AP2064A - Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors - Google Patents

Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors

Info

Publication number
AP2064A
AP2064A AP2005003452A AP2005003452A AP2064A AP 2064 A AP2064 A AP 2064A AP 2005003452 A AP2005003452 A AP 2005003452A AP 2005003452 A AP2005003452 A AP 2005003452A AP 2064 A AP2064 A AP 2064A
Authority
AP
ARIPO
Prior art keywords
pyrazolo
preparation
kinase inhibitors
quinazoline derivatives
quinazoline
Prior art date
Application number
AP2005003452A
Other languages
English (en)
Other versions
AP2005003452A0 (en
Inventor
Gabriella Traquandi
Maria Gabriella Brasca
Roberto D'alessio
Original Assignee
Nerviano Medical Sciences Srl
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33476970&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AP2064(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Nerviano Medical Sciences Srl filed Critical Nerviano Medical Sciences Srl
Publication of AP2005003452A0 publication Critical patent/AP2005003452A0/xx
Application granted granted Critical
Publication of AP2064A publication Critical patent/AP2064A/xx

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
    • C07D487/12Heterocyclic 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
    • C07D487/14Ortho-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
    • 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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • 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
    • C07D401/10Heterocyclic 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 aromatic 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
    • 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
    • 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
    • C07D487/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (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)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AP2005003452A 2003-05-22 2004-04-27 Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors AP2064A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US47266103P 2003-05-22 2003-05-22
PCT/EP2004/050612 WO2004104007A1 (en) 2003-05-22 2004-04-27 Pyrazolo-quinazoline derivatives,process for their preparation and their use as kinase inhibitors

Publications (2)

Publication Number Publication Date
AP2005003452A0 AP2005003452A0 (en) 2005-12-31
AP2064A true AP2064A (en) 2009-10-30

Family

ID=33476970

Family Applications (1)

Application Number Title Priority Date Filing Date
AP2005003452A AP2064A (en) 2003-05-22 2004-04-27 Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors

Country Status (36)

Country Link
US (9) US7482354B2 (is)
EP (1) EP1636236B1 (is)
JP (1) JP5043432B2 (is)
KR (1) KR101084871B1 (is)
CN (2) CN102079746A (is)
AP (1) AP2064A (is)
AR (2) AR044543A1 (is)
AU (1) AU2004240772B2 (is)
BR (2) BR122019010200B8 (is)
CA (1) CA2526578C (is)
CO (1) CO5721006A2 (is)
CR (1) CR8102A (is)
CY (1) CY1114708T1 (is)
DK (1) DK1636236T3 (is)
EA (1) EA010904B1 (is)
EC (1) ECSP056194A (is)
ES (1) ES2436524T3 (is)
GE (1) GEP20094664B (is)
HR (1) HRP20050967B8 (is)
IL (1) IL172046A (is)
IS (1) IS2939B (is)
ME (1) ME00142B (is)
MX (1) MXPA05012573A (is)
MY (1) MY142019A (is)
NO (1) NO334992B1 (is)
NZ (1) NZ543661A (is)
OA (1) OA13170A (is)
PL (1) PL1636236T3 (is)
PT (1) PT1636236E (is)
RS (2) RS20050944A (is)
SI (1) SI1636236T1 (is)
TN (1) TNSN05298A1 (is)
TW (1) TWI349672B (is)
UA (1) UA80763C2 (is)
WO (1) WO2004104007A1 (is)
ZA (1) ZA200509486B (is)

