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公开(公告)号：US09975856B2
公开(公告)日：2018-05-22
申请号：US15287023
申请日：2016-10-06
Applicant: Genentech, Inc.
Inventor： Stephan Bachmann , Serena Maria Fantasia , Francis Gosselin , Chong Han , Stefan Hildbrand , Theresa Humphries , Christian Jenny , Ngiap-Kie Lim , Andrew McClory , Christian Moessner , Pankaj Rege , Scott Savage , Haiming Zhang
IPC: C07D231/56 , C07D405/04 , C07C309/73 , C07C69/73 , C07F5/04 , C07C69/612 , C07F5/02
CPC classification number: C07D231/56 , C07C69/612 , C07C69/73 , C07C69/738 , C07C309/73 , C07D405/04 , C07F5/025 , C07F5/04
Abstract: Processes are described for the preparation of estrogen receptor modulating compound, (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid I: and salts thereof, and intermediates useful for the preparation of I.
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公开(公告)号：US20180036416A1
公开(公告)日：2018-02-08
申请号：US15782744
申请日：2017-10-12
Applicant: Graybug Vision,Inc.
Inventor： Jeffrey L. Cleland , Ming Yang , John G. Bauman , Nu Hoang , Emmett Cunningham
IPC: C07D513/04 , C07D403/06 , C07C69/73 , C07D495/04
CPC classification number: A61K47/54 , A61K47/542 , A61K47/543 , A61K47/55 , A61K47/59 , A61K47/593 , A61K47/60 , C07C69/73 , C07C2601/08 , C07D403/06 , C07D495/04 , C07D513/04
Abstract: The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.
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公开(公告)号：US20180028673A1
公开(公告)日：2018-02-01
申请号：US15782755
申请日：2017-10-12
Applicant: Graybug Vision, Inc.
Inventor： Jeffrey L. Cleland , Ming Yang , John G. Bauman , Nu Hoang , Emmett Cunningham
IPC: C07D513/04 , C07D403/06 , C07C69/73 , C07D495/04
CPC classification number: A61K47/54 , A61K47/542 , A61K47/543 , A61K47/55 , A61K47/59 , A61K47/593 , A61K47/60 , C07C69/73 , C07C2601/08 , C07D403/06 , C07D495/04 , C07D513/04
Abstract: The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.
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公开(公告)号：US20180022688A1
公开(公告)日：2018-01-25
申请号：US15548760
申请日：2016-01-27
Inventor： Zhenwen Duan , Shuren Guo , Xuemei Li
CPC classification number: C07C69/73 , A61K31/216 , C07C67/03 , C07C67/48 , C07C67/56 , C07C69/732 , C07C2602/10
Abstract: The invention relates to new compounds as well as a separation method, a synthetic method and use thereof. It is demonstrated by an assay on activity that the compound has an activity of inhibiting an HMG-CoA reductase. In addition, the invention also relates to a derivative of the compound.
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公开(公告)号：US20170369417A1
公开(公告)日：2017-12-28
申请号：US15694982
申请日：2017-09-04
Applicant: Emory University
Inventor： Huw M. L. Davies , Spandan Chennamadhavuni , Andrei Bakin
IPC: C07C69/73 , A61K31/194 , C07D317/60 , C07D307/80 , C07D307/79 , C07D209/34 , C07D209/26 , C07D209/24 , C07C259/06 , C07C205/56 , C07C201/12 , C07C69/738 , C07C69/736 , C07C69/734 , C07C69/732 , C07C69/65 , C07C69/618 , C07C69/604 , C07C67/31 , C07C57/42 , C07C51/00 , A61K31/405 , A61K31/36 , A61K31/357 , A61K31/343 , A61K31/216 , C07D317/68 , C07D319/18
CPC classification number: C07C69/73 , A61K31/194 , A61K31/216 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/405 , C07C51/00 , C07C57/42 , C07C67/31 , C07C69/604 , C07C69/618 , C07C69/65 , C07C69/732 , C07C69/734 , C07C69/736 , C07C69/738 , C07C201/12 , C07C205/56 , C07C259/06 , C07D209/24 , C07D209/26 , C07D209/34 , C07D307/79 , C07D307/80 , C07D317/60 , C07D317/68 , C07D319/18
Abstract: The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula I, pharmaceutical compositions having a compound of formula I, and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula I to a subject in need thereof.
