HUP0401729A2 - IV típusú foszfodiészteráz inhibitor hatású alkin-aril-naftiridin-4(1H)-on-származékok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

IV típusú foszfodiészteráz inhibitor hatású alkin-aril-naftiridin-4(1H)-on-származékok és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0401729A2
HUP0401729A2 HU0401729A HUP0401729A HUP0401729A2 HU P0401729 A2 HUP0401729 A2 HU P0401729A2 HU 0401729 A HU0401729 A HU 0401729A HU P0401729 A HUP0401729 A HU P0401729A HU P0401729 A2 HUP0401729 A2 HU P0401729A2
Authority
HU
Hungary
Prior art keywords
alkyl
group
son
hydroxyl
optionally substituted
Prior art date
Application number
HU0401729A
Other languages
English (en)
Inventor
Daniel Guay
Mario Girard
Pierre Hamel
Sebastien Laliberte
Richard Friesen
Original Assignee
Merck Frosst Canada & Co.
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 Merck Frosst Canada & Co. filed Critical Merck Frosst Canada & Co.
Publication of HUP0401729A2 publication Critical patent/HUP0401729A2/hu
Publication of HUP0401729A3 publication Critical patent/HUP0401729A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61P1/04—Drugs 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
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P11/14—Antitussive agents
    • 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
    • A61P11/16—Central respiratory analeptics
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • 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

Abstract

A találmány szerinti (I) általános képletű vegyületek ésgyógyszerészetileg elfogadható sóik foszfodiészteráz-4 inhibitorok,így asztmaellenes és gyulladásgátló szerként használhatók. A képletbenR jelentése hidrogénatom, alkil- vagy cikloalkilcsoport; R1 jelentésehidrogénatom, alkil-, cikloalkil-, alkoxi-, alkenil-, alkinil-, -C(O)-alkil-, -C(O)-aril-, alkil-SOn-alku-, alkil-SOn-(aril)-, fenil-,heteroaril- vagy heterocikloalkil-csoport, ahol valamennyi csoportadott esetben szubsztituálva van 1-3 egymástól függetlenül választottalkil-, alkoxi-, hidroxil-, -N-alkil-alkil-, alkil-SOn-alkil-, nitro-,CN, =N-O-alkil-, -O-N=alkil-csoporttal vagy halogénatommal; R2jelentése hiányzik, hidrogénatom, halogénatom, alkil-, cikloalkil-,alkil-cikloalkil-cikloalkil-, alkoxi-, fenil-, heteroaril-,heterocikloalkil-, nitro-, CN, =N-O-alkil-, -O-N=alkil-, -N-alkil-alkil-, -NHSOn-alkil-, -NHC(O)-alkil-, -NHC(O)-aril-, -C(O)-alkil-, -C(O)-O-alkil-, alkil(=N-OH)-, -C(N-NOH)-alkil-, alkil(oxi)alkil-fenil-, -SOnNH-alkil- vagy alkil-SOn-alkil-csoport, ahol a fenil-heteroaril- vagy heterocikloalkil-csoport adott esetben szubsztituálvavan halogénatommal, alkil-, alkoxi-, hidroxil-, -N-alkil-alkil- vagy -C(O)-O-alkil-csoporttal, és valamennyi alkilcsoport adott esetbenszubsztituálva van egymástól függetlenül 1-6 halogénatommal vagyhidroxilcsoporttal; n értéke 0, 1 vagy 2; R3 hiányzik, vagy jelentésehidrogénatom, hidroxil-, -N-alkil-alkil-csoport, halogénatom vagyalkilcsoport, ahol valamennyi alkilcsoport adott esetbenszubsztituálva van egymástól függetlenül 1-6 halogénatommal,hidroxilcsoporttal vagy -N-alkil-alkil-csoporttal; R4, R5, R6 és R7jelentése egymástól függetlenül hidrogén-, halogénatom, alkil-,alkoxi-, -SOn-alkil-, nitro-, ciano- vagy -N-alkil-alkil-csoport, ésvalamennyi alkilcsoport adott esetben szubsztituálva van egymástólfüggetlenül 1-6 halogénatommal vagy hidroxilcsoporttal; és R8jelentése fenil-, piridil-, pirimidil-, indolil-, kinolinil-, tienil-,piridonil-, oxazolil-, oxadiazolil-, tiazolil-, tiadiazolil- vagyimidazolilcsoport; vagy ezek oxidjai, amikor R8 jelentéseheteroarilcsoport; vagy hidrogénatom, alkil- vagy cikloalkilcsoport,és valamennyi alkilcsoport adott esetben szubsztituálva van 1-6egymástól független halogénatommal, -N-alkil-alkil-, -N-cikloalkil-alkil-, -N-cikloalkil-cikloalkil-, N-heterociklo-alkil-, -SOn-alkil-,-SOn-(aril)- vagy hidroxilcsoporttal. A találmány kiterjed avegyületeket tartalmazó gyógyszerkészítményekre is. Ó
HU0401729A 2001-08-29 2002-08-27 Alkyne-aryl-naphthyridin-4(1h)-one derivaties as phosphodiesterase-4 inhibitors and pharmaceutical compositions containing them HUP0401729A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31609301P 2001-08-29 2001-08-29
PCT/CA2002/001324 WO2003018579A1 (en) 2001-08-29 2002-08-27 Alkyne-aryl phosphodiesterase-4 inhibitors

