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MX2015001115A - Derivativos de piperidina fusionados con espiro para usarse como inhibidores del canal de potasio medular externo renal. - Google Patents

Derivativos de piperidina fusionados con espiro para usarse como inhibidores del canal de potasio medular externo renal.

Info

Publication number
MX2015001115A
MX2015001115A MX2015001115A MX2015001115A MX2015001115A MX 2015001115 A MX2015001115 A MX 2015001115A MX 2015001115 A MX2015001115 A MX 2015001115A MX 2015001115 A MX2015001115 A MX 2015001115A MX 2015001115 A MX2015001115 A MX 2015001115A
Authority
MX
Mexico
Prior art keywords
inhibitors
spiro
potassium channel
piperidine derivatives
outer medullary
Prior art date
Application number
MX2015001115A
Other languages
English (en)
Other versions
MX365986B (es
Inventor
Yang Yu
Alexander Pasternak
Jinlong Jiang
Takao Suzuki
Haifeng Tang
Xin Gu
Zhicai Wu
Shuzhi Dong
Fa-Xiang Ding
Jessica Frie
Original Assignee
Merck Sharp & Dohme
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
Priority claimed from PCT/CN2012/079184 external-priority patent/WO2014015495A1/en
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of MX2015001115A publication Critical patent/MX2015001115A/es
Publication of MX365986B publication Critical patent/MX365986B/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20Spiro-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
    • 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring 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
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/4995Pyrazines or piperazines forming part of bridged ring 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
    • A61K31/535Heterocyclic 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
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P7/10Antioedematous agents; Diuretics
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    • 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
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
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    • 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
    • C07D471/10Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención proporciona compuestos de Fórmula I (ver Fórmula) y las sales farmacéuticamente aceptables del mismo, que son inhibidores del canal de ROMK (Kir1.1); los compuestos se pueden usar como agentes diuréticos y/o natriuréticos y para la terapia y la profilaxis de afecciones médicas que incluyen enfermedades cardiovasculares tales como hipertensión, insuficiencia cardíaca y afecciones asociadas con excesiva retención de sal y agua.
MX2015001115A 2012-07-26 2013-07-25 Derivativos de piperidina fusionados con espiro para usarse como inhibidores del canal de potasio medular externo renal. MX365986B (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
PCT/CN2012/079184 WO2014015495A1 (en) 2012-07-26 2012-07-26 Inhibitors of the renal outer medullary potassium channel
US201261691390P 2012-08-21 2012-08-21
US201361759040P 2013-01-31 2013-01-31
PCT/US2013/052079 WO2014018764A1 (en) 2012-07-26 2013-07-25 Spiro - fused piperidine derivatives for use as inhibitors of the renal outer medullary potassium channel

Publications (2)

Publication Number Publication Date
MX2015001115A true MX2015001115A (es) 2015-04-08
MX365986B MX365986B (es) 2019-06-20

Family

ID=48916271

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015001115A MX365986B (es) 2012-07-26 2013-07-25 Derivativos de piperidina fusionados con espiro para usarse como inhibidores del canal de potasio medular externo renal.

Country Status (14)