Families Citing this family (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7482354B2 (en) 2003-05-22 2009-01-27 Nerviano Medical Sciences S.R.L. Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
CN1897950A (zh) 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
US7572914B2 (en) 2003-12-19 2009-08-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
US7772232B2 (en) 2004-04-15 2010-08-10 Bristol-Myers Squibb Company Quinazolinyl compounds as inhibitors of potassium channel function
ITMI20041033A1 (it) 2004-05-24 2004-08-24 Neuroscienze S C A R L Composti farmaceutici
WO2006023931A2 (en) 2004-08-18 2006-03-02 Takeda San Diego, Inc. Kinase inhibitors
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
AU2007213791A1 (en) * 2006-02-10 2007-08-16 Nerviano Medical Sciences S.R.L. Combinations comprising a CDK inhibitor and a growth factor antibody or anti-mitotic
KR20090007635A (ko) * 2006-05-09 2009-01-19 노파르티스 아게 철 킬레이터 및 항-신생물 약제를 포함하는 조합물 및 그의용도
US20080015193A1 (en) * 2006-06-20 2008-01-17 Mendoza Jose S Certain azoles exhibiting ATP-utilizing enzyme inhibitory activity, compositions, and uses thereof
US7517882B2 (en) * 2006-09-18 2009-04-14 Polaris Group Protein kinase inhibitors
GEP20135728B (en) 2006-10-09 2013-01-25 Takeda Pharmaceuticals Co Kinase inhibitors
KR101512284B1 (ko) * 2006-12-21 2015-04-15 네르비아노 메디칼 사이언시스 에스.알.엘. 치환된 피라졸로-퀴나졸린 유도체, 이의 제조방법, 및 키나제 억제제로서의 이의 용도
ZA200904912B (en) * 2006-12-21 2010-09-29 Nerviano Medical Sciences Srl Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
JPWO2009054332A1 (ja) 2007-10-23 2011-03-03 萬有製薬株式会社 ピリドン置換ジヒドロピラゾロピリミジノン誘導体
WO2009085185A1 (en) * 2007-12-19 2009-07-09 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
MX2010010975A (es) * 2008-04-07 2010-11-01 Amgen Inc Amino piridinas/pirimidinas gem-disustituidas y espirociclicas como inhibidores de ciclo celular.
TWI426074B (zh) * 2008-04-30 2014-02-11 Nerviano Medical Sciences Srl 5-(2-胺基-嘧啶-4-基)-2-芳基-1h-吡咯-3-羧醯胺之製造方法
EP2303891B1 (en) * 2008-06-26 2016-02-17 Les Laboratoires Servier Pyrazolo-quinazolines as protein kinase activity modulators
ES2532732T3 (es) 2008-07-29 2015-03-31 Nerviano Medical Sciences S.R.L. Uso de un inhibidor de CDK para el tratamiento del glioma
EP2320903B1 (en) * 2008-07-29 2017-01-18 Nerviano Medical Sciences S.r.l. THERAPEUTIC COMBINATION COMPRISING A CDKs INHIBITOR AND AN ANTINEOPLASTIC AGENT
JP5579724B2 (ja) * 2008-10-17 2014-08-27 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 ホスファチジルイノシトール−3−キナーゼ(pi−3キナーゼ)阻害剤としてのテトラ−アザ−複素環
CN102223885B (zh) 2008-11-24 2013-04-03 内尔维阿诺医学科学有限公司 用于治疗间皮瘤的cdk抑制剂
IT1395724B1 (it) * 2009-02-25 2012-10-19 Neuroscienze Pharmaness S C A R L Composti farmaceutici
EP2408776B1 (en) * 2009-03-20 2014-01-08 Nerviano Medical Sciences S.r.l. Use of a kinase inhibitor for the treatment of thymoma
EP2421872B1 (en) * 2009-04-22 2015-06-10 Boehringer Ingelheim International GmbH Thia-triaza-as-indacenes as pi3-kinases inhibitors for the treatment of cancer
US8586598B2 (en) 2009-04-29 2013-11-19 Nerviano Medical Sciences S.R.L. CDK inhibitor salts
AR076784A1 (es) 2009-05-26 2011-07-06 Nerviano Medical Sciences Srl Combinacion terapeutica que comprende un inhibidor de plk1 y un agente antineoplasico
WO2011012534A1 (en) * 2009-07-29 2011-02-03 Nerviano Medical Sciences S.R.L. Plk inhibitor salts
US20130045992A1 (en) * 2010-01-28 2013-02-21 President And Fellows Of Harvard College Compositions and Methods for Enhancing Proteasome Activity
US8735386B2 (en) * 2010-07-23 2014-05-27 Boehringer Ingelheim International Gmbh Aminopyrazoloquinazolines
JP5997143B2 (ja) * 2010-07-30 2016-09-28 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ タンパク質キナーゼ活性の調整剤としてのイソオキサゾロ−キナゾリン
BR112013006671A2 (pt) 2010-09-23 2016-06-07 Syngenta Participations Ag microbiocidas21
MX379532B (es) * 2010-10-25 2025-03-10 G1 Therapeutics Inc Inhibidores de cdk.
RU2652638C2 (ru) * 2010-12-17 2018-04-28 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Замещенные пиразолхиназолиновые производные в качестве ингибиторов киназы
CN103339134B (zh) * 2011-01-26 2015-12-23 内尔维阿诺医学科学有限公司 三环吡咯并衍生物、它们的制备方法和它们作为激酶抑制剂的应用
EP2668188B1 (en) * 2011-01-26 2016-05-18 Nerviano Medical Sciences S.r.l. Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