Publications (2)

Publication Number Publication Date
HUP0401729A2 true HUP0401729A2 (hu) 2004-12-28
HUP0401729A3 HUP0401729A3 (en) 2012-09-28

Family

ID=23227432

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0401729A HUP0401729A3 (en) 2001-08-29 2002-08-27 Alkyne-aryl-naphthyridin-4(1h)-one derivaties as phosphodiesterase-4 inhibitors and pharmaceutical compositions containing them

Country Status (28)

Country Link
US (2) US6743802B2 (hu)
EP (2) EP2305677A1 (hu)
JP (1) JP4157035B2 (hu)
KR (1) KR100928849B1 (hu)
CN (1) CN100338061C (hu)
AR (1) AR036365A1 (hu)
AU (1) AU2002322940B2 (hu)
BR (1) BR0212042A (hu)
CA (1) CA2456817C (hu)
DO (1) DOP2002000456A (hu)
EA (1) EA006800B1 (hu)
EC (1) ECSP044992A (hu)
GE (1) GEP20063805B (hu)
HK (1) HK1080073B (hu)
HR (1) HRP20040151A2 (hu)
HU (1) HUP0401729A3 (hu)
IL (1) IL160213A0 (hu)
IS (1) IS7138A (hu)
JO (1) JO2311B1 (hu)
MX (1) MXPA04001889A (hu)
NO (1) NO330521B1 (hu)
NZ (1) NZ530931A (hu)
PE (1) PE20030416A1 (hu)
PL (1) PL367716A1 (hu)
RS (1) RS17004A (hu)
UA (1) UA75957C2 (hu)
WO (1) WO2003018579A1 (hu)
ZA (1) ZA200400952B (hu)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO2311B1 (en) * 2001-08-29 2005-09-12 ميرك فروست كندا ليمتد Alkyl inhibitors Ariel phosphodiesterase-4
US7452911B2 (en) 2002-10-31 2008-11-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
DE10250708A1 (de) * 2002-10-31 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
US7351719B2 (en) 2002-10-31 2008-04-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds
US20060069115A1 (en) * 2002-11-15 2006-03-30 Scolnick Edward M Use of pde4 inhibitors as adjunct therapy for psychiatric disorders
AU2003286024A1 (en) * 2002-11-22 2004-06-18 Daniel Dube Use of phosphodiesterase-4 inhibitors as enhancers of cognition
AR042194A1 (es) * 2002-11-22 2005-06-15 Merck & Co Inc Metodo para preparar inhibidores de fosfodiesterasa - 4
GB0307863D0 (en) * 2003-04-04 2003-05-14 Merck Sharp & Dohme Therapeutic treatment
GB0322722D0 (en) * 2003-09-27 2003-10-29 Glaxo Group Ltd Compounds
GB0322726D0 (en) * 2003-09-27 2003-10-29 Glaxo Group Ltd Compounds
US7592373B2 (en) 2003-12-23 2009-09-22 Boehringer Ingelheim International Gmbh Amide compounds with MCH antagonistic activity and medicaments comprising these compounds
US7524862B2 (en) 2004-04-14 2009-04-28 Boehringer Ingelheim International Gmbh Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
DE102004017934A1 (de) 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE102004017930A1 (de) * 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
EP1742628A4 (en) * 2004-04-26 2009-06-03 Merck Frosst Canada Ltd ALTERNATIVE FORMS OF PHOSPHODIESTERASE-4-HEMMER N-CYCLOPROPYL-1- (3-1 / 4 (1-OXIDOPYRIDIN-3-YL) ETHYNYL-PHENYL) -4-OXO-1,4-DIYHDRO-1,8-NAPHTHYRIDINE- 3-carboxyamide
JP4264388B2 (ja) * 2004-07-01 2009-05-13 富士通株式会社 半導体チップの接合方法および接合装置
