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PE20090891A1 - Profarmacos dipeptoides como agonistas de los receptores de adenosina a1 - Google Patents

Profarmacos dipeptoides como agonistas de los receptores de adenosina a1

Info

Publication number
PE20090891A1
PE20090891A1 PE2008001244A PE2008001244A PE20090891A1 PE 20090891 A1 PE20090891 A1 PE 20090891A1 PE 2008001244 A PE2008001244 A PE 2008001244A PE 2008001244 A PE2008001244 A PE 2008001244A PE 20090891 A1 PE20090891 A1 PE 20090891A1
Authority
PE
Peru
Prior art keywords
methyl
amino
thiazol
chlorophenyl
thio
Prior art date
Application number
PE2008001244A
Other languages
English (en)
Inventor
Hans-Georg Lerchen
Ursula Krenz
Jorg Keldenich
Nicole Diedrichs
Thomas Krahn
Claudia Hirth-Dietrich
Barbara Albrecht-Kupper
Original Assignee
Bayer Schering 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40010616&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20090891(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of PE20090891A1 publication Critical patent/PE20090891A1/es

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    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
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    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61P9/06Antiarrhythmics
    • 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
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • C07K5/06095Arg-amino acid

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (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)
  • Cardiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
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  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Biomedical Technology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)

Abstract

REFERIDO A COMPUESTOS PROFARMACOS DERIVADOS DE 2-AMINO-6-({[2-(4-CLOROFENIL)-1,3-TIAZOL-4-IL]METIL}TIO)-4-[4-(2-HIDROXIETOXI)FENIL]PIRIDIN-3,5-DICARBONITRILO DE FORMULA (I): DONDE RA ESTA REPRESENTADO POR (*), L1 Y L2 SON CADA UNO UN ENLACE O -CH2-; R1, R2 Y R3 SON CADA UNO H O METILO; R4 Y R6 SON CADA UNO H O LOS GRUPOS LATERALES DE UN ALFA-AMINOACIDO NATURAL; R5 Y R7 SON CADA UNO H O METILO; L3 ES ALCANO(C2-C4)-DIILO SUSTITUIDO CON AMINO; R8, R9 Y R10 SON H O METILO; m ES 2, 3, 4, 5 O 6; L4 ES ALCANO(C2-C4-DIILO), SUSTITUIDO CON CARBOXILO; R11 ES H O METILO; n ES 1, 2, 3 O 4. SON COMPUESTOS PREFERIDOS DICLORHIDRATO DE L-LISIL-L-VALINATO DE 2-{4-[2-AMINO-6-({[2-(4-CLOROFENIL)-1,3-TIAZOL-4-IL]METIL}TIO)-3,5-DICIANOPIRIDIN-4-IL]FENOXI}ETILO; CLORHIDRATO DE B-ALANIL-L-VALINATO DE 2-{4-[2-AMINO-6-({[2-(4-CLOROFENIL)-1,3-TIAZOL-4-IL]METIL}TIO)-3,5-DICIANOPIRIDIN-4-IL]FENOXI}ETILO; DICLORHIDRATO DE L-ARGINIL-L-VALINATO DE 2-{4-[2-AMINO-6-({[2-(4-CLOROFENIL)-1,3-TIAZOL-4-IL]METIL}TIO)-3,5-DICIANOPIRIDIN-4-IL]FENOXI}ETILO; ENTRE OTROS. DICHOS COMPUESTOS SON AGONISTAS DEL RECEPTOR DE ADENOSINA A1, SIENDO UTILES PARA LA PREVENCION Y TERAPIA DE ENFERMEDADES, CARDIOVASCULARES, UROGENITALES, RESPIRATORIAS, ENTRE OTROS
PE2008001244A 2007-08-01 2008-07-22 Profarmacos dipeptoides como agonistas de los receptores de adenosina a1 PE20090891A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102007036076A DE102007036076A1 (de) 2007-08-01 2007-08-01 Dipeptoid-Produgs und ihre Verwendung

Publications (1)

Publication Number Publication Date
PE20090891A1 true PE20090891A1 (es) 2009-08-08

Family

ID=40010616

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001244A PE20090891A1 (es) 2007-08-01 2008-07-22 Profarmacos dipeptoides como agonistas de los receptores de adenosina a1

Country Status (26)

Country Link
US (3) US8703696B2 (es)
EP (1) EP2185552B1 (es)
JP (1) JP5486492B2 (es)
KR (1) KR101550077B1 (es)
CN (1) CN101821263B (es)
AR (1) AR067779A1 (es)
AU (1) AU2008280983B2 (es)
BR (1) BRPI0814963A2 (es)
CA (1) CA2695036C (es)
CL (1) CL2008002142A1 (es)
CY (1) CY1115114T1 (es)
DE (1) DE102007036076A1 (es)
DK (1) DK2185552T3 (es)
ES (1) ES2459441T3 (es)
HR (1) HRP20140470T1 (es)
IL (1) IL202892A (es)
JO (1) JO2941B1 (es)
PE (1) PE20090891A1 (es)
PL (1) PL2185552T3 (es)
PT (1) PT2185552E (es)
RU (2) RU2486183C9 (es)
SI (1) SI2185552T1 (es)
TW (1) TWI436766B (es)
UY (1) UY31244A1 (es)
WO (1) WO2009015811A1 (es)
ZA (1) ZA201000707B (es)

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WO2018153900A1 (de) 2017-02-22 2018-08-30 Bayer Aktiengesellschaft Selektive partielle adenosin a1 rezeptor-agonisten in kombination mit sglt-2-hemmern
WO2018153898A1 (de) * 2017-02-22 2018-08-30 Bayer Pharma Aktiengesellschaft Selektive partielle adenosin a1 rezeptor-agonisten in kombination mit mineralocorticoid-rezeptor-antagonisten
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ES2459441T3 (es) 2014-05-09
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US20150133364A1 (en) 2015-05-14
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