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CY1111596T1 - Υποκατεστημενες ακετοφαινονες χρησιμες ως αναστολεις pde4 - Google Patents

Υποκατεστημενες ακετοφαινονες χρησιμες ως αναστολεις pde4

Info

Publication number
CY1111596T1
CY1111596T1 CY20111100615T CY111100615T CY1111596T1 CY 1111596 T1 CY1111596 T1 CY 1111596T1 CY 20111100615 T CY20111100615 T CY 20111100615T CY 111100615 T CY111100615 T CY 111100615T CY 1111596 T1 CY1111596 T1 CY 1111596T1
Authority
CY
Cyprus
Prior art keywords
represent
independently
pde4 inhibitors
haloalkyl
hydroxyalkyl
Prior art date
Application number
CY20111100615T
Other languages
English (en)
Inventor
Jakob Felding
Simon Feldbaek Nielsen
Original Assignee
Leo Pharma A/S
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 Leo Pharma A/S filed Critical Leo Pharma A/S
Publication of CY1111596T1 publication Critical patent/CY1111596T1/el

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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 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
    • C07D213/61Halogen atoms or nitro radicals
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Toxicology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Η παρούσα εφεύρεση αφορά ένωση σύμφωνα με τον τύπο: (I), όπου τα Χ1, Χ2, Χ3, Χ4 και Χ5 ανεξαρτήτως το ένα από το άλλο αντιπροσωπεύουν -CH- ή Ν, ή τα Χ3, Χ4 και Χ5 ανεξαρτήτως το ένα από το άλλο αντιπροσωπεύουν -CH- ή Ν, και τα Χ1 και Χ2 ανεξαρτήτως το ένα από το άλλο αντιπροσωπεύουν C και σχηματίζουν τμήμα ενός επιπλέον 6-μελούς αρωματικού δακτυλίου, το R1 αντιπροσωπεύει υδρογόνο, αλκυλ, αλκενυλ, αλκυνυλ, αλογονοαλκυλ, υδροξυαλκυλ, ή αλκυλκαρβονυλ, όλα από τα οποία είναι προαιρετικώς υποκατεστημένα, τα R2 και R3 ανεξαρτήτως αντιπροσωπεύουν υδρογόνο, -CH2-C(O)NR-R', αλκυλ, κυκλοαλκυλ, αλκενυλ, κυκλοαλκενυλ, αλκυνυλ, αλογονοαλκυλ, υδροξυαλκυλ, ετεροκυκλοαλκενυλ, αλκυλαρυλ, αρυλαλκυλ, αλκυλαλκοξυκαρβονυλ, αλκυλκαρβονυλοξυ, ή αλκοξυαλκυλ, όλα από τα οποία είναι προαιρετικώς υποκατεστημένα, το R11 αντιπροσωπεύει υδρογόνο, αλογόνο, κυανό, αμινο, αλκοξυ ή αλκυλαμινο, τα Χ1-Χ5 αντιπροσωπεύουν -CH- ή Ν, συμπεριλαμβανομένων Ν-οξειδίων, εναντιομερών και διαστερεομερών, και φαρμακευτικώς αποδεκτά άλατα, υδρίτες, ή διαλυτώματα αυτών. Η εφεύρεση περαιτέρω αφορά διεργασίες για την παρασκευή των εν λόγω ενώσεων, τις εν λόγω ενώσεις για χρήση στη θεραπεία, φαρμακευτικές συνθέσεις που περιλαμβάνουν τις εν λόγω ενώσεις, μεθόδους θεραπείας ασθενειών, π.χ., δερματικών ασθενειών, με τις εν λόγω ενώσεις, και τη χρήση των εν λόγω ενώσεων στην κατασκευή φαρμάκων.
CY20111100615T 2006-12-22 2011-06-28 Υποκατεστημενες ακετοφαινονες χρησιμες ως αναστολεις pde4 CY1111596T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US87168906P 2006-12-22 2006-12-22
US94547007P 2007-06-21 2007-06-21
EP07846434A EP2125736B1 (en) 2006-12-22 2007-12-21 Substituted acetophenones useful as pde4 inhibitors

Publications (1)

Publication Number Publication Date
CY1111596T1 true CY1111596T1 (el) 2015-10-07

Family

ID=39156588

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20111100615T CY1111596T1 (el) 2006-12-22 2011-06-28 Υποκατεστημενες ακετοφαινονες χρησιμες ως αναστολεις pde4

Country Status (24)

