PE20180252A1 - Moduladores alostericos positivos del receptor muscarinico m2 - Google Patents

Moduladores alostericos positivos del receptor muscarinico m2

Info

Publication number
PE20180252A1
PE20180252A1 PE2017002542A PE2017002542A PE20180252A1 PE 20180252 A1 PE20180252 A1 PE 20180252A1 PE 2017002542 A PE2017002542 A PE 2017002542A PE 2017002542 A PE2017002542 A PE 2017002542A PE 20180252 A1 PE20180252 A1 PE 20180252A1
Authority
PE
Peru
Prior art keywords
alosteric
same
muscarinic
positive modulators
fluorine
Prior art date
Application number
PE2017002542A
Other languages
English (en)
Inventor
Alexandros Vakalopoulos
Henrik Teller
Alexander Straub
Markus Brechmann
Thomas Muller
Mark Meininghaus
Reppel Katrin Nowak
Hanna Tinel
Klaus Munter
Daniela Fliegner
Thomas Mondritzki
Arapinis Mellissa Boultadakis
Tobias Marquardt
Anne Sophie Rebstock
Matthias Beat Wittwer
Original Assignee
Bayer Pharma 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 Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of PE20180252A1 publication Critical patent/PE20180252A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Referido a un compuesto de la formula (I) donde: R1 es NR4R5; R4 es H, metilo, alquilo -(C2-C4) entre otros; R5 es alquilo -(C1-C6), cicloalquilo-(C3-C6), entre otros; Ar1 es un grupo de la formula (a) donde R3A es fluor, entre otros; R3B es hidrogeno o fluor; R3C es hidrogeno, fluor o cloro; R2 es -L1-Ar2, entre otros, donde L1 es un enlace, entre otros; Ar2 es fenilo. Estos compuestos son moduladores alostericos positivos del receptor muscarinico M2. Tambien se refiere a los procesos de preparacion de los mismos y uso de los mismos, por si solos o en combinaciones para tratar y/o prevenir enfermedades y al uso de las mismos para producir medicamentos para tratar y/o prevenir trastornos cardiovasculares y/o trastornos renales.
PE2017002542A 2015-06-09 2016-06-06 Moduladores alostericos positivos del receptor muscarinico m2 PE20180252A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15171127 2015-06-09
EP16156676 2016-02-22

Publications (1)

Publication Number Publication Date
PE20180252A1 true PE20180252A1 (es) 2018-02-02

Family

ID=56101466

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017002542A PE20180252A1 (es) 2015-06-09 2016-06-06 Moduladores alostericos positivos del receptor muscarinico m2

Country Status (27)

Country Link
US (2) US10435403B2 (es)
EP (2) EP3307741B1 (es)
JP (1) JP6908536B2 (es)
KR (1) KR20180016485A (es)
CN (1) CN107949562B (es)
AU (1) AU2016274433B2 (es)
BR (1) BR112017026561A2 (es)
CA (1) CA2988468A1 (es)
CL (1) CL2017003124A1 (es)
CO (1) CO2017012622A2 (es)
CR (1) CR20170566A (es)
CU (1) CU20170158A7 (es)
DO (1) DOP2017000288A (es)
EA (1) EA035465B1 (es)
EC (1) ECSP17081322A (es)
HK (1) HK1254348A1 (es)
IL (2) IL256119A (es)
MX (1) MX370113B (es)
NI (1) NI201700154A (es)
PE (1) PE20180252A1 (es)
PH (1) PH12017502224A1 (es)
SG (1) SG11201710164QA (es)
TN (1) TN2017000498A1 (es)
TW (1) TW201716405A (es)
UY (1) UY36714A (es)
WO (1) WO2016198342A1 (es)
ZA (1) ZA201800125B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2018014868A (es) 2016-06-02 2019-09-13 Cloudbreak Therapeutics Llc Composiciones y metodos de uso de nintedanib para mejorar el exito de la cirugia del glaucoma.
JP2019524722A (ja) 2016-07-11 2019-09-05 バイエル・ファルマ・アクティエンゲゼルシャフト 7−置換1−ピリジル−ナフチリジン−3−カルボン酸アミドおよびその使用
JOP20190045A1 (ar) * 2016-09-14 2019-03-14 Bayer Ag مركبات أميد حمض 1- أريل-نفثيريدين-3-كربوكسيليك مستبدلة في الموضع 7 واستخدامها.
JOP20190086A1 (ar) * 2016-10-21 2019-04-18 Novartis Ag مشتقات نافثيريدينون جديدة واستخدامها في معالجة عدم انتظام ضربات القلب
CN110215899B (zh) * 2019-04-01 2022-03-25 重庆科技学院 一种氨基酸功能化的金属有机骨架材料及其制备方法和应用
WO2021050692A2 (en) * 2019-09-10 2021-03-18 Cloudbreak Therapeutics, Llc Methods for alleviating pterygium-associated worry about eye appearance
CN111057045A (zh) * 2019-12-18 2020-04-24 安徽红杉生物医药科技有限公司 Hcv ns3/4a蛋白酶抑制剂中间体及其合成方法、应用
CN114105881B (zh) 2020-08-31 2024-01-26 沈阳海诺威医药科技有限公司 血小板聚集抑制剂及其制备方法和用途
CN113072480B (zh) * 2021-04-13 2022-09-30 常州佳德医药科技有限公司 一种手性(-)-5-氮杂螺[2.4]庚烷-7-醇、制备方法及应用

