公开(公告)号：US12049436B2

公开(公告)日：2024-07-30

申请号：US17536383

申请日：2021-11-29

申请人： RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITY ,  INSTITUTE FOR BASIC SCIENCE

发明人： Hyoyoung Lee ,  Suresh Vasimalla ,  Seungeun Lee

IPC分类号： C07C231/10 ,  B01J21/06 ,  B01J35/39 ,  B01J37/16 ,  C01G23/08 ,  C07C233/65 ,  C07D295/192 ,  C07D401/04

CPC分类号： C07C231/10 ,  B01J21/063 ,  B01J35/39 ,  B01J37/16 ,  C01G23/08 ,  C07C233/65 ,  C07D295/192 ,  C07D401/04

摘要： Provided is a preparing method of an amide directly from a tertiary amine by using a reduced titanium dioxide (Blue TiO2), which is formed by mixing a titanium dioxide having an anatase phase and a rutile phase with a reducing agent and selectively reducing any one of the anatase phase and the rutile phase, as a photocatalyst.

公开(公告)号：US20230286906A1

公开(公告)日：2023-09-14

申请号：US17780052

申请日：2020-11-25

申请人： CANOPY GROWTH CORPORATION

发明人： SIAWASH AHMAR ,  JUNG YUN KIM ,  PING SHAN LAI ,  JEFFREY ALAN OMEARA ,  AZADEH PIRI SEDIGH ,  QUANG HUY TO

IPC分类号： C07C233/65 ,  C07C259/10 ,  C07C233/92 ,  C07D213/40 ,  C07D239/26 ,  C07D261/14 ,  C07D263/32 ,  C07D271/06 ,  C07D257/04 ,  C07C233/83 ,  C07D233/64 ,  C07D487/04 ,  C07D295/192 ,  C07D295/26 ,  C07D295/24 ,  C07D207/16 ,  C07D207/12 ,  C07D209/44 ,  C07D209/08 ,  C07D203/18 ,  C07D205/04 ,  C07C255/00 ,  C07C233/78 ,  C07C233/69 ,  C07C233/66

CPC分类号： C07C233/65 ,  C07C259/10 ,  C07C233/92 ,  C07D213/40 ,  C07D239/26 ,  C07D261/14 ,  C07D263/32 ,  C07D271/06 ,  C07D257/04 ,  C07C233/83 ,  C07D233/64 ,  C07D487/04 ,  C07D295/192 ,  C07D295/26 ,  C07D295/24 ,  C07D207/16 ,  C07D207/12 ,  C07D209/44 ,  C07D209/08 ,  C07D203/18 ,  C07D205/04 ,  C07C255/00 ,  C07C233/78 ,  C07C233/69 ,  C07C233/66 ,  C07C2601/08 ,  C07C2601/02

摘要： This disclosure relates generally to cannabinoid derivatives having the structural formula (I), pharmaceutical compositions comprising them, and methods of using the cannabinoid derivatives. In some embodiments, R1 is —CH2CH═C(CH3)2, R2 is methyl, R3 is CsHn, R4 is —C(O)N(R4a)(R4b), R5 is H, R6 is OH, and R7 is H. Compounds of the present disclosure were tested in agonist and antagonist mode for both the CB1 and CB2 receptors. The tested compounds were generally found to exhibit activity in antagonist mode at the CB1 and CB2 receptor.

公开(公告)号：US20180327374A1

公开(公告)日：2018-11-15

申请号：US15774157

申请日：2016-11-07

申请人： Michael T. RUDD ,  Edward J. BRNARDIC ,  Yuntae KIM ,  Robert S. MEISSNER ,  Vanessa RADA ,  Shawn J. STACHEL ,  Celina V. ZERBINATTI ,  Merck Sharp & Dohme Corp.

发明人： Michael T. Rudd ,  Edward J. Brnardic ,  Yuntae Kim ,  Robert S. Meissner ,  Vanessa L. Rada ,  Shawn J. Stachel ,  Celina V. Zerbinatti

IPC分类号： C07D295/16 ,  C07D243/08 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08 ,  C07D513/04 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61P3/10

CPC分类号： C07D295/16 ,  A61K31/496 ,  A61P3/10 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D213/74 ,  C07D213/85 ,  C07D243/08 ,  C07D295/192 ,  C07D295/205 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04 ,  C07D515/04

摘要： In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US20180215707A1

公开(公告)日：2018-08-02

申请号：US15128932

申请日：2015-03-25

申请人： Piramal Enterprises Limited

发明人： Rajiv SHARMA ,  Bichismita SAHU ,  Sunil Vasantrao MALI ,  Deepak SINGH

IPC分类号： C07C317/32 ,  C07D335/06 ,  C07D295/088 ,  C07D295/192 ,  C07D207/27 ,  C07C237/52 ,  C07D295/26 ,  C07D311/22 ,  C07D265/36 ,  C07C311/21 ,  C07C381/10 ,  C07D213/30 ,  C07D231/12 ,  C07D233/58 ,  C07D257/04 ,  C07D305/08 ,  C07D211/14 ,  C07D295/135

