KR101730933B1 - 5-알키닐-피리미딘 - Google Patents

5-알키닐-피리미딘 Download PDF

Info

Publication number
KR101730933B1
KR101730933B1 KR1020127022277A KR20127022277A KR101730933B1 KR 101730933 B1 KR101730933 B1 KR 101730933B1 KR 1020127022277 A KR1020127022277 A KR 1020127022277A KR 20127022277 A KR20127022277 A KR 20127022277A KR 101730933 B1 KR101730933 B1 KR 101730933B1
Authority
KR
South Korea
Prior art keywords
mmol
compound
group
ethyl
membered
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
KR1020127022277A
Other languages
English (en)
Korean (ko)
Other versions
KR20120118514A (ko
Inventor
지그프리트 슈나이더
더크 케슬러
데어 빈 라스 반
토비아스 분베르그
Original Assignee
베링거 인겔하임 인터내셔날 게엠베하
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 베링거 인겔하임 인터내셔날 게엠베하 filed Critical 베링거 인겔하임 인터내셔날 게엠베하
Publication of KR20120118514A publication Critical patent/KR20120118514A/ko
Application granted granted Critical
Publication of KR101730933B1 publication Critical patent/KR101730933B1/ko
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • 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
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/5355Non-condensed oxazines and containing further 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
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • 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
    • C07D471/10Spiro-condensed systems
    • 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
    • C07D487/08Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Laminated Bodies (AREA)
  • Steroid Compounds (AREA)
KR1020127022277A 2010-01-26 2011-01-26 5-알키닐-피리미딘 Expired - Fee Related KR101730933B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10151723 2010-01-26
EP10151723.3 2010-01-26
PCT/EP2011/051061 WO2011092198A1 (en) 2010-01-26 2011-01-26 5-alkynyl-pyrimidines

Publications (2)

Publication Number Publication Date
KR20120118514A KR20120118514A (ko) 2012-10-26
KR101730933B1 true KR101730933B1 (ko) 2017-05-11

Family

ID=42224366

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127022277A Expired - Fee Related KR101730933B1 (ko) 2010-01-26 2011-01-26 5-알키닐-피리미딘

Country Status (39)

Country Link
US (3) US8633183B2 (https=)
EP (1) EP2528903B1 (https=)
JP (1) JP5746219B2 (https=)
KR (1) KR101730933B1 (https=)
CN (1) CN102781923B (https=)
AP (1) AP3107A (https=)
AR (1) AR080020A1 (https=)
AU (1) AU2011209344B2 (https=)
BR (1) BR112012019437A2 (https=)
CA (1) CA2787407C (https=)
CL (1) CL2012001821A1 (https=)
CO (1) CO6640285A2 (https=)
CY (1) CY1118129T1 (https=)
DK (1) DK2528903T3 (https=)
EA (1) EA027501B1 (https=)
ES (1) ES2598230T3 (https=)
GE (1) GEP20156229B (https=)
HR (1) HRP20161308T1 (https=)
HU (1) HUE030721T2 (https=)
IL (1) IL220674A (https=)
IN (1) IN2012DN06602A (https=)
LT (1) LT2528903T (https=)
MA (1) MA33939B1 (https=)
ME (1) ME02511B (https=)
MX (1) MX2012008128A (https=)
MY (1) MY160241A (https=)
NZ (1) NZ601121A (https=)
PE (1) PE20121695A1 (https=)
PH (1) PH12012501520A1 (https=)
PL (1) PL2528903T3 (https=)
PT (1) PT2528903T (https=)
RS (1) RS55265B1 (https=)
SG (1) SG182675A1 (https=)
SI (1) SI2528903T1 (https=)
TN (1) TN2012000369A1 (https=)
TW (1) TWI596093B (https=)
UA (1) UA110471C2 (https=)
UY (1) UY33199A (https=)
WO (1) WO2011092198A1 (https=)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20110196A1 (es) 2008-07-29 2011-04-03 Boehringer Ingelheim Int 5-alquinil-pirimidinas
CN104945420A (zh) 2009-06-29 2015-09-30 因塞特公司 作为pi3k抑制剂的嘧啶酮类
US8680108B2 (en) 2009-12-18 2014-03-25 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
US8618111B2 (en) * 2010-01-26 2013-12-31 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
US8633183B2 (en) 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
AR081823A1 (es) 2010-04-14 2012-10-24 Incyte Corp DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd
US8598164B2 (en) 2010-05-06 2013-12-03 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
EP2655374B1 (en) 2010-12-20 2019-10-23 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
US8466162B2 (en) * 2011-01-26 2013-06-18 Boehringer Ingelheim International Gmbh 5-alkynyl-pyridines
MX355907B (es) 2011-02-02 2018-05-04 Vertex Pharma Pirrolopirazina-piperidina espirociclica-amidas como moduladores de canales de ionicos.
JP5940562B2 (ja) 2011-02-18 2016-06-29 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated イオンチャネルのモジュレーターとしてのクロマン−スピロ環式ピペリジンアミド
MX347982B (es) * 2011-03-14 2017-05-22 Vertex Pharma Morfolina-piperidina espirociclica-amidas como moduladores de canales ionicos.
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2012135009A1 (en) * 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
KR102507287B1 (ko) 2011-09-02 2023-03-07 인사이트 홀딩스 코포레이션 Pi3k 억제제로서 헤테로시클릴아민
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
AR092211A1 (es) * 2012-09-24 2015-04-08 Merck Patent Ges Mit Beschränkter Haftung Derivados de hidropirrolopirrol
AU2014368945C1 (en) 2013-12-20 2019-05-16 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis and combinations thereof
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
WO2016028971A1 (en) 2014-08-21 2016-02-25 Bristol-Myers Squibb Company Tied-back benzamide derivatives as potent rock inhibitors
SI3831833T1 (sl) 2015-02-27 2023-03-31 Incyte Holdings Corporation Postopki za pripravo inhibitorja PI3K
CN104744376A (zh) * 2015-03-14 2015-07-01 长沙深橙生物科技有限公司 一种2-异丙基嘧啶衍生物的制备方法
CN104803922A (zh) * 2015-03-14 2015-07-29 长沙深橙生物科技有限公司 一种嘧啶衍生物的制备方法
CN104803921A (zh) * 2015-03-14 2015-07-29 长沙深橙生物科技有限公司 一种苯取代嘧啶衍生物的制备方法
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
CA3101323A1 (en) 2018-06-01 2019-12-05 Incyte Corporation Dosing regimen for the treatment of pi3k related disorders
CN117177744A (zh) 2021-01-29 2023-12-05 塞迪拉治疗股份有限公司 Cdk2抑制剂及其使用方法
MX2023015436A (es) 2021-06-26 2024-02-21 Cedilla Therapeutics Inc Inhibidores de cdk2 y metodos de uso de los mismos.