WO2006004191A1 (en) * 2004-07-05 2006-01-12 Astellas Pharma Inc. Pyrrolopyridazine derivatives which inhibit pde iv and tnf alfa
US7687490B2 (en) * 2005-04-12 2010-03-30 Meiji Seika Kaisha, Ltd. 2-thioethenyl substituted carbapenem derivatives
JP2006016407A (ja) * 2005-06-15 2006-01-19 Yamaha Motor Co Ltd ホスホジエステラーゼ阻害剤
EP2258357A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
JP2009509980A (ja) * 2005-09-28 2009-03-12 メルク フロスト カナダ リミテツド 篩分けされたラクトースを含むエアゾール粉末製剤
AU2006304787A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
JP2009519336A (ja) 2005-12-13 2009-05-14 ワイス ジベンゾナフチリジン誘導体およびそれらの使用方法
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2021000A2 (en) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenesis by modulating angiotensin
JP2009536667A (ja) 2006-05-09 2009-10-15 ブレインセルス，インコーポレイティド ５ｈｔ受容体介在性の神経新生
US7998971B2 (en) 2006-09-08 2011-08-16 Braincells Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
EP2121633A2 (en) 2007-02-12 2009-11-25 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
AU2008240279A1 (en) * 2007-04-11 2008-10-23 Alcon Research, Ltd. Use of an inhibitor of TNFa plus an antihistamine to treat allergic rhinitis and allergic conjunctivitis
US20090182035A1 (en) * 2007-04-11 2009-07-16 Alcon Research, Ltd. Use of a combination of olopatadine and cilomilast to treat non-infectious rhinitis and allergic conjunctivitis
EP2546232A1 (en) 2007-06-20 2013-01-16 Merck Sharp & Dohme Corp. Diphenyl Substituted Alkanes
NZ584876A (en) * 2007-10-25 2012-06-29 Merck Frosst Canada Ltd Inhalation compositions comprising montelukast acid and a pde-4-inhibitor or an inhaled corticosteroid
WO2009128057A2 (en) 2008-04-18 2009-10-22 UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN et al Psycho-pharmaceuticals
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
MX2012003693A (es) * 2009-10-01 2012-04-19 Alcon Res Ltd Composiciones de olopatadine y usos de las mismas.
FR2952934B1 (fr) * 2009-11-23 2012-06-22 Sanofi Aventis Derives de pyridino-pyridinones, leur preparation et leur application en therapeutique
WO2011099305A1 (en) 2010-02-12 2011-08-18 Raqualia Pharma Inc. 5-ht4 receptor agonists for the treatment of dementia
EP2680842A4 (en) * 2011-03-02 2014-10-29 Bionomics Ltd METHOD FOR THE TREATMENT OF A DISEASE OR A SENSE OF THE CENTRAL NERVOUS SYSTEM
CN103183675A (zh) * 2011-12-27 2013-07-03 山东轩竹医药科技有限公司 磷酸二酯酶-4抑制剂
CN102643268B (zh) * 2011-12-30 2014-05-21 沈阳药科大学 喹啉类及噌啉类化合物及其应用
US20150119399A1 (en) 2012-01-10 2015-04-30 President And Fellows Of Harvard College Beta-cell replication promoting compounds and methods of their use
CN103214478B (zh) * 2012-01-19 2015-07-15 山东轩竹医药科技有限公司 吡啶并氧代哒嗪衍生物
PE20151332A1 (es) 2013-02-19 2015-09-20 Pfizer Compuestos de azabencimidazol
WO2016012896A1 (en) 2014-07-24 2016-01-28 Pfizer Inc. Pyrazolopyrimidine compounds
CN106795165B (zh) 2014-08-06 2019-09-10 辉瑞公司 咪唑并哒嗪化合物
CN113423435A (zh) 2018-12-28 2021-09-21 雷杰纳荣制药公司 使用花生四烯酸15-脂氧合酶(alox15)抑制剂治疗呼吸系统病症

