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公开(公告)号：US20180305362A1
公开(公告)日：2018-10-25
申请号：US15768668
申请日：2016-10-14
发明人： Wanjun Zheng , Xiaojie Zhu , Hong Du , Maarten Postema , Yimin Jiang , Jing Li , Robert Yu , Hyeong-wook Choi , Jaemoon Lee , Frank Fang , Daniel Custar
IPC分类号： C07D487/04 , C07D519/00 , A61P35/00
CPC分类号： C07D487/04 , A61P35/00 , C07D519/00
摘要： We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
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公开(公告)号：US10101343B2
公开(公告)日：2018-10-16
申请号：US15434326
申请日：2017-02-16
IPC分类号： G01N33/82 , C07K16/28 , G01N33/574
摘要： Described herein are antibodies, and antigen-binding fragments thereof, that are specific for folate receptor alpha, related polynucleotides, expression vectors, and cells that express the described antibodies. Also provided are methods of using the described antibodies, and antigen-binding fragments thereof, and related kits. Provided herein are also methods for diagnosing cancers, such as breast cancer, thyroid cancer, colorectal cancer, endometrial cancer, fallopian tube cancer, ovarian cancer, or lung cancer, using the described antibodies, and antigen-binding fragments thereof. The methods involve determining the amount of folate receptor alpha in a sample derived from a subject and comparing this level with the level of folate receptor alpha in a control sample or reference sample.
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公开(公告)号：US20180273532A1
公开(公告)日：2018-09-27
申请号：US15841767
申请日：2017-12-14
发明人： Roch Boivin , Eric Carlson , Atsushi Endo , Hans Hansen , Lynn D. Hawkins , Sally Ishizaka , Matthew Mackey , Sridhar Narayan , Takashi Satoh , Shawn Schiller
IPC分类号： C07D471/04 , A61K31/55 , C07D487/04 , A61K31/519
CPC分类号： C07D471/04 , A61K31/519 , A61K31/55 , C07D487/04 , Y02P20/582
摘要： Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
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公开(公告)号：US10072005B2
公开(公告)日：2018-09-11
申请号：US15875069
申请日：2018-01-19
发明人： Andrew Payne , Jose Luis Castro Pineiro , Louise Michelle Birch , Afzal Khan , Alan James Braunton , James Edward Kitulagoda , Motohiro Soejima
IPC分类号： C07D471/04 , A61K31/437 , C07D401/04
CPC分类号： C07D471/04 , C07D401/04
摘要： 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.
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公开(公告)号：US09969812B2
公开(公告)日：2018-05-15
申请号：US15382821
申请日：2016-12-19
发明人： Yoshimasa Sakamoto , Yusuke Adachi , Junji Matsui , Yu Kato , Yoichi Ozawa , Takanori Abe , Ken Ito , Yuya Nakazawa , Sho Tachino , Katsuhisa Suzuki , Kishan Agarwala , Kana Hoshino , Masahiko Katayama
IPC分类号： A61K39/395 , C07K16/28 , C07K16/30 , C07K14/705 , C07K16/32 , A61K31/337 , A61K31/47 , A61K33/24 , C12N9/14 , C07K14/71 , A61K39/00
CPC分类号： C07K16/32 , A61K31/337 , A61K31/47 , A61K33/24 , A61K39/395 , A61K39/3955 , A61K39/39558 , A61K2039/505 , C07K14/705 , C07K14/71 , C07K16/28 , C07K16/2863 , C07K16/3023 , C07K16/303 , C07K2317/20 , C07K2317/24 , C07K2317/34 , C07K2317/52 , C07K2317/56 , C07K2317/565 , C07K2317/76 , C07K2317/92 , C07K2319/21 , C07K2319/42 , C12N9/14 , C12Y301/03001 , A61K2300/00
摘要： The present invention provides an anti-human Notch4 antibody or a Notch4 binding fragment thereof that may have neutralizing activity against human Notch4, as well as a pharmaceutical composition comprising the same as the active ingredient. The present inventors obtained a mouse anti-human Notch4 antibody that has high neutralizing activity and binding affinity towards human Notch4 and determined the complementarity determining region (CDR) sequence of the mouse anti-human Notch4 antibody. This enabled the production of a humanized antibody comprising the variable region of heavy and light chains as well as the CDR sequence of the mouse anti-human Notch4 antibody.
