HUP0001796A2 - Dipeptid-benzamidinek mint kininogenáz inhibitorok, és a vegyületeket tartalmazó gyógyszerkészítmények - Google Patents

Dipeptid-benzamidinek mint kininogenáz inhibitorok, és a vegyületeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0001796A2
HUP0001796A2 HU0001796A HUP0001796A HUP0001796A2 HU P0001796 A2 HUP0001796 A2 HU P0001796A2 HU 0001796 A HU0001796 A HU 0001796A HU P0001796 A HUP0001796 A HU P0001796A HU P0001796 A2 HUP0001796 A2 HU P0001796A2
Authority
HU
Hungary
Prior art keywords
carbon atom
group
alkyl
atom alkyl
cycloalkyl
Prior art date
Application number
HU0001796A
Other languages
English (en)
Inventor
Dorit Baucke
Wilfried Hornberger
Hans Wolfgang Höffken
Udo Lange
Helmut Mack
Thomas Pfeiffer
Werner Seitz
Thomas Zierke
Original Assignee
Basf Aktiengesellschaft
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 Basf Aktiengesellschaft filed Critical Basf Aktiengesellschaft
Publication of HUP0001796A2 publication Critical patent/HUP0001796A2/hu
Publication of HUP0001796A3 publication Critical patent/HUP0001796A3/hu

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022—Peptides 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
    • C07K5/0222—Peptides 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/78—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)

Abstract

A találmány az (I) általános képletű, kininogenáz inhibitor hatásúvegyületekre, valamint ezek gyógyászatilag elfogadható savakkalképzett sóira vonatkozik, mely képletben l=0 vagy 1, m=0, 1 vagy 2,n=0, 1 vagy 2, R H vagy 1-4 szénatomos alkilcsoport, R1 HOOC-, (1-6szénatomos alkil)-OOC-, benzil-OOC- vagy -OH, R2 H-, 1-4 szénatomosalkil- vagy R1-(CH2)m- képletű csoport, R3 H- vagy 1-4 szénatomosalkilcsoport, amely -OH vagy -COOH csoporttal szubsztituált lehet, R4H-, 1-4 szénatomos alkil-, HOOC-(1-4 szénatomos alkilén)-, R5 1-8szénatomos alkil-, cikloalkil-(CR8R9)r-, (r = 0 vagy 1, R8, R9=H-,cikloalkil- vagy 1-4 szénatomos alkilcsoport), ahol a cikloalkilrészlegfeljebb négy CH-csoportja egymástól függetlenül CR10R11 csoporttal(R10=H- vagy 1-4 szénatomos alkil, R11=1-4 szénatomos alkil) és/vagy acikloalkilrész CR8R9-re kötődő CH-csoportja CR12-vel (R12=1-4szénatomos alkil) és/vagy egy vagy két C-C egyszeres kötés a gyűrűbenegy C=C kettős kötéssel helyettesített lehet, R6 H-, 1-4 szénatomosalkilcsoport vagy R4 és R5 együttesen -CH2-CH2-CH(R7)-, (R7=H-, fenil-vagy ciklohexilcsoport), R2 és R5 együttesen -CH2-CH2- vagy -CH2-CH2-CH2- képletű csoport, ahol a hidrogénatom 1-4 szénatomos alkil-,fenil- vagy cikloalkilcsoporttal helyettesítve lehet. A találmánytárgyát képezik továbbá a kiindulási vegyületek. Ó
HU0001796A 1996-08-14 1997-07-29 Dipeptide benzamidine as a kininogenase inhibitor and pharmaceutical compositions containing them HUP0001796A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19632772A DE19632772A1 (de) 1996-08-14 1996-08-14 Neue Benzamidine
PCT/EP1997/004105 WO1998006740A1 (de) 1996-08-14 1997-07-29 Dipeptidische benzamidine als kininogenasen-inhibitoren

Publications (2)

Publication Number Publication Date
HUP0001796A2 true HUP0001796A2 (hu) 2000-11-28
HUP0001796A3 HUP0001796A3 (en) 2001-12-28

Family

ID=7802623

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0001796A HUP0001796A3 (en) 1996-08-14 1997-07-29 Dipeptide benzamidine as a kininogenase inhibitor and pharmaceutical compositions containing them

Country Status (18)

