HUP0101616A1 - Szubsztituált benzamidok, előállításuk és alkalmazásuk cisztein-proteáz inhibitorokként - Google Patents

Szubsztituált benzamidok, előállításuk és alkalmazásuk cisztein-proteáz inhibitorokként

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Publication number
HUP0101616A1
HUP0101616A1 HU0101616A HUP0101616A HUP0101616A1 HU P0101616 A1 HUP0101616 A1 HU P0101616A1 HU 0101616 A HU0101616 A HU 0101616A HU P0101616 A HUP0101616 A HU P0101616A HU P0101616 A1 HUP0101616 A1 HU P0101616A1
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HU
Hungary
Prior art keywords
group
alkyl
phenyl
substituted
optionally
Prior art date
Application number
HU0101616A
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English (en)
Inventor
Monika Knopp
Wilfried Lubisch
Achim Möller
Hans-Jörg Treiber
Original Assignee
Basf 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.)
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Publication date
Application filed by Basf Ag filed Critical Basf Ag
Publication of HUP0101616A1 publication Critical patent/HUP0101616A1/hu
Publication of HUP0101616A3 publication Critical patent/HUP0101616A3/hu

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/77—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/78—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)

Abstract

A találmány tárgyát az (I) általános képletű benzamidok - ahol R1egyenes vagy elágazó láncú alkilcsoport, ahol ezen szénlánc adottesetben szubsztituált fenil-, ciklohexil-, indolil-csoportot és -SCH3csoportot hordozhat, R2 -NR5CO-R6 és -NHR5SO2-R6 általános képletűcsoport, R3 halogénatom, alkil-, -NHCO-alkil, -NHSO2-alkil, nitro-,alkoxi-, ciano-, karboxi-, -CONH2, -COO-alkil, -SO2-alkil, -SO2-fenil-SO2NH-alkil, -SO2NH2 és aminocsoport, A adott esetben szubsztituáltaromás és heteroaromás ciklusos csoport, így naftil-, kinolinil-,kinoxalil-, benzimidazolil-, benzotienil-, kinazolil-, fenil-,tienil-, imidazolil-, piridil-, pirimidil- és piridazil-csoport, B -(CH2)m-, -(CH2)m-O-(CH2)o-, -(CH2)p-S-(CH2)m-, -(CH2)o-SO-(CH2)m-, -(CH2)o-SO2-(CH2)m-, -CH=CH-, etinilén-, -CO-CH=CH-, -(CH2)o-CO-(CH2)m-, -(CH2)m-NHCO- (CH2)o-, -(CH2)m-CONH-(CH2)o-, -(CH2)m-NHSO2-(CH2)o-, -NH-CO-CH=CH-, -(CH2)m-SO2NH-(CH2)o- csoport, A és B együttkondenzált, 2-3 gyűrűtagból álló, l-2 gyűrűtag nitrogénatomottartalmazó heterociklusos csoportot is jelenthet, R5 hidrogénatom ésalkilcsoport, R6 hidrogénatom, fenil-, naftilcsoport, adott esetbenszubsztituált fenilgyűrűvel szubsztituált alkilcsoport, n, p egymástólfüggetlenül 0, 1 vagy 2, és m, o egymástól függetlenül 0, 1, 2, 3 vagy4 - és tautomer, lehetséges enantiomer és diasztereomer formáik, E- ésZ-izomereik, valamint fiziológiailag elfogadható sóik képezik, ésezeket tartalmazó cisztein-proteázokat gátló hatásúgyógyszerkészítmények képezik. Ó
HU0101616A 1998-04-20 1999-04-19 Substituted benzamides, their production and their use as cysteine protease inhibitors HUP0101616A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19817461A DE19817461A1 (de) 1998-04-20 1998-04-20 Neue substituierte Benzamide, deren Herstellung und Anwendung
PCT/EP1999/002617 WO1999054293A1 (de) 1998-04-20 1999-04-19 Substituierte benzamide, deren herstellung und anwendung als inhibitoren von cystein-proteasen

Publications (2)

Publication Number Publication Date
HUP0101616A1 true HUP0101616A1 (hu) 2001-09-28
HUP0101616A3 HUP0101616A3 (en) 2002-10-28

Family

ID=7865113

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0101616A HUP0101616A3 (en) 1998-04-20 1999-04-19 Substituted benzamides, their production and their use as cysteine protease inhibitors

Country Status (21)

