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AR045798A1 - ACID DERIVATIVES 1- (CARBOXIALQUIL) - CICLOPENTILCARBONIL - AMINO- BENZAZEPINA - N- ACETICS REPLACED WITH AMIDOMETILO, PROCESS AND INTERMEDIATE PRODUCTS FOR THEIR PREPARATION AND MEDICINES CONTAINING THESE COMPOUNDS - Google Patents

ACID DERIVATIVES 1- (CARBOXIALQUIL) - CICLOPENTILCARBONIL - AMINO- BENZAZEPINA - N- ACETICS REPLACED WITH AMIDOMETILO, PROCESS AND INTERMEDIATE PRODUCTS FOR THEIR PREPARATION AND MEDICINES CONTAINING THESE COMPOUNDS

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Publication number
AR045798A1
AR045798A1 ARP040103409A ARP040103409A AR045798A1 AR 045798 A1 AR045798 A1 AR 045798A1 AR P040103409 A ARP040103409 A AR P040103409A AR P040103409 A ARP040103409 A AR P040103409A AR 045798 A1 AR045798 A1 AR 045798A1
Authority
AR
Argentina
Prior art keywords
alkyl
compounds
whose
alkanoyl
amino acid
Prior art date
Application number
ARP040103409A
Other languages
Spanish (es)
Inventor
Dagmar Holtje
Ivan Fischer
Dieter Ziegler
Michael Weske
Katrin Michaelis
Josef Messinger
Axel Pahl
Yasmin Karimi-Nejad
Original Assignee
Solvay Pharm Gmbh
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 DE10344848A external-priority patent/DE10344848A1/en
Application filed by Solvay Pharm Gmbh filed Critical Solvay Pharm Gmbh
Publication of AR045798A1 publication Critical patent/AR045798A1/en

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    • 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
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
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    • 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
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P17/06Antipsoriatics
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    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
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    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • AHUMAN NECESSITIES
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    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • 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
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • C07K5/0222Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. Pro, Trp
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Genetics & Genomics (AREA)
  • Reproductive Health (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)