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66.发明申请公开(公告)号：US20180092901A1
公开(公告)日：2018-04-05
申请号：US15554577
申请日：2016-03-03
发明人： Andrew Evan DENKER , Yu KATO , Kimiyo TABATA , Yusaku HORI
IPC分类号： A61K31/47 , A61K39/395 , A61K45/06 , C07K16/28
CPC分类号： A61K31/47 , A61K39/39558 , A61K45/06 , A61K2039/505 , A61K2300/00 , C07K16/2818 , C07K16/2827 , C07K2317/76
摘要： The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a multi-RTK inhibitor, and the use of the combination therapies for the treatment of cancer. The multi-RTK inhibitor may be represented by Formula (I): wherein R1 is C1-6 alkyl or C3-8 cycloalkyl, R2 is a hydrogen atom or C1-6 alkoxy, and R3 is a hydrogen atom or a halogen atom. A tumor therapeutic agent is disclosed that combines a compound or pharmaceutically acceptable salt thereof represented by Formula I and an anti-PD-1 antibody.
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公开(公告)号：US09856276B2
公开(公告)日：2018-01-02
申请号：US15196600
申请日：2016-06-29
发明人： Atsushi Endo , Charles E. Chase , Francis G. Fang
IPC分类号： C07D307/12 , C07F7/18 , C07D405/06 , C07D405/12 , C07D493/04 , C07D407/06 , C07D307/38
CPC分类号： C07F7/1804 , C07D307/12 , C07D307/38 , C07D405/06 , C07D405/12 , C07D407/06 , C07D493/04 , Y02P20/55
摘要： In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):
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公开(公告)号：US20170252342A1
公开(公告)日：2017-09-07
申请号：US15519676
申请日：2015-10-21
发明人： Margaret MOLINE , Gina PASTINO , Yurie AKIMOTO , Yasuhiro ZAIMA , Nobuya SUZUKI , Nobuo YOSHIDA
IPC分类号： A61K31/506 , A61K9/48 , A61K9/20 , A61K9/00
CPC分类号： A61K31/506 , A61K9/0053 , A61K9/2018 , A61K9/2054 , A61K9/48 , A61K9/4858 , A61K9/4866
摘要： In the present invention, compound such as (1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl) cyclopropanecarboxamide have been found to be potent orexin receptor antagonists, and may be useful in the treatment of sleep disorders such as insomnia, as well as for other therapeutic uses.
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公开(公告)号：US20170240560A1
公开(公告)日：2017-08-24
申请号：US15501658
申请日：2015-08-04
IPC分类号： C07D493/22 , C07D313/00 , C07D493/08 , C07B57/00
CPC分类号： C07D493/22 , C07B57/00 , C07D313/00 , C07D493/08 , C07D493/18
摘要： The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries.
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公开(公告)号：US20170204068A1
公开(公告)日：2017-07-20
申请号：US15328166
申请日：2015-08-03
发明人： Yuzo Watanabe
IPC分类号： C07D239/34
CPC分类号： C07D239/34 , C07D239/36
摘要： There are provided a method for producing 2,4-disubstituted pyrimidine-5-ol, and particularly, 2,4-dimethylpyrimidine-5-ol and an intermediate thereof used in industrial production. The production method according to the present invention includes a step of producing 2,4-disubstituted pyrimidine-5-ol according to a hydrolysis reaction of a 2,4-disubstituted-5-(4-(nitrophenyl)oxy)pyrimidine compound and is suitable for industrial production since an inexpensive and easily available starting material can be used, regioselectivity of a substituent group is easily controlled, impurities are easily controlled, and 2,4-disubstituted pyrimidine-5-ol can be produced without using reagents and intermediates causing health problems, risks and the like.
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