CN105492388B - 三环苯并氧杂硼杂环戊烯化合物及其用途 - Google Patents

三环苯并氧杂硼杂环戊烯化合物及其用途 Download PDF

Info

Publication number
CN105492388B
CN105492388B CN201480049562.3A CN201480049562A CN105492388B CN 105492388 B CN105492388 B CN 105492388B CN 201480049562 A CN201480049562 A CN 201480049562A CN 105492388 B CN105492388 B CN 105492388B
Authority
CN
China
Prior art keywords
mycobacterium
compound
formula
azulene
dihydro
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201480049562.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN105492388A (zh
Inventor
阿利 M.R.K.(D.)
V.S.埃尔南德斯
J.J.普拉特纳
李先锋
D.巴罗斯-阿圭尔
I.焦尔达诺
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GlaxoSmithKline Intellectual Property No 2 Ltd
Anacor Pharmaceuticals LLC
Original Assignee
GlaxoSmithKline Intellectual Property No 2 Ltd
Anacor Pharmaceuticals LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by GlaxoSmithKline Intellectual Property No 2 Ltd, Anacor Pharmaceuticals LLC filed Critical GlaxoSmithKline Intellectual Property No 2 Ltd
Priority to CN201811396796.1A priority Critical patent/CN110003253B/zh
Publication of CN105492388A publication Critical patent/CN105492388A/zh
Application granted granted Critical
Publication of CN105492388B publication Critical patent/CN105492388B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201480049562.3A 2013-08-09 2014-08-08 三环苯并氧杂硼杂环戊烯化合物及其用途 Active CN105492388B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201811396796.1A CN110003253B (zh) 2013-08-09 2014-08-08 三环苯并氧杂硼杂环戊烯化合物及其用途

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361864496P 2013-08-09 2013-08-09
US61/864,496 2013-08-09
US201361918976P 2013-12-20 2013-12-20
US61/918,976 2013-12-20
PCT/US2014/050370 WO2015021396A2 (en) 2013-08-09 2014-08-08 Tricyclic benzoxaborole compounds and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201811396796.1A Division CN110003253B (zh) 2013-08-09 2014-08-08 三环苯并氧杂硼杂环戊烯化合物及其用途

Publications (2)

Publication Number Publication Date
CN105492388A CN105492388A (zh) 2016-04-13
CN105492388B true CN105492388B (zh) 2018-12-21

Family

ID=52462052

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201480049562.3A Active CN105492388B (zh) 2013-08-09 2014-08-08 三环苯并氧杂硼杂环戊烯化合物及其用途
CN201811396796.1A Active CN110003253B (zh) 2013-08-09 2014-08-08 三环苯并氧杂硼杂环戊烯化合物及其用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201811396796.1A Active CN110003253B (zh) 2013-08-09 2014-08-08 三环苯并氧杂硼杂环戊烯化合物及其用途

Country Status (35)

