PE20170664A1 - Agonistas del receptor de apelina(apj) y usos de los mismos - Google Patents

Agonistas del receptor de apelina(apj) y usos de los mismos

Info

Publication number
PE20170664A1
PE20170664A1 PE2016002511A PE2016002511A PE20170664A1 PE 20170664 A1 PE20170664 A1 PE 20170664A1 PE 2016002511 A PE2016002511 A PE 2016002511A PE 2016002511 A PE2016002511 A PE 2016002511A PE 20170664 A1 PE20170664 A1 PE 20170664A1
Authority
PE
Peru
Prior art keywords
alkyl
apj
apeline
same
receptor agonists
Prior art date
Application number
PE2016002511A
Other languages
English (en)
Inventor
Rangan Maitra
James Barnwel Thomas
Scott P Runyon
Sanju Narayanan
Original Assignee
Res Triangle Inst
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 Res Triangle Inst filed Critical Res Triangle Inst
Publication of PE20170664A1 publication Critical patent/PE20170664A1/es

Links

Classifications

    • 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic 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
    • A61K31/42—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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61P1/16—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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/28—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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 containing two hetero rings
    • C07D405/12—Heterocyclic 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 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)

Abstract

Se refiere a un compuesto de formula I, donde: R1 es fenilo sustituido; R2 es alquilo C1-C8, heteroarilo, entre otros; R3 es alquilo C1-C8, alquil C1-C8-cicloalquil C3-C8 o cicloalquil C3-C8; R4, R5 y R6 son independientemente adamantanilo, arilo, alquilo C1-C8, entre otros; Z es H2 u =O. Son compuestos preferidos: acido (S)-2-ciclohexil-2-(5-(2,6-dimetoxifenil)-1-(4-fluorofenil)-1H-pirazol-3-carboxamido)acetico; acido (S)-3-(5-(2,6-dimetoxifenil)1-(4-fluorofenil)-1H-pirazol-3-carboxamido)-5-metilhexanoico; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son agonistas del receptor de apelina (APJ), siendo utiles en el tratamiento de asma, cardiomiopatia, diabetes, entre otros
PE2016002511A 2014-06-06 2015-06-05 Agonistas del receptor de apelina(apj) y usos de los mismos PE20170664A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462008688P 2014-06-06 2014-06-06
PCT/US2015/034427 WO2015188073A1 (en) 2014-06-06 2015-06-05 Apelin receptor (apj) agonists and uses thereof

Publications (1)

Publication Number Publication Date
PE20170664A1 true PE20170664A1 (es) 2017-06-10

Family

ID=53524940

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016002511A PE20170664A1 (es) 2014-06-06 2015-06-05 Agonistas del receptor de apelina(apj) y usos de los mismos

Country Status (15)

