CA2787407C - 5-alkynyl-pyrimidines - Google Patents

5-alkynyl-pyrimidines Download PDF

Info

Publication number
CA2787407C
CA2787407C CA2787407A CA2787407A CA2787407C CA 2787407 C CA2787407 C CA 2787407C CA 2787407 A CA2787407 A CA 2787407A CA 2787407 A CA2787407 A CA 2787407A CA 2787407 C CA2787407 C CA 2787407C
Authority
CA
Canada
Prior art keywords
membered
denotes
independently
group selected
mmol
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
CA2787407A
Other languages
English (en)
French (fr)
Other versions
CA2787407A1 (en
Inventor
Siegfried Schneider
Dirk Kessler
Lars Van Der Veen
Tobias Wunberg
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.)
Boehringer Ingelheim International GmbH
Original Assignee
Boehringer Ingelheim International GmbH
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 Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of CA2787407A1 publication Critical patent/CA2787407A1/en
Application granted granted Critical
Publication of CA2787407C publication Critical patent/CA2787407C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic 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
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/26—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (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)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (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)
  • Steroid Compounds (AREA)
  • Laminated Bodies (AREA)
CA2787407A 2010-01-26 2011-01-26 5-alkynyl-pyrimidines Expired - Fee Related CA2787407C (en)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
CA2787407A1 CA2787407A1 (en) 2011-08-04
CA2787407C true CA2787407C (en) 2015-11-24

Family

ID=42224366

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2787407A Expired - Fee Related CA2787407C (en) 2010-01-26 2011-01-26 5-alkynyl-pyrimidines

Country Status (39)

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

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2011000729A (es) 2008-07-29 2011-03-15 Boehringer Ingelheim Int 5-alquinil-pirimidinas.
PE20120493A1 (es) 2009-06-29 2012-05-20 Incyte Corp Pirimidinonas como inhibidores de pi3k
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
TW201130842A (en) 2009-12-18 2011-09-16 Incyte Corp Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
UY33198A (es) * 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.
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
WO2011140425A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
ES2764848T3 (es) 2010-12-20 2020-06-04 Incyte Holdings Corp N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K
US8466162B2 (en) * 2011-01-26 2013-06-18 Boehringer Ingelheim International Gmbh 5-alkynyl-pyridines
TWI520964B (zh) 2011-02-02 2016-02-11 維泰克斯製藥公司 作為離子通道調節劑之吡咯并吡－螺環哌啶醯胺
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
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
EP2686325B1 (en) * 2011-03-14 2016-12-14 Vertex Pharmaceuticals Incorporated Morpholine-spirocyclic piperidine amides as modulators of ion channels
WO2012135009A1 (en) * 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
KR20230038593A (ko) 2011-09-02 2023-03-20 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
ES2841137T3 (es) 2013-12-20 2021-07-07 Sagimet Biosciences Inc Moduladores heterocíclicos de la síntesis de lípidos y combinaciones de los mismos
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
JP6633618B2 (ja) 2014-08-21 2020-01-22 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 強力なｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体
PH12017501538B1 (en) 2015-02-27 2024-02-14 Incyte Holdings Corp Salts of p13k inhibitor and processes for their preparation
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
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
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
CN112469418A (zh) 2018-06-01 2021-03-09 因赛特公司 治疗pi3k相关病症的给药方案
US20240174680A1 (en) * 2021-01-29 2024-05-30 Cedilla Therapeutics, Inc. Cdk2 inhibitors and methods of using the same
US12053459B2 (en) 2021-06-26 2024-08-06 Cedilla Therapeutics, Inc. CDK2 inhibitors and methods of using the same

Family Cites Families (24)

* 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
JPH08504798A (ja) 1992-12-18 1996-05-21 ザ ウエルカム ファウンデーション リミテッド 酵素阻害薬としての，ピリミジン，ピリジン，プテリジノンおよびインダゾール誘導体
US5622954A (en) 1994-05-11 1997-04-22 Fmc Corporation 5[W(substituted aryl)alkenylene and alkynylene]-2,4-diaminopyrimidines as pesticides
RU2277911C2 (ru) 2000-02-25 2006-06-20 Ф.Хоффманн-Ля Рош Аг Модуляторы аденозиновых рецепторов
DK1303495T3 (da) * 2000-07-24 2010-09-20 Krenitsky Pharmaceuticals Inc Substituerede 5-alkylnylpyrimidiner med neurotrofisk aktivitet
CN100430389C (zh) * 2002-08-16 2008-11-05 阿斯利康(瑞典)有限公司 抑制磷酸肌醇3-激酶β
JP2007502298A (ja) * 2003-08-14 2007-02-08 スミスクライン ビーチャム コーポレーション 化合物
ES2309591T3 (es) 2003-12-24 2008-12-16 Astrazeneca Ab Pirimidinas con actividad tie2(tek).
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
CN101056633A (zh) * 2004-10-12 2007-10-17 应用研究系统Ars股份公司 用于贫血治疗的PI3激酶γ抑制剂
US7776869B2 (en) 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
US20080146599A1 (en) 2005-02-01 2008-06-19 Astrazeneca Ab Pyrimidine Compounds Having Tie-2 (Tek) Inhibitory Activity
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
US20080194552A1 (en) 2005-03-31 2008-08-14 Astrazeneca Ab Aminopyrimidine Derivatives With Tie2 Inhibiting Activity
GB0506467D0 (en) * 2005-03-31 2005-05-04 Astrazeneca Ab Compounds
TW200801012A (en) * 2006-04-26 2008-01-01 Piramed Ltd Phosphoinositide 3-kinase inhibitor compounds and methods of use
EP2057129A1 (en) 2006-08-24 2009-05-13 AstraZeneca AB Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
JP5283633B2 (ja) 2006-12-29 2013-09-04 テイボテク・フアーマシユーチカルズ Ｈｉｖ阻害性５，６−置換ピリミジン
EP2022785A1 (en) 2007-06-20 2009-02-11 Bayer Schering Pharma Aktiengesellschaft Alkynylpyrimidines as Tie2 kinase inhibitors
MX2011000729A (es) * 2008-07-29 2011-03-15 Boehringer Ingelheim Int 5-alquinil-pirimidinas.
US8633183B2 (en) * 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
UY33198A (es) * 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.