Country Link
US (1) US6436925B1 (hu)
EP (1) EP1073632A1 (hu)
JP (1) JP2002512220A (hu)
KR (1) KR20010042837A (hu)
CN (1) CN1306509A (hu)
AU (1) AU743245B2 (hu)
BG (1) BG104856A (hu)
BR (1) BR9909776A (hu)
CA (1) CA2328430A1 (hu)
CZ (1) CZ20003890A3 (hu)
DE (1) DE19817461A1 (hu)
HR (1) HRP20000777A2 (hu)
HU (1) HUP0101616A3 (hu)
ID (1) ID26305A (hu)
IL (1) IL138676A0 (hu)
NO (1) NO20005265D0 (hu)
PL (1) PL343466A1 (hu)
SK (1) SK14122000A3 (hu)
TR (1) TR200003069T2 (hu)
WO (1) WO1999054293A1 (hu)
ZA (1) ZA200006758B (hu)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001002344A1 (fr) * 1999-07-01 2001-01-11 Taisho Pharmaceutical Co., Ltd. Derives d'acide aminobenzoique
US6846813B2 (en) * 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
PE20020506A1 (es) * 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
DE10114762A1 (de) * 2001-03-26 2002-10-02 Knoll Gmbh Verwendung von Cysteinprotease-Inhibitoren
JP2005504040A (ja) * 2001-08-03 2005-02-10 スミスクライン ビーチャム コーポレーション カテプシンＫ阻害剤としてのα−ケトアミド誘導体
GB0124938D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124932D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124941D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124939D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124931D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124933D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124936D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124934D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
US7282512B2 (en) 2002-01-17 2007-10-16 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin K inhibitors
EP1474395B1 (en) 2002-02-12 2007-10-17 Smithkline Beecham Corporation Nicotinamide derivates useful as p38 inhibitors
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
EP1562897B1 (en) 2002-11-12 2009-09-16 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer s disease
GB0228410D0 (en) 2002-12-05 2003-01-08 Glaxo Group Ltd Novel Compounds
GB0308185D0 (en) * 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308201D0 (en) * 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308186D0 (en) * 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0318814D0 (en) * 2003-08-11 2003-09-10 Smithkline Beecham Corp Novel compounds
EP2615087A3 (en) * 2003-12-22 2013-08-07 Ajinomoto Co., Inc. Phenylalanine derivatives
GB0402143D0 (en) * 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
US20080051416A1 (en) * 2004-10-05 2008-02-28 Smithkline Beecham Corporation Novel Compounds
GB0512429D0 (en) * 2005-06-17 2005-07-27 Smithkline Beecham Corp Novel compound
EP2439205B1 (en) 2006-12-29 2015-03-11 AbbVie Deutschland GmbH & Co KG Carboxamide compounds and their use as calpain inhibitors
TWI453019B (zh) 2007-12-28 2014-09-21 Abbvie Deutschland 甲醯胺化合物
UY32404A (es) * 2009-01-30 2010-08-31 Novartis Ag 4-aril-butan-1,3-diamidas
TWI519530B (zh) * 2009-02-20 2016-02-01 艾伯維德國有限及兩合公司 羰醯胺化合物及其作為鈣蛋白酶（ｃａｌｐａｉｎ）抑制劑之用途
JP2015512427A (ja) 2012-04-03 2015-04-27 アッヴィ・ドイチュラント・ゲー・エム・ベー・ハー・ウント・コー・カー・ゲー カルボキサミド化合物およびそれのカルパイン阻害薬ｖとしての使用
CN106536520B (zh) 2014-06-27 2020-08-14 诺格拉制药有限公司 芳基受体调制剂及其制备和使用方法
WO2017156071A1 (en) 2016-03-09 2017-09-14 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
EP3481835A4 (en) 2016-07-05 2020-02-26 Blade Therapeutics, Inc. CALPAIN MODULATORS AND THEIR THERAPEUTIC USES
CN110023304A (zh) 2016-09-28 2019-07-16 布莱德治疗公司 钙蛋白酶调节剂及其治疗用途

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NZ305626A (en) * 1995-03-24 2000-01-28 Axys Pharm Inc Reversible protease inhibitors
EP0923535A4 (en) 1996-08-28 2001-01-10 Smithkline Beecham Corp CYSTEINE PROTEASE INHIBITORS
RU2190599C2 (ru) * 1996-12-11 2002-10-10 Басф Акциенгезельшафт Новые кетобензамиды

Also Published As

Publication number Publication date
AU3818699A (en) 1999-11-08
US6436925B1 (en) 2002-08-20
DE19817461A1 (de) 1999-10-21
HUP0101616A3 (en) 2002-10-28
CN1306509A (zh) 2001-08-01
EP1073632A1 (de) 2001-02-07
TR200003069T2 (tr) 2009-01-21
ZA200006758B (en) 2001-12-12
CA2328430A1 (en) 1999-10-28
SK14122000A3 (sk) 2001-05-10
BG104856A (en) 2001-05-31
PL343466A1 (en) 2001-08-13
IL138676A0 (en) 2001-10-31
KR20010042837A (ko) 2001-05-25
ID26305A (id) 2000-12-14
JP2002512220A (ja) 2002-04-23
NO20005265L (no) 2000-10-19
HRP20000777A2 (en) 2001-06-30
CZ20003890A3 (cs) 2001-11-14
BR9909776A (pt) 2000-12-19
WO1999054293A1 (de) 1999-10-28
NO20005265D0 (no) 2000-10-19
AU743245B2 (en) 2002-01-24

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