CY1113764T1 - Βενζοϊκου οξεος (1-φαινυλ-2-πυριδιν-4-υλ) αιθυλ εστερες ως αναστολεις φωσφοδιεστερασης - Google Patents

Βενζοϊκου οξεος (1-φαινυλ-2-πυριδιν-4-υλ) αιθυλ εστερες ως αναστολεις φωσφοδιεστερασης

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Publication number
CY1113764T1
CY1113764T1 CY20121101183T CY121101183T CY1113764T1 CY 1113764 T1 CY1113764 T1 CY 1113764T1 CY 20121101183 T CY20121101183 T CY 20121101183T CY 121101183 T CY121101183 T CY 121101183T CY 1113764 T1 CY1113764 T1 CY 1113764T1
Authority
CY
Cyprus
Prior art keywords
inhibitors
phosphosteration
fenyl
estes
pyridin
Prior art date
Application number
CY20121101183T
Other languages
English (en)
Inventor
Gabriele Amari
Elisabetta Armani
Maurizio Delcanale
Original Assignee
Chiesi Farmaceutici S.P.A.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40674203&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CY1113764(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Chiesi Farmaceutici S.P.A. filed Critical Chiesi Farmaceutici S.P.A.
Publication of CY1113764T1 publication Critical patent/CY1113764T1/el

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M15/00—Inhalators
    • A61M15/0065—Inhalators with dosage or measuring devices
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • 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
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M16/00—Devices for influencing the respiratory system of patients by gas treatment, e.g. mouth-to-mouth respiration; Tracheal tubes
    • A61M16/10—Preparation of respiratory gases or vapours
    • A61M16/14—Preparation of respiratory gases or vapours by mixing different fluids, one of them being in a liquid phase
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • 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
    • C07D213/60—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 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
    • C07D213/61—Halogen atoms or nitro radicals
    • 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
    • C07D213/89—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 with hetero atoms directly attached to the ring nitrogen atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Emergency Medicine (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Η παρούσα εφεύρεση αφορά σε αναστολείς του ενζύμου φωσφοδιεστεράση 4 (PDE4). Ειδικότερα, η εφεύρεση αφορά σε ενώσεις οι οποίες είναι παράγωγα -φαινύλ-2-πυριδινύλ αλκύλ αλκοολών, μεθόδους παρασκευής τέτοιων ενώσεων, συνθέσεις που περιλαμβάνουν αυτές, συνδυασμούς και θεραπευτικές χρήσεις αυτών (I) όπου το n είναι Ο ή I, τα R1 και R2 μπορεί να είναι τα ίδια ή διαφορετικά και επιλέγονται από την ομάδα που αποτελείται από: - γραμμική ή διακλαδισμένη C1-C6 αλκύλ, -OR3 όπου το R3 είναι C1-C6 αλκύλ προαιρετικά υποκατεστημένο με μία ή περισσότερες C3-C7 κυκλοαλκύλ ομάδες και - HNSO2R4 όπου το R4 είναι C1-C4 αλκύλ προαιρετικά υποκατεστημένο με ένα ή περισσότερα άτομα αλογόνου ή με C1-C4 ομάδα, όπου τουλάχιστον ένα των R1 και R2 είναι HNSO2R4. Οι άλλες μεταβλητές είναι όπως ορίζεται στις αξιώσεις.
CY20121101183T 2009-02-06 2012-12-04 Βενζοϊκου οξεος (1-φαινυλ-2-πυριδιν-4-υλ) αιθυλ εστερες ως αναστολεις φωσφοδιεστερασης CY1113764T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09001660A EP2216327A1 (en) 2009-02-06 2009-02-06 Benzoic acid (1-phenyl-2-pyridin-4-yl)ethyl esters as phosphodiesterase inhibitors
EP10704746A EP2393782B1 (en) 2009-02-06 2010-02-04 Benzoic acid (1-phenyl-2-pyridin-4-yl) ethyl esters as phosphodiesterase inhibitors