WO2012117021A2 (en) 2011-03-03 2012-09-07 Syngenta Participations Ag Novel microbiocidal oxime ethers
PT2688887E (pt) 2011-03-23 2015-07-06 Amgen Inc Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3
WO2012154967A1 (en) 2011-05-12 2012-11-15 Proteostasis Therapeutics, Inc. Proteostasis regulators
WO2013092460A1 (en) 2011-12-20 2013-06-27 Syngenta Participations Ag Cyclic bisoxime microbicides
EP2807166B1 (en) * 2012-01-23 2016-04-06 Boehringer Ingelheim International GmbH 5,8-dihydro-6h-pyrazolo[3,4-h]quinazolines as igf-1r/ir inhibitors
EP2641901A1 (en) 2012-03-22 2013-09-25 Syngenta Participations AG. Novel microbiocides
US9604980B2 (en) 2012-11-07 2017-03-28 Nerviano Medical Sciences S.R.L. Substituted pyrimidinyl and pyridinyl-pyrrolopyridinones, process for their preparation and their use as kinase inhibitors
US9849135B2 (en) 2013-01-25 2017-12-26 President And Fellows Of Harvard College USP14 inhibitors for treating or preventing viral infections
US9527857B2 (en) 2013-03-15 2016-12-27 GI Therapeutics, Inc. HSPC-sparing treatments for RB-positive abnormal cellular proliferation
US20140271460A1 (en) 2013-03-15 2014-09-18 G1 Therapeutics, Inc. Highly Active Anti-Neoplastic and Anti-Proliferative Agents
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
CN106132963B (zh) 2014-04-07 2019-08-06 荷兰转化研究中心有限责任公司 (5,6-二氢)嘧啶并[4,5-e]吲嗪
WO2015161283A1 (en) 2014-04-17 2015-10-22 G1 Therapeutics, Inc. Tricyclic lactams for use in hspc-sparing treatments for rb-positive abnormal cellular proliferation
ES2873959T3 (es) 2014-05-28 2021-11-04 Piramal Entpr Ltd Combinación farmacéutica que comprende un inhibidor de CDK y un inhibidor de tiorredoxina reductasa para el tratamiento del cáncer
WO2016040858A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
WO2016040848A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors
EP3324952B1 (en) 2015-07-17 2020-12-16 Institut Pasteur 5-hydroxytryptamine 1b receptor-stimulating agent for use as a promoter of satellite cells self-renewal and/or differentiation
WO2018011382A1 (en) 2016-07-15 2018-01-18 Institut Pasteur 5-hydroxytryptamine 1b receptor-stimulating agent for skin and/or hair repair
US11168088B2 (en) 2016-11-11 2021-11-09 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Pyridylamino substituted heterotricyclic compounds, and preparation method and pharmaceutical use thereof
WO2019011715A1 (en) 2017-07-11 2019-01-17 Nerviano Medical Sciences S.R.L. PYRAZOLO-QUINAZOLINE DERIVATIVES AS INHIBITORS OF CHOLINE KINASE
CN107383019B (zh) * 2017-07-28 2019-10-15 江苏艾凡生物医药有限公司 吡唑并[4,3-h]喹唑啉类化合物及其用途
KR102464677B1 (ko) * 2017-08-11 2022-11-10 셍커 파마슈티컬스 (지앙수) 엘티디. 단백질 인산화효소 억제제로 작용하는 1h-피라졸로[4,3-h]퀴나졸린 화합물
PT3980013T (pt) * 2019-06-06 2024-10-23 Arcus Biosciences Inc Processos de preparação de compostos de aminopirimidina
WO2021043190A1 (zh) * 2019-09-05 2021-03-11 成都赛诺希亚生物科技有限公司 异噁唑并[5,4-h]喹唑啉类化合物作为蛋白激酶抑制剂
WO2021084541A1 (en) * 2019-10-31 2021-05-06 Sol-Gel Technologies Ltd. Treatment of hair loss disorders with a topical egfr inhibitor
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
CN116547280A (zh) * 2020-10-08 2023-08-04 雷多纳治疗公司 用于治疗癌症的苯并[h]喹唑啉-4-胺和噻吩并[3,2-h]喹唑啉-4-胺衍生物
US20230416271A1 (en) * 2020-11-26 2023-12-28 Chengdu Cynogen Bio-Pharmaceutical Technology Co., Ltd. Heteroarylquinazoline compounds as protein kinase inhibitors
CN114685520B (zh) * 2020-12-25 2024-08-30 武汉誉祥医药科技有限公司 三并环化合物及其药物组合物和应用
CN116528871A (zh) * 2020-12-31 2023-08-01 恒元生物医药科技(苏州)有限公司 一种吡唑并喹唑啉类化合物、其制备方法及应用
EP4289852A4 (en) 2021-02-08 2025-02-26 NovaOnco JS Therapeutics Co., Ltd. 5,6-DIHYDROTHIENO[3,4-H]QUINAZOLINE COMPOUND
JP2024524213A (ja) * 2021-06-22 2024-07-05 タクシス ファーマシューティカルズ, インコーポレイテッド 治療化合物
CN113527310B (zh) * 2021-07-30 2022-09-23 上海市肺科医院 用于减轻自身免疫性疾病患者不良炎性反应的小分子化合物及其应用
CN118382626A (zh) * 2021-12-10 2024-07-23 山东绿叶制药有限公司 蛋白激酶抑制剂及其制备方法和应用
CN120530121A (zh) * 2023-01-17 2025-08-22 北京哲源科技有限责任公司 吡唑并喹唑啉类化合物的立体异构体和氘代衍生物及应用
AU2024284206A1 (en) * 2023-06-08 2025-12-11 Yantai Transheal Biotechnology Co., Ltd. Salt form and crystal form of plk1 kinase inhibitor, and preparation method therefor and use thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2119975A (en) * 1936-08-26 1938-06-07 Beatrice S Nazel Fluid pressure hammer

