KR101568799B1 - 융합된 방향족 ｐｔｐ-1ｂ 억제제 - Google Patents

융합된 방향족 ｐｔｐ-1ｂ 억제제 Download PDF

Info

Publication number
KR101568799B1
KR101568799B1 KR1020097017809A KR20097017809A KR101568799B1 KR 101568799 B1 KR101568799 B1 KR 101568799B1 KR 1020097017809 A KR1020097017809 A KR 1020097017809A KR 20097017809 A KR20097017809 A KR 20097017809A KR 101568799 B1 KR101568799 B1 KR 101568799B1
Authority
KR
South Korea
Prior art keywords
pharmaceutically acceptable
compound
acceptable salt
bromo
methyl
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.)
Expired - Fee Related
Application number
KR1020097017809A
Other languages
English (en)
Korean (ko)
Other versions
KR20090108102A (ko
Inventor
존 콜루치
마리-끌레르 윌슨
융신 한
끌로드 뒤프렌느
미셸 벨레
척 케이. 라우
크리스토퍼 베일리
Original Assignee
카네크 파마 인코포레이티드
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 카네크 파마 인코포레이티드 filed Critical 카네크 파마 인코포레이티드
Publication of KR20090108102A publication Critical patent/KR20090108102A/ko
Application granted granted Critical
Publication of KR101568799B1 publication Critical patent/KR101568799B1/ko
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/60—Quinoline or hydrogenated quinoline ring systems
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3808—Acyclic saturated acids which can have further substituents on alkyl
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3834—Aromatic acids (P-C aromatic linkage)
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020097017809A 2007-01-26 2008-01-24 융합된 방향족 ｐｔｐ-1ｂ 억제제 Expired - Fee Related KR101568799B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US89770007P 2007-01-26 2007-01-26
US60/897,700 2007-01-26
PCT/CA2008/000172 WO2008089581A1 (en) 2007-01-26 2008-01-24 Fused aromatic ptp-1b inhibitors

Publications (2)

Publication Number Publication Date
KR20090108102A KR20090108102A (ko) 2009-10-14
KR101568799B1 true KR101568799B1 (ko) 2015-11-12

Family

ID=39644072

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020097017809A Expired - Fee Related KR101568799B1 (ko) 2007-01-26 2008-01-24 융합된 방향족 ｐｔｐ-1ｂ 억제제

Country Status (16)

Country Link
US (4) US8168815B2 (enExample)
EP (1) EP2114971B1 (enExample)
JP (1) JP5570223B2 (enExample)
KR (1) KR101568799B1 (enExample)
CN (1) CN102317296B (enExample)
AU (1) AU2008209296B2 (enExample)
BR (1) BRPI0806789B8 (enExample)
CA (1) CA2675142C (enExample)
DK (1) DK2114971T3 (enExample)
ES (1) ES2547386T3 (enExample)
IL (1) IL199742A (enExample)
MX (1) MX2009007911A (enExample)
NZ (2) NZ578296A (enExample)
RU (1) RU2462469C2 (enExample)
WO (1) WO2008089581A1 (enExample)
ZA (1) ZA200904679B (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2547386T3 (es) * 2007-01-26 2015-10-05 Kaneq Pharma Inc. Inhibidores de la PTP-1B aromáticos condensados
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
CN104411710A (zh) * 2012-04-16 2015-03-11 卡内克制药公司 作为ptp-1b抑制剂前体的稠合的芳族膦酸酯衍生物
WO2014141110A2 (en) * 2013-03-14 2014-09-18 Curadev Pharma Pvt. Ltd. Aminonitriles as kynurenine pathway inhibitors
CA2977839C (en) * 2014-02-28 2022-07-26 The Royal Institution For The Advancement Of Learning / Mcgill University Tc-ptp inhibitors as apc activators for immunotherapy
CN108159069A (zh) * 2018-01-26 2018-06-15 广东省微生物研究所（广东省微生物分析检测中心） 灰树花多糖f2在制备治疗高脂血症药物、预防或延缓动脉粥样硬化药物中的应用
WO2023220833A1 (en) * 2022-05-19 2023-11-23 Kanyr Pharma Inc. Combined inhibition of tyrosine phosphatases tcptp and ptp1b and pd-1 blockage immunotherapy in the treatment of cancer
WO2024123585A1 (en) * 2022-12-05 2024-06-13 Merck Sharp & Dohme Llc Substituted quinazoline derivatives and methods of use thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006055525A2 (en) 2004-11-15 2006-05-26 Ceptyr, Inc. Protein tyrosine phosphatase inhibitors and methods of use thereof

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI83421C (fi) * 1989-06-21 1991-07-10 Huhtamaeki Oy Foerfarande foer framstaellning av farmakologiskt anvaendbara metylenbisfosfonsyraderivat.
WO1997028149A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Method for raising hdl cholesterol levels
US6174874B1 (en) * 1998-09-21 2001-01-16 Merck Frosst Canada & Co. Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B)
US6486142B2 (en) * 1999-12-22 2002-11-26 Merck Frosst Canada & Co. Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
CA2402414A1 (en) * 2000-03-22 2001-09-27 Christopher Bayly Sulfur substituted aryldifluoromethylphosphonic acids as ptp-1b inhibitors
AU7705601A (en) 2000-07-25 2002-02-05 Merck & Co Inc N-substituted indoles useful in the treatment of diabetes
HRP20050181A2 (en) 2002-08-29 2006-03-31 Merck & Co. Inc. Indoles having anti-diabetic activity
EP1713822B1 (en) * 2004-01-30 2010-03-17 Medivir AB Hcv ns-3 serine protease inhibitors
CN1942428A (zh) 2004-04-13 2007-04-04 默克公司 Cetp抑制剂
DOP2005000123A (es) 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
ES2547386T3 (es) * 2007-01-26 2015-10-05 Kaneq Pharma Inc. Inhibidores de la PTP-1B aromáticos condensados

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006055525A2 (en) 2004-11-15 2006-05-26 Ceptyr, Inc. Protein tyrosine phosphatase inhibitors and methods of use thereof

Also Published As

Publication number Publication date
EP2114971B1 (en) 2015-06-17
BRPI0806789B1 (pt) 2020-01-28
BRPI0806789A2 (pt) 2011-09-13
JP2010516715A (ja) 2010-05-20
WO2008089581A1 (en) 2008-07-31
US8168815B2 (en) 2012-05-01
NZ578296A (en) 2012-07-27
IL199742A (en) 2014-03-31
US9334295B2 (en) 2016-05-10
NZ600947A (en) 2012-12-21
CA2675142A1 (en) 2008-07-31
US20150045325A1 (en) 2015-02-12
EP2114971A1 (en) 2009-11-11
CN102317296B (zh) 2015-05-27
US20100022477A1 (en) 2010-01-28
BRPI0806789B8 (pt) 2021-05-25
CA2675142C (en) 2014-08-19
EP2114971A4 (en) 2011-07-06
AU2008209296B2 (en) 2012-12-20
MX2009007911A (es) 2009-07-31
CN102317296A (zh) 2012-01-11
ZA200904679B (en) 2010-04-28
US20130281365A1 (en) 2013-10-24
JP5570223B2 (ja) 2014-08-13
RU2009132092A (ru) 2011-03-10
DK2114971T3 (en) 2015-08-31
RU2462469C2 (ru) 2012-09-27
US20120178679A1 (en) 2012-07-12
AU2008209296A1 (en) 2008-07-31
IL199742A0 (en) 2010-04-15
ES2547386T3 (es) 2015-10-05
US8927526B2 (en) 2015-01-06
US8481742B2 (en) 2013-07-09
KR20090108102A (ko) 2009-10-14
HK1165806A1 (en) 2012-10-12

Similar Documents

Publication Publication Date Title
KR101568799B1 (ko) 융합된 방향족 ｐｔｐ-1ｂ 억제제
US6448429B1 (en) Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
JP2003528106A (ja) Ｐｔｐ−１ｂ阻害薬としての硫黄置換アリールジフルオロメチルホスホン酸類
US20020058644A1 (en) Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
US6777433B2 (en) Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
US6583126B2 (en) Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
US6486141B2 (en) Phosphonic acid biaryl derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
US20040176330A1 (en) Aryldifluoromethylphosphonic acids for treatment of diabetes
HK1165806B (en) Fused aromatic ptp-1b inhibitors

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

PN2301 Change of applicant

St.27 status event code: A-3-3-R10-R13-asn-PN2301

St.27 status event code: A-3-3-R10-R11-asn-PN2301

N231 Notification of change of applicant
PN2301 Change of applicant

St.27 status event code: A-3-3-R10-R13-asn-PN2301

St.27 status event code: A-3-3-R10-R11-asn-PN2301

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

FPAY Annual fee payment

Payment date: 20181018

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

FPAY Annual fee payment

Payment date: 20191106

Year of fee payment: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20211107

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20211107