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006044823A2 (en) 2004-10-18 2006-04-27 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
WO2006082371A1 (en) 2005-02-01 2006-08-10 Astrazeneca Ab Pyrimidine compounds having tie2 (tek) inhibitory activity
WO2006103449A2 (en) 2005-03-31 2006-10-05 Astrazeneca Ab Saminopyrimidine derivates with tie2 inhibiting activity
WO2008155140A1 (en) 2007-06-20 2008-12-24 Bayer Schering Pharma Aktiengesellschaft Alkynylpyrimidines as tie2 kinase inhibitors

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3832570A1 (de) 1988-09-24 1990-03-29 Hoechst Ag 7-substituierte derivate der 3,5-dihydroxyhept-6-insaeure, verfahren zur ihrer herstellung, ihre verwendung als arzneimittel, sowie zwischenprodukte
WO1994014780A1 (en) 1992-12-18 1994-07-07 The Wellcome Foundation Limited Pyrimidine, pyridine, pteridinone and indazole derivatives as enzyme inhibitors
US5622954A (en) 1994-05-11 1997-04-22 Fmc Corporation 5[W(substituted aryl)alkenylene and alkynylene]-2,4-diaminopyrimidines as pesticides
JP4064671B2 (ja) 2000-02-25 2008-03-19 エフ.ホフマン−ラ ロシュ アーゲー アデノシン受容体モジュレーター
DK1303495T3 (da) 2000-07-24 2010-09-20 Krenitsky Pharmaceuticals Inc Substituerede 5-alkylnylpyrimidiner med neurotrofisk aktivitet
CN101260104A (zh) * 2002-08-16 2008-09-10 阿斯利康(瑞典)有限公司 抑制磷酸肌醇3-激酶β
US20060205740A1 (en) 2003-08-14 2006-09-14 Reno Michael J Chemical compounds
EP1737462B1 (en) 2003-12-24 2008-07-30 AstraZeneca AB Pyrimidines with tie2 (tek) activity
JP2006044823A (ja) * 2004-07-30 2006-02-16 Hitachi Building Systems Co Ltd 乗客コンベアのハンドレール案内装置
AU2005293556A1 (en) * 2004-10-12 2006-04-20 Merck Serono Sa PI3 Kinase gamma inhibitors for the treatment of anaemia
US20100048543A1 (en) 2005-02-01 2010-02-25 Astrazeneca Ab Pyrimidine compounds having ties (tek) inhibitory activity
US20070135437A1 (en) 2005-03-04 2007-06-14 Alsgen, Inc. Modulation of neurodegenerative diseases
WO2006106721A1 (ja) 2005-03-30 2006-10-12 Shionogi & Co., Ltd. チロシンキナーゼ阻害作用を有するピリミジン誘導体
GB0506467D0 (en) * 2005-03-31 2005-05-04 Astrazeneca Ab Compounds
CN101511840A (zh) * 2006-04-26 2009-08-19 吉宁特有限公司 磷酸肌醇3-激酶抑制剂化合物及其使用方法
JP2010501537A (ja) 2006-08-24 2010-01-21 アストラゼネカ アクチボラグ 増殖性障害の治療に有用なモルホリノピリミジン誘導体
EP2114902B1 (en) 2006-12-29 2014-09-17 Janssen R&D Ireland Hiv inhibiting 5,6-substituted pyrimidines
PE20110196A1 (es) * 2008-07-29 2011-04-03 Boehringer Ingelheim Int 5-alquinil-pirimidinas
US8633183B2 (en) 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
US8618111B2 (en) * 2010-01-26 2013-12-31 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006044823A2 (en) 2004-10-18 2006-04-27 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
WO2006082371A1 (en) 2005-02-01 2006-08-10 Astrazeneca Ab Pyrimidine compounds having tie2 (tek) inhibitory activity
WO2006103449A2 (en) 2005-03-31 2006-10-05 Astrazeneca Ab Saminopyrimidine derivates with tie2 inhibiting activity
WO2008155140A1 (en) 2007-06-20 2008-12-24 Bayer Schering Pharma Aktiengesellschaft Alkynylpyrimidines as tie2 kinase inhibitors

