AU2011232516B2 - Chemical compounds - Google Patents

Chemical compounds Download PDF

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Publication number
AU2011232516B2
AU2011232516B2 AU2011232516A AU2011232516A AU2011232516B2 AU 2011232516 B2 AU2011232516 B2 AU 2011232516B2 AU 2011232516 A AU2011232516 A AU 2011232516A AU 2011232516 A AU2011232516 A AU 2011232516A AU 2011232516 B2 AU2011232516 B2 AU 2011232516B2
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AU
Australia
Prior art keywords
indol
dihydro
amine
acetyl
methyl
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.)
Ceased
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AU2011232516A
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English (en)
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AU2011232516A1 (en
AU2011232516A8 (en
Inventor
Jeffrey Michael Axten
Seth Wilson Grant
Dirk A. Heerding
Jesus Raul Medina
Stuart Paul Romeril
Jun Tang
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GlaxoSmithKline LLC
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GlaxoSmithKline LLC
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Publication of AU2011232516A1 publication Critical patent/AU2011232516A1/en
Publication of AU2011232516A8 publication Critical patent/AU2011232516A8/en
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Publication of AU2011232516B2 publication Critical patent/AU2011232516B2/en
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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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
    • 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
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • 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)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2011232516A 2010-03-25 2011-03-23 Chemical compounds Ceased AU2011232516B2 (en)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US31747610P 2010-03-25 2010-03-25
US61/317,476 2010-03-25
US35286310P 2010-06-09 2010-06-09
US61/352,863 2010-06-09
US38148010P 2010-09-10 2010-09-10
US61/381,480 2010-09-10
US38815110P 2010-09-30 2010-09-30
US61/388,151 2010-09-30
US41906810P 2010-12-02 2010-12-02
US61/419,068 2010-12-02
PCT/US2011/029511 WO2011119663A1 (en) 2010-03-25 2011-03-23 Chemical compounds

Publications (3)

Publication Number Publication Date
AU2011232516A1 AU2011232516A1 (en) 2012-10-04
AU2011232516A8 AU2011232516A8 (en) 2012-12-13
AU2011232516B2 true AU2011232516B2 (en) 2014-08-07

Family

ID=46160738

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2011232516A Ceased AU2011232516B2 (en) 2010-03-25 2011-03-23 Chemical compounds

Country Status (15)

Country Link
US (1) US20120077828A1 (OSRAM)
EP (1) EP2549868B1 (OSRAM)
JP (1) JP5876031B2 (OSRAM)
KR (1) KR101676077B1 (OSRAM)
CN (1) CN102917588B (OSRAM)
AR (1) AR080792A1 (OSRAM)
AU (1) AU2011232516B2 (OSRAM)
EA (1) EA022325B1 (OSRAM)
ES (1) ES2530955T3 (OSRAM)
IL (1) IL222120A (OSRAM)
MX (1) MX2012011045A (OSRAM)
SG (1) SG183954A1 (OSRAM)
TW (1) TW201202241A (OSRAM)
UY (1) UY33288A (OSRAM)
WO (1) WO2011119663A1 (OSRAM)

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WO2016126026A2 (ko) * 2015-02-04 2016-08-11 서울대학교병원 당뇨병 치료 조성물 및 이의 용도
WO2017002095A1 (en) 2015-07-02 2017-01-05 Acerta Pharma B.V. Solid forms and formulations of (s)-4-(8-amino-3-(1 -(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamide
TW201722957A (zh) * 2015-09-15 2017-07-01 葛蘭素史克智慧財產（第二）有限公司 化學化合物
WO2017046739A1 (en) * 2015-09-15 2017-03-23 Glaxosmithkline Intellectual Property (No.2) Limited Imidazolidinone derivatives as inhibitors of perk
JOP20170083B1 (ar) * 2016-04-07 2022-03-14 Glaxosmithkline Ip Dev Ltd أميدات هتيروسيكلية مفيدة كمعدلات بروتين
CN115650985B (zh) * 2016-04-15 2024-08-02 癌症研究科技有限公司 作为ret激酶抑制剂的杂环化合物
US11026945B2 (en) * 2016-04-29 2021-06-08 The Trustees Of The University Of Pennsylvania Protein kinase RNA-like endoplasmic reticulum kinase (PERK) inhibitors for prevention and/or treatment of lung injury and/or inflammation
WO2017216792A1 (en) 2016-06-13 2017-12-21 Ramot At Tel-Aviv University Ltd. Perk inhibitors and uses thereof in treating diseases associated with aggregation-prone proteins
CA3029097A1 (en) 2016-06-21 2017-12-28 Nerviano Medical Sciences S.R.L. N-(substituted-phenyl)-sulfonamide derivatives as perk kinase inhibitors
AU2017300123A1 (en) * 2016-07-20 2019-01-31 Glaxosmithkline Intellectual Property Development Limited Isoquinoline derivatives as PERK inhibitors
CN109982693A (zh) * 2016-09-22 2019-07-05 香港大学 细胞异常分化和isr相关疾病的预防和治疗方法
US20190388426A1 (en) 2017-01-30 2019-12-26 Université de Liège Perk and ire-1a inhibitors against neurodevelopmental disorders
CN106974910B (zh) * 2017-03-02 2019-11-12 深圳大学 含索拉非尼和gsk2656157的药物组合物及用途
CN106963769B (zh) * 2017-03-03 2019-10-25 深圳大学 含pi3k抑制剂和perk抑制剂的药物组合物及其应用
HUE069999T2 (hu) 2017-03-06 2025-04-28 Tsubota Lab Inc Kompozíció miópia megelõzésében vagy szuppressziójában történõ alkalmazásra
JP6594570B2 (ja) * 2017-03-20 2019-10-23 フォーマ セラピューティクス，インコーポレイテッド ピルビン酸キナーゼ（ｐｋｒ）活性化剤としてのピロロピロール組成物
WO2019021208A1 (en) * 2017-07-27 2019-01-31 Glaxosmithkline Intellectual Property Development Limited USEFUL INDAZOLE DERIVATIVES AS PERK INHIBITORS
WO2019090088A1 (en) 2017-11-02 2019-05-09 Calico Life Sciences Llc Modulators of the integrated stress pathway
CN108003163B (zh) * 2017-11-30 2020-11-24 武汉九州钰民医药科技有限公司 用作激酶抑制剂的吡唑并嘧啶类化合物及其应用
CN111100130B (zh) * 2018-10-29 2022-07-15 四川大学 4-氨基吡咯并嘧啶衍生物及其制备方法和用途
CN111213632B (zh) * 2019-11-19 2022-03-01 长春中医药大学 动物药环氧树脂标本制作方法
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