CN102548557B - 用于降低β-淀粉状蛋白生成的化合物 - Google Patents

用于降低β-淀粉状蛋白生成的化合物 Download PDF

Info

Publication number
CN102548557B
CN102548557B CN201080043469.3A CN201080043469A CN102548557B CN 102548557 B CN102548557 B CN 102548557B CN 201080043469 A CN201080043469 A CN 201080043469A CN 102548557 B CN102548557 B CN 102548557B
Authority
CN
China
Prior art keywords
dihydro
pyrimidine
chloro
pyrano
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
CN201080043469.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN102548557A (zh
Inventor
K·M·博伊
J·M·盖尔农
J·E·马科
R·E·奥尔森
施建良
L·A·汤普森三世
邬永金
徐力
张云惠
D·S·策夫
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 CN102548557A publication Critical patent/CN102548557A/zh
Application granted granted Critical
Publication of CN102548557B publication Critical patent/CN102548557B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/113Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201080043469.3A 2009-07-31 2010-07-28 用于降低β-淀粉状蛋白生成的化合物 Expired - Fee Related CN102548557B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US23020209P 2009-07-31 2009-07-31
US61/230202 2009-07-31
US61/230,202 2009-07-31
US32420110P 2010-04-14 2010-04-14
US61/324201 2010-04-14
US61/324,201 2010-04-14
PCT/US2010/043487 WO2011014535A1 (en) 2009-07-31 2010-07-28 COMPOUNDS FOR THE REDUCTION OF β-AMYLOID PRODUCTION

Publications (2)

Publication Number Publication Date
CN102548557A CN102548557A (zh) 2012-07-04
CN102548557B true CN102548557B (zh) 2014-12-24

Family

ID=43066942

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080043469.3A Expired - Fee Related CN102548557B (zh) 2009-07-31 2010-07-28 用于降低β-淀粉状蛋白生成的化合物

Country Status (28)

