzzo , David D. Manning
IPC分类号： A61K47/48 , C07D519/04 , A61K38/00
CPC分类号： A61K47/48023 , A61K31/337 , A61K31/475 , A61K38/00 , A61K47/551 , A61K47/6803 , A61K47/6889 , C07D519/04 , Y02A50/411
摘要： The present invention relates to ligand-therapeutic agent conjugate compounds, silicon linkers for the conjugate compounds, compositions, methods for making them, and methods for the treatment of cancer using the conjugate compounds. The silicon-based linkers described herein can be used to deliver desired therapeutic agents to particular cells or tissue types targeted by the ligand.
摘要翻译： 本发明涉及配体治疗剂缀合物化合物，用于缀合化合物的硅接头，组合物，其制备方法，以及使用该缀合物化合物治疗癌症的方法。 本文所述的硅基接头可用于将期望的治疗剂递送至由配体靶向的特定细胞或组织类型。
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公开(公告)号：US09045501B2
公开(公告)日：2015-06-02
申请号：US14203033
申请日：2014-03-10
发明人： Peter R. Guzzo , David D. Manning , William Earley
IPC分类号： A61K31/5517 , C07D513/06 , C07D487/04 , C07D513/04 , A61K31/439 , A61K31/55 , A61K45/06 , C07D453/02
CPC分类号： C07D513/06 , A61K31/439 , A61K31/55 , A61K31/5517 , A61K45/06 , C07D453/02 , C07D487/04 , C07D513/04
摘要： Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
摘要翻译： 公开了新的5-HT 3受体调节剂。 这些化合物用于治疗各种疾病，包括化疗诱发的恶心和呕吐，术后恶心呕吐和肠易激综合征。 制备这些化合物的方法也在本发明中描述。
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6.发明申请ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROBENZAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN 有权ARYL-和HETEROARYL取代的四氢苯并噻唑并用于阻断肾上腺素，多巴胺和丝氨酸蛋白酶公开(公告)号：US20140296514A1
公开(公告)日：2014-10-02
申请号：US14304833
申请日：2014-06-13
发明人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Fleming , Wenge Cui , Richard E. Olson
IPC分类号： C07D223/16 , C07D413/04 , C07D409/04 , C07D405/14 , C07D401/14 , C07D403/14 , C07D413/14 , C07D403/04 , C07D401/04
CPC分类号： C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
摘要翻译： 本发明的化合物由以下芳基 - 和杂芳基取代的四氢苯并吖庚因和具有式I（AE）和式（II）的二氢苯并氮杂衍生物表示：其中指定为*的碳原子为R或S构型， X和R 1 -R 9如本文所定义。
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7.发明申请LIGAND-THERAPEUTIC AGENT CONJUGATES, SILICON-BASED LINKERS, AND METHODS FOR MAKING AND USING THEM 审中-公开配体治疗药物联合用硅胶连接剂及其制备和使用方法公开(公告)号：US20160235858A1
公开(公告)日：2016-08-18
申请号：US15141885
申请日：2016-04-29
发明人： Peter R. Guzzo , David D. Manning
IPC分类号： A61K47/48 , A61K31/337 , A61K31/475
CPC分类号： A61K31/337 , A61K31/475 , A61K38/00 , A61K47/551 , A61K47/6803 , A61K47/6889 , C07D519/04 , Y02A50/411
摘要： The present invention relates to ligand-therapeutic agent conjugate compounds, silicon linkers for the conjugate compounds, compositions, methods for making them, and methods for the treatment of cancer using the conjugate compounds. The silicon-based linkers described herein can be used to deliver desired therapeutic agents to particular cells or tissue types targeted by the ligand.
摘要翻译： 本发明涉及配体治疗剂缀合物化合物，用于缀合化合物的硅接头，组合物，其制备方法，以及使用该缀合物化合物治疗癌症的方法。 本文所述的硅基接头可用于将期望的治疗剂递送至由配体靶向的特定细胞或组织类型。
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公开(公告)号：US09085531B2
公开(公告)日：2015-07-21
申请号：US14268753
申请日：2014-05-02
发明人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
IPC分类号： C07D403/04 , C07D217/02 , A61K31/47 , C07D217/00 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D217/20
CPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/00 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.
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9.发明申请LIGAND-THERAPEUTIC AGENT CONJUGATES, SILICON-BASED LINKERS, AND METHODS FOR MAKING AND USING THEM 有权配体治疗药物联合用硅胶连接剂及其制备和使用方法公开(公告)号：US20140274951A1
公开(公告)日：2014-09-18
申请号：US14209460
申请日：2014-03-13
发明人： Peter R. Guzzo , David D. Manning
IPC分类号： A61K47/48
CPC分类号： A61K47/48023 , A61K31/337 , A61K31/475 , A61K38/00 , A61K47/551 , A61K47/6803 , A61K47/6889 , C07D519/04 , Y02A50/411
摘要： The present invention relates to ligand-therapeutic agent conjugate compounds, silicon linkers for the conjugate compounds, compositions, methods for making them, and methods for the treatment of cancer using the conjugate compounds. The silicon-based linkers described herein can be used to deliver desired therapeutic agents to particular cells or tissue types targeted by the ligand.
摘要翻译： 本发明涉及配体治疗剂缀合物化合物，用于缀合化合物的硅接头，组合物，其制备方法，以及使用该缀合物化合物治疗癌症的方法。 本文所述的硅基接头可用于将期望的治疗剂递送至由配体靶向的特定细胞或组织类型。
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