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公开(公告)号：US09808531B2
公开(公告)日：2017-11-07
申请号：US15273686
申请日：2016-09-22
Applicant: Graybug Vision, Inc.
Inventor： Jeffrey L. Cleland , Ming Yang , John G. Bauman , Nu Hoang , Emmett Cunningham
IPC: A61K47/48 , C07D495/04 , C07D513/04 , C07C69/73 , C07D403/06
CPC classification number: A61K47/54 , A61K47/542 , A61K47/543 , A61K47/55 , A61K47/59 , A61K47/593 , A61K47/60 , C07C69/73 , C07C2601/08 , C07D403/06 , C07D495/04 , C07D513/04
Abstract: The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.
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公开(公告)号：US20170305874A1
公开(公告)日：2017-10-26
申请号：US15492340
申请日：2017-04-20
Inventor： Spencer S. Walse , Daniel Kuzmich
IPC: C07D307/83 , C07C69/732 , C07C67/327 , C07C45/66 , C07C49/497 , C07C69/734 , C07C51/09 , C07C2601/16 , C07C2601/14
CPC classification number: C07D307/83 , C07C45/66 , C07C45/72 , C07C49/497 , C07C51/09 , C07C67/31 , C07C67/327 , C07C69/732 , C07C69/734 , C07C2601/14 , C07C2601/16 , C07C49/403 , C07C69/73
Abstract: A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R1 is ethenyl, R2 and R3 is methyl, and n is 1), (±)-anastrephin (2) (wherein: R2 is ethenyl, R1 and R3 is methyl and n is 1), and analogs thereof (wherein: R1 is H, C1-5 alkyl, C2-6 alkenyl or C2-6 alkynyl, R2 is H, C1-5 alkyl, C2-6 alkenyl or C2-6 alkynyl, R1 and R2 together with the carbon atom they are attached form a C3-6 cycloalkyl ring, R3 is C1-5 alkyl and n is 0-2):
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公开(公告)号：US09796895B2
公开(公告)日：2017-10-24
申请号：US14426805
申请日：2013-09-26
Applicant: Dow Global Technologies LLC
Inventor： Xin Jin , Dwight Latham , Steven Crain , Mark Sonnenschein
CPC classification number: C09K5/08 , C07C69/73 , C08G18/3206 , C08G18/348 , C08G61/12 , C08G61/128 , C08G2261/334 , C08G2261/592 , C08J9/14 , C08J9/146 , C08J2203/14 , C08J2203/142 , C08J2203/144 , C08J2203/162 , C08J2205/06 , C08J2333/06
Abstract: Embodiments of the present disclosure are directed towards using a carbon-Michael compound. As an example, a method of using a carbon-Michael compound to reduce heat transfer can include locating the carbon-Michael compound between a heat provider and a heat receptor, where the carbon-Michael compound is a reaction product of a multifunctional acrylate compound with a multifunctional Michael donor, and the heat provider has a temperature from 100 C to 290 C.
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公开(公告)号：US20170174607A1
公开(公告)日：2017-06-22
申请号：US15382782
申请日：2016-12-19
Applicant: International Flavors & Fragrances Inc.
