公开(公告)号：US10426737B2

公开(公告)日：2019-10-01

申请号：US15104723

申请日：2014-12-17

申请人： Novartis AG

发明人： Luis Brito ,  Delai Chen ,  Gabriel Grant Gamber ,  Andrew Geall ,  Kevin Love ,  Thomas Zabawa ,  Frederic Zecri

IPC分类号： C07C219/06 ,  C07C219/16 ,  C07C229/12 ,  C07C235/08 ,  C07C323/52 ,  A61K9/51 ,  C07D319/06 ,  C07D233/60 ,  C07D207/12 ,  C07D207/16 ,  C07D211/22 ,  C07D295/088 ,  C07D211/62 ,  A61K47/18 ,  A61K9/127 ,  A61K31/7105 ,  A61K31/713 ,  C12N15/88 ,  A61K38/18 ,  A61K38/22 ,  A61K39/12 ,  C07D211/06 ,  C07D211/46 ,  C07D233/64 ,  C07D295/13 ,  C12N7/00 ,  C12N15/113 ,  A61K39/00

摘要： This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R3, n, p, L1 and L2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

公开(公告)号：US10406133B2

公开(公告)日：2019-09-10

申请号：US16145703

申请日：2018-09-28

申请人： Alkermes Pharma Ireland Limited

发明人： Tarek A. Zeidan ,  Scott Duncan ,  Christopher P. Hencken ,  Thomas Andrew Wynn ,  Carlos N. Sanrame

IPC分类号： C07C229/30 ,  A61K31/225 ,  C07D491/113 ,  C07D211/06 ,  C07D207/40 ,  C07D295/088 ,  C07D211/38 ,  C07D209/52 ,  C07C317/18 ,  C07D207/06 ,  C07C233/91 ,  C07C233/18 ,  C07C229/16 ,  C07C219/08 ,  C07C317/28

摘要： The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

公开(公告)号：US10344012B2

公开(公告)日：2019-07-09

申请号：US15686422

申请日：2017-08-25

申请人： CORSAIR PHARMA, INC.

发明人： Cyrus K. Becker ,  Meenakshi S. Venkatraman ,  Xiaoming Zhang ,  Jürg Pfister

IPC分类号： C07D313/00 ,  C07C69/712 ,  C07D317/40 ,  C07D321/00 ,  C07D453/02 ,  C07D257/06 ,  C07D263/24 ,  C07D265/30 ,  C07D295/088 ,  C07D211/60 ,  C07D295/145 ,  C07D307/20 ,  C07C219/16 ,  C07C235/20 ,  C07C59/54 ,  C07C69/734 ,  C07C235/34 ,  C07D207/08 ,  C07D263/26 ,  C07D317/34 ,  A61K9/70 ,  A61K31/165 ,  A61K31/216 ,  A61K31/335 ,  C07C59/31

摘要： Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.

公开(公告)号：US20190084994A1

公开(公告)日：2019-03-21

申请号：US16194608

申请日：2018-11-19

申请人： ENANTA PHARMACEUTICALS, INC.

发明人： Yao-Ling Qiu ,  Xuri Gao ,  Wei Li ,  Hui Cao ,  Meizhong Jin ,  Jorden Kass ,  Xiaowen Peng ,  Yat Sun Or

IPC分类号： C07D493/08 ,  C07D493/04 ,  C07D451/04 ,  C07D401/04 ,  C07D327/10 ,  C07D317/72 ,  C07D313/04 ,  C07D309/08 ,  C07D307/33 ,  C07D307/32 ,  C07D303/34 ,  C07D303/26 ,  C07D295/088 ,  C07D277/26 ,  C07D263/52 ,  C07D261/20 ,  C07D261/08 ,  C07D261/02 ,  C07D257/04 ,  C07D233/64 ,  C07D231/12 ,  C07D213/89 ,  C07D213/81 ,  C07D213/52 ,  C07D211/54 ,  C07D207/16 ,  C07C235/56 ,  C07B59/00 ,  C07C323/62 ,  C07C317/44 ,  C07C323/42 ,  C07C317/32 ,  C07C311/53 ,  A61K31/655 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/445 ,  A61K31/4425 ,  A61K31/4409 ,  A61K31/4402 ,  A61K31/44 ,  A61K31/439 ,  A61K31/426 ,  A61K31/421 ,  A61K31/4164 ,  A61K31/416 ,  A61K31/415 ,  A61K31/41 ,  A61K31/401 ,  A61K31/39 ,  A61K31/365 ,  A61K31/357 ,  A61K31/351 ,  A61K31/341 ,  A61K31/336 ,  A61K31/335 ,  A61K31/325 ,  A61K31/277 ,  A61K31/223 ,  A61K31/215 ,  A61K31/196 ,  A61K31/18 ,  A61K31/167