Country Link
US (2) US8952166B2 (es)
EP (1) EP2877471B1 (es)
JP (1) JP6166783B2 (es)
KR (1) KR20150036142A (es)
CN (1) CN104540826B (es)
AR (1) AR092031A1 (es)
AU (1) AU2013295722B2 (es)
BR (1) BR112015001419A8 (es)
CA (1) CA2876508A1 (es)
ES (1) ES2606016T3 (es)
MX (1) MX365986B (es)
RU (1) RU2642066C2 (es)
TW (1) TW201410675A (es)
WO (1) WO2014018764A1 (es)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9073882B2 (en) 2010-10-27 2015-07-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9056859B2 (en) 2010-10-29 2015-06-16 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
RU2014110401A (ru) 2011-08-19 2015-09-27 Мерк Шарп И Доум Корп. Ингибиторы внешнего медуллярного калиевого канала почек
US9527830B2 (en) 2011-09-16 2016-12-27 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2771005B1 (en) 2011-10-25 2016-05-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013062900A1 (en) 2011-10-25 2013-05-02 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9139585B2 (en) 2011-10-31 2015-09-22 Merck Sharp & Dohme Corp. Inhibitors of the Renal Outer Medullary Potassium channel
EP2773206B1 (en) 2011-10-31 2018-02-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9493474B2 (en) 2011-10-31 2016-11-15 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2790511B1 (en) 2011-12-16 2016-09-14 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2925322B1 (en) 2012-11-29 2018-10-24 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9573961B2 (en) 2012-12-19 2017-02-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2014126944A2 (en) 2013-02-18 2014-08-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9765074B2 (en) 2013-03-15 2017-09-19 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP3027625B1 (en) 2013-07-31 2018-05-30 Merck Sharp & Dohme Corp. Spiro-fused derivatives of piperidine useful for the treatment of inter alia hypertension and acute or chronic heart failure
WO2015065866A1 (en) 2013-10-31 2015-05-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2015103756A1 (en) * 2014-01-09 2015-07-16 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2016008064A1 (en) * 2014-07-14 2016-01-21 Merck Sharp & Dohme Corp. Inhibitors of renal outer medullary potassium channel
CN106488912A (zh) * 2014-07-14 2017-03-08 默沙东公司 肾外髓质钾通道的抑制剂
SG11201701315VA (en) 2014-08-28 2017-03-30 Asceneuron Sa Glycosidase inhibitors
US20170275302A1 (en) * 2014-10-14 2017-09-28 Alexander Pasternak Inhibitors of the renal outer medullary potassium channel
WO2016065582A1 (en) * 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2016065603A1 (en) 2014-10-31 2016-05-06 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2016065602A1 (en) 2014-10-31 2016-05-06 Merck Sharp & Dohme Corp. Inhibitors of renal outer medullary potassium channel
WO2016069428A1 (en) * 2014-10-31 2016-05-06 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
CA2966788A1 (en) 2014-12-08 2016-06-16 Shanghai Hengrui Pharmaceutical Co., Ltd. Pyridinecarboxamide derivatives, preparation method therefor and pharmaceutical uses thereof
US10513518B2 (en) * 2015-01-29 2019-12-24 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2016127358A1 (en) 2015-02-12 2016-08-18 Merck Sharp & Dohme Corp. Inhibitors of renal outer medullary potassium channel
US11261183B2 (en) 2016-02-25 2022-03-01 Asceneuron Sa Sulfoximine glycosidase inhibitors
MX381953B (es) 2016-02-25 2025-03-13 Asceneuron S A Sales de derivados de piperazina obtenidas por adicion de acidos.
AU2017222958B2 (en) 2016-02-25 2019-07-18 Asceneuron S. A. Glycosidase inhibitors
US10851108B2 (en) 2016-04-20 2020-12-01 Bristol-Myers Squibb Company Substituted bicyclic heterocyclic compounds
KR20190015305A (ko) * 2016-06-07 2019-02-13 지앙수 헨그루이 메디슨 컴퍼니 리미티드 신장 외수질 칼륨 채널 억제제로서 약학적으로 허용 가능한 염
PE20190503A1 (es) 2016-08-01 2019-04-10 Aptinyx Inc Moduladores del receptor nmda espiro-lactam y uso de los mismos
BR112019001921A2 (pt) 2016-08-01 2019-05-14 Aptinyx Inc. moduladores do receptor nmda de espiro-lactama e seus usos
MX388786B (es) 2016-08-01 2025-03-20 Aptinyx Inc Moduladores nmda espiro-lactam y métodos de uso de los mismos.
CN106432214B (zh) * 2016-08-09 2019-05-07 成都拿盛科技有限公司 一种制备romk通道抑制剂中间体的方法
US10723723B2 (en) 2016-11-03 2020-07-28 Bristol-Myers Squibb Company Substituted bicycle heterocyclic derivatives useful as ROMK channel inhibitors
DK3630752T3 (da) 2017-06-01 2021-08-09 Bristol Myers Squibb Co Substituerede nitrogenholdige forbindelser
CN107569495A (zh) * 2017-08-10 2018-01-12 新疆医科大学 依普利酮对慢性心力衰竭患者辅助性t细胞活化/增殖的抑制作用
BR112020011161A2 (pt) * 2017-12-06 2020-11-17 Jiangsu Hengrui Medicine Co., Ltd. forma cristalina de um inibidor de canal medular renal externo, composição farmacêutica que a compreende, método de preparação da referida forma cristalina e composição farmacêutica e uso das mesmas
CN109879863B (zh) * 2017-12-06 2020-10-20 江苏恒瑞医药股份有限公司 一种肾外髓质分泌钾通道抑制剂的晶型及其制备方法
WO2019152687A1 (en) 2018-01-31 2019-08-08 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
US11731972B2 (en) * 2018-08-22 2023-08-22 Asceneuron Sa Spiro compounds as glycosidase inhibitors
BR112021003022A2 (pt) 2018-08-22 2021-05-11 Asceneuron Sa sais de adição de ácido de ácido succínico ou ácido fumárico, de ácido monossuccínico, de ácido monofumárico e de adição de ácido succínico ou sal de adição de ácido fumárico, métodos para preparar um sal de adição de ácido do ácido succínico ou ácido fumárico, para tratar uma tauopatia e para inibir uma glicosidase, e, forma de dosagem oral sólida
WO2020039028A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Tetrahydro-benzoazepine glycosidase inhibitors
US12016852B2 (en) 2018-08-22 2024-06-25 Asceneuron Sa Pyrrolidine glycosidase inhibitors
CN110669031B (zh) * 2019-11-26 2021-04-16 青岛海洋生物医药研究院股份有限公司 天然产物异猴头菌酮j的全合成方法

