ATE540933T1 - Pyrimidinverbindungen als interleukin-12 (il-12) inhibitoren - Google Patents

Pyrimidinverbindungen als interleukin-12 (il-12) inhibitoren

Info

Publication number
ATE540933T1
ATE540933T1 AT02804468T AT02804468T ATE540933T1 AT E540933 T1 ATE540933 T1 AT E540933T1 AT 02804468 T AT02804468 T AT 02804468T AT 02804468 T AT02804468 T AT 02804468T AT E540933 T1 ATE540933 T1 AT E540933T1
Authority
AT
Austria
Prior art keywords
alkyl
aryl
heteroaryl
pyrimidine compounds
nrc
Prior art date
Application number
AT02804468T
Other languages
English (en)
Inventor
Mitsunori Ono
Lijun Sun
Teresa Przewloka
Shijie Zhang
Elena Kostik
Weiwen Ying
Yumiko Wada
Keizo Koya
Yaming Wu
Dan Zhou
Noriaki Tatsuta
Original Assignee
Synta Pharmaceuticals Corp
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 Synta Pharmaceuticals Corp filed Critical Synta Pharmaceuticals Corp
Priority claimed from PCT/US2002/038161 external-priority patent/WO2003047516A2/en
Application granted granted Critical
Publication of ATE540933T1 publication Critical patent/ATE540933T1/de

Links

Classifications

    • 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
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • C07D403/02Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AT02804468T 2001-11-30 2002-11-27 Pyrimidinverbindungen als interleukin-12 (il-12) inhibitoren ATE540933T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10/000,742 US6693097B2 (en) 2001-11-30 2001-11-30 Pyrimidine compounds
US10/192,347 US6660733B2 (en) 2001-11-30 2002-07-10 2,4,6-trisubstituted-pyrimidine compounds
PCT/US2002/038161 WO2003047516A2 (en) 2001-11-30 2002-11-27 Pyrimidine compounds

Publications (1)

Publication Number Publication Date
ATE540933T1 true ATE540933T1 (de) 2012-01-15

Family

ID=21692824

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02804468T ATE540933T1 (de) 2001-11-30 2002-11-27 Pyrimidinverbindungen als interleukin-12 (il-12) inhibitoren

Country Status (6)