Abstract

Se describen compuestos con actividad inhibidora de la endopeptidasa neutra (NEP) y/o la endopeptidasa humana soluble (hSEP), así como medicamentos que contienen estos compuestos, en particular medicamentos adecuados para tratamiento o prevención de enfermedades cardiovasculares, disfunción sexual y/o condiciones adversas asociadas con apoptosis. Reivindicación 1: Compuestos de la fórmula general (1), en donde: R1 es hidrógeno o un grupo formador de un éster biolábil; R2 es hidrógeno, alquilo C1-4 o hidroxialquilo C1-4, cuyo grupo hidroxilo está esterificado opcionalmente con alcanoilo C2-4 o un residuo de aminoácido; y R3 es alquilo C1-4; alcoxi(C1-4)-alquilo(C1-4); hidroxialquilo C1-4, que está sustituido opcionalmente con un segundo grupo hidroxilo y cuyos grupos hidroxilo están esterificados cada uno opcionalmente con alcanoilo C2-4 o un residuo de aminoácido; (alquil C0-4)2amino-alquilo(C1-4); cicloalquilo C3-7; cicloalquil(C3-7)-alquilo(C1-4); fenil-alquilo(C1-4), cuyo grupo fenilo está sustituido opcionalmente 1-2 veces con alquilo C1-4, alcoxi C1-4 y/o halógeno; naftil-alquilo(C1-4); oxoalquilo C3-6; fenilcarbonilmetilo, cuyo grupo fenilo está sustituido opcionalmente 1-2 veces con alquilo C1-4, alcoxi C1-4 y/o halógeno, o 2-oxoazepanilo; o R2 y R3 juntos son alquileno C4-7, cuyos grupos metileno están reemplazados opcionalmente 1-2 veces por carbonilo, nitrógeno, oxígeno y/o azufre, y/o que están sustituidos opcionalmente una sola vez con hidroxi, que está esterificado opcionalmente con alcanoilo C2-4 o un residuo de aminoácido; alquilo C1-4; hidroxialquilo C1-4, cuyo grupo hidroxilo está esterificado opcionalmente con alcanoilo C2-4 o un residuo de aminoácido; fenilo o bencilo; y R4 es hidrógeno o un grupo formador de un éster biolábil, y sales fisiológicamente compatibles de los ácidos de fórmula (1) y/o sales de adición de ácido fisiológicamente compatibles de los compuestos de fórmula (1).Compounds with neutral endopeptidase (NEP) and / or soluble human endopeptidase (hSEP) inhibitory activity are described, as well as medications containing these compounds, in particular drugs suitable for treatment or prevention of cardiovascular diseases, sexual dysfunction and / or conditions side effects associated with apoptosis. Claim 1: Compounds of the general formula (1), wherein: R1 is hydrogen or a group forming a bi-volatile ester; R 2 is hydrogen, C 1-4 alkyl or C 1-4 hydroxyalkyl, whose hydroxyl group is optionally esterified with C 2-4 alkanoyl or an amino acid residue; and R3 is C1-4 alkyl; (C1-4) alkoxy-(C1-4) alkyl; C1-4 hydroxyalkyl, which is optionally substituted with a second hydroxyl group and whose hydroxyl groups are each optionally esterified with C2-4 alkanoyl or an amino acid residue; (C0-4 alkyl) 2 amino (C1-4) alkyl; C3-7 cycloalkyl; cycloalkyl (C3-7) -alkyl (C1-4); phenyl (C1-4) alkyl, whose phenyl group is optionally substituted 1-2 times with C1-4 alkyl, C1-4 alkoxy and / or halogen; naphthyl-C1-4 alkyl; C3-6 oxoalkyl; phenylcarbonylmethyl, whose phenyl group is optionally substituted 1-2 times with C1-4 alkyl, C1-4 alkoxy and / or halogen, or 2-oxoazepanyl; or R2 and R3 together are C4-7 alkylene, whose methylene groups are optionally replaced 1-2 times by carbonyl, nitrogen, oxygen and / or sulfur, and / or which are optionally substituted only once with hydroxy, which is optionally esterified with C2-4 alkanoyl or an amino acid residue; C1-4 alkyl; C1-4 hydroxyalkyl, whose hydroxyl group is optionally esterified with C2-4 alkanoyl or an amino acid residue; phenyl or benzyl; and R4 is hydrogen or a biolábil ester forming group, and physiologically compatible salts of the acids of formula (1) and / or physiologically compatible acid addition salts of the compounds of formula (1).

ARP040103409A 2003-09-26 2004-09-22 ACID DERIVATIVES 1- (CARBOXIALQUIL) - CICLOPENTILCARBONIL - AMINO- BENZAZEPINA - N- ACETICS REPLACED WITH AMIDOMETILO, PROCESS AND INTERMEDIATE PRODUCTS FOR THEIR PREPARATION AND MEDICINES CONTAINING THESE COMPOUNDS AR045798A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10344848A DE10344848A1 (en) 2003-09-26 2003-09-26 New amidomethyl substituted 1-(carboxyalkyl)-cyclopentylcarbonylamino-benzazepine-n-acetic acid derivatives useful to treat cardiovascular disorders or diseases; hypertension; sexual dysfunction; or neurodegenerative disorders
EP04100065 2004-01-12

Publications (1)

Publication Number Publication Date
AR045798A1 true AR045798A1 (en) 2005-11-16

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ARP040103409A AR045798A1 (en) 2003-09-26 2004-09-22 ACID DERIVATIVES 1- (CARBOXIALQUIL) - CICLOPENTILCARBONIL - AMINO- BENZAZEPINA - N- ACETICS REPLACED WITH AMIDOMETILO, PROCESS AND INTERMEDIATE PRODUCTS FOR THEIR PREPARATION AND MEDICINES CONTAINING THESE COMPOUNDS

Country Status (14)

Country Link
EP (1) EP1670814A1 (en)
JP (1) JP4824562B2 (en)
KR (1) KR101264934B1 (en)
AR (1) AR045798A1 (en)
AU (1) AU2004276002B2 (en)
BR (1) BRPI0414744A (en)
CA (1) CA2539895A1 (en)
IL (1) IL174373A (en)
MX (1) MXPA06003226A (en)
NO (1) NO20061821L (en)
RU (1) RU2368601C2 (en)
SA (1) SA04250283B1 (en)
TW (1) TWI332947B (en)
WO (1) WO2005030795A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1753433A1 (en) * 2004-05-14 2007-02-21 Solvay Pharmaceuticals GmbH Pharmaceutical compositions comprising nep-inhibitors, inhibitors of the endogenous endothelin producing system and pde v inhibitors
MXPA06014448A (en) * 2004-06-23 2007-03-01 Solvay Pharm Gmbh Pharmaceutical compositions comprising nep-inhibitors, inhibitors of the endogenous endothelin producing system and at1-receptor antagonists.
EP1827448A1 (en) 2004-12-15 2007-09-05 Solvay Pharmaceuticals GmbH Pharmaceutical compositions comprising nep-inhibitors, inhibitors of the endogenous endothelin producing system and hmg coa reductase inhibitors
ATE464904T1 (en) * 2005-02-18 2010-05-15 Solvay Pharm Gmbh PHARMACEUTICAL COMPOSITIONS CONTAINING NEP INHIBITORS, INHIBITORS OF THE ENDOGENE ENDOTHELIN PRODUCING SYSTEM AND DIURETICS
AU2008287285B2 (en) * 2007-04-13 2013-05-16 Southern Research Institute Anti-angiogenic agents and methods of use
AR071375A1 (en) * 2008-04-22 2010-06-16 Solvay Pharm Gmbh FORMULATIONS FOR ACTIVE PHARMACEUTICAL INGREDIENTS OF DEFICIENT PERMEABILITY, PREPARATION AND PRODUCT PROCESS
PL424452A1 (en) * 2018-01-31 2019-08-12 Forty-Four Pharmaceuticals Spółka Z Ograniczoną Odpowiedzialnością Inhibitors of inactive endopeptidase (NEP) and human soluble endopeptidase (hSEP) for prevention and treatment of eye diseases

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI960867A0 (en) * 1993-08-26 1996-02-26 Yamanouchi Pharma Co Ltd Benzazepine derivative, its pharmaceutical mixture and intermediate
DE19502644A1 (en) * 1995-01-28 1996-08-01 Merck Patent Gmbh 4-amino-benzoylguanidine derivatives
DE19510566A1 (en) * 1995-03-23 1996-09-26 Kali Chemie Pharma Gmbh Benzazepine, benzoxazepine and benzothiazepine N-acetic acid derivatives and process for their preparation and medicaments containing these compounds
DE19750002A1 (en) * 1997-11-12 1999-05-20 Solvay Pharm Gmbh Phosphonic acid-substituted benzazepinone-N-acetic acid derivatives and processes for their preparation and pharmaceuticals containing these compounds
DE19906310A1 (en) * 1999-02-16 2000-08-17 Solvay Pharm Gmbh Use of 3-(1-(2-aralkyl-2-carboxyethyl)-1-cyclopentanecarboxamido)-2,3,4,5-tetrahydro-2-oxo-1H-benz(b)azepine-1-acetic acid derivatives for treating hypertension
CN100591689C (en) * 2002-01-16 2010-02-24 索尔瓦药物有限公司 Solid salts of benzazepine compounds and their use in the preparation of pharmaceutical compounds

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KR101264934B1 (en) 2013-05-20
RU2006113946A (en) 2007-11-10
BRPI0414744A (en) 2006-11-21
MXPA06003226A (en) 2006-05-22
HK1096105A1 (en) 2007-05-25
SA04250283B1 (en) 2008-05-26
AU2004276002A1 (en) 2005-04-07
TWI332947B (en) 2010-11-11
CA2539895A1 (en) 2005-04-07
JP2007535482A (en) 2007-12-06
RU2368601C2 (en) 2009-09-27
IL174373A (en) 2011-12-29
EP1670814A1 (en) 2006-06-21
JP4824562B2 (en) 2011-11-30
WO2005030795A1 (en) 2005-04-07
TW200524874A (en) 2005-08-01
IL174373A0 (en) 2006-08-01
AU2004276002B2 (en) 2010-07-22
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