CPC分类号： C07D493/08 ,  A61K31/167 ,  A61K31/18 ,  A61K31/196 ,  A61K31/215 ,  A61K31/223 ,  A61K31/277 ,  A61K31/325 ,  A61K31/335 ,  A61K31/336 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/365 ,  A61K31/39 ,  A61K31/401 ,  A61K31/41 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/439 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4425 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/655 ,  C07B59/001 ,  C07B2200/05 ,  C07B2200/07 ,  C07C235/56 ,  C07C311/53 ,  C07C317/32 ,  C07C317/44 ,  C07C323/42 ,  C07C323/62 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/44 ,  C07C2602/46 ,  C07C2603/74 ,  C07D207/16 ,  C07D211/54 ,  C07D213/52 ,  C07D213/81 ,  C07D213/89 ,  C07D231/12 ,  C07D233/64 ,  C07D257/04 ,  C07D261/02 ,  C07D261/08 ,  C07D261/20 ,  C07D263/52 ,  C07D277/26 ,  C07D295/088 ,  C07D303/26 ,  C07D303/34 ,  C07D307/32 ,  C07D307/33 ,  C07D309/08 ,  C07D313/04 ,  C07D317/72 ,  C07D327/10 ,  C07D401/04 ,  C07D451/04 ,  C07D493/04

摘要： The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-L-R  (I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US20190029972A1

公开(公告)日：2019-01-31

申请号：US16158608

申请日：2018-10-12

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： Jiajia Dong ,  K. Barry Sharpless ,  Jeffery W. Kelly ,  Aleksandra Baranczak ,  Wentao Chen

IPC分类号： A61K31/05 ,  C07D295/088 ,  C07K2/00 ,  C07K1/113 ,  A61K31/197 ,  A61K31/397 ,  A61K31/4745 ,  A61K31/53 ,  A61K31/515 ,  A61K31/65 ,  A61K31/198 ,  A61K31/4709 ,  A61K31/40 ,  A61K31/136 ,  A61K31/485 ,  C07D277/82 ,  A61K31/70 ,  C07K1/02 ,  A61K31/7048 ,  C07D295/26 ,  A61K31/4045 ,  A61K31/4353 ,  A61K51/04 ,  C07C305/26 ,  A61K31/473 ,  A61K38/31 ,  A61K31/4168 ,  A61K31/439 ,  A61K31/56 ,  A61K31/505 ,  A61K31/407 ,  A61K31/655 ,  A61K31/47 ,  C07D295/185 ,  A61K31/5513 ,  A61K47/54 ,  A61K31/4245 ,  A61K31/14

摘要： This application describes a compound represented by Formula (I): YZX1—S(O)(X2)F)m]n  (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or —CH2CH2—, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

公开(公告)号：US10080733B2

公开(公告)日：2018-09-25

申请号：US15782128

申请日：2017-10-12

申请人： Alkermes Pharma Ireland Limited

发明人： Tarek A. Zeidan ,  Scott Duncan ,  Christopher P. Hencken ,  Thomas Andrew Wynn ,  Carlos N. Sanrame

IPC分类号： C07D491/113 ,  A61K31/225 ,  C07C317/28 ,  C07D211/38 ,  C07D295/088 ,  C07D207/40 ,  C07D211/06 ,  C07D207/06 ,  C07D209/52 ,  C07C317/18 ,  C07C219/08 ,  C07C229/16 ,  C07C233/18 ,  C07C233/91