Country Link
US (2) US10377718B2 (es)
EP (1) EP3152200A1 (es)
JP (1) JP6767878B2 (es)
KR (1) KR102509043B1 (es)
CN (1) CN106459004B (es)
AU (1) AU2015269247B2 (es)
BR (1) BR112016028119A2 (es)
CA (1) CA2949559C (es)
IL (1) IL248988A0 (es)
MA (1) MA39999A (es)
MX (1) MX2016014890A (es)
PE (1) PE20170664A1 (es)
RU (1) RU2705800C2 (es)
WO (1) WO2015188073A1 (es)
ZA (1) ZA201607850B (es)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170174633A1 (en) * 2014-03-25 2017-06-22 Research Triangle Institute Pyrazole compounds selective for neurotensin 2 receptor
WO2015188073A1 (en) 2014-06-06 2015-12-10 Research Triangle Institute Apelin receptor (apj) agonists and uses thereof
GB201415569D0 (en) 2014-09-03 2014-10-15 C4X Discovery Ltd Therapeutic Compounds
WO2016176473A1 (en) * 2015-04-28 2016-11-03 Sanford-Burnham Medical Researc Institute Apelin receptor agonists and methods of use thereof
HUE050317T2 (hu) 2015-05-20 2020-11-30 Amgen Inc APJ receptor triazol agonistái
AU2016340264B2 (en) * 2015-10-14 2021-01-07 Bristol-Myers Squibb Company 2,4-dihydroxy-nicotinamides as APJ agonists
EP3386976A1 (en) * 2015-12-09 2018-10-17 Research Triangle Institute, International Improved apelin receptor (apj) agonists and uses thereof
WO2017106396A1 (en) * 2015-12-16 2017-06-22 Bristol-Myers Squibb Company Heteroarylhydroxypyrimidinones as agonists of the apj receptor
GB201601703D0 (en) 2016-01-29 2016-03-16 C4X Discovery Ltd Therapeutic compounds
CN109195963B (zh) * 2016-03-24 2021-04-23 百时美施贵宝公司 作为apj激动剂的6-羟基-4-氧代-1，4-二氢嘧啶-5-甲酰胺
EP3452466B1 (en) 2016-05-03 2020-08-12 Amgen Inc. Heterocyclic triazole compounds as agonists of the apj receptor
CN114507217A (zh) * 2016-10-12 2022-05-17 三角研究所 杂环爱帕琳肽受体(apj)激动剂及其用途
EP3526198B1 (en) * 2016-10-14 2020-08-12 Bristol-Myers Squibb Company 3-sulfonyl-5-aminopyridine-2,4-diol apj agonists
KR20190075968A (ko) 2016-10-19 2019-07-01 어바이브, 인크. 심혈관-관련 질환의 치료를 위한 아펠린의 신규 peg화 리포솜 제제
WO2018093579A1 (en) 2016-11-16 2018-05-24 Amgen Inc. Triazole phenyl compounds as agonists of the apj receptor
EP3541805B1 (en) 2016-11-16 2020-10-14 Amgen Inc. Heteroaryl-substituted triazoles as apj receptor agonists
WO2018093576A1 (en) 2016-11-16 2018-05-24 Amgen Inc. Alkyl substituted triazole compounds as agonists of the apj receptor
MA46827A (fr) 2016-11-16 2019-09-25 Amgen Inc Composés de triazole à substitution cycloalkyle en tant qu'agonistes du récepteur apj
WO2018097944A1 (en) 2016-11-16 2018-05-31 Amgen Inc. Triazole furan compounds as agonists of the apj receptor
US10689367B2 (en) 2016-11-16 2020-06-23 Amgen Inc. Triazole pyridyl compounds as agonists of the APJ receptor
WO2018207881A1 (ja) * 2017-05-12 2018-11-15 武田薬品工業株式会社 複素環化合物
US11149040B2 (en) 2017-11-03 2021-10-19 Amgen Inc. Fused triazole agonists of the APJ receptor
US11807624B2 (en) 2018-05-01 2023-11-07 Amgen Inc. Substituted pyrimidinones as agonists of the APJ receptor
JP2022545698A (ja) * 2019-08-29 2022-10-28 リサーチ トライアングル インスティテュート アペリン受容体アゴニストのための方法および使用
KR102278410B1 (ko) 2020-11-17 2021-07-19 주식회사 클레스앤피 개인 건강 상태 동시 측정이 가능한 고성능 딥러닝 지정맥 인증 시스템 및 방법
CA3208025A1 (en) * 2021-02-25 2022-09-01 Scott P. Runyon Heteroaryl derivatives as apelin receptor agonists
US20240041878A1 (en) * 2022-05-31 2024-02-08 BioAge Labs, Inc. Apelin receptor modulators for treatment of a disorder or disease associated with bbb permeability