Family Cites Families (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2988551A (en) 1954-07-30 1961-06-13 Union Chimique Belge Sa Piperazine derivatives
GB949088A (en) 1961-06-26 1964-02-12 Lepetit Spa Diazabicyclo-octane derivatives
US3435002A (en) 1967-05-15 1969-03-25 Gen Electric Polyamide acid resins and polyimides therefrom
GB1575310A (en) 1976-11-16 1980-09-17 Anphar Sa Piperidine derivatives
FR2522325B1 (fr) 1982-02-26 1985-08-09 Delalande Sa Nouveaux derives aryliques de la piperazine, de l'homopiperazine et de n,n'-dialkyl diamino-1,2 ethane, leur procede de preparation et leur application en therapeutique
NL8202636A (nl) 1982-06-29 1984-01-16 Gist Brocades Nv Piperazinederivaten, werkwijzen ter bereiding daarvan en farmaceutische preparaten die deze verbindingen bevatten.
US5145885A (en) 1983-08-15 1992-09-08 Ciba-Geigy Corporation Photopolymerizable compositions containing aminoaryl ketone photoinitiators
EP0138754B1 (de) 1983-08-15 1988-05-25 Ciba-Geigy Ag Photohärtbare Gemische
US4579863A (en) 1983-12-06 1986-04-01 Warner-Lambert Company Substituted trans-1,2-diaminocyclohexyl amide compounds
US4661607A (en) 1984-09-21 1987-04-28 Chugai Seiyaku Kabushiki Kaisha Furoxanthone derivatives useful as diuretics
US4845079A (en) 1985-01-23 1989-07-04 Luly Jay R Peptidylaminodiols
US5066643A (en) 1985-02-19 1991-11-19 Sandoz Ltd. Fluorine and chlorine statine or statone containing peptides and method of use
US4894437A (en) 1985-11-15 1990-01-16 The Upjohn Company Novel renin inhibiting polypeptide analogs containing S-aryl-D- or L- or DL-cysteinyl, 3-(arylthio)lactic acid or 3-(arylthio)alkyl moieties
US4885292A (en) 1986-02-03 1989-12-05 E. R. Squibb & Sons, Inc. N-heterocyclic alcohol renin inhibitors
GB8603120D0 (en) 1986-02-07 1986-03-12 Pfizer Ltd Anti-dysrhythmia agents
US4980283A (en) 1987-10-01 1990-12-25 Merck & Co., Inc. Renin-inhibitory pepstatin phenyl derivatives
US5089471A (en) 1987-10-01 1992-02-18 G. D. Searle & Co. Peptidyl beta-aminoacyl aminodiol carbamates as anti-hypertensive agents
US5034512A (en) 1987-10-22 1991-07-23 Warner-Lambert Company Branched backbone renin inhibitors
US5063207A (en) 1987-10-26 1991-11-05 Warner-Lambert Company Renin inhibitors, method for using them, and compositions containing them
US5055466A (en) 1987-11-23 1991-10-08 E. R. Squibb & Sons, Inc. N-morpholino derivatives and their use as anti-hypertensive agents
US5036054A (en) 1988-02-11 1991-07-30 Warner-Lambert Company Renin inhibitors containing alpha-heteroatom amino acids
US5036053A (en) 1988-05-27 1991-07-30 Warner-Lambert Company Diol-containing renin inhibitors
DE3841520A1 (de) 1988-12-09 1990-06-13 Hoechst Ag Enzymhemmende harnstoffderivate von dipeptiden, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung
US5106835A (en) 1988-12-27 1992-04-21 American Cyanamid Company Renin inhibitors
US5063208A (en) 1989-07-26 1991-11-05 Abbott Laboratories Peptidyl aminodiol renin inhibitors