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3906365A1 (de) 1988-07-15 1990-01-18 Bayer Ag 7-(1-pyrrolidinyl)-3-chinolon- und -naphthyridoncarbonsaeure-derivate, verfahren sowie substituierte (oxa)diazabicyclooctane und -nonane als zwischenprodukte zu ihrer herstellung, und sie enthaltende antibakterielle mittel und futterzusatzstoffe
IT1239283B (it) * 1989-11-08 1993-10-19 Erba Carlo Spa Uso di un agente muscarinico da solo o insieme ad un noto farmaco antiaritmico per la prevenzione e/o il trattamento dell'aritmia ventricolare.
BR9407283A (pt) 1993-08-13 1996-10-01 Dong Wha Pharm Co Ltd Derivados do ácido carboxílico quinolônico e processo de preparação
US6964966B2 (en) 2001-04-25 2005-11-15 Wockhardt Limited Generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments
AU2002361493A1 (en) 2001-12-13 2003-06-23 Wockhardt Limited New generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments
CN1168446C (zh) * 2002-08-26 2004-09-29 夏国瑾 氢溴酸槟榔碱作为制备抗心律失常药物的应用
CA2526423A1 (en) * 2003-05-21 2004-12-29 Board Of Regents, The University Of Texas System Inhibition of protein kinase c-mu (pkd) as a treatment for cardiac hypertrophy and heart failure
JP2005012561A (ja) 2003-06-19 2005-01-13 Sony Corp 画像処理装置、画像処理方法および画像投射装置
US7488739B2 (en) 2003-07-24 2009-02-10 Astellas Pharma Inc. Quinolone derivative or salt thereof
WO2005026145A2 (en) 2003-09-12 2005-03-24 Warner-Lambert Company Llc Quinolone antibacterial agents
WO2005026165A1 (en) 2003-09-12 2005-03-24 Warner-Lambert Company Llc Quinolone antibacterial agents
DE10343098A1 (de) * 2003-09-18 2005-04-14 Bayer Healthcare Ag Tetrahydrochinoxaline und ihre Verwendung
WO2005049602A1 (en) 2003-11-18 2005-06-02 Warner-Lambert Company Llc Quinolone antibacterial agents
EP1709045A1 (en) 2003-12-09 2006-10-11 Vertex Pharmaceuticals Incorporated Naphthyridine derivatives and their use as modulators of muscarinic receptors
NZ551128A (en) * 2004-05-20 2010-03-26 Diamedica Inc Use of hepatic parasympathetic tone modulator and diabetes drug combinations for treating insulin resistance
AR057555A1 (es) * 2005-10-27 2007-12-05 Merck Frosst Canada Ltd Un inhibidor de fosfodiesterasa-4 4-oxo-1-(3-sustituido fenil-1,4-dihidro-1,8-naftiridin-3-carboxamida y un procedimiento de preparacion del mismo
CN101411705B (zh) * 2007-10-17 2011-06-01 北京赛德维康医药研究院 用于防治动脉粥样硬化的药物组合物
WO2010093341A1 (en) 2009-02-10 2010-08-19 Janssen Pharmaceutica N.V. C-7 isoxazolinyl quinolone/naphthyridine derivatives useful as antibacterial agents
EA022494B1 (ru) 2009-12-17 2016-01-29 Мерк Шарп Энд Домэ Корп. Соединения хинолинамида в качестве положительных аллостерических модуляторов мускаринового рецептора m1
US20130289019A1 (en) * 2012-04-26 2013-10-31 Amazing Grace, Inc. Methods of treating behaviorial and/or mental disorders
CN103183676B (zh) * 2013-03-12 2015-04-08 中国医学科学院医药生物技术研究所 一组1-取代-1,8萘啶甲酰胺衍生物及制备和应用
GB201409044D0 (en) 2014-05-21 2014-07-02 Ucl Business Plc New compounds
SG11201703199UA (en) 2014-11-03 2017-05-30 Bayer Pharma AG Hydroxyalkyl-substituted phenyltriazole derivatives and uses thereof
MX2017016013A (es) 2015-06-09 2018-04-20 Je Il Pharmaceutical Co Ltd Compuesto derivativo triciclico, metodo para prepararlo y composicion farmaceutica que comprende el mismo.
LT3307734T (lt) 2015-06-09 2020-05-11 Abbvie Inc. Branduolinio receptoriaus moduliatoriai (ror), skirti uždegiminių ir autoimuninių ligų gydymui
JP2019524722A (ja) 2016-07-11 2019-09-05 バイエル・ファルマ・アクティエンゲゼルシャフト 7−置換1−ピリジル−ナフチリジン−3−カルボン酸アミドおよびその使用
JOP20190045A1 (ar) 2016-09-14 2019-03-14 Bayer Ag مركبات أميد حمض 1- أريل-نفثيريدين-3-كربوكسيليك مستبدلة في الموضع 7 واستخدامها.

