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1. 发明申请

US20160145279A1 STAT6 INHIBITORS 有权
标题翻译： STAT6抑制剂
公开(公告)号：US20160145279A1
公开(公告)日：2016-05-26
申请号：US14889802
申请日：2014-05-08
申请人： Board of Regents, The University of Texas System , Baylor College of Medicine
发明人： John S. McMURRAY , Pijus Kumar MANDAL , Pietro MORLACCHI , Morgan KNIGHT , David B. CORRY
IPC分类号： C07F9/6561 , C07F9/553 , C07F9/62 , C07F9/6533 , C07F9/6509 , C07F9/60 , C07F9/572 , C07F9/6558
CPC分类号： C07F9/6561 , A61K9/0043 , A61K9/0073 , A61K45/06 , C07F9/12 , C07F9/5532 , C07F9/5535 , C07F9/572 , C07F9/5725 , C07F9/5728 , C07F9/60 , C07F9/62 , C07F9/650952 , C07F9/6533 , C07F9/65583 , C07K5/06034 , C07K5/06139
摘要： The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer.
摘要翻译：本公开提供可用于抑制STAT6途径的化合物。还提供了相关的药物组合物和使用该化合物的方法。在一些实施方案中，所述化合物可用于治疗疾病，例如过敏性肺病，过敏性鼻炎，慢性肺阻塞性疾病或癌症。

2. 发明申请

US20120277189A1 WATER-SOLUBLE BENZOAZEPINE COMPOUND AND ITS PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：水溶性苯并噻唑化合物及其药物组合物
公开(公告)号：US20120277189A1
公开(公告)日：2012-11-01
申请号：US13461665
申请日：2012-05-01
申请人： Makoto Komatsu , Fumitaka Goto , Yasuhiro Menjo , Keigo Yamada , Takakuni Matsuda , Yusuke Kato
发明人： Makoto Komatsu , Fumitaka Goto , Yasuhiro Menjo , Keigo Yamada , Takakuni Matsuda , Yusuke Kato
IPC分类号： C07F9/553 , A61P7/02 , A61P9/12 , A61P7/00 , A61K31/675 , A61P9/08
CPC分类号： C07F9/5535 , Y02P20/55
摘要： The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.
摘要翻译：本发明提供由以下通式（1）表示的苯并吖庚因化合物或其盐，其中R表示氢原子，任选被保护基保护的羟基等，R 1表示氢原子或羟基保护基基团，X表示氧原子或硫原子。本发明的苯并吖庚因化合物及其盐在水中的溶解性高，适合用于注射。

3. 发明申请

US20110082110A1 WATER-SOLUBLE BENZOAZEPINE COMPOUND AND ITS PHARMACEUTICAL COMPOSITION 审中-公开
公开(公告)号：US20110082110A1
公开(公告)日：2011-04-07
申请号：US12966629
申请日：2010-12-13
申请人： Makoto Komatsu , Fumitaka Goto , Yasuhiro Menjo , Keigo Yamada , Takakuni Matsuda , Yusuke Kato
发明人： Makoto Komatsu , Fumitaka Goto , Yasuhiro Menjo , Keigo Yamada , Takakuni Matsuda , Yusuke Kato
IPC分类号： A61K31/675 , C07F9/553 , A61P7/02 , A61P9/08 , A61P13/12
CPC分类号： C07F9/5535 , Y02P20/55
摘要： The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

4. 发明申请

US20110071084A1 BENZAZEPINE DERIVATIVES USEFUL AS VASOPRESSIN ANTAGONISTS 有权
标题翻译：苯并噻吩衍生物可用作VASOPRESSIN拮抗剂
公开(公告)号：US20110071084A1
公开(公告)日：2011-03-24
申请号：US12666751
申请日：2008-06-26
申请人： Kazumi Kondo , Yasuhiro Menjo , Takahiro Tomoyasu , Shin Miyamura , Yuso Tomohira , Takakuni Matsuda , Keigo Yamada , Yusuke Kato
发明人： Kazumi Kondo , Yasuhiro Menjo , Takahiro Tomoyasu , Shin Miyamura , Yuso Tomohira , Takakuni Matsuda , Keigo Yamada , Yusuke Kato
IPC分类号： A61K31/55 , C07D223/16 , C07D403/12 , C07F9/553 , C07D405/12 , C07D413/12 , C07D401/12 , C07D405/14 , C07K5/083 , A61K31/675 , A61K38/06 , A61K38/05 , A61P9/12 , A61P9/00 , A61P7/02
CPC分类号： C07D223/16 , C07D405/12 , C07F9/5535 , Y02P20/55
摘要： The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxo-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.
摘要翻译：本发明提供苯并氮杂化合物，其可以长时间保持托伐普坦的血液水平，从而能够提供所需的药物作用。本发明的苯并氮杂化合物由通式（1）表示，其中R1表示-CO-（CH2）n-COR2基团（其中n为1〜4的整数，R2为（2-1）羟基基团;（2-2）任选被羟基，低级烷酰基，低级烷酰氧基，低级烷氧基羰基氧基，环烷氧基羰基氧基或5-甲基-2-氧代-1,3-二氧戊环的低级烷氧基，二氧代-4-基;或（2-3）任选被羟基 - 低级烷基取代的氨基）等。