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3907220B2 (ja) * 1994-06-30 2007-04-18 エーザイ・アール・アンド・ディー・マネジメント株式会社 複素環含有化合物
CA2223081C (en) 1995-06-07 2001-03-06 Pfizer Inc. Heterocyclic ring-fused pyrimidine derivatives
WO1998028281A1 (en) 1996-12-23 1998-07-02 Celltech Therapeutics Limited Fused polycyclic 2-aminopyrimidine derivatives, their preparation and their use as protein tyrosine kinase inhibitors
GB9713087D0 (en) 1997-06-20 1997-08-27 Celltech Therapeutics Ltd Chemical compounds
GB9911053D0 (en) 1999-05-12 1999-07-14 Pharmacia & Upjohn Spa 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents
GEP20053476B (en) 1999-08-12 2005-03-25 Upjohn Co 3(5)-Amino-Pyrazole Derivatives, Process for Their Preparation and Their Use as Antitumor Agents
US6387900B1 (en) 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
KR100904157B1 (ko) 2000-08-10 2009-06-23 파마시아 이탈리아 에스.피.에이. 키나제 억제제로서 활성인 비사이클로-피라졸, 이의제조방법 및 이를 포함하는 약제학적 조성물
MXPA03001306A (es) 2000-08-11 2003-10-15 Boehringer Ingelheim Pharma Compuestos heterociclicos utiles como inhibidores de las quinasas de tirosina.
US20040019046A1 (en) 2000-11-27 2004-01-29 Paolo Pevarello Phenylacetamido-pyrazole derivatives and their use as antitumor agents
EP1379524A2 (en) 2001-01-26 2004-01-14 Pharmacia Italia S.p.A. Chromane derivatives, process for their preparation and their use as antitumor agents
WO2003013655A2 (en) * 2001-08-10 2003-02-20 Pharmacia Corporation Carbonic anhydrase inhibitors
US20030100594A1 (en) * 2001-08-10 2003-05-29 Pharmacia Corporation Carbonic anhydrase inhibitor
ES2357502T3 (es) 2001-09-26 2011-04-27 Pfizer Italia S.R.L. Derivados de aminoindazol activos como inhibidores de quinasa, procedimiento para su preparación y composiciones farmaceuticas que los contienen.
MXPA04008130A (es) * 2002-02-19 2004-11-26 Pharmacia Corp Derivados triciclicos de pirazol para el tratamiento de la inflamacion.
US7482354B2 (en) * 2003-05-22 2009-01-27 Nerviano Medical Sciences S.R.L. Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
KR101512284B1 (ko) * 2006-12-21 2015-04-15 네르비아노 메디칼 사이언시스 에스.알.엘. 치환된 피라졸로-퀴나졸린 유도체, 이의 제조방법, 및 키나제 억제제로서의 이의 용도

