EA201500930A1 - Новые ингибиторы - Google Patents

Новые ингибиторы

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Publication number
EA201500930A1
EA201500930A1 EA201500930A EA201500930A EA201500930A1 EA 201500930 A1 EA201500930 A1 EA 201500930A1 EA 201500930 A EA201500930 A EA 201500930A EA 201500930 A EA201500930 A EA 201500930A EA 201500930 A1 EA201500930 A1 EA 201500930A1
Authority
EA
Eurasian Patent Office
Prior art keywords
release
formation
present
pyroglutamic acid
intramolecular cyclization
Prior art date
Application number
EA201500930A
Other languages
English (en)
Other versions
EA029451B1 (ru
Inventor
Ульрих Хайзер
Мирко Буххольц
Роберт Зоммер
Ханс-Ульрих Демут
Антье Майер
Original Assignee
Пробиодруг Аг
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 Пробиодруг Аг filed Critical Пробиодруг Аг
Publication of EA201500930A1 publication Critical patent/EA201500930A1/ru
Publication of EA029451B1 publication Critical patent/EA029451B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further 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
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
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    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • 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]
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    • A61P3/00—Drugs for disorders of the metabolism
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    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Cardiology (AREA)
  • Toxicology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
  • Nutrition Science (AREA)
  • Dermatology (AREA)

Abstract

Настоящее изобретение относится к соединению формулы (I) или его фармацевтически приемлемой соли, сольвату или полиморфной форме, включая все их таутомеры и стереоизомеры, в которой R, R, R, Rи Rявляются такими, как определено в настоящем изобретении, в качестве ингибиторов глутаминилциклазы (QC, ЕС 2.3.2.5). QC катализирует внутримолекулярную циклизацию N-концевых остатков глутамина с образованием пироглутаминовой кислоты (5-оксопролил, pGlu*) с выделением аммиака и внутримолекулярную циклизацию N-концевых остатков глутамина с образованием пироглутаминовой кислоты с выделением воды.
EA201500930A 2013-03-15 2014-03-14 Новые ингибиторы EA029451B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361790604P 2013-03-15 2013-03-15
PCT/EP2014/055106 WO2014140279A1 (en) 2013-03-15 2014-03-14 Novel inhibitors

Publications (2)

Publication Number Publication Date
EA201500930A1 true EA201500930A1 (ru) 2016-04-29
EA029451B1 EA029451B1 (ru) 2018-03-30

Family

ID=50434164

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201500930A EA029451B1 (ru) 2013-03-15 2014-03-14 Новые ингибиторы

Country Status (18)

Country Link
US (1) US9512115B2 (ru)
EP (1) EP2970235B1 (ru)
JP (1) JP6454651B2 (ru)
KR (2) KR102279084B1 (ru)
CN (2) CN108218849B (ru)
AU (1) AU2014230249B2 (ru)
CA (1) CA2904465C (ru)
DK (1) DK2970235T3 (ru)
EA (1) EA029451B1 (ru)
ES (1) ES2750645T3 (ru)
HK (1) HK1216531A1 (ru)
IL (1) IL240693B (ru)
MX (1) MX367855B (ru)
NZ (1) NZ712352A (ru)
PL (1) PL2970235T3 (ru)
SG (1) SG11201506609VA (ru)
WO (1) WO2014140279A1 (ru)
ZA (1) ZA201506156B (ru)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016097305A1 (en) 2014-12-19 2016-06-23 Probiodrug Ag Novel method for the detection of pglu-abeta peptides
CN105152977B (zh) * 2015-09-28 2017-06-23 西南大学 D‑对羟基苯甘氨酸衍生物及其制备方法和应用
WO2019010491A1 (en) * 2017-07-07 2019-01-10 University Of Pittsburgh-Of The Commonwealth System Of Higher Education COMBINATIONS OF MEDICINES FOR THE PROTECTION AGAINST THE DEATH OF NEURONAL CELLS
DK3658141T3 (da) 2017-07-24 2023-02-06 Stichting Het Nederlands Kanker Inst Antoni Van Leeuwenhoek Ziekenhuis Behandling af patologiske tilstande ved direkte og indirekte målretning af Sirpalpha-CD47-interaktion
ES2812698T3 (es) * 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
EP3589632B1 (en) 2018-02-23 2020-09-23 FRAUNHOFER-GESELLSCHAFT zur Förderung der angewandten Forschung e.V. Novel inhibitors of bacterial glutaminyl cyclases for use in the treatment of periodontal and related diseases
TWI715156B (zh) * 2018-08-31 2021-01-01 財團法人國家衛生研究院 苯并咪唑化合物及其用於治療阿茲海默症或亨丁頓氏症之用途
CN111333496B (zh) * 2020-05-02 2023-10-13 武汉诺安药业有限公司 一种阿达帕林的制备方法
CN112500361B (zh) * 2020-12-27 2023-05-12 甘肃瀚聚药业有限公司 一种(s)-4-苯基-2-恶唑烷酮的制备方法
CN112939797A (zh) * 2021-02-03 2021-06-11 山东邹平大展新材料有限公司 一种法匹拉韦中间体2-胺基丙二酰胺的制备方法
AU2022203580A1 (en) * 2021-09-17 2023-04-06 Academia Sinica Methods of Increasing Cell Phagocytosis
CN114295746A (zh) * 2021-12-27 2022-04-08 卓和药业集团股份有限公司 一种匹伐他汀钙的分析检测方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004098625A2 (en) * 2003-05-05 2004-11-18 Probiodrug Ag Medical use of inhibitors of glutaminyl and glutamate cyclases
JP5599614B2 (ja) * 2006-11-09 2014-10-01 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
MX2011002106A (es) 2008-09-04 2011-04-07 Probiodrug Ag Inhibidores novedosos.
SG178953A1 (en) * 2009-09-11 2012-04-27 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
US8809508B2 (en) 2011-03-16 2014-08-19 Probiodrug Ag Diagnostic antibody assay
US8945510B2 (en) 2011-05-27 2015-02-03 Probiodrug Ag Radiolabeled glutaminyl cyclase (QC) inhibitors and uses of same

Also Published As

Publication number Publication date
IL240693A0 (en) 2015-10-29
CN108218849B (zh) 2022-03-01
IL240693B (en) 2019-09-26
EP2970235B1 (en) 2019-06-19
US9512115B2 (en) 2016-12-06
MX2015012630A (es) 2016-07-06
US20160031869A1 (en) 2016-02-04
BR112015023454A2 (pt) 2017-12-05
KR102279084B1 (ko) 2021-07-20
KR20210091830A (ko) 2021-07-22
JP2016513632A (ja) 2016-05-16
CN108218849A (zh) 2018-06-29
CN105263927A (zh) 2016-01-20
HK1216531A1 (zh) 2016-11-18
AU2014230249B2 (en) 2016-09-01
JP6454651B2 (ja) 2019-01-23
CA2904465C (en) 2021-07-13
KR20150128928A (ko) 2015-11-18
ZA201506156B (en) 2017-11-29
MX367855B (es) 2019-09-09
CN105263927B (zh) 2019-03-15
PL2970235T3 (pl) 2019-12-31
AU2014230249A1 (en) 2015-10-08
EP2970235A1 (en) 2016-01-20
NZ712352A (en) 2016-07-29
WO2014140279A1 (en) 2014-09-18
EA029451B1 (ru) 2018-03-30
ES2750645T3 (es) 2020-03-26
DK2970235T3 (da) 2019-09-23
CA2904465A1 (en) 2014-09-18
SG11201506609VA (en) 2015-09-29

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