BR112015029182A2 - composto para uso em modulação da rota wnt, uso do composto, método, composição farmacêutica, forma anidra, uso de uma base livre anidra - Google Patents

composto para uso em modulação da rota wnt, uso do composto, método, composição farmacêutica, forma anidra, uso de uma base livre anidra

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Publication number
BR112015029182A2
BR112015029182A2 BR112015029182A BR112015029182A BR112015029182A2 BR 112015029182 A2 BR112015029182 A2 BR 112015029182A2 BR 112015029182 A BR112015029182 A BR 112015029182A BR 112015029182 A BR112015029182 A BR 112015029182A BR 112015029182 A2 BR112015029182 A2 BR 112015029182A2
Authority
BR
Brazil
Prior art keywords
compound
anhydrous
pharmaceutical composition
free base
modulation
Prior art date
Application number
BR112015029182A
Other languages
English (en)
Other versions
BR112015029182B1 (pt
BR112015029182A8 (pt
Inventor
Jeyaraj Duraiswamy Athisayamani
Alam Jenefer
Yei Ho Soo
Eliane Blanchard Stephanie
Arun Adsool Vikrant
Original Assignee
Agency Science Tech & Res
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 Agency Science Tech & Res filed Critical Agency Science Tech & Res
Publication of BR112015029182A2 publication Critical patent/BR112015029182A2/pt
Publication of BR112015029182A8 publication Critical patent/BR112015029182A8/pt
Publication of BR112015029182B1 publication Critical patent/BR112015029182B1/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • 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
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P9/10—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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • C07D473/08—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1 and 3, e.g. theophylline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

resumo composto para uso em modulação da rota wnt, uso do composto, método, composição farmacêutica, forma anidra, uso de uma base livre anidra a invenção se refere ao uso de compostos de estrutura geral (i) em modulação da rota wnt, (i) em que r1, r2, r3, r4 e r5 são cada um, independentemente, h ou um grupo alquil; d é selecionado a partir do grupo consistindo de h, halogênio, alquil, cicloalquil, aril e dialquilamino, cada um (diferente de h e halogênio) sendo opcionalmente substituído; ar é um grupo aril ou heteroaril, opcionalmente substituído; cy é um aril, heteroaril ou um anel saturado contendo pelo menos um heteroátomo, cada um sendo opcionalmente substituído; e n é um inteiro de 1 a 3.
BR112015029182-1A 2013-05-23 2014-05-19 Composto para uso em modulação da rota wnt, composição farmacêutica e uso BR112015029182B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1309333.1 2013-05-23
GBGB1309333.1A GB201309333D0 (en) 2013-05-23 2013-05-23 Purine diones as WNT pathway modulators
PCT/SG2014/000217 WO2014189466A1 (en) 2013-05-23 2014-05-19 Purine diones as wnt pathway modulators

Publications (3)

Publication Number Publication Date
BR112015029182A2 true BR112015029182A2 (pt) 2017-07-25
BR112015029182A8 BR112015029182A8 (pt) 2020-03-17
BR112015029182B1 BR112015029182B1 (pt) 2023-10-03

Family

ID=48784655

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BR112015029182-1A BR112015029182B1 (pt) 2013-05-23 2014-05-19 Composto para uso em modulação da rota wnt, composição farmacêutica e uso

Country Status (13)

Country Link
US (6) US9926320B2 (pt)
EP (1) EP2999699B1 (pt)
JP (1) JP6506742B2 (pt)
KR (2) KR102153989B1 (pt)
CN (2) CN109776537B (pt)
AU (2) AU2014269134B2 (pt)
BR (1) BR112015029182B1 (pt)
CA (1) CA2912757C (pt)
DK (1) DK2999699T3 (pt)
ES (1) ES2802923T3 (pt)
GB (1) GB201309333D0 (pt)
SG (1) SG11201509593TA (pt)
WO (1) WO2014189466A1 (pt)

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TWI676626B (zh) * 2014-04-23 2019-11-11 美商美國禮來大藥廠 抑制瞬時受體電位ａ１離子通道
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CN105440034B (zh) * 2015-11-16 2017-08-15 山东罗欣药业集团股份有限公司 一种利格列汀及其中间体的制备方法
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
CN106632332B (zh) * 2016-09-26 2018-07-06 杭州新博思生物医药有限公司 一种伊曲茶碱的制备方法
EP3681886A4 (en) * 2017-09-14 2021-05-05 Agency For Science, Technology And Research MODULATORS OF THE WNT SIGNAL PATH
EP4233871A3 (en) 2018-01-31 2023-11-01 Eli Lilly and Company Inhibiting the transient receptor potential a1 ion channel
US10961534B2 (en) 2018-07-13 2021-03-30 University of Pittsburgh—of the Commonwealth System of Higher Education Methods of treating porphyria
CN114025764A (zh) * 2019-05-22 2022-02-08 新加坡科技研究局 药物组合
CN114072131B (zh) * 2019-05-22 2024-03-19 新加坡科技研究局 口服制剂、其制备方法及其用途
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CN115279377A (zh) * 2020-01-08 2022-11-01 新加坡科技研究局 联合疗法
WO2023072263A1 (zh) * 2021-10-29 2023-05-04 南京明德新药研发有限公司 5-取代的吡啶-2(1h)-酮类化合物及其应用
CN114671875A (zh) * 2022-04-27 2022-06-28 成都施贝康生物医药科技有限公司 新型二氢嘧啶类化合物、异构体或盐及其制备方法和用途

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Also Published As

Publication number Publication date
CN109776537A (zh) 2019-05-21
US20160090386A1 (en) 2016-03-31
DK2999699T3 (da) 2020-07-13
BR112015029182B1 (pt) 2023-10-03
KR102062262B1 (ko) 2020-01-03
AU2017219132A1 (en) 2017-09-14
AU2014269134A1 (en) 2015-12-10
US20200190086A1 (en) 2020-06-18
US10844063B2 (en) 2020-11-24
CA2912757C (en) 2021-11-30
WO2014189466A1 (en) 2014-11-27
GB201309333D0 (en) 2013-07-10
EP2999699A4 (en) 2016-10-26
KR102153989B1 (ko) 2020-09-09
CN109776537B (zh) 2021-12-14
KR20160029024A (ko) 2016-03-14
ES2802923T3 (es) 2021-01-21
KR20200000504A (ko) 2020-01-02
AU2014269134B2 (en) 2017-06-15
JP2016519165A (ja) 2016-06-30
US20170334912A1 (en) 2017-11-23
US20230174533A1 (en) 2023-06-08
CA2912757A1 (en) 2014-11-27
SG11201509593TA (en) 2015-12-30
US20210155623A1 (en) 2021-05-27
AU2017219132B2 (en) 2019-04-18
US9926320B2 (en) 2018-03-27
CN105452248A (zh) 2016-03-30
US11555037B2 (en) 2023-01-17
US20180170932A1 (en) 2018-06-21
EP2999699A1 (en) 2016-03-30
EP2999699B1 (en) 2020-04-29
BR112015029182A8 (pt) 2020-03-17
US10472360B2 (en) 2019-11-12
JP6506742B2 (ja) 2019-04-24
US10526335B2 (en) 2020-01-07

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