公开(公告)号：US11680037B2

公开(公告)日：2023-06-20

申请号：US17387004

申请日：2021-07-28

Applicant: DAIKIN INDUSTRIES, LTD.

Inventor： Masahiro Higashi ,  Moe Hosokawa ,  Akiyoshi Yamauchi ,  Sumi Ishihara ,  Yosuke Kishikawa

IPC: C07C235/12 ,  C07C55/02 ,  C07C65/21 ,  C07C233/47

CPC classification number: C07C235/12 ,  C07C55/02 ,  C07C65/21 ,  C07C233/47

Abstract: A novel branched fluorine-containing compound represented by formula (1):




wherein L represents a predetermined carbon-containing linker moiety; Rf, in each occurrence, is the same or different and represents fluoroalkyl optionally having at least one ether bond; Y, in each occurrence, is the same or different and represents a predetermined divalent linking group or a bond; RY, in each occurrence, is the same or different and represents hydrogen or an organic group; L represents an (n1+n2)-valent carbon-containing linker moiety having at least one carbon atom; n1 represents a number greater than or equal to 1; n2 represents a number greater than or equal to 1; n1+n2 is a number from 3 to 6; X, in each occurrence, is the same or different and represents a divalent linking group or a bond; A, in each occurrence, is the same or different and represents -ArSO3M or the like; M, in each occurrence, is the same or different and represents hydrogen, —NR4, or a metal salt; and R represents hydrogen or a C1-4 organic group.

公开(公告)号：US10053417B2

公开(公告)日：2018-08-21

申请号：US15806722

申请日：2017-11-08

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Erik Fenster ,  Melissa Fleury ,  Adam D. Hughes

IPC: A61K31/40 ,  A61K31/42 ,  A61K31/44 ,  A61K31/197 ,  A61K31/397 ,  A61K31/5375 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D213/56 ,  C07C235/34 ,  C07D261/04 ,  C07D295/32 ,  C07C243/38 ,  A61K31/341 ,  A61K31/4409 ,  C07D213/86 ,  C07D213/87 ,  C07C235/80 ,  A61K31/4406 ,  A61K31/192 ,  C07D213/65 ,  A61K45/06 ,  A61K31/495 ,  A61K31/4015 ,  C07D307/68 ,  C07D213/61 ,  C07D211/62 ,  C07D211/60 ,  C07D211/48 ,  C07D211/46 ,  C07D211/42 ,  C07D211/38 ,  C07D211/22 ,  C07C243/32 ,  C07C243/24 ,  C07D493/10 ,  C07D207/16 ,  C07D207/12 ,  C07D207/08 ,  C07D265/30 ,  C07C235/78 ,  C07C235/74 ,  C07C235/20 ,  C07C235/12 ,  C07C233/56 ,  C07D261/02 ,  C07D239/36 ,  C07D405/06 ,  C07D401/04 ,  C07D233/06 ,  C07D309/08 ,  C07C259/04 ,  C07D213/75 ,  C07D491/107

CPC classification number: C07C243/38 ,  A61K31/192 ,  A61K31/197 ,  A61K31/341 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07C233/56 ,  C07C235/12 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C235/80 ,  C07C243/24 ,  C07C243/32 ,  C07C259/04 ,  C07C2601/08 ,  C07C2601/16 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/38 ,  C07D211/42 ,  C07D211/46 ,  C07D211/48 ,  C07D211/60 ,  C07D211/62 ,  C07D213/56 ,  C07D213/61 ,  C07D213/65 ,  C07D213/75 ,  C07D213/86 ,  C07D213/87 ,  C07D233/06 ,  C07D239/36 ,  C07D261/02 ,  C07D261/04 ,  C07D265/30 ,  C07D295/32 ,  C07D307/68 ,  C07D309/08 ,  C07D401/04 ,  C07D405/06 ,  C07D491/107 ,  C07D493/10

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US09951002B2

公开(公告)日：2018-04-24

申请号：US15818424

申请日：2017-11-20

Applicant: Arcturus Therapeutics, Inc.

Inventor： Joseph E. Payne ,  Padmanabh Chivukula

IPC: C07C323/52 ,  C12N15/113

CPC classification number: C07C323/52 ,  A61K47/18 ,  A61K47/20 ,  C07C235/12 ,  C07C237/12 ,  C07C271/22 ,  C07C323/25 ,  C07C323/60 ,  C07C333/04 ,  C07J41/0055 ,  C11C3/04 ,  C12N15/111 ,  C12N15/113 ,  C12N15/1137 ,  C12N2310/14 ,  C12N2320/32

Abstract: What is described is a compound having the formula wherein R1 is branched alkyl of the structure (CH3(CH2)m)2CH—, wherein m is 2 or 3; R2 is a linear alkyl of 1, 2, 3, 4, 5, 6, 7, 8, or 9 carbons, a branched alkyl of 3, 4, 5, 6, 7, 8, or 9 carbons, or an alkenyl or alkynyl of 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 carbons; R3 is —(CH2)p—, wherein p is 2, 3, 4, 5 or 6; R4 and R5 are the same or different, each a hydrogen, or a linear or branched alkyl of 1, 2, 3, 4, 5 or 6 carbons; L1 and L2 are the same or different, of the structure —(CH2)n—, wherein n is 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, or 18; L3 is a bond; X1 is —CO—O— whereby -L2-CO—O—R2 is formed; X2 is S or O; and X3 is —CO—O— whereby -L1-CO—O—R1 is formed; and wherein m+n+p is 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, or 27; or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20170369425A1

公开(公告)日：2017-12-28

申请号：US15543261

申请日：2016-01-15

Applicant: SHOWA DENKO K.K.