Country Link
US (4) US8486952B2 (enExample)
EP (1) EP2459197B1 (enExample)
JP (1) JP5680082B2 (enExample)
KR (1) KR20140015126A (enExample)
CN (1) CN102548557B (enExample)
AR (1) AR077434A1 (enExample)
AU (1) AU2010279019B2 (enExample)
BR (1) BR112012002270A2 (enExample)
CA (1) CA2766515A1 (enExample)
CO (1) CO6430430A2 (enExample)
DK (1) DK2459197T3 (enExample)
EA (1) EA020322B1 (enExample)
ES (1) ES2554327T3 (enExample)
HR (1) HRP20151133T1 (enExample)
HU (1) HUE026705T2 (enExample)
IL (1) IL217173A (enExample)
MX (1) MX2012000973A (enExample)
MY (1) MY156274A (enExample)
NZ (1) NZ597701A (enExample)
PE (1) PE20120897A1 (enExample)
PL (1) PL2459197T3 (enExample)
PT (1) PT2459197E (enExample)
SG (1) SG177526A1 (enExample)
SI (1) SI2459197T1 (enExample)
SM (1) SMT201600011B (enExample)
TW (1) TWI468402B (enExample)
WO (1) WO2011014535A1 (enExample)
ZA (1) ZA201200409B (enExample)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010099279A1 (en) * 2009-02-27 2010-09-02 Dow Agrosciences Llc N-alkoxyamides of 6-(substituted phenyl)-4-aminopicolinates and 2-(substituted phenyl)-6-amino-4-pyrimidinecarboxylates and their use as selective herbicides for crops
WO2012029991A1 (en) 2010-09-02 2012-03-08 Takeda Pharmaceutical Company Limited Fused triazoles for the treatment or prophylaxis of mild cognitive impairment
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
TW201309655A (zh) * 2011-01-28 2013-03-01 必治妥美雅史谷比公司 降低β-類澱粉生成之化合物
KR101946499B1 (ko) 2011-04-08 2019-02-11 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염 치료를 위한 피리미딘 유도체
US9206195B2 (en) 2011-08-09 2015-12-08 Boehringer Ingelheim International Gmbh Dihydrothienopyrimidines
EP2776439B1 (en) 2011-11-09 2018-07-04 Janssen Sciences Ireland UC Purine derivatives for the treatment of viral infections
EA039373B1 (ru) 2012-02-08 2022-01-19 Янссен Сайенсиз Айрлэнд Юси Производные пиперидино-пиримидина для лечения вирусных инфекций
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
CA2874800C (en) 2012-07-13 2021-04-06 Janssen R&D Ireland Macrocyclic purines for the treatment of viral infections
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
NZ705589A (en) 2012-10-10 2019-05-31 Janssen Sciences Ireland Uc Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
AU2013346793B2 (en) 2012-11-16 2018-03-08 Janssen Sciences Ireland Uc Heterocyclic substituted 2-amino-quinazoline derivatives for the treatment of viral infections
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
KR102225233B1 (ko) 2013-02-21 2021-03-09 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염의 치료를 위한 2-아미노피리미딘 유도체
WO2014127816A1 (en) 2013-02-21 2014-08-28 Boehringer Ingelheim International Gmbh Dihydropteridinones ii
JP6052527B2 (ja) 2013-02-21 2016-12-27 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ジヒドロプテリジノンi
MX366481B (es) 2013-03-29 2019-07-09 Janssen Sciences Ireland Uc Deaza-purinonas macrociclicas para el tratamiento de infecciones virales.
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為fgfr抑制劑之雙環雜環
MY188071A (en) 2013-05-24 2021-11-16 Janssen Sciences Ireland Uc Pyridone derivatives for the treatment of viral infections and further diseases
EP3004080B1 (en) 2013-06-04 2018-10-10 Acturum Real Estate AB Triazole compounds and their use as gamma secretase modulators
WO2014195321A1 (en) 2013-06-04 2014-12-11 Acturum Life Science AB Triazole compounds and their use as gamma secretase modulators
ES2665421T3 (es) 2013-06-04 2018-04-25 Acturum Real Estate Ab Compuestos de pirimidina y su uso como moduladores de la gamma secretasa
KR101499329B1 (ko) * 2013-06-17 2015-03-06 주식회사 대웅제약 (2-(3,4-다이메톡시페닐)-5-(3-메톡시프로필)벤조퓨란)의결정형 및 이의 제조방법
CN109369643B (zh) 2013-06-27 2021-05-18 爱尔兰詹森科学公司 用于治疗病毒感染和其他疾病的吡咯并[3,2-d]嘧啶衍生物
EP3027624B1 (en) 2013-07-30 2018-09-12 Janssen Sciences Ireland UC Thieno[3,2-d]pyrimidines derivatives for the treatment of viral infections
RU2016131875A (ru) * 2014-01-20 2018-02-26 Ф. Хоффманн-Ля Рош Аг Производные n-фениллактама, способные стимулировать нейрогенез, и их применение при лечении заболеваний нервной системы
WO2015153709A1 (en) * 2014-04-02 2015-10-08 Bristol-Myers Squibb Company Difluoromethoxy compound with low bioactivation potential for the reduction of beta-amyloid production
CN105272975B (zh) * 2014-06-10 2019-03-26 中国科学院上海药物研究所 一类具有1,2,4-恶二唑片段结构的吲哚生物碱及其制备方法和用途
TWI713455B (zh) 2014-06-25 2020-12-21 美商伊凡克特治療公司 MnK抑制劑及其相關方法
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
RU2732576C2 (ru) * 2015-07-21 2020-09-21 Гуанчжоу Максиновел Фармасьютикалс Ко., Лтд. Пиримидиновое соединение с конденсированными кольцами, его промежуточное соединение, способ получения, композиция и применение
SG11201803242TA (en) 2015-10-29 2018-05-30 Effector Therapeutics Inc Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2
KR20180070696A (ko) 2015-10-29 2018-06-26 이펙터 테라퓨틱스, 인크. Mnk1 및 mnk2를 억제하는 피롤로-, 피라졸로-, 이미다조-피리미딘 및 피리딘 화합물
WO2017087808A1 (en) 2015-11-20 2017-05-26 Effector Therapeutics, Inc. Heterocyclic compounds that inhibit the kinase activity of mnk useful for treating various cancers
WO2018002319A1 (en) 2016-07-01 2018-01-04 Janssen Sciences Ireland Uc Dihydropyranopyrimidines for the treatment of viral infections
WO2018060317A1 (en) 2016-09-29 2018-04-05 Janssen Sciences Ireland Uc Pyrimidine prodrugs for the treatment of viral infections and further diseases
WO2018152117A1 (en) 2017-02-14 2018-08-23 Effector Therapeutics, Inc. Piperidine-substituted mnk inhibitors and methods related thereto
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019101984A1 (en) 2017-11-27 2019-05-31 F. Hoffmann-La Roche Ag Pyrimidine derivatives
US10751345B2 (en) 2018-02-21 2020-08-25 AI Therapeutics, Inc. Combination therapy with apilimod and glutamatergic agents
TW202415645A (zh) 2018-03-01 2024-04-16 愛爾蘭商健生科學愛爾蘭無限公司 2,4-二胺基喹唑啉衍生物及其醫學用途
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
US11130757B2 (en) 2018-10-24 2021-09-28 Effector Therapeutics Inc. Crystalline forms of MNK inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008136756A1 (en) * 2007-05-08 2008-11-13 Astrazeneca Ab Pyrrolopyrimidin-7-one derivatives and their use as pharmaceuticals
WO2009087127A1 (en) * 2008-01-11 2009-07-16 F. Hoffmann-La Roche Ag Modulators for amyloid beta