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9212693D0 (en) 1992-06-15 1992-07-29 Celltech Ltd Chemical compounds
GB9212673D0 (en) 1992-06-15 1992-07-29 Celltech Ltd Chemical compounds
EP0577024B1 (de) 1992-07-01 1996-10-16 Hoechst Aktiengesellschaft 3,4,5-Substituierte Benzoylguanidine, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament
GB9222253D0 (en) 1992-10-23 1992-12-09 Celltech Ltd Chemical compounds
US5622977A (en) 1992-12-23 1997-04-22 Celltech Therapeutics Limited Tri-substituted (aryl or heteroaryl) derivatives and pharmaceutical compositions containing the same
GB9226830D0 (en) 1992-12-23 1993-02-17 Celltech Ltd Chemical compounds
DE4306152A1 (de) 1993-02-27 1994-09-01 Hoechst Ag Positiv arbeitendes strahlungsempfindliches Gemisch und damit hergestelltes Aufzeichnungsmaterial
GB9304920D0 (en) 1993-03-10 1993-04-28 Celltech Ltd Chemical compounds
GB9304919D0 (en) 1993-03-10 1993-04-28 Celltech Ltd Chemical compounds
US5455252A (en) 1993-03-31 1995-10-03 Syntex (U.S.A.) Inc. Optionally substituted 6,8-quinolines
DE4318756A1 (de) 1993-06-05 1994-12-08 Hoechst Ag Substituierte Benzoylguanidine, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament
GB9326600D0 (en) 1993-12-22 1994-03-02 Celltech Ltd Chemical compounds
GB9326173D0 (en) 1993-12-22 1994-02-23 Celltech Ltd Chemical compounds and process
ATE260911T1 (de) 1993-12-22 2004-03-15 Celltech R&D Ltd Trisubstituierte phenyl-derivate, verfahren zu deren herstellung und deren verwendung als phosphodiesterase (typ iv) hemmstoffe
US5786354A (en) 1994-06-21 1998-07-28 Celltech Therapeutics, Limited Tri-substituted phenyl derivatives and processes for their preparation
US6245774B1 (en) 1994-06-21 2001-06-12 Celltech Therapeutics Limited Tri-substituted phenyl or pyridine derivatives
GB9412573D0 (en) 1994-06-22 1994-08-10 Celltech Ltd Chemical compounds
GB9412571D0 (en) 1994-06-22 1994-08-10 Celltech Ltd Chemical compounds
GB9412672D0 (en) 1994-06-23 1994-08-10 Celltech Ltd Chemical compounds
EP0765867A1 (de) 1995-09-27 1997-04-02 Hoechst Aktiengesellschaft Substituierte Benzoylguanidine, Verfahren zu ihrer Herstellung, ihre Verwendung als Antiarrhytmika oder Diagnostikum sowie sie enthaltendes Medikament
GB9526246D0 (en) 1995-12-21 1996-02-21 Celltech Therapeutics Ltd Chemical compounds
GB9526243D0 (en) 1995-12-21 1996-02-21 Celltech Therapeutics Ltd Chemical compounds
GB9526245D0 (en) 1995-12-21 1996-02-21 Celltech Therapeutics Ltd Chemical compounds
DE19622370A1 (de) 1996-06-04 1997-12-11 Hoechst Ag Ortho-substituierte Benzoylguanidine, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament
GB9625184D0 (en) 1996-12-04 1997-01-22 Celltech Therapeutics Ltd Chemical compounds
ATE244216T1 (de) 1996-12-11 2003-07-15 Abbott Gmbh & Co Kg Ketobenzamide als calpain-inhibitoren
CA2268190A1 (en) 1997-08-06 1999-02-18 Suntory Limited 1-aryl-1,8-naphthylidin-4-one derivative as type iv phosphodiesterase inhibitor
WO1999009504A1 (en) 1997-08-20 1999-02-25 First Data Corporation Interactive tax payment system
EP0978516A4 (en) 1998-01-29 2001-01-10 Suntory Ltd 1-CYCLOALKYL-1,8-NAPHTHYRIDINE-4-ONE DERIVATIVES HAVING PHOSPHODIESTERASE IV INHIBITING ACTIVITY
CA2340180A1 (en) * 1998-08-11 2000-02-24 Pfizer Products Inc. 1-aryl,-3-arylmethyl-1,8-naphthyridn-2(1h)-ones
JO2311B1 (en) * 2001-08-29 2005-09-12 ميرك فروست كندا ليمتد Alkyl inhibitors Ariel phosphodiesterase-4
IS7839A (is) * 2002-11-22 2004-05-23 Merck Frosst Canada Ltd. 4-oxó-1-(3-setið fenýl-1,4-díhýdró-1,8-naftýridín-3-karboxamíð fosfódíesterasa-4 hindrar

