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

    • 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
    • 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
    • A61K31/53—Heterocyclic 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (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 (5)

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

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6693097B2 (en) * 2001-11-30 2004-02-17 Synta Pharmaceuticals Corp. Pyrimidine compounds
BR0214809A (pt) * 2001-11-30 2004-09-14 Synta Pharmaceuticals Corp Compostos de pirimidina
AU2003284142A1 (en) 2002-10-15 2004-05-04 Synta Pharmaceuticals Corp Aromatic bicyclic heterocyles to modulate 1L-12 production
WO2005000404A2 (en) * 2003-05-29 2005-01-06 Synta Pharmaceuticals, Corp. Heterocyclic compounds for preventing and treating disorders associated with excessive bone loss
TW200530588A (en) 2003-11-10 2005-09-16 Synta Pharmaceuticals Corp Compositions and methods for modulating c-Rel-dependent cytokine production
JP4851337B2 (ja) * 2003-11-10 2012-01-11 シンタ ファーマシューティカルズ コーポレーション ヘテロアリールヒドラゾン化合物
EP1687004A4 (de) * 2003-11-10 2009-04-08 Synta Pharmaceuticals Corp Pyridin-verbindungen
CA2545340A1 (en) * 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
TWI380816B (zh) * 2004-04-13 2013-01-01 Synta Pharmaceuticals Corp 抑制介白素-12(il-12)生成之二鹽抑制劑
AU2005262322B2 (en) * 2004-07-01 2012-07-26 Synta Pharmaceuticals Corp. 2-substituted heteroaryl 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
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
AU2005310143A1 (en) * 2004-11-19 2006-06-08 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
WO2008125691A2 (en) * 2007-04-17 2008-10-23 Novartis Ag Ethers of naphtalene carboxylic acid amides as cancer cure
EP2197853B1 (de) 2007-10-09 2011-11-09 Dow AgroSciences LLC Insektizide pyrimidinyl-aryl-hydrazone
ES2532119T3 (es) 2007-10-09 2015-03-24 Dow Agrosciences Llc Derivados de azinilo sustituido insecticidas
EP2197857B1 (de) * 2007-10-09 2013-03-06 Dow AgroSciences LLC (1,3,5)-triazinylphenylhydrazone als insektizid
US20110098267A1 (en) * 2008-02-07 2011-04-28 Synta Pharmaceuticals Corporation Topical formulations for the treatment of psoriasis
PL3354650T3 (pl) 2008-12-19 2022-06-13 Vertex Pharmaceuticals Incorporated Związki przydatne jako inhibitory kinazy atr
WO2010074284A1 (ja) 2008-12-26 2010-07-01 味の素株式会社 ピラゾロピリミジン化合物
ES2587232T3 (es) 2010-07-20 2016-10-21 Vestaron Corporation Triazinas y pirimidinas insecticidas
PH12013500763B1 (en) * 2010-10-27 2018-07-04 Prometic Pharma Smt Ltd Phenylketone carboxylate compounds and pharmaceutical uses thereof
AU2015209133B2 (en) 2014-01-24 2019-10-03 AI Therapeutics, Inc. Apilimod compositions and methods for using same
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
ES2734081T3 (es) * 2014-11-07 2019-12-04 Ai Therapeutics Inc Apilimod para el uso en el tratamiento de melanoma
CN107249638B (zh) 2014-11-07 2021-05-14 人工智能治疗公司 阿匹莫德用于治疗肾癌
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
US10751345B2 (en) 2018-02-21 2020-08-25 AI Therapeutics, Inc. Combination therapy with apilimod and glutamatergic agents
US12589097B2 (en) 2018-02-21 2026-03-31 OrphAl Therapeutics Inc. Apilimod compositions and methods of use
US20210077500A1 (en) 2019-09-12 2021-03-18 Al Therapeutics, Inc. Pikfyve inhibitors for cancer therapy
US20230135152A1 (en) 2020-02-11 2023-05-04 AcuraStem Incorporated Pikfyve kinase inhibitors
BR112023025552A2 (pt) 2021-06-11 2024-02-27 Orphai Therapeutics Inc Composições estabilizadas de apilimod e usos das mesmas
US20250282767A1 (en) 2022-05-02 2025-09-11 AcuraStem Incorporated Pikfyve kinase inhibitors

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Publication number Priority date Publication date Assignee Title
US6706264B1 (en) 1994-03-14 2004-03-16 Genetics Institute, Llc Use of IL-12 antagonists in the treatment of conditions promoted by an increase in levels of IFN-y
CA2366932C (en) 1999-04-15 2009-08-25 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
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
BR0214809A (pt) 2001-11-30 2004-09-14 Synta Pharmaceuticals Corp Compostos de pirimidina
US6693097B2 (en) 2001-11-30 2004-02-17 Synta Pharmaceuticals Corp. Pyrimidine compounds
JP4851337B2 (ja) 2003-11-10 2012-01-11 シンタ ファーマシューティカルズ コーポレーション ヘテロアリールヒドラゾン化合物
TWM281199U (en) * 2005-05-06 2005-11-21 Inventec Appliances Corp Pointer pen having connection interface

Also Published As

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

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