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公开(公告)号：US20180265463A1
公开(公告)日：2018-09-20
申请号：US15539260
申请日：2015-12-24
Applicant: Kyoto University , National University Corporation Tokyo University of Agriculture and Technology
Inventor： Mizuki Watanabe , Risa Asano , Kazuo Nagasawa , Motonari Uesugi
IPC: C07C401/00 , C07D209/48 , C07D495/04 , A61P3/04 , A61P1/16 , A61P3/10 , A61P9/00 , A61P35/00
CPC classification number: C07C401/00 , A61K31/59 , A61K31/593 , A61P1/16 , A61P3/04 , A61P3/10 , A61P9/00 , A61P35/00 , C07C2601/14 , C07C2602/24 , C07D209/48 , C07D211/46 , C07D295/125 , C07D495/04
Abstract: The present invention relates to vitamin D3 derivatives of the following formula, wherein each symbol has the same meaning as defined herein, and pharmaceutical or medical use thereof for treating metabolic disease, liver disease, obesity, diabetes, cardiovascular disease, or cancer in a patient in need thereof.
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公开(公告)号：US10053470B2
公开(公告)日：2018-08-21
申请号：US15499443
申请日：2017-04-27
Applicant: Exelixis, Inc.
Inventor： James William Leahy
IPC: C07D519/00 , C07D473/38 , C07D473/34 , C07D405/12 , C07D215/12 , C07D215/14 , C07D215/38 , C07D413/14 , C07D401/14 , C07D241/44 , C07D401/12 , C07D417/14 , C07D487/04
CPC classification number: C07D519/00 , C07D213/30 , C07D213/38 , C07D215/12 , C07D215/14 , C07D215/38 , C07D241/44 , C07D295/125 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/14 , C07D417/14 , C07D473/34 , C07D473/38 , C07D487/04 , C07D495/04
Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof as well as methods of making and using the compounds.
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公开(公告)号：US09828352B2
公开(公告)日：2017-11-28
申请号：US14905727
申请日：2014-07-10
Inventor： Giovanni Bottegoni , Alessio De Simone , Gian Filippo Ruda , Andrea Cavalli , Tiziano Bandiera , Daniele Piomelli
IPC: C07D209/20 , C07D209/88 , C07D211/38 , C07D211/14 , C07D213/30 , C07D295/13 , C07D295/125 , A61K31/495 , A61K31/496 , A61K31/5377
CPC classification number: C07D295/13 , C07D209/88 , C07D211/14 , C07D211/38 , C07D213/30 , C07D295/125
Abstract: The invention provides compounds of Formula (I) or pharmaceutically acceptable salts thereof wherein Ar′, R1, R2, R3, R4, X, Y are as defined in the description of invention, as multi-target directed ligands (MTDLs) that are at the same time inhibitors of the fatty acid amide hydrolase (FAAH) enzyme and modulators of the D3 dopamine receptor (D3DR), their methods of preparation, formulations and therapeutic applications thereof.
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公开(公告)号：US20170226131A1
公开(公告)日：2017-08-10
申请号：US15499443
申请日：2017-04-27
Applicant: James William Leahy
Inventor： James William Leahy
IPC: C07D519/00 , C07D473/34 , C07D405/12 , C07D215/12 , C07D215/14 , C07D487/04 , C07D413/14 , C07D401/14 , C07D241/44 , C07D401/12 , C07D417/14 , C07D473/38 , C07D215/38
CPC classification number: C07D519/00 , C07D213/30 , C07D213/38 , C07D215/12 , C07D215/14 , C07D215/38 , C07D241/44 , C07D295/125 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/14 , C07D417/14 , C07D473/34 , C07D473/38 , C07D487/04 , C07D495/04
Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof as well as methods of making and using the compounds.