Country Link
US (6) US6693097B2 (de)
JP (1) JP2010248208A (de)
AT (1) ATE540933T1 (de)
ES (1) ES2377947T3 (de)
HK (1) HK1068890A1 (de)
ZA (1) ZA200404215B (de)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL162189A0 (en) * 2001-11-30 2005-11-20 Synta Pharmaceuticals Corp Pyrimidine compounds
US6693097B2 (en) * 2001-11-30 2004-02-17 Synta Pharmaceuticals Corp. Pyrimidine compounds
EP1556140A4 (de) 2002-10-15 2006-04-19 Synta Pharmaceuticals Corp Neue verbindungen
CA2527079A1 (en) * 2003-05-29 2005-01-06 Synta Pharmaceuticals, Corp. Heterocyclic compounds for preventing and treating disorders associated with excessive bone loss
CA2545340A1 (en) * 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
US7338951B2 (en) * 2003-11-10 2008-03-04 Synta Pharmaceuticals Corp. Pyridine compounds
WO2005046619A2 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Compositions and methods for modulating c-rel-dependent cytokine production
CA2545259A1 (en) * 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Heteroaryl-hydrazone compounds
CA2563895C (en) * 2004-04-13 2012-10-16 Synta Pharmaceuticals Corp. Disalt inhibitors of il-12 production
AU2005262322B2 (en) * 2004-07-01 2012-07-26 Synta Pharmaceuticals Corp. 2-substituted heteroaryl compounds
WO2006053109A1 (en) * 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Heteroaryl compounds
TW200630363A (en) * 2004-11-10 2006-09-01 Synta Pharmaceuticals Corp Process for preparing trisubstituted pyrimidine compounds
JP2008519850A (ja) * 2004-11-10 2008-06-12 シンタ ファーマシューティカルズ コーポレーション Il−12調節化合物
US7851466B2 (en) * 2004-11-19 2010-12-14 Synta Pharmaceuticals Corp. Pyrimidine compounds and uses thereof
WO2006128172A2 (en) * 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating b cell regulated autoimmune disorders
TW200804307A (en) * 2005-10-27 2008-01-16 Synta Pharmaceuticals Corp Process for preparing mesylate salts of IL-12 inhibitory compounds
CA2683049A1 (en) * 2007-04-17 2008-10-23 Novartis Ag Organic compounds
ES2372900T3 (es) 2007-10-09 2012-01-27 Dow Agrosciences Llc Pirimidinil-aril-hidrazonas insecticidas.
EP2195302B1 (de) 2007-10-09 2015-02-18 Dow AgroSciences LLC Substituierte azinylderivate als insektizide
ES2403040T3 (es) 2007-10-09 2013-05-13 Dow Agrosciences Llc (1,3,5)-triazinil-fenil-hidrazonas insecticidas
WO2009100406A2 (en) * 2008-02-07 2009-08-13 Synta Pharmaceuticals Corp. Topical formulations for the treatment of psoriasis
EP2376485B1 (de) 2008-12-19 2017-12-06 Vertex Pharmaceuticals Incorporated Als inhibitoren von atr-kinase geeignete pyrazinderivate
JP5578490B2 (ja) 2008-12-26 2014-08-27 味の素株式会社 ピラゾロピリミジン化合物
AU2011282215B2 (en) 2010-07-20 2015-04-16 Vestaron Corporation Insecticidal triazines and pyrimidines
SG190035A1 (en) 2010-10-27 2013-06-28 Prometic Biosciences Inc Phenylketone carboxylate compounds and pharmaceutical uses thereof
MX2016009590A (es) 2014-01-24 2017-05-09 Lam Therapeutics Inc Composiciones de apilimod y métodos para usar las mismas.
CN104163788A (zh) * 2014-07-07 2014-11-26 湖南华腾制药有限公司 一种吡啶衍生物的制备方法
EP3215158B1 (de) 2014-11-07 2019-05-08 AI Therapeutics, Inc. Apilimod zur verwendung bei der behandlung von nierenkrebs
CA2966356A1 (en) * 2014-11-07 2016-05-12 Lam Therapeutics, Inc. Apilimod for use in the treatment of melanoma
US20180078561A1 (en) 2015-03-31 2018-03-22 Lam Therapeutics, Inc. Active metabolites of apilimod and uses thereof
TWI746449B (zh) 2015-07-20 2021-11-21 美商Ai治療公司 使用阿吡莫德治療癌症之方法
WO2019046316A1 (en) 2017-08-28 2019-03-07 Acurastem Inc. PIKFYVE KINASE INHIBITORS
BR112020016256A2 (pt) 2018-02-21 2020-12-15 AI Therapeutics, Inc. Terapia de combinação com apilimod e agentes gluta-matérgicos
AR119934A1 (es) 2019-09-12 2022-01-19 Ai Therapeutics Inc Inhibidores de pikfyve para terapia contra el cáncer
WO2021163727A1 (en) 2020-02-11 2021-08-19 AcuraStem Incorporated Pikfyve kinase inhibitors
EP4351585A1 (de) 2021-06-11 2024-04-17 Orphai Therapeutics Inc. Stabilisierte apilimodzusammensetzungen und verwendungen davon
WO2023215133A1 (en) 2022-05-02 2023-11-09 AcuraStem Incorporated Pikfyve kinase inhibitors

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6830751B1 (en) * 1994-03-14 2004-12-14 Genetics Institute, Llc Use of IL-12 antagonists in the treatment of rheumatoid arthritis
JP3989175B2 (ja) 1999-04-15 2007-10-10 ブリストル−マイヤーズ スクイブ カンパニー 環状タンパク質チロシンキナーゼ阻害剤
US6384032B1 (en) 1999-06-17 2002-05-07 Shionogi Bioresearch Corp. Inhibitors of IL-12 production
US6680315B2 (en) * 2000-06-15 2004-01-20 Synta Pharmaceuticals Corp. Triazine compounds
IL162189A0 (en) * 2001-11-30 2005-11-20 Synta Pharmaceuticals Corp Pyrimidine compounds
US6693097B2 (en) * 2001-11-30 2004-02-17 Synta Pharmaceuticals Corp. Pyrimidine compounds
CA2545259A1 (en) * 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Heteroaryl-hydrazone compounds
TWM281199U (en) * 2005-05-06 2005-11-21 Inventec Appliances Corp Pointer pen having connection interface

Also Published As

Publication number Publication date
JP2010248208A (ja) 2010-11-04
US6660733B2 (en) 2003-12-09
US6858606B2 (en) 2005-02-22
US20050250787A1 (en) 2005-11-10
US20040024206A1 (en) 2004-02-05
US20040048873A1 (en) 2004-03-11
US6693097B2 (en) 2004-02-17
ES2377947T3 (es) 2012-04-03
US20060025409A1 (en) 2006-02-02
ZA200404215B (en) 2006-12-27
HK1068890A1 (en) 2005-05-06
US7470685B2 (en) 2008-12-30
US20030114446A1 (en) 2003-06-19
US20030139403A1 (en) 2003-07-24
US7067514B2 (en) 2006-06-27
US7465725B2 (en) 2008-12-16

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