CPC分类号： C07C317/32 ,  A61K31/165 ,  A61K31/18 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/402 ,  A61K31/5375 ,  C07C205/36 ,  C07C211/45 ,  C07C215/70 ,  C07C217/48 ,  C07C217/76 ,  C07C217/88 ,  C07C225/22 ,  C07C229/42 ,  C07C233/29 ,  C07C233/54 ,  C07C237/22 ,  C07C237/52 ,  C07C255/46 ,  C07C255/50 ,  C07C309/89 ,  C07C311/08 ,  C07C311/21 ,  C07C311/37 ,  C07C317/24 ,  C07C317/44 ,  C07C323/09 ,  C07C381/10 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/10 ,  C07D207/27 ,  C07D211/14 ,  C07D213/30 ,  C07D231/12 ,  C07D233/58 ,  C07D257/04 ,  C07D265/36 ,  C07D295/088 ,  C07D295/135 ,  C07D295/192 ,  C07D295/26 ,  C07D305/08 ,  C07D311/22 ,  C07D317/72 ,  C07D335/06 ,  C07F5/025 ,  C07F7/1804

摘要： The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.

公开(公告)号：US10012868B2

公开(公告)日：2018-07-03

申请号：US15273784

申请日：2016-09-23

申请人： FUJIFILM Corporation

发明人： Yuki Nakazawa ,  Shunya Katoh ,  Hiroshi Matsuyama ,  Daisuke Hayashi ,  Masaru Yoshikawa

IPC分类号： G02F1/1333 ,  G02F1/13363 ,  C09K19/58 ,  C07C235/60 ,  C08F222/10 ,  C09D4/00 ,  G02F1/1335 ,  C07C233/18 ,  C07C233/52 ,  C07D295/192 ,  C07D307/12 ,  C09K19/30 ,  C09K19/04 ,  G02F1/1337

CPC分类号： G02F1/13363 ,  C07C233/18 ,  C07C233/52 ,  C07C235/60 ,  C07C2601/16 ,  C07D295/192 ,  C07D307/12 ,  C08F222/1006 ,  C08F2222/102 ,  C09D4/00 ,  C09K19/3068 ,  C09K19/586 ,  C09K2019/044 ,  C09K2019/0448 ,  C09K2219/03 ,  G02F1/133553 ,  G02F1/133723 ,  G02F1/133784 ,  G02F2001/133302 ,  G02F2001/133543 ,  G02F2001/133638 ,  G02F2202/023 ,  G02F2202/28

摘要： The present invention provides a polymerizable compound denoted by Formula (I): in the formula, Z1 and Z2 represent an arylene group, and the like, m represents 1 or 2, n represents an integer of 0 or 1, and when m is 2, n is 0, L1, L2, L3, and L4 each independently represent a linking group such as —C(═O)O— and —OC(═O)—, T3 represents -Sp4-R4, X represents —O—, and the like, r represents 1 to 4, Sp1, Sp2, Sp3, Sp4, and Sp5 each independently represent a single bond or a linking group, R1 and R2 each independently represent a polymerizable group, and R3, R4, and R5 each independently represent a hydrogen atom, a polymerizable group, or the like; a polymerizable composition containing the polymerizable compound described above; a film formed of the polymerizable composition described above; and a half mirror for displaying a projection image including the film described above.

公开(公告)号：US09981922B2

公开(公告)日：2018-05-29

申请号：US15043121

申请日：2016-02-12

申请人： Imago Biosciences, Inc.

发明人： Hugh Y. Rienhoff, Jr. ,  John M. McCall ,  Michael Clare ,  Cassandra Celatka ,  Amy E. Tapper

IPC分类号： C07D249/06 ,  C07C309/30 ,  A61K9/00 ,  A61K31/496 ,  C07D239/26 ,  A61K31/506 ,  C07D295/192 ,  A61K31/495 ,  C07D279/12 ,  A61K31/54 ,  C07D205/04 ,  A61K31/397 ,  C07D295/26 ,  C07D215/54 ,  C07C53/18 ,  C07D231/12 ,  C07D263/32 ,  A61K31/541 ,  C07B59/00 ,  C07D403/12 ,  A61K31/4192 ,  C07D401/12 ,  A61K31/454 ,  C07D249/08 ,  A61K31/4196 ,  C07D211/66 ,  A61K31/445 ,  C07D239/42 ,  C07D491/107 ,  C07D413/12 ,  A61K31/5377 ,  C07D498/08 ,  A61K31/5383 ,  C07D471/10 ,  A61K31/435 ,  C07D401/04 ,  A61K31/41 ,  C07D487/04 ,  A61K31/4162 ,  C07D487/08 ,  A61K31/4995 ,  A61K31/551 ,  C07D237/08 ,  A61K31/501 ,  A61K9/16 ,  A61K9/48