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1318997T3 (da) * 2000-09-15 2006-09-25 Vertex Pharma Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
PE20090957A1 (es) * 2007-08-06 2009-07-13 Schering Corp Moduladores de gamma secretasa
MX2010003397A (es) * 2007-09-28 2010-04-09 Schering Corp Moduladores de la gamma secretasa.
MX2010006243A (es) * 2007-12-06 2010-08-31 Schering Corp Moduladores de gamma secretasa.
US20100298359A1 (en) * 2007-12-06 2010-11-25 Xianhai Huang Gamma secretase modulators
CA2708300A1 (en) * 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
CA2708151A1 (en) * 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
KR101247840B1 (ko) * 2008-02-22 2013-03-26 에프. 호프만-라 로슈 아게 아밀로이드 베타 조절제
JP5502089B2 (ja) 2008-10-09 2014-05-28 エフ.ホフマン−ラ ロシュ アーゲー アミロイドβのモジュレーター
MX2011004680A (es) * 2008-11-06 2011-05-25 Astrazeneca Ab Moduladores de beta amiloide.
US8822462B2 (en) 2009-01-28 2014-09-02 Emory University Subunit selective NMDA receptor potentiators for the treatment of neurological conditions
UY32622A (es) 2009-05-12 2010-12-31 Astrazeneca Ab Nuevos compuestos para el tratamiento de patologías relacionadas con ab(beta)
EA021047B1 (ru) 2009-07-15 2015-03-31 Янссен Фармасьютикалз, Инк. Замещенные производные триазола и имидазола в качестве модуляторов гамма-секретазы

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008136756A1 (en) * 2007-05-08 2008-11-13 Astrazeneca Ab Pyrrolopyrimidin-7-one derivatives and their use as pharmaceuticals
WO2009087127A1 (en) * 2008-01-11 2009-07-16 F. Hoffmann-La Roche Ag Modulators for amyloid beta