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公开(公告)号：US20170155047A1
公开(公告)日：2017-06-01
申请号：US15323905
申请日：2015-07-03
Applicant: Novaled GmbH
Inventor： Sascha Dorok , Ina Steudtner , Ulrich Heggemann , Steffen Runge , Manuela Klose
IPC: H01L51/00 , C07C279/18 , H01L51/44 , C07D295/13 , C07C211/53 , H01L51/42 , C07D233/50 , C07D235/30
CPC classification number: H01L51/005 , C07C211/53 , C07C279/18 , C07C2601/02 , C07D233/50 , C07D235/30 , C07D295/125 , C07D295/13 , C08G73/02 , C08G73/026 , H01L51/002 , H01L51/0046 , H01L51/0061 , H01L51/0067 , H01L51/0069 , H01L51/0072 , H01L51/424 , H01L51/4253 , H01L51/441 , Y02E10/549
Abstract: The invention relates to an electronic device comprising a compound having Formula (1): ABx (1), wherein A is a structural moiety that consists of at least two atoms and comprises a conjugated system of delocalized electrons, each B is independently selected from an imine functional group (1a), wherein R1, R2, R3, R4 are independently selected from C1-C30 alkyl, C2-C30 alkenyl, C2-C3 alkinyl, C3-C30 cycloalkyl, C6-C30 aryl, C2-C30 heteroaryl, C7-C30 arylalkyl, C3-C30 heteroarylalkyl, the wave line represents a covalent bond to the imine nitrogen atom, G is in each group (1a) independently selected from a quarternary carbon atom and from a cyclopropenylidene structural moiety, x is an integer equal one or higher, preferably equal two or higher, and the lone electron pair of the imine nitrogen atom and/or the pi-electrons of the imine double bond of at least one group B is conjugated with the conjugated system of delocalized electrons comprised in the structural moiety A, with the proviso that two or more of the substituents R1, R2, R3, R4 may be connected to form a ring that may contain also unsaturation and, if any of the substituents R1, R2, R3, R4 comprises two or more carbon atoms, up to one third of the overall count of the carbon atoms in the substituent or in any ring formed by two connected substituents can be replaced with heteroatoms independently selected from O, S, N and B as well as to an electrically semiconducting material and a compound for use in the electronic device.
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公开(公告)号：US09629831B2
公开(公告)日：2017-04-25
申请号：US14742465
申请日：2015-06-17
Applicant: Millennium Pharmaceuticals, Inc.
Inventor： Bing-Yan Zhu , Wenrong Huang
IPC: C07D213/75 , A61K31/44 , C07C237/42 , C07C255/60 , C07C257/18 , C07C259/18 , C07C311/16 , C07C311/46 , C07C317/40 , C07C317/44 , C07D213/81 , C07D213/82 , C07D217/22 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D295/125 , C07D333/38 , C07D401/12 , C07D409/12 , C07D409/14 , A61K31/616 , A61K45/06 , A61K9/20 , A61K9/48
CPC classification number: A61K31/44 , A61K9/20 , A61K9/2013 , A61K9/2054 , A61K9/48 , A61K9/4858 , A61K9/4866 , A61K31/616 , A61K45/06 , A61K2201/094 , C07C237/42 , C07C255/60 , C07C257/18 , C07C259/18 , C07C311/16 , C07C311/46 , C07C317/40 , C07C317/44 , C07D213/75 , C07D213/81 , C07D213/82 , C07D217/22 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D295/125 , C07D333/38 , C07D401/12 , C07D409/12 , C07D409/14
Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
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公开(公告)号：US09505726B2
公开(公告)日：2016-11-29
申请号：US14547632
申请日：2014-11-19
Applicant: Roche Palo Alto LLC
Inventor： Chris Allen Broka , Ronald Charles Hawley
IPC: A61K31/166 , C07C233/64 , C07D241/12 , C07C237/32 , C07D265/30 , C07D405/14 , C07D417/12 , C07C237/42 , C07D213/56 , C07D213/61 , C07D213/81 , C07D231/14 , C07D241/24 , C07D261/18 , C07D263/34 , C07D277/56 , C07D285/06 , C07D295/125 , C07D307/68 , C07D309/08 , C07D333/38 , C07D401/12 , C07D403/12
CPC classification number: C07D241/12 , C07C237/32 , C07C237/42 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/56 , C07D213/61 , C07D213/81 , C07D231/14 , C07D241/24 , C07D261/18 , C07D263/34 , C07D265/30 , C07D277/56 , C07D285/06 , C07D295/125 , C07D307/68 , C07D309/08 , C07D333/38 , C07D401/12 , C07D403/12 , C07D405/14 , C07D417/12
Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
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公开(公告)号：US20160263090A1
公开(公告)日：2016-09-15
申请号：US15162214
申请日：2016-05-23
Applicant: InterMune, Inc.