CPC分类号： C07D249/06 ,  A61K9/0053 ,  A61K9/1623 ,  A61K9/4858 ,  A61K31/397 ,  A61K31/41 ,  A61K31/4162 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/435 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/07 ,  C07B2200/13 ,  C07C53/18 ,  C07C309/30 ,  C07D205/04 ,  C07D211/66 ,  C07D215/54 ,  C07D231/12 ,  C07D237/08 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D263/32 ,  C07D279/12 ,  C07D295/192 ,  C07D295/26 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107 ,  C07D498/08 ,  A61K2300/00

摘要： Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

公开(公告)号：US09981901B2

公开(公告)日：2018-05-29

申请号：US15356292

申请日：2016-11-18

申请人： FOSUN ORINOVE PHARMATECH, INC.

发明人： John B. Patterson ,  David G. Lonergan ,  Gary A. Flynn ,  Qingping Zeng ,  Peter V. Pallai

IPC分类号： C07C235/42 ,  A61K31/166 ,  C07C65/21 ,  C07C65/26 ,  C07C65/11 ,  C07C233/65

CPC分类号： 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

摘要： 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.

公开(公告)号：US09957402B2

公开(公告)日：2018-05-01

申请号：US15309954

申请日：2015-05-12

申请人： DIC Corporation

发明人： Masanori Miyamoto ,  Youichi Tanimoto ,  Sei Yamamoto ,  Azusa Yogo ,  Akihiro Kondou ,  Tomokazu Yamada

IPC分类号： C08F2/46 ,  C08F2/50 ,  C08G61/04 ,  C09D11/38 ,  B41J2/01 ,  C07C237/34 ,  C09D11/101 ,  B41M5/50 ,  C07C237/20 ,  C07D295/192 ,  C09D11/107 ,  C07D295/033

CPC分类号： C09D11/38 ,  B41J2/01 ,  B41M5/50 ,  C07C229/38 ,  C07C237/20 ,  C07C237/34 ,  C07D295/033 ,  C07D295/192 ,  C09D11/101 ,  C09D11/107 ,  C09D11/36

摘要： A compound obtained through Michael addition reaction of an α-aminoacetophenone skeleton-containing compound (I) represented by the following general formula (1) and a reactive compound (II) having a function as a Michael acceptor is used as a photopolymerization initiator. In the general formula (1), R1 represents an aliphatic group, R2 to R3 each independently represent an aliphatic group, etc., R4 to R7 each independently represent a hydrogen atom, X1 represents a single bond or a C1-6 alkylene group, X2 represents a carbonyl group, Y1 and Y2 represent a group represented by the following general formula (2). However, when Y1 and Y2 both have a structure represented by the general formula (2), X5 in at least one of them is —NH—. In the general formula (2), X3 and X4 each independently represent a linear or branched alkylene group having 2 to 6 carbon atoms, X5 represents a single bond, —O— or —NH—.

公开(公告)号：US09944653B2

公开(公告)日：2018-04-17

申请号：US15587068

申请日：2017-05-04

申请人： The University of Liverpool

发明人： Martin Leuwer ,  Paul O'Neill ,  Neil Berry ,  Chandrakala Pidathala

IPC分类号： C07D491/107 ,  C07D205/04 ,  C07D265/30 ,  C07D295/192 ,  C07D211/06 ,  C07D493/10

CPC分类号： C07D491/107 ,  C07D205/04 ,  C07D211/06 ,  C07D265/30 ,  C07D295/192 ,  C07D493/10

摘要： The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.

公开(公告)号：US09873710B2

公开(公告)日：2018-01-23

申请号：US15339041

申请日：2016-10-31

申请人： Health Innovation Ventures B.V.

发明人： Jeffrey Bruce Smaill ,  Adam Vorn Patterson ,  Amir Ashoorzadeh ,  Christopher Paul Guise ,  Alexandra Marie Mowday ,  David Francis Ackerley ,  Elsie May Williams ,  Janine Naomi Copp

IPC分类号： C07F9/09 ,  C07C255/58 ,  C07C309/66 ,  C07C317/48 ,  C07D295/13 ,  C07D295/192 ,  C07C309/69 ,  C07C317/36 ,  C07D295/104

CPC分类号： C07F9/09 ,  C07C255/58 ,  C07C309/66 ,  C07C309/69 ,  C07C317/36 ,  C07C317/48 ,  C07D295/104 ,  C07D295/13 ,  C07D295/192 ,  C07F9/091

摘要： The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds.