CN102971325B - 用于减少β-淀粉样蛋白产生的化合物 - Google Patents

用于减少β-淀粉样蛋白产生的化合物 Download PDF

Info

Publication number
CN102971325B
CN102971325B CN201180034655.5A CN201180034655A CN102971325B CN 102971325 B CN102971325 B CN 102971325B CN 201180034655 A CN201180034655 A CN 201180034655A CN 102971325 B CN102971325 B CN 102971325B
Authority
CN
China
Prior art keywords
bridge
nitrilo
cyclopenta
oxa
methyne
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
CN201180034655.5A
Other languages
English (en)
Chinese (zh)
Other versions
CN102971325A (zh
Inventor
K.M.博伊
J.M.盖尔农
J.E.马科
L.A.汤普森三世
邬永金
张云惠
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.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN102971325A publication Critical patent/CN102971325A/zh
Application granted granted Critical
Publication of CN102971325B publication Critical patent/CN102971325B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06Peri-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201180034655.5A 2010-07-15 2011-07-12 用于减少β-淀粉样蛋白产生的化合物 Expired - Fee Related CN102971325B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US36442510P 2010-07-15 2010-07-15
US61/364425 2010-07-15
US61/364,425 2010-07-15
PCT/US2011/043628 WO2012009309A1 (en) 2010-07-15 2011-07-12 Compounds for the reduction of beta-amyloid production

Publications (2)

Publication Number Publication Date
CN102971325A CN102971325A (zh) 2013-03-13
CN102971325B true CN102971325B (zh) 2016-01-20

Family

ID=44511486

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180034655.5A Expired - Fee Related CN102971325B (zh) 2010-07-15 2011-07-12 用于减少β-淀粉样蛋白产生的化合物

Country Status (18)

Country Link
US (1) US8637523B2 (https=)
EP (1) EP2593461B1 (https=)
JP (1) JP5755739B2 (https=)
KR (1) KR20130041944A (https=)
CN (1) CN102971325B (https=)
AR (1) AR082241A1 (https=)
AU (1) AU2011279412B2 (https=)
BR (1) BR112013000920A2 (https=)
CA (1) CA2805294A1 (https=)
CO (1) CO6670589A2 (https=)
EA (1) EA021527B1 (https=)
IL (1) IL224202A (https=)
MX (1) MX2013000514A (https=)
NZ (1) NZ606950A (https=)
SG (1) SG186392A1 (https=)
TW (1) TW201206946A (https=)
WO (1) WO2012009309A1 (https=)
ZA (1) ZA201301178B (https=)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0696663B2 (ja) 1986-08-04 1994-11-30 東レ株式会社 樹脂組成物
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
KR101473081B1 (ko) 2013-01-25 2014-12-16 영남대학교 산학협력단 고리형 2-다이아조-1,3-다이카보닐 화합물을 출발물질로 하는 고리형 베타-엔아미노아마이드 유도체 및 우라실 유도체의 합성방법
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
WO2014180524A1 (en) * 2013-05-06 2014-11-13 Merck Patent Gmbh Macrocycles as kinase inhibitors
DK3004080T3 (da) 2013-06-04 2019-01-02 Acturum Real Estate Ab Triazolforbindelser og deres anvendelse som gamma-sekretase-modulatorer
US9611254B2 (en) 2013-06-04 2017-04-04 Acturum Life Science AB Triazole compounds and their use as gamma secretase modulators
NO3004079T3 (https=) 2013-06-04 2018-06-16
EP3126355A1 (en) * 2014-04-02 2017-02-08 Bristol-Myers Squibb Company Difluoromethoxy compound with low bioactivation potential for the reduction of beta-amyloid production
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
JP6847099B2 (ja) 2015-09-29 2021-03-24 バイエル ファーマ アクチエンゲゼルシャフト 新規な大環状スルホンジイミン化合物
ES2819869T3 (es) 2015-10-08 2021-04-19 Bayer Pharma AG Nuevos compuestos macrocíclicos modificados
WO2017060322A2 (en) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Ptefb-inhibitor-adc
EP3601236A1 (en) 2017-03-28 2020-02-05 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
ES2900199T3 (es) 2017-03-28 2022-03-16 Bayer Ag Novedosos compuestos macrocíclicos inhibidores de PTEFB
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
CN111471056B (zh) * 2019-01-23 2021-07-02 成都先导药物开发股份有限公司 一种大环类免疫调节剂
CN113412260B (zh) * 2019-01-29 2022-08-02 山东轩竹医药科技有限公司 己酮糖激酶抑制剂及其用途
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Fgfr阻害剤の誘導体
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009073777A1 (en) * 2007-12-06 2009-06-11 Schering Corporation Gamma secretase modulators
WO2009076352A1 (en) * 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
WO2009087127A1 (en) * 2008-01-11 2009-07-16 F. Hoffmann-La Roche Ag Modulators for amyloid beta

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007058627A1 (en) * 2005-11-16 2007-05-24 S*Bio Pte Ltd Oxygen linked pyrimidine derivatives
US7932261B2 (en) * 2006-02-06 2011-04-26 Janssen Pharmaceutica Nv Macrocycle derivatives useful as inhibitors of β-secretase (BACE)
ITMI20061513A1 (it) 2006-07-31 2008-02-01 Poli Costruzione Materiali Trazione Spa Unita' frenante compatta a disco per veicoli su rotaia

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009073777A1 (en) * 2007-12-06 2009-06-11 Schering Corporation Gamma secretase modulators
WO2009076352A1 (en) * 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
WO2009087127A1 (en) * 2008-01-11 2009-07-16 F. Hoffmann-La Roche Ag Modulators for amyloid beta

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
β-Amyloid Peptide as a target for treatment of Alzheimer"s disease;Santiago Conde;《Expert Opin. Ther. Patents》;20020101;第12卷(第4期);第503-512页 *

Also Published As

Publication number Publication date
AU2011279412B2 (en) 2014-12-11
IL224202A (en) 2016-04-21
SG186392A1 (en) 2013-02-28
EA201270824A1 (ru) 2013-04-30
JP2013531040A (ja) 2013-08-01
EP2593461A1 (en) 2013-05-22
EA021527B1 (ru) 2015-07-30
TW201206946A (en) 2012-02-16
BR112013000920A2 (pt) 2016-05-17
KR20130041944A (ko) 2013-04-25
EP2593461B1 (en) 2016-08-17
AR082241A1 (es) 2012-11-21
ZA201301178B (en) 2014-07-30
MX2013000514A (es) 2013-02-27
US8637523B2 (en) 2014-01-28
NZ606950A (en) 2014-08-29
CN102971325A (zh) 2013-03-13
JP5755739B2 (ja) 2015-07-29
CO6670589A2 (es) 2013-05-15
AU2011279412A1 (en) 2013-03-07
US20120184565A1 (en) 2012-07-19
CA2805294A1 (en) 2012-01-19
WO2012009309A1 (en) 2012-01-19

Similar Documents

Publication Publication Date Title
CN102971325B (zh) 用于减少β-淀粉样蛋白产生的化合物
TWI468402B (zh) 降低β-類澱粉生成之化合物
CN102356081B (zh) 减少β-淀粉状蛋白生成的双环化合物
US8637525B2 (en) Compounds for the reduction of beta-amyloid production
EP2668168B1 (en) COMPOUNDS FOR THE REDUCTION OF ß-AMYLOID PRODUCTION
CN118525021A (zh) 靶向malt1的蛋白降解化合物
CN113045569A (zh) 用作ret激酶抑制剂的化合物及其应用
WO2016001077A1 (en) Compounds inhibiting the enzyme monopolar spindle 1 kinase,pharmaceutical compositions and uses thereof
EP4444289A1 (en) Pyridopyrimidines and methods of their use
KR20240132285A (ko) 비시클릭 헤테로아렌 및 그의 사용 방법
HK1164732B (en) Compounds for the reduction of beta-amyloid production

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20160120

Termination date: 20170712