Publications (1)

Publication Number Publication Date
CY1113764T1 true CY1113764T1 (el) 2016-07-27

Family

ID=40674203

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20121101183T CY1113764T1 (el) 2009-02-06 2012-12-04 Βενζοϊκου οξεος (1-φαινυλ-2-πυριδιν-4-υλ) αιθυλ εστερες ως αναστολεις φωσφοδιεστερασης

Country Status (34)

Country Link
US (5) US8440834B2 (el)
EP (2) EP2216327A1 (el)
JP (2) JP5612610B2 (el)
KR (1) KR101337728B1 (el)
CN (1) CN102317262B (el)
AR (1) AR075243A1 (el)
AU (1) AU2010211274B2 (el)
BR (1) BRPI1005695A8 (el)
CA (1) CA2751494C (el)
CL (1) CL2011001876A1 (el)
CO (1) CO6400217A2 (el)
CY (1) CY1113764T1 (el)
EA (1) EA019113B1 (el)
ES (1) ES2395528T3 (el)
GE (1) GEP20135919B (el)
HK (1) HK1162508A1 (el)
HR (1) HRP20121004T1 (el)
IL (1) IL214446A (el)
JO (1) JO2761B1 (el)
MA (1) MA33105B1 (el)
ME (1) ME02325B (el)
MX (1) MX2011007857A (el)
MY (1) MY152048A (el)
NZ (1) NZ594413A (el)
PE (1) PE20120055A1 (el)
PL (1) PL2393782T3 (el)
PT (1) PT2393782E (el)
RS (1) RS52605B (el)
SG (1) SG173208A1 (el)
SI (1) SI2393782T1 (el)
TN (1) TN2011000346A1 (el)
TW (1) TWI459945B (el)
UA (1) UA102574C2 (el)
WO (1) WO2010089107A1 (el)