Country Link
US (3) US8148537B2 (el)
EP (1) EP2125736B1 (el)
JP (1) JP5342451B2 (el)
KR (1) KR101507717B1 (el)
AT (1) ATE503742T1 (el)
AU (1) AU2007336538B2 (el)
BR (1) BRPI0721113A2 (el)
CA (1) CA2673370C (el)
CR (1) CR10877A (el)
CY (1) CY1111596T1 (el)
DE (1) DE602007013617D1 (el)
DK (1) DK2125736T3 (el)
GT (1) GT200900172A (el)
HK (1) HK1135392A1 (el)
HR (1) HRP20110464T1 (el)
IL (1) IL199383A (el)
MX (1) MX2009006593A (el)
MY (1) MY146022A (el)
NO (1) NO20092372L (el)
NZ (1) NZ577863A (el)
PL (1) PL2125736T3 (el)
PT (1) PT2125736E (el)
RU (1) RU2493149C2 (el)
WO (1) WO2008077404A1 (el)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2012007229A (es) 2009-12-22 2012-07-30 Leo Pharma As Composicion cutanea que comprende analogo de vitamina d y mezcla de solvente y tensioactivos.
US20130023501A1 (en) 2009-12-22 2013-01-24 Leo Pharma A/S Pharmaceutical composition comprising solvent mixture and a vitamin d derivative or analogue
CA2785253A1 (en) 2009-12-22 2011-06-30 Leo Pharma A/S Calcipotriol monohydrate nanocrystals
CN102775345A (zh) * 2011-05-13 2012-11-14 上海特化医药科技有限公司 制备罗氟司特的方法及中间体
RU2663448C2 (ru) * 2012-11-30 2018-08-06 Лео Фарма А/С Способ ингибирования экспрессии ил-22 активированными т-клетками
WO2014096018A1 (en) * 2012-12-19 2014-06-26 Leo Pharma A/S Methods for the preparation of substituted acetophenones
EP4059921A1 (en) 2013-10-22 2022-09-21 Chiesi Farmaceutici S.p.A. Process for the preparation of a pde4 inhibitor
BR112016029510A2 (pt) 2014-06-23 2017-08-22 Leo Pharma As métodos para a preparação de um composto, e, composto intermediário.
WO2017089347A1 (en) 2015-11-25 2017-06-01 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods and pharmaceutical compositions for the treatment of braf inhibitor resistant melanomas
DK3390407T3 (da) 2015-12-18 2023-11-06 Union Therapeutics As Fremgangsmåder til fremstilling af heterocykliske 1,3-benzodioxolforbindelser
KR101702648B1 (ko) * 2016-05-10 2017-02-03 주식회사 엑티브온 피부 외용제용 보존제, 이를 포함하는 화장료 조성물 및 약학 조성물
BR112019025028A2 (pt) 2017-06-20 2020-06-16 Leo Pharma A/S Método para preparar um composto.

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW263495B (el) * 1992-12-23 1995-11-21 Celltech Ltd
GB9401460D0 (en) * 1994-01-26 1994-03-23 Rhone Poulenc Rorer Ltd Compositions of matter
DE69636086T2 (de) * 1995-05-19 2006-11-30 Kyowa Hakko Kogyo Co., Ltd. Sauerstoff enthaltende heterocyclische verbindungen
US6514996B2 (en) * 1995-05-19 2003-02-04 Kyowa Hakko Kogyo Co., Ltd. Derivatives of benzofuran or benzodioxole
EP0943613A4 (en) * 1996-11-19 2002-07-10 Kyowa Hakko Kogyo Kk HETEROCYCLIC COMPOUNDS CONTAINING OXYGEN
WO2004082683A1 (ja) * 2003-03-17 2004-09-30 Kyowa Hakko Kogyo Co., Ltd. 慢性皮膚疾患の治療および/または予防剤
WO2006040645A1 (en) * 2004-10-11 2006-04-20 Ranbaxy Laboratories Limited N-(3,5-dichloropyridin-4-yl)-2,4,5-alkoxy and 2,3,4-alkoxy benzamide derivatives as pde-iv (phophodiesterase type-iv) inhibitors for the treatment of inflammatory diseases such as asthma
CA2611562A1 (en) * 2005-06-10 2006-12-21 Memory Pharmaceuticals Corporation Trisubstituted amines as phosphodiesterase 4 inhibitors

Also Published As

Publication number Publication date
US8497380B2 (en) 2013-07-30
CR10877A (es) 2009-07-10
US8148537B2 (en) 2012-04-03
PT2125736E (pt) 2011-07-01
AU2007336538A1 (en) 2008-07-03
HK1135392A1 (en) 2010-06-04
CA2673370A1 (en) 2008-07-03
DE602007013617D1 (de) 2011-05-12
US20130012716A1 (en) 2013-01-10
MX2009006593A (es) 2009-07-02
JP5342451B2 (ja) 2013-11-13
RU2493149C2 (ru) 2013-09-20
GT200900172A (es) 2011-10-05
US20120165539A1 (en) 2012-06-28
HRP20110464T1 (hr) 2011-07-31
ATE503742T1 (de) 2011-04-15
US8324394B2 (en) 2012-12-04
NZ577863A (en) 2012-04-27
US20100035908A1 (en) 2010-02-11
KR20090098990A (ko) 2009-09-18
DK2125736T3 (da) 2011-07-11
JP2010513334A (ja) 2010-04-30
EP2125736B1 (en) 2011-03-30
WO2008077404A1 (en) 2008-07-03
BRPI0721113A2 (pt) 2014-10-07
PL2125736T3 (pl) 2011-09-30
KR101507717B1 (ko) 2015-04-08
AU2007336538B2 (en) 2012-04-05
EP2125736A1 (en) 2009-12-02
IL199383A (en) 2015-02-26
RU2009128191A (ru) 2011-01-27
CA2673370C (en) 2015-11-17
NO20092372L (no) 2009-07-14
MY146022A (en) 2012-06-15

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