Also Published As

Publication number Publication date
JP5680082B2 (ja) 2015-03-04
MY156274A (en) 2016-01-29
US20110212937A1 (en) 2011-09-01
ES2554327T3 (es) 2015-12-18
WO2011014535A1 (en) 2011-02-03
SI2459197T1 (sl) 2015-12-31
TWI468402B (zh) 2015-01-11
EP2459197B1 (en) 2015-10-14
AU2010279019A1 (en) 2012-02-09
NZ597701A (en) 2012-12-21
SG177526A1 (en) 2012-02-28
PT2459197E (pt) 2015-12-18
HUE026705T2 (en) 2016-07-28
IL217173A (en) 2016-05-31
EA201270225A1 (ru) 2012-07-30
BR112012002270A2 (pt) 2016-06-14
PL2459197T3 (pl) 2016-04-29
CO6430430A2 (es) 2012-04-30
PE20120897A1 (es) 2012-07-23
ZA201200409B (en) 2013-06-26
SMT201600011B (it) 2016-02-25
US20130178462A1 (en) 2013-07-11
HK1164732A1 (zh) 2012-09-28
HRP20151133T1 (hr) 2015-11-20
CA2766515A1 (en) 2011-02-03
JP2013500975A (ja) 2013-01-10
US20150336975A1 (en) 2015-11-26
MX2012000973A (es) 2012-03-06
US8486952B2 (en) 2013-07-16
AR077434A1 (es) 2011-08-24
KR20140015126A (ko) 2014-02-06
IL217173A0 (en) 2012-02-29
EA020322B1 (ru) 2014-10-30
EP2459197A1 (en) 2012-06-06
CN102548557A (zh) 2012-07-04
US20150152089A1 (en) 2015-06-04
DK2459197T3 (en) 2016-01-25
AU2010279019B2 (en) 2014-12-18
TW201107311A (en) 2011-03-01

Similar Documents

Publication Publication Date Title
CN102548557B (zh) 用于降低β-淀粉状蛋白生成的化合物
CN104470925B (zh) 作为激酶抑制剂的咪唑并三嗪甲腈
JP6437559B2 (ja) Wee−1キナーゼ阻害剤として有用なピリミドピリミジノン
TWI719949B (zh) 稠合五環咪唑衍生物
CN104812762B (zh) 取代的环状嘧啶和三嗪以及它们的用途
TWI480282B (zh) 稠合雜環衍生物及其用途
CN105939997B (zh) 作为dlk抑制剂的吡唑衍生物及其用途
US8637525B2 (en) Compounds for the reduction of beta-amyloid production
JP2022548822A (ja) がんの治療における使用のためのヘテロ環式化合物
TWI726888B (zh) 核受體調節劑
TWI596095B (zh) Dihydropyridazine-3,5-dione derivatives
CN110088096A (zh) 作为泛素特异性蛋白酶7的抑制剂的哌啶衍生物
CN103328451B (zh) 降低β-淀粉样物质生成的化合物
TW201722933A (zh) 苯內醯胺化合物
TW201602100A (zh) 選擇性經取代之喹啉化合物
JP2017518276A (ja) ブルトン型チロシンキナーゼ(btk)インヒビターとしての多フルオロ置換化合物
CN105189515A (zh) 作为溴结构域抑制剂的呋喃并吡啶类
CN110003178A (zh) 二杂芳基化合物及其用途
TW201706258A (zh) 作為tnf信號傳遞調節劑之吲唑酮
KR20240026911A (ko) 골수성 세포 2 작용제 상에서 발현되는 유발 수용체로서의 헤테로고리 화합물 및 사용 방법
CN116096719A (zh) 作为alk5抑制剂的哒嗪基氨基衍生物
CN101981031A (zh) 具有促肾上腺皮质激素释放因子拮抗活性的三环化合物和含有它们的药物组合物
CN102171220A (zh) 用作CRF1拮抗剂的吡唑并[5,1-b]唑衍生物
CN107072993B (zh) 含有钠依赖性磷酸转运蛋白抑制剂的药物
CN112135818A (zh) 4-羟基哌啶衍生物及其作为泛素特异性蛋白酶19(usp19)的抑制剂的用途

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

Granted publication date: 20141224

Termination date: 20190728

CF01 Termination of patent right due to non-payment of annual fee