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2119975A (en) * 1936-08-26 1938-06-07 Beatrice S Nazel Fluid pressure hammer

Also Published As

Publication number Publication date
MEP25908A (bs) 2010-06-10
ME00142B (me) 2010-10-10
JP2007502851A (ja) 2007-02-15
US20070185143A1 (en) 2007-08-09
NO334992B1 (no) 2014-08-18
BRPI0410563A (pt) 2006-06-20
HRP20050967A2 (en) 2007-05-31
WO2004104007A1 (en) 2004-12-02
ES2436524T3 (es) 2014-01-02
IS8132A (is) 2005-11-18
US20210300935A1 (en) 2021-09-30
TWI349672B (en) 2011-10-01
CN1826343A (zh) 2006-08-30
US7482354B2 (en) 2009-01-27
TW200505924A (en) 2005-02-16
UA80763C2 (en) 2007-10-25
US20130338148A1 (en) 2013-12-19
RS20050944A (sr) 2008-06-05
US8981089B2 (en) 2015-03-17
US20090124605A1 (en) 2009-05-14
BRPI0410563B8 (pt) 2021-05-25
SI1636236T1 (sl) 2014-01-31
CY1114708T1 (el) 2016-10-05
EA200501849A1 (ru) 2006-06-30
ZA200509486B (en) 2008-09-25
RS52899B (sr) 2014-02-28
EA010904B1 (ru) 2008-12-30
NZ543661A (en) 2009-05-31
US20170190714A1 (en) 2017-07-06
OA13170A (en) 2006-12-13
MY142019A (en) 2010-08-16
MXPA05012573A (es) 2006-02-22
IL172046A (en) 2017-03-30
AP2005003452A0 (en) 2005-12-31
AR102722A2 (es) 2017-03-22
CA2526578C (en) 2012-01-24
EP1636236B1 (en) 2013-10-09
HRP20050967B8 (hr) 2014-04-25
AR044543A1 (es) 2005-09-21
PL1636236T3 (pl) 2014-02-28
US10280176B2 (en) 2019-05-07
BR122019010200B8 (pt) 2021-07-27
US20150158876A1 (en) 2015-06-11
US20170050972A1 (en) 2017-02-23
HRP20050967B1 (hr) 2014-03-28
CA2526578A1 (en) 2004-12-02
ECSP056194A (es) 2006-04-19
US8541429B2 (en) 2013-09-24
CR8102A (es) 2006-08-09
JP5043432B2 (ja) 2012-10-10
US9637497B2 (en) 2017-05-02
US20190194214A1 (en) 2019-06-27
NO20055496L (no) 2006-02-14
AU2004240772A1 (en) 2004-12-02
AU2004240772B2 (en) 2011-04-28
TNSN05298A1 (fr) 2007-07-10
US9464090B2 (en) 2016-10-11
IS2939B (is) 2016-03-15
US20250011333A1 (en) 2025-01-09
DK1636236T3 (da) 2013-12-09
KR20060015294A (ko) 2006-02-16
NO20055496D0 (no) 2005-11-21
CN102079746A (zh) 2011-06-01
PT1636236E (pt) 2013-12-16
BRPI0410563B1 (pt) 2020-12-01
CO5721006A2 (es) 2007-01-31
BR122019010200B1 (pt) 2020-12-15
GEP20094664B (en) 2009-04-10
EP1636236A1 (en) 2006-03-22
KR101084871B1 (ko) 2011-11-21