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5998004A (ja) 1982-11-25 1984-06-06 Kureha Chem Ind Co Ltd １，２，４―トリアゾール誘導体及び除草剤
DE3316300A1 (de) 1982-05-07 1983-11-24 Kureha Kagaku Kogyo K.K., Tokyo Heribizide zusammensetzung mit einem gehalt an einem derivat des 1,2,4-triazols als wirkstoff
JPS58194866A (ja) 1982-05-07 1983-11-12 Kureha Chem Ind Co Ltd トリアゾ−ル誘導体及び該誘導体を含有する除草剤
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5965695A (en) 1990-05-15 1999-10-12 Chiron Corporation Modified peptide and peptide libraries with protease resistance, derivatives thereof and methods of producing and screening such
FR2665898B1 (fr) * 1990-08-20 1994-03-11 Sanofi Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2713225B1 (fr) 1993-12-02 1996-03-01 Sanofi Sa N-pipéridino-3-pyrazolecarboxamide substitué.
FR2692575B1 (fr) * 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
US5994341A (en) 1993-07-19 1999-11-30 Angiogenesis Technologies, Inc. Anti-angiogenic Compositions and methods for the treatment of arthritis
FR2711140B1 (fr) 1993-10-12 1996-01-05 Sanofi Sa 1-Naphtylpyrazole-3-carboxamides substitués actifs sur la neurotensine, leur préparation, les compositions pharmaceutiques en contenant.
FR2732967B1 (fr) 1995-04-11 1997-07-04 Sanofi Sa 1-phenylpyrazole-3-carboxamides substitues, actifs sur la neurotensine, leur preparation, les compositions pharmaceutiques en contenant
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
FR2741621B1 (fr) 1995-11-23 1998-02-13 Sanofi Sa Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant
FR2742148B1 (fr) * 1995-12-08 1999-10-22 Sanofi Sa Nouveaux derives du pyrazole-3-carboxamide, procede pour leur preparation et compositions pharmaceutiques les contenant
FR2757869B1 (fr) 1996-12-31 1999-05-21 Rhodia Chimie Sa Utilisation de melanges a base de pt et de composes de metaux de transition autres que le pt pour ameliorer les proprietes de resistance a l'arc des elastomeres silicones
GB9925962D0 (en) 1999-11-02 1999-12-29 Novartis Ag Organic compounds
DE60201988T2 (de) 2001-05-03 2005-12-15 F. Hoffmann-La Roche Ag Pharmazeutische dosierungsform von amorphem nilfenavir mesylat
CA2446904A1 (en) 2001-05-24 2003-04-03 Alexza Molecular Delivery Corporation Delivery of drug esters through an inhalation route
TWI231757B (en) 2001-09-21 2005-05-01 Solvay Pharm Bv 1H-Imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity
US7109216B2 (en) 2001-09-21 2006-09-19 Solvay Pharmaceuticals B.V. 1H-imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity
AR036608A1 (es) 2001-09-24 2004-09-22 Bayer Corp Derivados de imidazol, composiciones farmaceuticas y el uso de dichos derivados para la fabricacion de un medicamento para el tratamiento de la obesidad
AR038967A1 (es) 2002-03-18 2005-02-02 Solvay Pharm Bv Derivados de 2,3 - diaril - pirazolidinas como inhibidores de enzimas que degradan la neurotensina
US7319110B2 (en) 2002-09-19 2008-01-15 Solvay Pharmaceuticals B.V. 1H-1,2,4-triazole-3-carboxamide derivatives having cannabinoid-CB1 receptor agonistic, partial agonistic, inverse agonistic or antagonistic activity
WO2005054204A2 (en) * 2003-11-26 2005-06-16 Synchrony Biosciences, Inc. Pharmaceutical compounds that regenerate in vivo
TW200526641A (en) 2003-12-26 2005-08-16 Daiichi Seiyaku Co Amidopyrazole derivatives
WO2005099705A2 (en) 2004-03-24 2005-10-27 Bayer Pharmaceuticals Corporation Preparation of imidazole derivatives and methods of use
US20060094744A1 (en) 2004-09-29 2006-05-04 Maryanoff Cynthia A Pharmaceutical dosage forms of stable amorphous rapamycin like compounds
EP1803719A4 (en) 2004-10-19 2008-07-02 Daiichi Seiyaku Co 1,5-DIHETEROCYCLUS-1H-triazole
CA2598043A1 (en) * 2005-02-25 2006-08-31 Rigel Pharmaceuticals, Inc. Benzisothiazoles useful for treating or preventing hcv infection
US20080200527A1 (en) * 2005-06-17 2008-08-21 Carex Sa Cannabinoid Receptor Modulators
EP1993560B1 (en) 2006-03-10 2011-12-28 Jenrin Discovery Cannabinoid receptor antagonists/inverse agonists useful for treating obesity