Inventor： Brad Owen Buckman , John Beamond Nicholas , Johnnie Y. Ramphal , Kumaraswamy Emayan , Scott D. Seiwert
IPC: A61K31/437 , A61K9/00
CPC classification number: A61K31/437 , A61K9/007 , C07D211/86 , C07D213/64 , C07D217/24 , C07D221/04 , C07D223/10 , C07D295/125 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D495/04 , C07D498/04 , C07D513/04
Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
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公开(公告)号：US20160168116A1
公开(公告)日：2016-06-16
申请号：US14969837
申请日：2015-12-15
Applicant: MannKind Corporation
Inventor： John B. Patterson , David G. Lonergan , Gary A. Flynn , Qingpeng Zeng , Peter V. Pallai
IPC: C07D333/58 , C07D333/22 , C07D239/26 , C07D321/10 , C07C65/30 , C07C205/44 , C07D317/54 , C07D231/12 , C07D307/80 , C07D213/69 , C07D319/18 , C07D261/08 , C07D213/48 , C07C47/565 , C07D215/14 , C07D217/16 , C07D295/192 , C07C235/84 , C07C317/24 , C07D295/15 , C07D241/18 , C07C47/575
CPC classification number: C07C65/21 , A61K31/11 , A61K31/135 , A61K31/166 , A61K31/192 , A61K31/357 , A61K31/381 , A61K31/505 , A61K31/5375 , A61K31/5377 , C07C47/55 , C07C47/565 , C07C47/575 , C07C65/11 , C07C65/26 , C07C65/30 , C07C205/44 , C07C205/61 , C07C223/02 , C07C233/65 , C07C235/42 , C07C235/84 , C07C251/24 , C07C317/24 , C07C321/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/48 , C07D213/64 , C07D213/69 , C07D213/74 , C07D215/14 , C07D217/16 , C07D231/12 , C07D235/08 , C07D239/26 , C07D239/54 , C07D241/18 , C07D249/18 , C07D261/08 , C07D277/34 , C07D295/125 , C07D295/15 , C07D295/192 , C07D307/80 , C07D317/54 , C07D319/08 , C07D319/18 , C07D321/10 , C07D333/22 , C07D333/58 , C07D401/12 , C07D403/12 , C07D417/10 , Y02A50/389 , Y02A50/393
Abstract: Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Abstract translation: 在体外直接抑制IRE-1α活性的化合物，其前药和药学上可接受的盐。 这样的化合物和前药可用于治疗与未折叠的蛋白质应答相关的疾病，并可用作单一药剂或联合疗法。
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10.发明授权
公开(公告)号：US09315488B2
公开(公告)日：2016-04-19
申请号：US14726337
申请日：2015-05-29
Applicant: AbbVie Inc.
Inventor： Hong Ding , Steven W. Elmore , Lisa Hasvold , Laura A. Hexamer , Aaron R. Kunzer , William J. McClellan , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Michael D. Wendt
IPC: C07D295/155 , C07D209/08 , C07D211/58 , C07D401/12 , C07D309/04
CPC classification number: C07D401/12 , A61K31/407 , A61K31/495 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D209/08 , C07D209/32 , C07D211/58 , C07D211/96 , C07D213/64 , C07D215/20 , C07D217/16 , C07D231/56 , C07D235/26 , C07D241/04 , C07D249/04 , C07D295/125 , C07D295/14 , C07D295/155 , C07D309/04 , C07D309/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D417/12 , C07D471/04 , C07D487/04
Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