Also Published As

Publication number Publication date
JO2311B1 (en) 2005-09-12
AR036365A1 (es) 2004-09-01
PL367716A1 (en) 2005-03-07
NO20041293D0 (no) 2004-03-26
UA75957C2 (en) 2006-06-15
RS17004A (sr) 2007-02-05
ECSP044992A (es) 2004-04-28
IL160213A0 (en) 2004-07-25
NO330521B1 (no) 2011-05-09
EP1436290A1 (en) 2004-07-14
DOP2002000456A (es) 2003-02-28
WO2003018579A1 (en) 2003-03-06
CN100338061C (zh) 2007-09-19
US6743802B2 (en) 2004-06-01
MXPA04001889A (es) 2004-06-15
JP2005508313A (ja) 2005-03-31
NO20041293L (no) 2004-05-27
JP4157035B2 (ja) 2008-09-24
AU2002322940B2 (en) 2007-03-01
US20030114478A1 (en) 2003-06-19
HK1080073A1 (en) 2006-04-21
CA2456817A1 (en) 2003-03-06
CA2456817C (en) 2010-11-30
NZ530931A (en) 2005-12-23
ZA200400952B (en) 2004-10-22
KR100928849B1 (ko) 2009-11-30
GEP20063805B (en) 2006-04-25
HUP0401729A3 (en) 2012-09-28
US20050070569A1 (en) 2005-03-31
IS7138A (is) 2004-01-30
EP2305677A1 (en) 2011-04-06
EP1436290B1 (en) 2013-09-18
EP1436290B8 (en) 2013-12-04
KR20040034672A (ko) 2004-04-28
HK1080073B (zh) 2008-08-08
CN1639161A (zh) 2005-07-13
PE20030416A1 (es) 2003-05-15
BR0212042A (pt) 2004-08-17
EA200400361A1 (ru) 2004-08-26
HRP20040151A2 (en) 2006-05-31
EA006800B1 (ru) 2006-04-28