EP1903052A3 (en) 2006-07-28 2008-04-02 Faust Pharmaceuticals SA APJ receptor ligands and uses thereof
US20100256357A1 (en) 2006-08-09 2010-10-07 Agouron Pharmaceuticals, Inc. Heterocycles useful as inhibitors of carbonic anhydrase
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
JP5464395B2 (ja) 2008-02-01 2014-04-09 大陽日酸株式会社 重水素化された芳香環又は複素環を有する化合物の製造方法
WO2009154754A2 (en) 2008-06-17 2009-12-23 Concert Pharmaceuticals, Inc. Synthesis of deuterated morpholine derivatives
WO2010033511A1 (en) 2008-09-16 2010-03-25 Concert Pharmaceuticals, Inc. Deuterated 2-amino-3-hydroxypropanoic acid derivatives
JP2012507523A (ja) 2008-11-04 2012-03-29 アンカー セラピューティクス，インコーポレイテッド Ａｐｊ受容体化合物
CN101519430A (zh) 2009-03-20 2009-09-02 中国农业大学 一类新型保幼激素合成抑制剂－苯丙-甘-亮三肽酰胺类似物
US8343976B2 (en) * 2009-04-20 2013-01-01 Institute For Oneworld Health Compounds, compositions and methods comprising pyrazole derivatives
WO2011005052A2 (en) 2009-07-10 2011-01-13 Green Gross Corporation Novel arylpiperazine-containing imidazole 4-carboxamide derivatives and pharmaceutical composition comprising same
DE102009036604A1 (de) * 2009-07-30 2011-02-03 Aicuris Gmbh & Co. Kg Substituierte Bis-Arylpyrazolamide mit terminaler primärer Amidfunktionalisierung und ihre Verwendung
WO2011156557A2 (en) * 2010-06-11 2011-12-15 Thomas James B Compounds active at the neurotensin receptor
WO2012014204A1 (en) * 2010-07-27 2012-02-02 Joma International As Components of photovoltaic cells, cells constructed therefrom and related manufacturing processes
RU2013156864A (ru) 2011-05-23 2015-06-27 Санофи Способ получения дейтерированных соединений, содержащих n-алкильные группы
CA2835216A1 (en) * 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
PT2736888E (pt) 2011-07-26 2016-02-17 Sanofi Sa Derivados do ácido 3-heteroaroilamino-propiónico e o seu uso como produtos farmacêuticos
WO2013079223A1 (en) 2011-12-02 2013-06-06 Phenex Pharmaceuticals Ag Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rorϒ, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases
JP2013231000A (ja) * 2012-04-27 2013-11-14 Dainippon Sumitomo Pharma Co Ltd ３−アミノメチルピラゾール誘導体
EP2855440A1 (en) 2012-05-31 2015-04-08 Phenex Pharmaceuticals AG Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ror[gamma]
JO3215B1 (ar) * 2012-08-09 2018-03-08 Phenex Pharmaceuticals Ag حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy
IN2015DN01662A (es) 2012-09-18 2015-07-03 Auspex Pharmaceuticals Inc
LT2897939T (lt) * 2012-09-21 2017-05-10 Sanofi Benzimidazolo karboksirūgšties amido dariniai metabolinių arba širdies ir kraujagyslių ligų gydymui
WO2014053533A1 (en) 2012-10-05 2014-04-10 Sanofi Use of substituted 3-heteroaroylamino-propionic acid derivatives as pharmaceuticals for prevention/treatment of atrial fibrillation
WO2014100431A1 (en) 2012-12-20 2014-06-26 Concert Pharmaceuticals, Inc. Deuterated alk inhibitors
EP3401314B1 (en) 2013-03-15 2023-11-08 Araxes Pharma LLC Covalent inhibitors of kras g12c
EP2984098A2 (en) 2013-04-12 2016-02-17 Achillion Pharmaceuticals, Inc. Deuterated nucleoside prodrugs useful for treating hcv
DK3057953T3 (en) 2013-10-17 2018-11-19 Vertex Pharma CO CRYSTALS OF (S) -N-METHYL-8- (1 - ((2'-METHYL- [4,5'-BIPYRIMIDIN] -6-YL) AMINO) PROPAN-2-YL) QUINOLIN-4-CARBOXAMIDE AND DEUTERATED DERIVATIVES THEREOF AS DNA-PK INHIBITORS
US20170174633A1 (en) 2014-03-25 2017-06-22 Research Triangle Institute Pyrazole compounds selective for neurotensin 2 receptor
US10570128B2 (en) 2014-05-28 2020-02-25 Sanford Burnham Prebys Medical Discovery Institute Agonists of the apelin receptor and methods of use thereof
WO2015188073A1 (en) 2014-06-06 2015-12-10 Research Triangle Institute Apelin receptor (apj) agonists and uses thereof
EP3386976A1 (en) 2015-12-09 2018-10-17 Research Triangle Institute, International Improved apelin receptor (apj) agonists and uses thereof
CN114507217A (zh) 2016-10-12 2022-05-17 三角研究所 杂环爱帕琳肽受体(apj)激动剂及其用途
JPWO2018101398A1 (ja) 2016-12-01 2019-11-07 宇司 永石 炎症性腸疾患の治療方法およびそれに用いるための医薬組成物