Country Link
US (1) US6440937B1 (hu)
EP (1) EP0918792B1 (hu)
JP (1) JP2000517300A (hu)
KR (1) KR20000030004A (hu)
CN (1) CN1233256A (hu)
AT (1) ATE196637T1 (hu)
AU (1) AU717692B2 (hu)
BR (1) BR9711134A (hu)
CA (1) CA2263344A1 (hu)
CZ (1) CZ31199A3 (hu)
DE (2) DE19632772A1 (hu)
ES (1) ES2151741T3 (hu)
HU (1) HUP0001796A3 (hu)
IL (1) IL128231A0 (hu)
NO (1) NO990667L (hu)
TW (1) TW442471B (hu)
WO (1) WO1998006740A1 (hu)
ZA (1) ZA977240B (hu)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9602263D0 (sv) 1996-06-07 1996-06-07 Astra Ab New amino acid derivatives
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds
DE19632773A1 (de) * 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren
AR013084A1 (es) 1997-06-19 2000-12-13 Astrazeneca Ab Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
WO1999064392A1 (fr) 1998-06-08 1999-12-16 Ajinomoto Co., Inc. Derive de benzamidine
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
AU764121B2 (en) 1999-01-13 2003-08-07 Astrazeneca Ab New amidinobenzylamine derivatives and their use as thrombin inhibitors
JP4489976B2 (ja) * 1999-04-09 2010-06-23 ビーエーエスエフ ソシエタス・ヨーロピア 補体プロテアーゼの低分子インヒビター
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
SE0001803D0 (sv) 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin inhibitors
DE10049937A1 (de) * 2000-10-06 2002-04-11 Knoll Ag Niedermolekulare Inhibitoren von Serinproteasen mit Polyhydroxyalkyl- und Polyhydroxycycloalkylresten
AR035216A1 (es) * 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
US7129233B2 (en) 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
DE10064797A1 (de) * 2000-12-22 2002-06-27 Knoll Ag Orale und parenterale pharmazeutische Formulierung, umfassend eine niedermolekulare Thrombininhibitor-Pro-Pharmakon
DE10117730A1 (de) * 2001-04-09 2002-10-10 Basf Ag Umsetzung von (Di)Aminen in Gegenwart einer Lysinoxidase und eines Reduktionsmittels
AR034517A1 (es) * 2001-06-21 2004-02-25 Astrazeneca Ab Formulacion farmaceutica
SE0201661D0 (sv) * 2002-05-31 2002-05-31 Astrazeneca Ab New salts
SE0201659D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
US6849084B2 (en) * 2002-12-31 2005-02-01 Intek Technology L.L.C. Stent delivery system
US7781424B2 (en) * 2003-05-27 2010-08-24 Astrazeneca Ab Modified release pharmaceutical formulation
EP1736465A4 (en) * 2004-03-31 2009-06-17 Ajinomoto Kk ANILINE DERIVATIVES
US7524354B2 (en) * 2005-07-07 2009-04-28 Research Foundation Of State University Of New York Controlled synthesis of highly monodispersed gold nanoparticles
TW200827336A (en) * 2006-12-06 2008-07-01 Astrazeneca Ab New crystalline forms
US20090061000A1 (en) * 2007-08-31 2009-03-05 Astrazeneca Ab Pharmaceutical formulation use 030
CA3168591A1 (en) 2010-01-06 2011-07-14 Takeda Pharmaceutical Company Limited Plasma kallikrein binding proteins
JP2014506257A (ja) * 2011-01-06 2014-03-13 ダイアックス コーポレーション 血漿カリクレイン結合タンパク質
JP2016513682A (ja) 2013-03-15 2016-05-16 ダイアックス コーポレーション 抗血漿カリクレイン抗体
ES2856076T3 (es) 2014-01-21 2021-09-27 Takeda Pharmaceuticals Co Proteínas de unión a calicreína plasmática y usos de las mismas en el tratamiento de angioedema hereditario
KR102555955B1 (ko) 2014-03-27 2023-07-18 다케다 파머수티컬 컴패니 리미티드 당뇨병성 황반 부종의 치료를 위한 조성물 및 방법
EP3387018A1 (en) 2015-12-11 2018-10-17 Dyax Corp. Plasma kallikrein inhibitors and uses thereof for treating hereditary angioedema attack

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU675981B2 (en) 1992-12-02 1997-02-27 Bristol-Myers Squibb Company Guanidinyl-substituted heterocyclic thrombin inhibitors
SE9301916D0 (sv) 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
ZA951617B (en) 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
BR9607582A (pt) 1995-02-17 1998-07-07 Basf Ag Composto e peptídeo ou substância peptidomimética
DE19632773A1 (de) 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren

Also Published As

Publication number Publication date
EP0918792A1 (de) 1999-06-02
NO990667D0 (no) 1999-02-12
CA2263344A1 (en) 1998-02-19
AU717692B2 (en) 2000-03-30
AU3771597A (en) 1998-03-06
ATE196637T1 (de) 2000-10-15
CN1233256A (zh) 1999-10-27
WO1998006740A1 (de) 1998-02-19
JP2000517300A (ja) 2000-12-26
ZA977240B (en) 1999-02-15
CZ31199A3 (cs) 1999-06-16
EP0918792B1 (de) 2000-09-27
HUP0001796A3 (en) 2001-12-28
DE59702414D1 (de) 2000-11-02
IL128231A0 (en) 1999-11-30
TW442471B (en) 2001-06-23
BR9711134A (pt) 1999-08-17
DE19632772A1 (de) 1998-02-19
KR20000030004A (ko) 2000-05-25
ES2151741T3 (es) 2001-01-01
US6440937B1 (en) 2002-08-27
NO990667L (no) 1999-04-12

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