Also Published As

Publication number Publication date
EP3692991A1 (de) 2020-08-12
US10435403B2 (en) 2019-10-08
BR112017026561A2 (pt) 2018-08-14
ZA201800125B (en) 2019-07-31
CU20170158A7 (es) 2018-06-05
AU2016274433A1 (en) 2018-01-04
IL256119A (en) 2018-02-28
CL2017003124A1 (es) 2018-06-01
DOP2017000288A (es) 2018-01-31
CA2988468A1 (en) 2016-12-15
NI201700154A (es) 2018-10-19
TN2017000498A1 (en) 2019-04-12
MX2017016055A (es) 2018-02-21
HK1254348A1 (zh) 2019-07-19
JP6908536B2 (ja) 2021-07-28
IL272017A (en) 2020-02-27
WO2016198342A1 (de) 2016-12-15
JP2018516970A (ja) 2018-06-28
US20190367516A1 (en) 2019-12-05
EP3307741A1 (de) 2018-04-18
CO2017012622A2 (es) 2018-03-28
KR20180016485A (ko) 2018-02-14
CR20170566A (es) 2018-03-20
PH12017502224A1 (en) 2018-06-04
UY36714A (es) 2016-12-30
AU2016274433B2 (en) 2020-07-16
ECSP17081322A (es) 2018-01-31
EP3307741B1 (de) 2020-10-28
EA201890002A1 (ru) 2018-04-30
SG11201710164QA (en) 2018-01-30
CN107949562A (zh) 2018-04-20
CN107949562B (zh) 2021-07-23
TW201716405A (zh) 2017-05-16
EA035465B1 (ru) 2020-06-22
US20180297994A1 (en) 2018-10-18
MX370113B (es) 2019-12-02

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