Similar Documents

Publication Publication Date Title
HUP0401729A2 (hu) IV típusú foszfodiészteráz inhibitor hatású alkin-aril-naftiridin-4(1H)-on-származékok és ezeket tartalmazó gyógyszerkészítmények
CA2475432A1 (en) 2,4,6-triamino-1,3,5-triazine derivative
FI891548A0 (fi) Administrering av monoaminakridiner i kolinergiska bristtillstaond av nervceller.
NO20015447D0 (no) Kinolinderivater som inhibitorer av MEK enzymer
HUP0303124A2 (hu) IKB-Kináz (IKK-béta) gátló aktivitással rendelkező piridinszármazékok, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
AR018175A1 (es) Compuestos de indol-3-glioxilamidas sustituidas, utiles como medicamentos antitumorales, composiciones farmaceuticas formuladas con dichos derivados,utilizacion de dichos derivados para la preparacion de medicamentos antitumorales y los medicamentos asi preparados.
HUP0400704A2 (hu) Heterociklusos éterrel szubsztituált imidazokinolinok, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
MEP24608A (en) Azetidine derivatives, preparation thereof and pharmaceutical compositions containing same
HUP0202263A2 (hu) Benzimidazol-, indol- és imidazo-piridin-származékok és ezeket tartalmazó gyógyszerkészítmények
HUP0301311A2 (hu) N-oxidok mint 4-fenil-piridin-származékok előgyógyszerei, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
MY111190A (en) Substituted thiazolidinedione derivatives
HUP0303756A2 (hu) 1-Aril- vagy 1-alkilszulfonil-heterociklobenzazolok és eljárás ezek elõállítására és ezeket tartalmazó gyógyszerkészítmények
WO2003055441A3 (en) Medicaments
HUP0102563A2 (hu) Indolszármazékok és alkalmazásuk rosszindulatú és egyéb, patológiás sejtproliferáción alapuló megbetegedések kezelésére
HUP0103256A2 (hu) Tio-benzimidazol-származékok, és a vegyületeket tartalmazó gyógyászati készítmények
JP2008513485A5 (hu)
EP0322738A3 (en) Benzylidene-malononitrile derivatives for the inhibition of proliferative processes in mammalian cells
ATE370735T1 (de) Phenylpyridazinderivate und diese enthaltende arzneimittel
TR199902367T2 (xx) 16-Hidroksi-11-(ikameli fenil)-estra-4,9-dien t�revleri.
HUP0103896A2 (hu) Oxigéntartalmú heterociklusos vegyületek, ezeket tartalmazó gyógyászati készítmények és alkalmazásuk
KR920019746A (ko) 신규한 시클로헥실벤즈아미드 유도체, 그의 제조방법 및 약제로서의 용도
WO2003082861A3 (en) Morpholinyl-urea derivatives for use of the treatment of inflammatory diseases
NO995638L (no) Heterobicykliske forbindelser til fremstilling av pyridonkarboksylsyrederivater
HUP0003577A2 (hu) Tetrahidro-gamma-karbolinok, eljárás előállításukra, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények
CA2334317A1 (en) Antiviral pyrimidinedione derivatives and process for the preparation thereof

Legal Events

Date Code Title Description
GB9A Succession in title

Owner name: MERCK FROSST CANADA LTD., CA

Free format text: FORMER OWNER(S): MERCK FROSST CANADA & CO., CA

FD9A Lapse of provisional protection due to non-payment of fees