Country Link
US (5) US20160251380A1 (enExample)
EP (2) EP3030519B1 (enExample)
JP (2) JP6499175B2 (enExample)
KR (1) KR102093783B1 (enExample)
CN (2) CN105492388B (enExample)
AP (1) AP2016009046A0 (enExample)
AU (2) AU2014305792C1 (enExample)
BR (1) BR112016002651B1 (enExample)
CA (1) CA2919888C (enExample)
CL (1) CL2016000313A1 (enExample)
CR (1) CR20160064A (enExample)
CY (1) CY1125030T1 (enExample)
DK (1) DK3030519T3 (enExample)
DO (1) DOP2016000045A (enExample)
EA (1) EA032844B1 (enExample)
ES (1) ES2905413T3 (enExample)
HR (1) HRP20220384T1 (enExample)
HU (1) HUE057365T2 (enExample)
IL (1) IL243874B (enExample)
LT (1) LT3030519T (enExample)
MX (1) MX375556B (enExample)
MY (1) MY175823A (enExample)
NZ (1) NZ716350A (enExample)
PE (1) PE20160752A1 (enExample)
PH (1) PH12016500234B1 (enExample)
PL (1) PL3030519T3 (enExample)
PT (1) PT3030519T (enExample)
RS (1) RS62887B1 (enExample)
SA (1) SA516370551B1 (enExample)
SG (2) SG10201914073PA (enExample)
SI (1) SI3030519T1 (enExample)
SM (1) SMT202200113T1 (enExample)
UA (1) UA116908C2 (enExample)
WO (1) WO2015021396A2 (enExample)
ZA (1) ZA201600792B (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR094961A1 (es) * 2013-03-15 2015-09-09 Lilly Co Eli 1-hidroxi-benzooxaboroles como agentes antiparasitarios
KR101636431B1 (ko) 2013-07-30 2016-07-05 동아에스티 주식회사 트리사이클릭 벤즈옥사보롤 화합물, 이의 제조방법 및 용도
US20160251380A1 (en) 2013-08-09 2016-09-01 Glaxosmithkline Intellectual Property (No.2) Limited Tricyclic benzoxaborole compounds and uses thereof
CN106459097A (zh) 2014-07-01 2017-02-22 第三共株式会社 作为抗菌剂的三环苯并氧杂硼杂环戊烯类
MA41495A (fr) * 2015-02-12 2017-12-19 Anacor Pharmaceuticals Inc Composés benzoxaborole et leurs utilisations
PE20190119A1 (es) 2016-05-12 2019-01-17 Anacor Pharmaceuticals Inc Esteres de oxaborol y sus usos
CN109387594B (zh) * 2017-08-08 2021-01-19 武汉武药科技有限公司 一种分离和分析贝达喹啉光学异构体的方法
ES2949908T3 (es) * 2018-01-09 2023-10-03 Halcyon Labs Private Ltd Proceso para la preparación de Crisaborol y sus intermedios
EP4164645A4 (en) * 2020-06-15 2024-07-10 The Global Alliance for TB Drug Development, Inc. COMBINED ANTIBACTERIAL COMPOSITION AND ANTIBACTERIAL THERAPY METHOD
CN111606850B (zh) * 2020-07-07 2023-07-25 安徽贝克生物制药有限公司 贝达喹啉及其中间体的制备方法
US11793808B2 (en) 2021-02-22 2023-10-24 Mannkind Corp. Compositions of clofazimine, combinations comprising them, processes for their preparation, uses and methods comprising them
CA3239097A1 (en) 2022-06-23 2023-12-28 Shanghai Micurx Pharmaceutical Co., Ltd. Prodrugs of boron compounds and their use in treating bacterial infections
JP2025520237A (ja) * 2022-06-23 2025-07-03 ミクウルク ファーマシューティカルズ, インコーポレイテッド ホウ素化合物を用いて非結核性マイコバクテリア感染症を治療する方法及びその用途、並びに同じ疾患を治療するための医薬組成物
WO2024208907A1 (en) 2023-04-05 2024-10-10 Glaxosmithkline Intellectual Property (No. 2) Limited Synthesis of 3-(aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3h)-ol
CN117379430B (zh) * 2023-10-11 2026-07-21 深圳市第三人民医院(深圳市肝病研究所) 一种地拉韦啶的用途

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101505603A (zh) * 2005-12-30 2009-08-12 安纳考尔医药公司 含硼的小分子
CN101772302A (zh) * 2007-06-20 2010-07-07 安纳考尔医药公司 含硼小分子
CN102821609A (zh) * 2010-04-07 2012-12-12 葛兰素史密丝克莱恩有限责任公司 用于制备苯并氧杂硼杂环戊烯的方法
CN103140228A (zh) * 2010-09-07 2013-06-05 阿纳科制药公司 苯并氧杂硼杂环戊二烯衍生物用于治疗细菌感染
WO2013093615A1 (en) * 2011-12-22 2013-06-27 Micurx Pharmaceuticals, Inc. Tricyclic boron compounds for antimicrobial therapy

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998024753A1 (en) 1996-12-02 1998-06-11 Chisso Corporation Optically active nitro alcohol derivatives, optically active amino alcohol derivates, and process for preparing the same
US7446236B2 (en) 2002-12-02 2008-11-04 Solvias Ag Catalytic hydrogenation of carbon-heteroatom double bonds
ES2872962T3 (es) 2005-02-16 2021-11-03 Anacor Pharmaceuticals Inc Boronoftalidas para uso terapéutico
US7767657B2 (en) 2005-02-16 2010-08-03 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
JP5084717B2 (ja) 2005-03-08 2012-11-28 エージェンシー フォー サイエンス,テクノロジー アンド リサーチ キラル・ビスオキサゾリン触媒
KR100848491B1 (ko) 2007-01-16 2008-07-28 영진약품공업주식회사 베타아미노기를 갖는 2-싸이아졸리딘 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법
SG172040A1 (en) 2008-12-17 2011-07-28 Anacor Pharmaceuticals Inc Polymorphs of (s)-3-aminomethyl-7-(3-hydroxy-propoxy)-3h-benzo[c][1,2] oxaborol-1-ol
KR101636431B1 (ko) 2013-07-30 2016-07-05 동아에스티 주식회사 트리사이클릭 벤즈옥사보롤 화합물, 이의 제조방법 및 용도
US20160251380A1 (en) 2013-08-09 2016-09-01 Glaxosmithkline Intellectual Property (No.2) Limited Tricyclic benzoxaborole compounds and uses thereof
MA41495A (fr) * 2015-02-12 2017-12-19 Anacor Pharmaceuticals Inc Composés benzoxaborole et leurs utilisations