Also Published As

Publication number Publication date
WO2011092198A1 (en) 2011-08-04
KR101730933B1 (ko) 2017-05-11
PH12012501520A1 (en) 2022-10-05
HUE030721T2 (en) 2017-05-29
TN2012000369A1 (en) 2014-01-30
EP2528903A1 (en) 2012-12-05
CO6640285A2 (es) 2013-03-22
AR080020A1 (es) 2012-03-07
EA201201030A1 (ru) 2013-02-28
UA110471C2 (ru) 2016-01-12
RS55265B1 (sr) 2017-02-28
US9321771B2 (en) 2016-04-26
AU2011209344A1 (en) 2012-08-02
KR20120118514A (ko) 2012-10-26
IL220674A (en) 2017-08-31
NZ601121A (en) 2014-07-25
MX2012008128A (es) 2012-08-15
PT2528903T (pt) 2016-10-25
US20120028952A1 (en) 2012-02-02
PE20121695A1 (es) 2012-12-11
CY1118129T1 (el) 2017-06-28
LT2528903T (lt) 2016-10-25
TW201139408A (en) 2011-11-16
CN102781923A (zh) 2012-11-14
CL2012001821A1 (es) 2012-11-30
MY160241A (en) 2017-02-28
AU2011209344B2 (en) 2015-04-16
UY33199A (es) 2011-08-31
TWI596093B (zh) 2017-08-21
EA027501B1 (ru) 2017-08-31
IN2012DN06602A (enExample) 2015-10-23
MA33939B1 (fr) 2013-01-02
US20140073621A1 (en) 2014-03-13
ES2598230T3 (es) 2017-01-26
CN102781923B (zh) 2016-03-02
EP2528903B1 (en) 2016-07-20
JP5746219B2 (ja) 2015-07-08
DK2528903T3 (en) 2016-11-14
SG182675A1 (en) 2012-08-30
AP2012006360A0 (en) 2012-08-31
PL2528903T3 (pl) 2017-01-31
HRP20161308T1 (hr) 2016-12-02
US20160199383A1 (en) 2016-07-14
JP2013518079A (ja) 2013-05-20
GEP20156229B (en) 2015-01-26
AP3107A (en) 2015-01-31
CA2787407A1 (en) 2011-08-04
HK1175175A1 (zh) 2013-06-28
ME02511B (me) 2017-02-20
SI2528903T1 (sl) 2016-11-30
BR112012019437A2 (pt) 2018-03-20
US8633183B2 (en) 2014-01-21

Similar Documents

Publication Publication Date Title
CA2787407C (en) 5-alkynyl-pyrimidines
CA2971640A1 (en) Cot modulators and methods of use thereof
WO2018031680A1 (en) Novel compounds, uses and methods for their preparation
EP3193611A2 (en) Mk2 inhibitors and uses thereof
JP6943844B2 (ja) Ｐｉｍキナーゼ阻害剤の塩
CN101784545A (zh) 用作raf激酶抑制剂的嘧啶衍生物
WO2010012740A1 (en) 5-alkynyl-pyrimidines
CA3092770A1 (en) Substituted imidazolidin-2-one derivatives as prmt5 inhibitors
WO2022018072A1 (en) Tricyclic heterocycles
WO2024078581A1 (en) Selective bcl-xl protac compounds and uses thereof
CN102675305A (zh) 一类咪唑并吡啶类化合物及其制备方法和用途
CA3084528A1 (en) Pyrazolopyridinone compounds
JP2011513471A (ja) チアゾリル−ジヒドロ−インダゾール
WO2012061019A2 (en) Tricyclic mglur5 receptor modulators
TW202029963A (zh) 1,2,3,4-四氫喹㗁啉衍生物及其製備方法和應用
AU2011209343A1 (en) 5-alkynyl pyrimidines and their use as kinase inhibitors
EA046513B1 (ru) Замещенные производные имидазолидин-2-она в качестве ингибиторов prmt5
HK1175175B (en) 5-alkynyl-pyrimidines

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed

Effective date: 20220126