IPC: C07C67/317 , C07C67/00 , C07C45/27
CPC classification number: C07C67/317 , C07C45/27 , C07C45/54 , C07C67/00 , C07C67/313 , C07C2101/08 , C07C2101/10 , C07C2101/14 , C07C2101/16 , C07C2102/08 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C69/73 , C07C69/145 , C07C69/157 , C07C69/757 , C07C69/738 , C07C49/597 , C07C49/683 , C07C49/687 , C07C49/457 , C07C49/697 , C07C49/227 , C07C47/353
Abstract: Copper(II) bromide mediated oxidation of acylated enol and use of the reaction in the synthesis of α,β-unsaturated or α-bromo ketones or aldehydes are disclosed. The method provides an efficient and practical process for manufacturing dehydrohedione (DHH) and many other versatile α,β-unsaturated or α-bromo ketones or aldehydes in large scales to avoid using precious metal compounds.
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10.发明申请NOVEL AND SPECIFIC INHIBITORS OF CYTOCHROME P450 26 RETINOIC ACID HYDROXYLASE 有权细胞色素P450 26新戊酸羟化酶的新型特异性抑制剂
公开(公告)号：US20160200703A1
公开(公告)日：2016-07-14
申请号：US14912479
申请日：2014-08-20
Applicant: UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION , UNIVERSITY OF MONTANA
Inventor： Philippe DIAZ , Nina ISOHERRANEN , Brian BUTTRICK , Nicolas GUILLOTEAU
IPC: C07D339/06 , C07C323/65 , C07C69/616 , C07C59/72 , C07C59/86 , C07C59/54 , C07C229/44 , C07C229/42 , C07D317/30 , C07C69/738 , C07C323/62 , C07C69/734
CPC classification number: C07D317/30 , C07C57/50 , C07C59/54 , C07C59/72 , C07C59/86 , C07C69/616 , C07C69/73 , C07C69/734 , C07C69/738 , C07C229/42 , C07C229/44 , C07C317/44 , C07C323/62 , C07C323/65 , C07C2602/10 , C07C2602/28 , C07C2603/74 , C07D339/06
Abstract: The present disclosure is generally directed to compositions and methods for treating diseases that are ameliorated by the inhibition of CYP26 mediated retinoic acid metabolism. The compositions comprise compounds of formula (I). A repreid50000060307390 IB/345 nullsents aryl optionally substituted with one, two, three, or four groups that are each independently halogen, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)2, —OH, C1-C6 alkoxy, and C1-C6 haloalkoxy; X is a bond, —CH2—, —CHR5—, —C═CHR4—, —NR4—, —N═O—R4—, —O—, —S—, —SO—, —SO2—, —C(O)—, or —C(NR4)—, or X is of formula (a), (b) or (c), wherein each n is independently 1, 2, or 3; each R4 is independently hydrogen or C1-6 alkyl; R5 is independently hydrogen, C1-6 alkyl, or —OR6, where R6 is selected from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyL C3-12 cycloalkyl, heterocyclyl, aryl, arylC1-6 alkyl, heteroaryl, or heteroarylC1-6 alkyl; Y is C1-6 alkylene, C2-6 alkenylene, or C2-6 alkylylene moiety.
Abstract translation: 本公开一般涉及用于治疗通过抑制CYP26介导的视黄酸代谢而改善的疾病的组合物和方法。 组合物包含式（I）的化合物。 氰基，硝基，C 1-6烷基，C 1-6卤代烷基，-NH 2，-NH（C 1 -C 6烷基），C 1 -C 6卤代烷基， ，-N（C 1 -C 6烷基）2，-OH，C 1 -C 6烷氧基和C 1 -C 6卤代烷氧基; X是键，-CH 2 - ， - CHR 5 - ， - C = CHR 4 - ， - NR 4 - ， - N = O-R 4 - ， - O - ， - S - ， - SO - ， - SO 2 - O） - 或-C（NR 4） - 或X具有式（a），（b）或（c），其中每个n独立地为1,2或3; 每个R 4独立地是氢或C 1-6烷基; R5独立地是氢，C1-6烷基或-OR6，其中R6选自氢，C1-6烷基，C2-6烯基，C2-6炔基C3-12环烷基，杂环基，芳基，芳基C1- 6烷基，杂芳基或杂芳基C 1-6烷基; Y是C 1-6亚烷基，C 2-6亚烯基或C 2-6亚烷基部分。