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101505603A (zh) * 2005-12-30 2009-08-12 安纳考尔医药公司 含硼的小分子
CN101772302A (zh) * 2007-06-20 2010-07-07 安纳考尔医药公司 含硼小分子
CN102821609A (zh) * 2010-04-07 2012-12-12 葛兰素史密丝克莱恩有限责任公司 用于制备苯并氧杂硼杂环戊烯的方法
CN103140228A (zh) * 2010-09-07 2013-06-05 阿纳科制药公司 苯并氧杂硼杂环戊二烯衍生物用于治疗细菌感染
WO2013093615A1 (en) * 2011-12-22 2013-06-27 Micurx Pharmaceuticals, Inc. Tricyclic boron compounds for antimicrobial therapy

Also Published As

Publication number Publication date
RS62887B1 (sr) 2022-03-31
SA516370551B1 (ar) 2017-10-31
US20160251380A1 (en) 2016-09-01
CN110003253A (zh) 2019-07-12
AU2014305792A1 (en) 2016-03-10
WO2015021396A2 (en) 2015-02-12
CN110003253B (zh) 2022-03-18
PE20160752A1 (es) 2016-08-17
SG11201600787PA (en) 2016-03-30
AP2016009046A0 (en) 2016-02-29
US20210053999A1 (en) 2021-02-25
HK1219939A1 (zh) 2017-04-21
ES2905413T3 (es) 2022-04-08
JP6764970B2 (ja) 2020-10-07
US20200095266A1 (en) 2020-03-26
PT3030519T (pt) 2022-01-27
DK3030519T3 (da) 2022-01-31
EP3030519A2 (en) 2016-06-15
CN105492388A (zh) 2016-04-13
DOP2016000045A (es) 2016-04-29
SI3030519T1 (sl) 2022-04-29
CL2016000313A1 (es) 2016-09-23
MX375556B (es) 2025-03-06
HUE057365T2 (hu) 2022-05-28
JP2019123727A (ja) 2019-07-25
CA2919888C (en) 2022-10-18
US10858376B2 (en) 2020-12-08
AU2017210567B2 (en) 2019-08-01
KR102093783B1 (ko) 2020-03-26
AU2014305792B2 (en) 2017-05-04
HRP20220384T1 (hr) 2022-07-22
AU2014305792C1 (en) 2018-07-05
US20180044355A1 (en) 2018-02-15
SG10201914073PA (en) 2020-03-30
WO2015021396A9 (en) 2016-02-11
PH12016500234B1 (en) 2019-01-30
KR20160038901A (ko) 2016-04-07
CR20160064A (es) 2016-06-01
PL3030519T3 (pl) 2022-05-23
WO2015021396A3 (en) 2015-10-29
US20190241586A1 (en) 2019-08-08
IL243874B (en) 2018-11-29
JP2016527321A (ja) 2016-09-08
IL243874A0 (en) 2016-04-21
UA116908C2 (uk) 2018-05-25
US10308668B2 (en) 2019-06-04
BR112016002651B1 (pt) 2022-11-29
NZ716350A (en) 2022-12-23
MX2016001732A (es) 2016-05-18
EP3030519A4 (en) 2017-03-08
US10526352B2 (en) 2020-01-07
EP3030519B1 (en) 2022-01-05
PH12016500234A1 (en) 2016-05-16
ZA201600792B (en) 2022-05-25
EA032844B1 (ru) 2019-07-31
MY175823A (en) 2020-07-10
EP4029870A1 (en) 2022-07-20
CA2919888A1 (en) 2015-02-12
JP6499175B2 (ja) 2019-04-10
LT3030519T (lt) 2022-04-11
SMT202200113T1 (it) 2022-05-12
EA201690135A1 (ru) 2016-07-29
BR112016002651A2 (pt) 2017-08-01
CY1125030T1 (el) 2023-03-24
AU2017210567A1 (en) 2017-08-24

Similar Documents

Publication Publication Date Title
KR102093783B1 (ko) 트리시클릭 벤족사보롤 화합물 및 이의 용도
TWI730953B (zh) 苯并氧雜硼化合物及其用途
HK1240232B (en) 4-substituted benzoxaborole compounds and uses thereof
HK1240232A1 (en) 4-substituted benzoxaborole compounds and uses thereof

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
CP01 Change in the name or title of a patent holder
CP01 Change in the name or title of a patent holder

Address after: The Middlesex County

Patentee after: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) Ltd.

Patentee after: Anaco Pharmaceutical Co.,Ltd.

Address before: The Middlesex County

Patentee before: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) Ltd.

Patentee before: Anacor Pharmaceuticals, Inc.