Inventor： Toru TACHIBANA ,  Ryota NIIBAYASHI ,  Daisuke YAGYU

IPC: C07C235/12 ,  A61K8/67 ,  A23L33/15 ,  A61Q19/00

CPC classification number: C07C235/12 ,  A23L33/15 ,  A23V2002/00 ,  A61K8/44 ,  A61K8/673 ,  A61K31/197 ,  A61K2800/10 ,  A61Q19/00

Abstract: Provided is a compound represented by Formula (1) or a salt thereof (in the formula, R1 and R2 each independently represent a hydrogen atom or a linear or branched acyl group having 11 to 30 carbon atoms, a hydrocarbon group bonded to a carbonyl carbon of the acyl group is a saturated or unsaturated hydrocarbon group, and at least one of R1 and R2 represents the acyl group).

公开(公告)号：US20170327459A1

公开(公告)日：2017-11-16

申请号：US15600998

申请日：2017-05-22

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Erik Fenster ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07C243/38 ,  C07D491/107 ,  A61K31/192 ,  C07D405/06 ,  C07D401/04 ,  C07D309/08 ,  C07D307/68 ,  C07D295/32 ,  C07D265/30 ,  C07D261/04 ,  C07D261/02 ,  C07D239/36 ,  C07D233/06 ,  C07D213/87 ,  C07D213/86 ,  C07D213/75 ,  C07D213/65 ,  C07D213/61 ,  C07D213/56 ,  C07D211/62 ,  C07D211/60 ,  C07D211/48 ,  C07D211/46 ,  C07D211/42 ,  C07D211/38 ,  C07D211/22 ,  C07D207/16 ,  C07D207/14 ,  C07D207/12 ,  C07D207/09 ,  C07D207/08 ,  C07D205/04 ,  C07C259/04 ,  C07C243/32 ,  C07C243/24 ,  C07C235/80 ,  C07C235/78 ,  C07C235/74 ,  C07C235/34 ,  C07C235/20 ,  C07C235/12 ,  C07C233/56 ,  A61K45/06 ,  A61K31/5375 ,  A61K31/495 ,  A61K31/4409 ,  A61K31/4406 ,  A61K31/44 ,  A61K31/42 ,  A61K31/4015 ,  A61K31/40 ,  A61K31/397 ,  A61K31/341 ,  A61K31/197 ,  C07D493/10 ,  C07C2601/16 ,  C07C2601/08

CPC classification number: C07C243/38 ,  A61K31/192 ,  A61K31/197 ,  A61K31/341 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07C233/56 ,  C07C235/12 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C235/80 ,  C07C243/24 ,  C07C243/32 ,  C07C259/04 ,  C07C2601/08 ,  C07C2601/16 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/38 ,  C07D211/42 ,  C07D211/46 ,  C07D211/48 ,  C07D211/60 ,  C07D211/62 ,  C07D213/56 ,  C07D213/61 ,  C07D213/65 ,  C07D213/75 ,  C07D213/86 ,  C07D213/87 ,  C07D233/06 ,  C07D239/36 ,  C07D261/02 ,  C07D261/04 ,  C07D265/30 ,  C07D295/32 ,  C07D307/68 ,  C07D309/08 ,  C07D401/04 ,  C07D405/06 ,  C07D491/107 ,  C07D493/10

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US20170144967A1

公开(公告)日：2017-05-25

申请号：US15423008

申请日：2017-02-02

Applicant: Arcturus Therapeutics, Inc.

Inventor： Joseph E. Payne ,  Padmanabh Chivukula

IPC: C07C323/52 ,  C12N15/113

CPC classification number: C07C323/52 ,  A61K47/18 ,  A61K47/20 ,  C07C235/12 ,  C07C237/12 ,  C07C271/22 ,  C07C323/25 ,  C07C323/60 ,  C07C333/04 ,  C07J41/0055 ,  C11C3/04 ,  C12N15/111 ,  C12N15/113 ,  C12N15/1137 ,  C12N2310/14 ,  C12N2320/32

Abstract: What is described is a compound wherein R1 and R2 are the same or different, each a linear or branched alkyl with 1-9 carbons, or an alkenyl or alkynyl with 2 to 11 carbons; L1 and L2 are the same or different, each a linear alkyl having 3 to 18 carbons; X1 and X3 are —CO—O—; X3 is S or O; L3 is a lower alkyl; R3 is a lower alkyl; and R4 and R5 are the same or different, each a lower alkyl; or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20170114006A1

公开(公告)日：2017-04-27

申请号：US15381535

申请日：2016-12-16

Applicant: BioTheryX, Inc.