5. 发明授权

US07629379B2 Substituted phosphonate fluorescent sensors and use thereof 失效
公开(公告)号：US07629379B2
公开(公告)日：2009-12-08
申请号：US10557073
申请日：2004-05-14
申请人： John Robert Howe Wilson , Alice Caroline Sullivan , Siud Pui Man , Lesley Robson
发明人： John Robert Howe Wilson , Alice Caroline Sullivan , Siud Pui Man , Lesley Robson
IPC分类号： A61K31/35 , C07F9/28
CPC分类号： C07F9/65616 , C07F9/3882 , C07F9/4006 , C07F9/4028 , C07F9/4056 , C07F9/5535 , C07F9/5728 , C07F9/60 , C07F9/64 , C07F9/65031 , C07F9/65324 , C07F9/65335 , C07F9/6541 , C07F9/65522
摘要： The invention relates to new compounds of formula (1) wherein R is hydrogen or a linear or branched C1-40alkyl; where X is O, S, or NR1 where R1 is a hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2-40 alkynyl group, an aryl, a heteroaryl or C1-40 alkylaryl or alkylheteroaryl group and where one or both of C and D is OR2, SR2, NR3R4 where R2, R3 and R4 are each independently hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2-40 alkynyl group, an aryl or C1-40 alkylaryl group or a linear or branched C1-40 alkyl NR5R6 chain where R5 and R6 are each independently hydrogen, a linear or branched C1-40 alkyl; or an optionally complex metal ion Mn+/n wherein n is an integer from 1 to 8; or where one or both of C and D are amino acids or nucleic acids attached via either N, O or S; and wherein m is an integer from 1 to 8; and wherein either: I) A is a known aryl or heteroaryl fluorescent group and B is hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2- 40 alkynyl group, an aryl, a heteroaryl or C1-40 alkylaryl or alkylheteroaryl group or phosphonate P(O)(OR2)2; II) B is a known aryl or heteroaryl fluorescent group and A is hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2-40 alkynyl group, an aryl, a heteroaryl or C1-40 alkylaryl or alkylheteroaryl group or a linear or branched C1-40 alkyl NR5R6 chain, or a linear or branched C1-40 alkyl mono or di ester C1-40 alkylphosphonate or a linear or branched C1-40 alkylphosphonic acid; III) Both A and B are known aryl or heteroaryl fluorescent groups. The compounds are useful as fluorescent sensors for metal cations and have the advantages of excellent water solubility, selectivity and sensitivity to a variety of metal cations even in the presence of high concentrations of Ca+2 Na+ and K+, good cell permeability, flexible and simple syntheses, ease of attachment to polymers and bio-polymers to aid the identification of both chemical and biological processes as well as for assaying physiological samples and for the attachment to surfaces such as glasses, ceramics and apatites.

6. 发明申请

US20050107608A1 Ligands for use in catalytic processes 审中-公开
标题翻译：用于催化过程的配体
公开(公告)号：US20050107608A1
公开(公告)日：2005-05-19
申请号：US10494083
申请日：2002-11-30
申请人： Stephan Deblon , Hansjorg Gruzmacher , Pascal Marie , Hartmut Schonberg
发明人： Stephan Deblon , Hansjorg Gruzmacher , Pascal Marie , Hartmut Schonberg
IPC分类号： B01J27/18 , B01J31/24 , C07B61/00 , C07C5/03 , C07C5/05 , C07C13/26 , C07C13/263 , C07C43/196 , C07C49/753 , C07C209/52 , C07C209/70 , C07C211/27 , C07C211/48 , C07C231/12 , C07C231/18 , C07C233/11 , C07F7/08 , C07F9/24 , C07F9/36 , C07F9/48 , C07F9/50 , C07F9/553 , C07F9/572 , C07F9/58 , C07F9/6568 , C07F9/6571 , C07F9/6574 , C07F9/6584 , C07F15/00 , C07F15/06 , C07F9/6512
CPC分类号： B01J31/2447 , B01J31/1855 , B01J31/187 , B01J31/188 , B01J31/2295 , B01J31/2419 , B01J31/2438 , B01J2231/645 , B01J2531/16 , B01J2531/82 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/828 , B01J2531/845 , B01J2531/847 , C07B2200/07 , C07C5/03 , C07C17/16 , C07C209/52 , C07C231/12 , C07C231/18 , C07C253/30 , C07C303/08 , C07C303/38 , C07C303/40 , C07C2531/22 , C07C2601/18 , C07C2603/32 , C07F7/0829 , C07F9/4883 , C07F9/5018 , C07F9/5027 , C07F9/5045 , C07F9/5535 , C07F9/572 , C07F9/58 , C07F9/65683 , C07F9/65719 , C07F9/65844 , C07F15/0033 , C07F15/006 , C07F15/0073 , C07F15/0086 , C07F15/06 , C07C309/86 , C07C311/16 , C07C311/29 , C07C25/22 , C07C255/47 , C07C23/18 , C07C211/48 , C07C13/26 , C07C233/05
摘要： The invention relates to novel phosphorus compounds, to a method for producing said phosphorus compounds and their intermediate products. The invention also relates to the catalysts produced according to the invention on the basis of the phosphorus compounds and to their use in catalytic processes, especially in asymmetric catalytic processes.
摘要翻译：本发明涉及新型磷化合物，涉及一种生产所述磷化合物及其中间产物的方法。本发明还涉及根据本发明生产的基于磷化合物的催化剂及其在催化方法中的用途，特别是在不对称催化方法中。