Also Published As

Publication number Publication date
CO6640285A2 (es) 2013-03-22
PT2528903T (pt) 2016-10-25
CA2787407A1 (en) 2011-08-04
JP2013518079A (ja) 2013-05-20
PL2528903T3 (pl) 2017-01-31
US20160199383A1 (en) 2016-07-14
UY33199A (es) 2011-08-31
AU2011209344B2 (en) 2015-04-16
UA110471C2 (ru) 2016-01-12
AR080020A1 (es) 2012-03-07
US20140073621A1 (en) 2014-03-13
HUE030721T2 (en) 2017-05-29
JP5746219B2 (ja) 2015-07-08
US8633183B2 (en) 2014-01-21
GEP20156229B (en) 2015-01-26
TWI596093B (zh) 2017-08-21
LT2528903T (lt) 2016-10-25
PH12012501520A1 (en) 2022-10-05
TN2012000369A1 (en) 2014-01-30
PE20121695A1 (es) 2012-12-11
ES2598230T3 (es) 2017-01-26
WO2011092198A1 (en) 2011-08-04
CY1118129T1 (el) 2017-06-28
CA2787407C (en) 2015-11-24
AU2011209344A1 (en) 2012-08-02
MA33939B1 (fr) 2013-01-02
NZ601121A (en) 2014-07-25
EA201201030A1 (ru) 2013-02-28
US9321771B2 (en) 2016-04-26
HRP20161308T1 (hr) 2016-12-02
IN2012DN06602A (https=) 2015-10-23
AP2012006360A0 (en) 2012-08-31
ME02511B (me) 2017-02-20
EP2528903B1 (en) 2016-07-20
SI2528903T1 (sl) 2016-11-30
EP2528903A1 (en) 2012-12-05
MY160241A (en) 2017-02-28
MX2012008128A (es) 2012-08-15
US20120028952A1 (en) 2012-02-02
BR112012019437A2 (pt) 2018-03-20
HK1175175A1 (zh) 2013-06-28
IL220674A (en) 2017-08-31
CN102781923B (zh) 2016-03-02
DK2528903T3 (en) 2016-11-14
TW201139408A (en) 2011-11-16
KR20120118514A (ko) 2012-10-26
CL2012001821A1 (es) 2012-11-30
AP3107A (en) 2015-01-31
CN102781923A (zh) 2012-11-14
RS55265B1 (sr) 2017-02-28
SG182675A1 (en) 2012-08-30
EA027501B1 (ru) 2017-08-31

Similar Documents

Publication Publication Date Title
KR101730933B1 (ko) 5-알키닐-피리미딘
JP5551066B2 (ja) 新規化合物
JP5651110B2 (ja) 新規化合物
KR20110041536A (ko) 5-알키닐-피리미딘
TW201439064A (zh) 新型嘧啶和吡啶類化合物及其用途
JP2010529161A (ja) インドリノン誘導体及び癌等の症状を治療する際のそれらの使用
WO2006131552A1 (de) Alpha-carboline als cdk-1 inhibitoren
US9090564B2 (en) 5-alkynyl-pyridines
JP5670479B2 (ja) 5−アルキニルピリミジン及びそれらのキナーゼ阻害剤としての使用
CN106536488A (zh) 喹喔啉化合物、其制造方法及用途
HK1165197A (en) 5-alkynyl-pyridines
HK1175174A (en) 5-alkynyl pyrimidines and their use as kinase 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

A201 Request for examination
PA0201 Request for examination

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

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

P22-X000 Classification modified

St.27 status event code: A-2-2-P10-P22-nap-X000

P22-X000 Classification modified

St.27 status event code: A-2-2-P10-P22-nap-X000

D13-X000 Search requested

St.27 status event code: A-1-2-D10-D13-srh-X000

D14-X000 Search report completed

St.27 status event code: A-1-2-D10-D14-srh-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

PR1001 Payment of annual fee

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

Fee payment year number: 4

PR1001 Payment of annual fee

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

Fee payment year number: 5

PC1903 Unpaid annual fee

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

Not in force date: 20220422

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: 20220422