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EP2216327A1 (en) * 2009-02-06 2010-08-11 CHIESI FARMACEUTICI S.p.A. Benzoic acid (1-phenyl-2-pyridin-4-yl)ethyl esters as phosphodiesterase inhibitors
AU2011287711B2 (en) * 2010-08-03 2016-10-27 Chiesi Farmaceutici S.P.A. Dry powder formulation comprising a phosphodiesterase inhibitor
CA2807406C (en) * 2010-08-03 2018-12-11 Chiesi Farmaceutici S.P.A. Pharmaceutical formulation comprising a phosphodiesterase inhibitor
WO2012168226A1 (en) * 2011-06-06 2012-12-13 Chiesi Farmaceutici S.P.A. Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors
WO2013045280A1 (en) 2011-09-26 2013-04-04 Chiesi Farmaceutici S.P.A. Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors
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CN104822659A (zh) * 2012-12-05 2015-08-05 奇斯药制品公司 作为磷酸二酯酶抑制剂的1-苯基-2-吡啶基烷基醇衍生物
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US9763924B2 (en) * 2014-06-05 2017-09-19 Chiesi Farmaceutici S.P.A. Aminoester derivatives
US9326976B2 (en) 2014-06-05 2016-05-03 Chiesi Farmaceutici S.P.A. Carbamate derivatives
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
EP3487501A1 (en) * 2016-07-20 2019-05-29 Allergan, Inc. Methods, compositions, and compounds for treatment of dermatological and ocular conditions
EP3732164A1 (en) * 2017-12-28 2020-11-04 Chiesi Farmaceutici S.p.A. Use of 1-phenyl-2-pyridinyl alkyl alcohol derivatives for treating cystic fibrosis
CN112469443B (zh) 2018-07-27 2024-04-16 奇斯药制品公司 用于吸入用干粉制剂的新型载体颗粒
CN115466169B (zh) * 2021-06-10 2024-03-26 中国医学科学院药物研究所 取代邻苯二酚醚类化合物及其制备方法和应用
WO2023117985A1 (en) 2021-12-21 2023-06-29 Chiesi Farmaceutici S.P.A. Dry powder formulations filled in an inhaler with improved resistance to humidity
WO2023208982A1 (en) 2022-04-27 2023-11-02 Chiesi Farmaceutici S.P.A. Crystal form of a pde4 inhibitor
WO2024027901A1 (en) 2022-08-02 2024-02-08 Chiesi Farmaceutici S.P.A. Predictive biomarker of clinical response to a pde4 inhibitor
WO2024062007A1 (en) 2022-09-22 2024-03-28 Chiesi Farmaceutici S.P.A. Capsule inhaler for the administration of a phosphodiesterase-4 inhibitor
WO2024062006A1 (en) 2022-09-22 2024-03-28 Chiesi Farmaceutici S.P.A. Capsule inhaler for the administration of a phosphodiesterase-4 inhibitor
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WO2013045280A1 (en) 2011-09-26 2013-04-04 Chiesi Farmaceutici S.P.A. Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors
BR112014009471A2 (pt) 2011-10-21 2017-04-18 Chiesi Farm Spa compostos, combinação de um composto, composição farmacêutica, uso de um composto, dispositivo e kit
RU2637945C2 (ru) 2012-06-04 2017-12-08 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Производные 1-фенил-2-пиридинил-алкиловых спиртов в качестве ингибиторов фосфодиэстеразы
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EP2393782A1 (en) 2011-12-14
MA33105B1 (fr) 2012-03-01
EA201190099A1 (ru) 2012-02-28
MY152048A (en) 2014-08-15
CL2011001876A1 (es) 2011-10-28
US20130289010A1 (en) 2013-10-31
TWI459945B (zh) 2014-11-11
BRPI1005695A8 (pt) 2017-12-26
JO2761B1 (en) 2014-03-15
CA2751494A1 (en) 2010-08-12
GEP20135919B (en) 2013-09-10
ME02325B (me) 2016-06-20
PT2393782E (pt) 2012-12-26
IL214446A0 (en) 2011-09-27
US8648204B2 (en) 2014-02-11
US20100204256A1 (en) 2010-08-12
KR101337728B1 (ko) 2013-12-09
HK1162508A1 (en) 2012-08-31
US9056176B2 (en) 2015-06-16
BRPI1005695A2 (pt) 2017-06-06
AR075243A1 (es) 2011-03-16
AU2010211274B2 (en) 2016-03-17
JP2012516863A (ja) 2012-07-26
US20130012487A1 (en) 2013-01-10
US8859778B2 (en) 2014-10-14
SG173208A1 (en) 2011-09-29
TW201032804A (en) 2010-09-16
WO2010089107A1 (en) 2010-08-12
AU2010211274A1 (en) 2011-08-25
ES2395528T3 (es) 2013-02-13
JP5612610B2 (ja) 2014-10-22
PL2393782T3 (pl) 2013-02-28
US20140179647A1 (en) 2014-06-26
CN102317262B (zh) 2014-08-06
CO6400217A2 (es) 2012-03-15
US8440834B2 (en) 2013-05-14
SI2393782T1 (sl) 2013-01-31
US20140378423A1 (en) 2014-12-25
JP2015038079A (ja) 2015-02-26
RS52605B (en) 2013-04-30
KR20110094356A (ko) 2011-08-23
IL214446A (en) 2014-12-31
CN102317262A (zh) 2012-01-11
PE20120055A1 (es) 2012-02-16
HRP20121004T1 (hr) 2012-12-31
EP2393782B1 (en) 2012-09-12
CA2751494C (en) 2017-03-07
EP2216327A1 (en) 2010-08-11
MX2011007857A (es) 2011-08-15
EA019113B1 (ru) 2014-01-30
TN2011000346A1 (en) 2013-03-27
UA102574C2 (ru) 2013-07-25
NZ594413A (en) 2013-05-31

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