MX367855B - Inhibidores novedosos. - Google Patents

Inhibidores novedosos.

Info

Publication number
MX367855B
MX367855B MX2015012630A MX2015012630A MX367855B MX 367855 B MX367855 B MX 367855B MX 2015012630 A MX2015012630 A MX 2015012630A MX 2015012630 A MX2015012630 A MX 2015012630A MX 367855 B MX367855 B MX 367855B
Authority
MX
Mexico
Prior art keywords
pyroglutamic acid
intramolecular cyclization
novel inhibitors
inhibitors
under liberation
Prior art date
Application number
MX2015012630A
Other languages
English (en)
Other versions
MX2015012630A (es
Inventor
Demuth Hans-Ulrich
Heiser Ulrich
Buchholz Mirko
Sommer Robert
Meyer Antje
Original Assignee
Probiodrug Ag
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 Probiodrug Ag filed Critical Probiodrug Ag
Publication of MX2015012630A publication Critical patent/MX2015012630A/es
Publication of MX367855B publication Critical patent/MX367855B/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61P19/00Drugs for skeletal disorders
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P35/00Antineoplastic agents
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    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Nutrition Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)

Abstract

La invención se refiere a un compuesto de fórmula (I) o a una sal farmacéuticamente aceptable, solvato o polimorfo del mismo, incluyendo todos los tautómeros y estereoisómeros del mismo, en donde R1, R2, R3, R4 y R5 son como se define en la presente, como inhibidores de glutaminil ciclasa (QC, EC 2.3.2.5). La QC cataliza la ciclación intramolecular de los residuos de glutamina N-terminales en ácido piroglutámico (5-oxo-prolilo, pGlu*) bajo la liberación de amoníaco, y la ciclación intramolecular de los residuos de glutamato N-terminales en ácido piroglutámico bajo la liberación de agua.
MX2015012630A 2013-03-15 2014-03-14 Inhibidores novedosos. MX367855B (es)

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
MX2015012630A MX2015012630A (es) 2016-07-06
MX367855B true MX367855B (es) 2019-09-09

Family

ID=50434164

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015012630A MX367855B (es) 2013-03-15 2014-03-14 Inhibidores novedosos.

Country Status (18)

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

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170363645A1 (en) 2014-12-19 2017-12-21 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
EP3747437A1 (en) 2017-07-24 2020-12-09 Stichting Het Nederlands Kanker Instituut- Antoni van Leeuwenhoek Ziekenhuis Treating pathological conditions by direct and indirect targeting of sirpa - cd47 interaction
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
JP7301862B2 (ja) 2018-02-23 2023-07-03 フラウンホーファー-ゲゼルシャフト ツル フェルデルング デル アンゲヴァンテン フォルシュング エー ファウ 歯周病及び関連疾患の治療に用いる細菌性グルタミニルシクラーゼの新規阻害剤
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
EA009291B1 (ru) * 2003-05-05 2007-12-28 Пробиодруг Аг Применение эффекторов глутаминил- и глутаматциклаз
WO2008055950A1 (en) * 2006-11-09 2008-05-15 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
SG193828A1 (en) * 2008-09-04 2013-10-30 Probiodrug Ag Novel inhibitors
US8486940B2 (en) * 2009-09-11 2013-07-16 Probiodrug Ag Inhibitors
AU2012228236B2 (en) 2011-03-16 2016-10-27 Vivoryon Therapeutics N.V. Diagnostic antibody assay
EP2714098A1 (en) 2011-05-27 2014-04-09 Probiodrug AG Radiolabelled glutaminyl cyclase inhibitors

Also Published As

Publication number Publication date
WO2014140279A1 (en) 2014-09-18
HK1216531A1 (zh) 2016-11-18
CA2904465C (en) 2021-07-13
IL240693A0 (en) 2015-10-29
EP2970235A1 (en) 2016-01-20
EP2970235B1 (en) 2019-06-19
MX2015012630A (es) 2016-07-06
CN108218849A (zh) 2018-06-29
ZA201506156B (en) 2017-11-29
ES2750645T3 (es) 2020-03-26
KR20150128928A (ko) 2015-11-18
CA2904465A1 (en) 2014-09-18
KR20210091830A (ko) 2021-07-22
CN105263927A (zh) 2016-01-20
BR112015023454A2 (pt) 2017-12-05
PL2970235T3 (pl) 2019-12-31
JP6454651B2 (ja) 2019-01-23
SG11201506609VA (en) 2015-09-29
NZ712352A (en) 2016-07-29
US9512115B2 (en) 2016-12-06
JP2016513632A (ja) 2016-05-16
KR102279084B1 (ko) 2021-07-20
IL240693B (en) 2019-09-26
EA029451B1 (ru) 2018-03-30
CN105263927B (zh) 2019-03-15
DK2970235T3 (da) 2019-09-23
US20160031869A1 (en) 2016-02-04
EA201500930A1 (ru) 2016-04-29
CN108218849B (zh) 2022-03-01
AU2014230249A1 (en) 2015-10-08
AU2014230249B2 (en) 2016-09-01

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