Similar Documents

Publication Publication Date Title
TWI349672B (en) Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
AP2048A (en) Diazepinoindole derivatives as kinase inhibitors
IL173380A0 (en) Pyridinylamino-pyrimidine derivatives as protein kinase inhibitors
IL173200A0 (en) Piperidyl-quinazoline derivatives as tyrosine kinase inhibitors
IL165515A0 (en) Bisindolyl-maleimid derivatives as kinase inhibitors
IL172132A0 (en) Thienopyridone derivatives as kinase inhibitors
PL2125822T3 (pl) Podstawione pochodne pirazolochinazoliny, sposób ich wytwarzania oraz ich zastosowanie jako inhibitory kinaz
IL173381A0 (en) 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
ZA201202026B (en) PYROLO[2,3-b] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
HUP0402245A3 (en) Pyrimidinyl-aminobenzamide derivatives as glycogen synthase kinase 3betha inhibitors, their use, pharmaceutical compositions containing them and process for producing them
AU2003271566A8 (en) Pyrrolopyrazines as kinase inhibitors
EP1689393A4 (en) PREPARATION OF 1,7-DISUBSTITUTED AZABENZIMIDAZOLES AS KINASE INHIBITORS
IL182054A0 (en) Novel bis-azaindole derivatives, preparation and pharmaceutical use thereof as kinase inhibitors
EP1670466A4 (en) PREPARATION OF 1,6,7-TRISUBSTITUTED AZABENIC ZIMIDAZOLES AS KINASE-INHIBITORS
EP1590333A4 (en) GLYCOGENE SYNTHASE KINASE 3BETA INHIBITOR, COMPOSITION AND PROCESS FOR PREPARING THE SAME
IL179424A0 (en) Substituted oxazole -benzoisothiazole dioxide derivatives, process for their preparation and their use
IL179758A0 (en) Substituted tetrahydro - 2h - isoquinolin - 1 - one derivatives, method for the production thereof, and use of the same as medicaments
IL175300A0 (en) Indirubin-type compounds, compositions, and methods for their use
IL172375A0 (en) Chinazoline derivatives as aurora kinase inhibitors
PL377741A1 (pl) Pochodne diarylocykloalkilowe, sposób ich wytwarzania i ich zastosowanie jako środka leczniczego
PL378121A1 (pl) Sposób wytwarzania pirolotriazynowych inhibitorów kinazy
HUP0401522A2 (en) New 4-benzylidene-piperidine derivatives, pharmaceutical compositions containing the same and process for their preparation
IL186062A0 (en) Indanyl-piperazine derivatives, method for preparing same and pharmaceutical compositions containing same
ZA200904912B (en) Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
IL164248A0 (en) Acyl-3-carboxyphenylurea derivatives, processes for preparing them and their use