Also Published As

Publication number Publication date
JP2017523126A (ja) 2017-08-17
MX2016014890A (es) 2017-05-01
EP3152200A1 (en) 2017-04-12
RU2016144329A3 (es) 2018-11-23
JP6767878B2 (ja) 2020-10-14
KR20170012305A (ko) 2017-02-02
IL248988A0 (en) 2017-01-31
CN106459004B (zh) 2020-09-15
RU2016144329A (ru) 2018-07-11
MA39999A (fr) 2015-12-10
US20160207889A1 (en) 2016-07-21
US11401244B2 (en) 2022-08-02
AU2015269247B2 (en) 2019-10-24
CA2949559A1 (en) 2015-12-10
BR112016028119A2 (pt) 2017-08-22
US10377718B2 (en) 2019-08-13
ZA201607850B (en) 2018-05-30
WO2015188073A1 (en) 2015-12-10
US20190315693A1 (en) 2019-10-17
CA2949559C (en) 2023-08-29
CN106459004A (zh) 2017-02-22
RU2705800C2 (ru) 2019-11-12
AU2015269247A1 (en) 2016-12-01
KR102509043B1 (ko) 2023-03-09

Similar Documents

Publication Publication Date Title
PE20170664A1 (es) Agonistas del receptor de apelina(apj) y usos de los mismos
PE20210642A1 (es) Inhibidores de pd-1/pd-l1
CO2017002714A2 (es) Ácido 4-(3-fluoro-3-(2-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)etil)pirrolidin-1-il)-3-(3-(2-metoxietoxi)fenil)butanoico, o una sal del mismo
PE20181269A1 (es) Agonistas del receptor de apelina y metodos de uso
PH12016502154A1 (en) Pyridazonine herbicides
PE20170695A1 (es) Compuestos de indol carboxamida utiles como inhibidores de cinasas
PE20170947A1 (es) 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1
PE20180175A1 (es) Nuevos derivados de imidazolilmetilo 5-sustituidos
PE20161396A1 (es) Compuesto heterociclico
EA201791002A1 (ru) Новые соединения, модулирующие fxr (nr1h4)
PE20180508A1 (es) Amidas heterociclicas como inhibidores de quinasa
PE20161225A1 (es) 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer
PE20160874A1 (es) Compuestos quimicos
PE20140192A1 (es) Derivados de bencimidazol como inhibidores de cinasa pi3
PE20180024A1 (es) Triazolopirazinonas como inhibidores de pde1
PE20142185A1 (es) Pirrolidina-2-carboxamidas sustituidas
PE20151274A1 (es) Inhibidores de erk y sus usos
PE20160521A1 (es) Inhibidores de autotaxina que comprenden un nucleo ciclico de anillo heteroaromatico-bencil-amida
PE20141682A1 (es) Derivados de (4-fenilimidazol-2-il) etilamina utiles como moduladores de canal de sodio
PE20191020A1 (es) Compuestos quimicos
TN2018000020A1 (en) Colony stimulating factor-1 receptor (csf-1r) inhibitors.
PE20141167A1 (es) Piridopirazinas sustituidas como inhibidores novedosos de ptk
PE20170186A1 (es) Nuevos compuestos
PE20161363A1 (es) Moduladores del receptor acoplado a la proteina g40 (gpr40) de pirrolidina para el tratamiento de enfermedades como la diabetes
CL2020002588A1 (es) Compuestos derivados de indol, composiciones que los contienen, útiles en el tratamiento de infestación por helmintos, preferentemente trematodos, en mamíferos. (divisional de solicitud n° 03258-2016)