US5098924A (en) 1989-09-15 1992-03-24 E. R. Squibb & Sons, Inc. Diol sulfonamide and sulfinyl renin inhibitors
US5104869A (en) 1989-10-11 1992-04-14 American Cyanamid Company Renin inhibitors
US5114937A (en) 1989-11-28 1992-05-19 Warner-Lambert Company Renin inhibiting nonpeptides
US5215989A (en) 1989-12-08 1993-06-01 Merck & Co., Inc. Nitrogen-containing heterocyclic compounds as class III antiarrhythmic agents
US5064965A (en) 1990-03-08 1991-11-12 American Home Products Corporation Renin inhibitors
US5095119A (en) 1990-03-08 1992-03-10 American Home Products Corporation Renin inhibitors
US5075451A (en) 1990-03-08 1991-12-24 American Home Products Corporation Pyrrolimidazolones useful as renin inhibitors
US5071837A (en) 1990-11-28 1991-12-10 Warner-Lambert Company Novel renin inhibiting peptides
FR2673182A1 (fr) 1991-02-22 1992-08-28 Univ Caen Piperazines n,n'-disubstituees, leur procede de preparation et leur application en therapeutique.
ATE197047T1 (de) 1993-07-28 2000-11-15 Santen Pharmaceutical Co Ltd 1,4-di(phenylalkyl)piperazinderivate
US5614526A (en) 1995-06-09 1997-03-25 Hoffmann-La Roche Inc. Use of phenoxy-piperzine derivatives
DE69709647T2 (de) 1996-05-20 2002-11-07 Dupont Pharmaceuticals Research Laboratories, Inc. Cyclischer diarylalkyl diaminederivate als antogoniste von chemokinerezeptoren
DE19637237A1 (de) 1996-09-13 1998-03-19 Merck Patent Gmbh Piperazin-Derivate
JPH10203986A (ja) 1997-01-22 1998-08-04 Mitsubishi Chem Corp 眼疾患用薬剤
WO2000051611A1 (en) 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
EP1094063A1 (en) 1999-10-18 2001-04-25 Applied Research Systems ARS Holding N.V. 9-(Piperazinylalkyl)carbazoles as Bax-modulators
WO2002000631A2 (en) 2000-06-29 2002-01-03 Fujisawa Pharmaceutical Co., Ltd. Benzhydryl derivatives
US6352158B1 (en) 2000-07-06 2002-03-05 Warner Lambert Company Unit dose blister package with keyhole assisted opening feature
US6693099B2 (en) 2000-10-17 2004-02-17 The Procter & Gamble Company Substituted piperazine compounds optionally containing a quinolyl moiety for treating multidrug resistance
GB0031088D0 (en) 2000-12-20 2001-01-31 Smithkline Beecham Plc Medicaments
CN1172919C (zh) 2002-06-03 2004-10-27 上海医药工业研究院 芳烷醇哌嗪衍生物及其在制备抗抑郁症药物中的应用
GB0220214D0 (en) 2002-08-30 2002-10-09 Novo Pharmaceuticals De Ltd Compounds and their use
US20040204404A1 (en) 2002-09-30 2004-10-14 Robert Zelle Human N-type calcium channel blockers
AU2003275632A1 (en) 2002-10-25 2004-05-13 Mitsubishi Pharma Corporation N-oxide compounds
US7831263B2 (en) 2002-11-08 2010-11-09 Qualcomm Incorporated Apparatus and method for determining the location of a repeater
JPWO2004046110A1 (ja) 2002-11-15 2006-03-16 アステラス製薬株式会社 メラニン凝集ホルモン受容体拮抗剤
DE10329457A1 (de) 2003-04-03 2005-01-20 Merck Patent Gmbh Ethinylprolinderivate
BRPI0408444A (pt) 2003-04-03 2006-04-04 Merck Patent Gmbh derivados de 1-n-(fenil)-2-n-(fenil) pirazolidina-1,2-dicarboxamida como inibidores de fator xa de coagulação para o tratamento de trombose
