CY1111596T1 - Υποκατεστημενες ακετοφαινονες χρησιμες ως αναστολεις pde4 - Google Patents
Υποκατεστημενες ακετοφαινονες χρησιμες ως αναστολεις pde4Info
- 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
Links
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 title 1
- 150000008062 acetophenones Chemical class 0.000 title 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- -1 cyano, amino Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002500 effect on skin Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- 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
-
- 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
- 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
- A61P17/04—Antipruritics
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
-
- 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
- A61P17/10—Anti-acne agents
-
- 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
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- 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
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/12—Heterocyclic 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)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Toxicology (AREA)
- Epidemiology (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.
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 (23)
| 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) |
| 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 (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5732471B2 (ja) | 2009-12-22 | 2015-06-10 | レオ ファーマ アクティーゼルスカブ | 溶媒混合物およびビタミンd誘導体から成る医薬品組成物または類似体 |
| RU2555339C2 (ru) | 2009-12-22 | 2015-07-10 | Лео Фарма А/С | Нанокристаллы кальципотриола моногидрита |
| US20120322776A1 (en) | 2009-12-22 | 2012-12-20 | Leo Pharma A/S | Cutaneous composition comprising vitamin d analogue and a mixture of solvent and surfactants |
| 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 |
| WO2014083099A1 (en) * | 2012-11-30 | 2014-06-05 | Leo Pharma A/S | A method of inhibiting the expression of il-22 in activated t-cells |
| WO2014096018A1 (en) * | 2012-12-19 | 2014-06-26 | Leo Pharma A/S | Methods for the preparation of substituted acetophenones |
| HRP20240783T1 (hr) * | 2013-10-22 | 2024-09-27 | Chiesi Farmaceutici S.P.A. | Postupak priprave inhibitora pde4 |
| AU2015279428B2 (en) * | 2014-06-23 | 2018-02-15 | Leo Pharma A/S | Methods for the preparation of 1,3-benzodioxole heterocyclic compounds |
| 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 |
| TWI732808B (zh) | 2015-12-18 | 2021-07-11 | 丹麥商理奧藥品公司 | 1,3-苯并二氧雜環戊烯雜環化合物之製備方法 |
| KR101702648B1 (ko) * | 2016-05-10 | 2017-02-03 | 주식회사 엑티브온 | 피부 외용제용 보존제, 이를 포함하는 화장료 조성물 및 약학 조성물 |
| WO2018234299A1 (en) | 2017-06-20 | 2018-12-27 | Leo Pharma A/S | Methods for the preparation of 1,3-benzodioxole heterocyclic compounds |
| EP3838967A1 (en) | 2019-12-16 | 2021-06-23 | Spago Nanomedical AB | Immobilization of phenolic compounds |
| CN117924243B (zh) * | 2024-01-16 | 2025-09-12 | 沈阳药科大学 | 一种喹啉衍生物及其药用组合物和应用 |
Family Cites Families (8)
| 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 |
| US6514996B2 (en) * | 1995-05-19 | 2003-02-04 | Kyowa Hakko Kogyo Co., Ltd. | Derivatives of benzofuran or benzodioxole |
| DK0771794T3 (da) * | 1995-05-19 | 2006-09-11 | Kyowa Hakko Kogyo Kk | Oxygenholdige heterocykliske forbindelser |
| EP0943613A4 (en) * | 1996-11-19 | 2002-07-10 | Kyowa Hakko Kogyo Kk | Oxygenic heterocyclic compounds |
| AU2004222432A1 (en) * | 2003-03-17 | 2004-09-30 | Kyowa Hakko Kogyo Co., Ltd. | Therapeutic and/or preventive agent for chronic skin disease |
| 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 |
| JP2008543781A (ja) * | 2005-06-10 | 2008-12-04 | メモリー・ファーマシューティカルズ・コーポレイション | ホスフオジエステラーゼ4阻害剤 |
-
2007
- 2007-12-21 DE DE602007013617T patent/DE602007013617D1/de active Active
- 2007-12-21 DK DK07846434.4T patent/DK2125736T3/da active
- 2007-12-21 KR KR1020097015481A patent/KR101507717B1/ko not_active Expired - Fee Related
- 2007-12-21 WO PCT/DK2007/000564 patent/WO2008077404A1/en not_active Ceased
- 2007-12-21 MY MYPI20092592A patent/MY146022A/en unknown
- 2007-12-21 BR BRPI0721113-9A2A patent/BRPI0721113A2/pt not_active Application Discontinuation
- 2007-12-21 MX MX2009006593A patent/MX2009006593A/es active IP Right Grant
- 2007-12-21 JP JP2009541766A patent/JP5342451B2/ja not_active Expired - Fee Related
- 2007-12-21 CA CA2673370A patent/CA2673370C/en not_active Expired - Fee Related
- 2007-12-21 US US12/520,325 patent/US8148537B2/en not_active Expired - Fee Related
- 2007-12-21 RU RU2009128191/04A patent/RU2493149C2/ru not_active IP Right Cessation
- 2007-12-21 NZ NZ577863A patent/NZ577863A/en not_active IP Right Cessation
- 2007-12-21 HR HR20110464T patent/HRP20110464T1/hr unknown
- 2007-12-21 AT AT07846434T patent/ATE503742T1/de active
- 2007-12-21 AU AU2007336538A patent/AU2007336538B2/en not_active Ceased
- 2007-12-21 PL PL07846434T patent/PL2125736T3/pl unknown
- 2007-12-21 EP EP07846434A patent/EP2125736B1/en active Active
- 2007-12-21 PT PT07846434T patent/PT2125736E/pt unknown
-
2009
- 2009-06-16 IL IL199383A patent/IL199383A/en active IP Right Grant
- 2009-06-19 GT GT200900172A patent/GT200900172A/es unknown
- 2009-06-19 CR CR10877A patent/CR10877A/es unknown
- 2009-06-22 NO NO20092372A patent/NO20092372L/no not_active Application Discontinuation
-
2011
- 2011-06-28 CY CY20111100615T patent/CY1111596T1/el unknown
-
2012
- 2012-02-28 US US13/406,932 patent/US8324394B2/en not_active Expired - Fee Related
- 2012-07-11 US US13/546,758 patent/US8497380B2/en not_active Expired - Fee Related
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