CPC分类号： A61K31/225 ,  C07C219/08 ,  C07C229/16 ,  C07C233/18 ,  C07C233/91 ,  C07C317/18 ,  C07C317/28 ,  C07D207/06 ,  C07D207/40 ,  C07D209/52 ,  C07D211/06 ,  C07D211/38 ,  C07D295/088 ,  C07D491/113

摘要： The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

公开(公告)号：US10065936B2

公开(公告)日：2018-09-04

申请号：US15549409

申请日：2016-02-05

申请人： Gotion, Inc.

发明人： Nicole Holub ,  Juergen Herbel

IPC分类号： C07D295/088 ,  C07C303/32 ,  C07F5/02

摘要： The present invention relates to the preparation of sulfur containing ammonium and phosphonium borates KA, wherein K is a compound of formula (I), and A is an anion of formulae (IIa) or (IIb) by bringing into contact ammonium borates with sulfur containing ammonium or phosphonium halides or sulfonates.

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：US20180155304A1

公开(公告)日：2018-06-07

申请号：US15547317

申请日：2016-01-29

申请人： NOF CORPORATION ,  NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY

发明人： Yuta NAKAI ,  Kota TANGE ,  Hidetaka AKITA ,  Hideyoshi HARASHIMA ,  Ryohei TOGASHI ,  Naoya MIURA ,  Mio MAETA

IPC分类号： C07D295/088 ,  A61K9/127 ,  A61P29/00 ,  C07D311/72 ,  A61K31/573 ,  A61K31/713 ,  C12N15/64

CPC分类号： C07D295/088 ,  A61K9/127 ,  A61K9/1272 ,  A61K31/573 ,  A61K31/7088 ,  A61K31/713 ,  A61K45/00 ,  A61K47/22 ,  A61K48/00 ,  A61P29/00 ,  C07D311/00 ,  C07D311/72 ,  C12N15/64

摘要： The present invention aims to provide a cationic lipid that can be used as a nucleic acid delivery carrier, a lipid membrane structure using a cationic lipid, a nucleic acid-introducing agent using a cationic lipid, and a method of achieving nucleic acid introduction by using a nucleic acid-introducing agent containing a cationic lipid. A lipid membrane structure containing a cationic lipid represented by the formula (1) wherein each symbol is as defined in the DESCRIPTION, is superior in the stability in blood and tumor accumulation property. A nucleic acid-introducing agent using the cationic lipid can achieve high nucleic acid delivery efficiency of nucleic acid to be delivered into the cytoplasm.

公开(公告)号：US09982257B2

公开(公告)日：2018-05-29

申请号：US14414614

申请日：2013-07-12

申请人： WAVE LIFE SCIENCES LTD.

发明人： David Butler ,  Naoki Iwamoto ,  Meena ,  Nenad Svrzikapa ,  Gregory L. Verdine ,  Ivan Zlatev

IPC分类号： C12N15/113 ,  C07C317/28 ,  C07D295/088 ,  C07H21/00 ,  C12N15/11 ,  C12Q1/68

CPC分类号： C12N15/113 ,  C07C317/28 ,  C07D295/088 ,  C07H21/00 ,  C12N15/11 ,  C12N15/111 ,  C12N2310/11 ,  C12N2310/14 ,  C12N2310/31 ,  C12N2310/315 ,  C12N2330/30 ,  C12Q1/6876

摘要： The present invention relates to chirally controlled oligonucleotides, chirally controlled oligonucleotide compositions, and the method of making and using the same. The invention specifically encompasses the identification of the source of certain problems with prior methodologies for preparing chiral oligonucleotides, including problems that prohibit preparation of fully chirally controlled compositions, particularly compositions comprising a plurality of oligonucleotide types. In some embodiments, the present invention provides chirally controlled oligonucleotide compositions. In some embodiments, the present invention provides methods of making chirally controlled oligonucleotides and chirally controlled oligonucleotide compositions.