AU2012204843A1 - Novel sulfamide piperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof - Google Patents

Novel sulfamide piperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof Download PDF

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Publication number
AU2012204843A1
AU2012204843A1 AU2012204843A AU2012204843A AU2012204843A1 AU 2012204843 A1 AU2012204843 A1 AU 2012204843A1 AU 2012204843 A AU2012204843 A AU 2012204843A AU 2012204843 A AU2012204843 A AU 2012204843A AU 2012204843 A1 AU2012204843 A1 AU 2012204843A1
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AU
Australia
Prior art keywords
methyl
pyrrolo
pyrimidin
octane
octa
Prior art date
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Abandoned
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AU2012204843A
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English (en)
Inventor
Kevin Neil Dack
Daniel Rodriguez Greve
Jens Bjorn Jensen
Simon Feldbaek Nielsen
Soren Christian Schou
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Leo Pharma AS
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Leo Pharma AS
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Publication of AU2012204843A1 publication Critical patent/AU2012204843A1/en
Abandoned legal-status Critical Current

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    • 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Toxicology (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU2012204843A 2011-01-07 2012-01-06 Novel sulfamide piperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof Abandoned AU2012204843A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161430670P 2011-01-07 2011-01-07
US61/430,670 2011-01-07
PCT/EP2012/050187 WO2012093169A1 (en) 2011-01-07 2012-01-06 Novel sulfamide piperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof

Publications (1)

Publication Number Publication Date
AU2012204843A1 true AU2012204843A1 (en) 2013-05-02

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ID=45478318

Family Applications (1)

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AU2012204843A Abandoned AU2012204843A1 (en) 2011-01-07 2012-01-06 Novel sulfamide piperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof

Country Status (12)

Country Link
US (1) US9233964B2 (enExample)
EP (1) EP2661436B1 (enExample)
JP (1) JP2014501772A (enExample)
KR (1) KR20140058402A (enExample)
CN (1) CN103298817A (enExample)
AU (1) AU2012204843A1 (enExample)
BR (1) BR112013017184A2 (enExample)
CA (1) CA2823935A1 (enExample)
MX (1) MX2013007792A (enExample)
RU (1) RU2013136906A (enExample)
TW (1) TW201309703A (enExample)
WO (1) WO2012093169A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3145512B1 (en) * 2014-05-19 2019-07-17 Jiangsu Hengrui Medicine Co., Ltd. Substituted ethynyl heterobicyclic compounds as tyrosine kinase inhibitors
CN106661031B (zh) 2014-06-24 2019-07-23 大鹏药品工业株式会社 吡咯并嘧啶化合物或其盐、含有其的药物组合物及应用
CN110291090A (zh) * 2017-01-20 2019-09-27 利奥制药有限公司 作为新型jak激酶抑制剂的双环胺
US10799507B2 (en) 2017-02-03 2020-10-13 Leo Pharma A/S 5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-5-azaspiro[2.5]octane-8-carboxylic acid derivatives as novel JAK kinase inhibitors
CN108822048A (zh) * 2018-07-23 2018-11-16 上海昌肽生物科技有限公司 4-(4-乙基-4,7二氮杂螺环[3,3]辛基)-2-硝基苯胺的合成工艺
CN116730927A (zh) * 2023-03-21 2023-09-12 广州佳途科技股份有限公司 一种新型高效合成4,7-二氮杂螺[2.5]辛烷盐酸盐的方法

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WO2003022214A2 (en) * 2001-09-06 2003-03-20 Millennium Pharmaceuticals, Inc. Piperazine and homopiperazine compounds
AU2003284142A1 (en) * 2002-10-15 2004-05-04 Synta Pharmaceuticals Corp Aromatic bicyclic heterocyles to modulate 1L-12 production
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CA2545192A1 (en) * 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
RU2006120956A (ru) 2003-12-17 2008-01-27 Пфайзер Продактс Инк. (Us) Пирроло{2, 3-d}пиримидиновые соединения для лечения отторжения трансплантата
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
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
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JP2008545660A (ja) * 2005-05-20 2008-12-18 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 プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
CN102127078A (zh) * 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
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Also Published As

Publication number Publication date
JP2014501772A (ja) 2014-01-23
US20130345194A1 (en) 2013-12-26
CA2823935A1 (en) 2012-07-12
BR112013017184A2 (pt) 2016-09-20
EP2661436A1 (en) 2013-11-13
WO2012093169A1 (en) 2012-07-12
TW201309703A (zh) 2013-03-01
MX2013007792A (es) 2013-07-30
RU2013136906A (ru) 2015-02-20
CN103298817A (zh) 2013-09-11
EP2661436B1 (en) 2016-04-13
US9233964B2 (en) 2016-01-12
KR20140058402A (ko) 2014-05-14

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