7. 发明授权

US3501461A Azabicyclic phosphonate 失效
标题翻译：偶氮磷酸盐
公开(公告)号：US3501461A
公开(公告)日：1970-03-17
申请号：US3501461D
申请日：1968-01-18
申请人： ALLIED CHEM
发明人： NEWALLIS PETER E , CHEEMA ZAFARULLAH KHAN
IPC分类号： C07F9/165 , C07F9/553 , C07F9/40 , A01N9/36 , C07D41/04
CPC分类号： C07F9/5535 , C07F9/1651

8. 发明申请

US20190204330A1 APPLICATION OF CLICK CHEMISTRY FOR SIGNAL AMPLIFICATION IN IHC AND ISH ASSAYS 审中-公开
公开(公告)号：US20190204330A1
公开(公告)日：2019-07-04
申请号：US16226489
申请日：2018-12-19
申请人： Ventana Medical Systems, Inc.
发明人： Brian D. Kelly , Nathan W. Polaske
IPC分类号： G01N33/58 , C07F9/12 , C07F9/553 , C07F9/6518 , C07F9/6524 , C07F9/6509
CPC分类号： G01N33/582 , C07F9/12 , C07F9/5535 , C07F9/650947 , C07F9/6518 , C07F9/6524
摘要： Applicants have developed an amplification system and methodology for IHC and ISH staining that utilizes “click chemistry” to covalently bind reporter molecules to tissue.

9. 发明申请

US20160207949A1 NOVEL CYTOTOXIC AGENTS FOR CONJUGATION TO A CELL BINDING MOLECULE 有权
标题翻译：用于与细胞结合分子结合的新的细胞毒性剂
公开(公告)号：US20160207949A1
公开(公告)日：2016-07-21
申请号：US14914739
申请日：2013-09-02
申请人： HANGZHOU DAC BIOTECH CO., LTD
发明人： Robert Yongxin Zhao
IPC分类号： C07F9/6561 , A61K47/48 , A61K45/06 , C07K16/28 , A61K31/675 , A61K39/395
CPC分类号： C07F9/6561 , A61K31/675 , A61K39/3955 , A61K45/06 , A61K47/55 , A61K47/6803 , A61K47/6849 , C07F9/5535 , C07F9/65583 , C07K16/2803 , C07K16/2887 , C07K2317/24 , C07K2317/54 , C07K2317/55 , C07K2317/622 , C07K2317/626 , C07K2317/76
摘要： The present invention is related to novel cytotoxic agents, pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives, their conjugates with a cell-binding agent, the preparation and the therapeutic uses in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.
摘要翻译：本发明涉及新型细胞毒剂，吡咯并[2,1-c] [1,4]苯并二氮杂（PBD）衍生物，它们与细胞结合剂的缀合物，靶向治疗癌症的制备和治疗用途，自身免疫性疾病和感染性疾病。

10. 发明授权

US08785386B2 Benzazepine derivatives useful as vasopressin antagonists 有权
标题翻译：苯并氮平衍生物可用作加压素拮抗剂
公开(公告)号：US08785386B2
公开(公告)日：2014-07-22
申请号：US14034943
申请日：2013-09-24
申请人： Otsuka Phamaceutical Co., Ltd.
发明人： Kazumi Kondo , Yasuhiro Menjo , Takahiro Tomoyasu , Shin Miyamura , Yuso Tomohira , Takakuni Matsuda , Keigo Yamada , Yusuke Kato
IPC分类号： A61K38/00 , C07D223/16
CPC分类号： C07D223/16 , C07D405/12 , C07F9/5535 , Y02P20/55
摘要： The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.
摘要翻译：本发明提供苯并氮杂化合物，其可以长时间保持托伐普坦的血液水平，从而能够提供所需的药物作用。本发明的苯并氮杂化合物由通式（1）表示，其中R1表示-CO-（CH2）n-COR2基团（其中n为1〜4的整数，R2为（2-1）羟基基团;（2-2）任选被羟基，低级烷酰基，低级烷酰氧基，低级烷氧基羰基氧基，环烷氧基羰基氧基或5-甲基-2-氧代-1,3-二氧戊环的低级烷氧基，二氧杂环戊烯-4-基;或（2-3）任选被羟基 - 低级烷基取代的氨基）等。

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