DE502004009440D1 (de) 2003-04-03 2009-06-10 Merck Patent Gmbh Pyrrolidin-1,2-dicarbonsäure-1-(phenylamid)-2-(4-(3-oxo-morpholin-4-yl)-phenylamid) derivate und verwandte verbindungen als inhibitoren des koagulationsfaktors xa zur behandlung von thromboembolischen erkrankungen
US7557222B2 (en) 2003-06-18 2009-07-07 Merck Patent Gmbh 1-[(4-Ethynylphenyl)]-2-[(phenyl)]-pyrrolidine-1,2-dicarboxamide derivatives as inhibitors of coagulation factors Xa and VIIa for the treatment of thrombosis
US7514438B2 (en) 2003-08-13 2009-04-07 Amgen, Inc. Melanin concentrating hormone receptor antagonist
CN1897950A (zh) 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
PL1716147T3 (pl) * 2004-01-08 2008-03-31 Hoffmann La Roche Pochodne diazaspiropiperydyny jako inhibitory transportera 1 glicyny i transportera 2 glicyny
CA2580845A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
DE102004045796A1 (de) 2004-09-22 2006-03-23 Merck Patent Gmbh Arzneimittel enthaltend Carbonylverbindungen sowie deren Verwendung
DE102004047254A1 (de) 2004-09-29 2006-04-13 Merck Patent Gmbh Carbonylverbindungen
WO2006098342A1 (en) 2005-03-16 2006-09-21 Astellas Pharma Inc. Piperazinyl compounds
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
US7754724B2 (en) 2005-06-30 2010-07-13 Dow Agrosciences Llc N-substituted piperazines
ES2625378T3 (es) 2005-09-27 2017-07-19 Shionogi & Co., Ltd. Derivado de sulfonamida que tiene actividad antagonista del receptor de PGD2
MX2008008337A (es) 2005-12-21 2008-09-03 Schering Corp Fenoxipiperidinas y sus analogos utiles como antagonistas de histamina h3.
WO2008147864A2 (en) 2007-05-22 2008-12-04 Xenon Pharmaceuticals Inc. Methods of using piperazine compounds in treating sodium channel-mediated diseases or conditions
JP2011522843A (ja) 2008-06-13 2011-08-04 バイオノミクス リミテッド 新規なカリウムチャンネルブロッカー及びその使用
US8673920B2 (en) 2009-05-06 2014-03-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9073882B2 (en) 2010-10-27 2015-07-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9056859B2 (en) * 2010-10-29 2015-06-16 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
RU2014110401A (ru) 2011-08-19 2015-09-27 Мерк Шарп И Доум Корп. Ингибиторы внешнего медуллярного калиевого канала почек
US9527830B2 (en) 2011-09-16 2016-12-27 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2771005B1 (en) 2011-10-25 2016-05-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013062900A1 (en) 2011-10-25 2013-05-02 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2773206B1 (en) 2011-10-31 2018-02-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9493474B2 (en) 2011-10-31 2016-11-15 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9139585B2 (en) 2011-10-31 2015-09-22 Merck Sharp & Dohme Corp. Inhibitors of the Renal Outer Medullary Potassium channel
EP2790511B1 (en) 2011-12-16 2016-09-14 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel

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US9206198B2 (en) 2015-12-08
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