Inventor： Kyle W.H. Chan ,  Frank Mercurio ,  David I. Stirling

IPC: C07C235/12 ,  C07C237/12 ,  C07D207/16 ,  C07C237/22 ,  C07C233/47 ,  C07D307/24

CPC classification number: C07C235/12 ,  C07B2200/07 ,  C07C229/34 ,  C07C233/47 ,  C07C233/63 ,  C07C235/20 ,  C07C235/78 ,  C07C237/12 ,  C07C237/22 ,  C07C271/22 ,  C07D207/16 ,  C07D307/24

Abstract: Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds.

公开(公告)号：US20170101370A1

公开(公告)日：2017-04-13

申请号：US15347647

申请日：2016-11-09

Applicant: Arcturus Therapeutics, Inc.

Inventor： Joseph E. Payne ,  Padmanabh Chivukula

IPC: C07C323/25 ,  A61K47/18 ,  A61K47/20 ,  C07C333/04 ,  C07C271/22

CPC classification number: C07C323/52 ,  A61K47/18 ,  A61K47/20 ,  C07C235/12 ,  C07C237/12 ,  C07C271/22 ,  C07C323/25 ,  C07C323/60 ,  C07C333/04 ,  C07J41/0055 ,  C11C3/04 ,  C12N15/111 ,  C12N15/113 ,  C12N15/1137 ,  C12N2310/14 ,  C12N2320/32

Abstract: What is described is a compound of formula I wherein R is a linear alkyl of 1 to 12 carbons, or a linear alkenyl or alkynyl of 2 to 12 carbons; L is a linear alkylene or alkenylene of 5 to 18 carbons; X is —CO—O— or —O—CO—; Y is S or O; R1 is a linear or branched alkylene consisting of 1 to 6 carbons; and R2 and R3 are the same or different, consisting of a hydrogen or a linear or branched alkyl consisting of 1 to 6 carbons; and n is 1-6; or a salt, a solvate, or a pharmaceutical formulation thereof.

公开(公告)号：US09546131B2

公开(公告)日：2017-01-17

申请号：US14447473

申请日：2014-07-30

Applicant: BioTheryX, Inc.

Inventor： Kyle W. H. Chan ,  Frank Mercurio ,  David I. Stirling

IPC: C07C235/78 ,  C07C229/34 ,  C07D307/24 ,  C07D207/16 ,  C07C233/63 ,  C07C235/12 ,  C07C237/12 ,  C07C233/47 ,  C07C235/20 ,  C07C271/22

CPC classification number: C07C235/12 ,  C07B2200/07 ,  C07C229/34 ,  C07C233/47 ,  C07C233/63 ,  C07C235/20 ,  C07C235/78 ,  C07C237/12 ,  C07C237/22 ,  C07C271/22 ,  C07D207/16 ,  C07D307/24

Abstract: Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds.

Abstract translation: 本文公开了取代的联芳基烷基酰胺化合物，合成取代的联芳基烷基酰胺化合物的方法和用取代的联芳基烷基酰胺化合物治疗疾病和/或病症的方法。

公开(公告)号：US09422341B2

公开(公告)日：2016-08-23

申请号：US14377748

申请日：2013-02-07

Applicant: Stella Pharma Corporation ,  Osaka Prefecture University Public Corporation

Inventor： Mitsunori Kirihata ,  Kohki Uehara

IPC: C07K11/02 ,  C07C229/08 ,  C07C235/12 ,  C07K14/32 ,  C07C229/24 ,  C07D273/00 ,  C07C237/12 ,  C07K11/00

CPC classification number: C07K11/02 ,  C07C229/08 ,  C07C229/24 ,  C07C235/12 ,  C07C237/12 ,  C07D273/00 ,  C07K11/00 ,  C07K14/32

Abstract: The purpose of the present invention is to provide a novel method for producing cereulide and a derivative thereof; an intermediate for cereulide; and a novel cereulide derivative. A novel didepsipeptide, a novel tetradepsipeptide, a novel octadepsipeptide and a novel dodecadepsipeptide are prepared. A linear precursor of cereulide or a derivative thereof, which is composed of any one of the novel depsipeptides, is cyclized by forming an intramolecular amide bond.

Abstract translation: 本发明的目的是提供一种制备大戟素及其衍生物的新方法; 大众中间物 和一种新型的cereulide衍生物。 制备了一种新型的七叶皂苷肽，一种新型的四肽类，一种新的十八肽和一种新的十二十一生物肽。 通过形成分子内酰胺键将由任何一种新的缩肽组成的大脑或其衍生物的线性前体环化。