AR078142A1 - Compuestos inhibidores heteroarilicos biciclicos de pde4, las composiciones farmaceuticas que los contienen y el uso de los mismos para la preparacion de medicamentos. - Google Patents
Compuestos inhibidores heteroarilicos biciclicos de pde4, las composiciones farmaceuticas que los contienen y el uso de los mismos para la preparacion de medicamentos.Info
- Publication number
- AR078142A1 AR078142A1 ARP100103047A ARP100103047A AR078142A1 AR 078142 A1 AR078142 A1 AR 078142A1 AR P100103047 A ARP100103047 A AR P100103047A AR P100103047 A ARP100103047 A AR P100103047A AR 078142 A1 AR078142 A1 AR 078142A1
- Authority
- AR
- Argentina
- Prior art keywords
- hyderoarilic
- medicines
- bicycle
- preparation
- pharmaceutical compositions
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 title 1
- MSYGAHOHLUJIKV-UHFFFAOYSA-N 3,5-dimethyl-1-(3-nitrophenyl)-1h-pyrazole-4-carboxylic acid ethyl ester Chemical compound CC1=C(C(=O)OCC)C(C)=NN1C1=CC=CC([N+]([O-])=O)=C1 MSYGAHOHLUJIKV-UHFFFAOYSA-N 0.000 abstract 2
- 102000011017 Type 4 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 abstract 2
- 108010037584 Type 4 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 abstract 2
- 102000004127 Cytokines Human genes 0.000 abstract 1
- 108090000695 Cytokines Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 230000000770 proinflammatory effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- 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
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- 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
- A61P27/00—Drugs for disorders of the senses
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/04—Artificial tears; Irrigation solutions
-
- 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
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
- A61P27/14—Decongestants or antiallergics
-
- 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
- A61P37/00—Drugs for immunological or allergic 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
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto caracterizado porque tiene la formula estructural (1) o una de sus sales, en donde: R1 es -(CH2)sG1G2G3 R2 es metilo; s es 6; G1 es nulo; G2 es heterocicloalquilo, el cual puede estar opcionalmente sustituido; G3 es nulo; y R20 y R24 son hidrogeno. Dichos compuestos pueden ser utiles como inhibidores de fosfodiesterasa 4 (PDE4) para el tratamiento o la prevencion de enfermedades inflamatorias y otras enfermedades que incluyen niveles elevados de citoquinas y mediadores pro inflamatorios.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12/544,185 US8138205B2 (en) | 2006-07-07 | 2009-08-19 | Heteroarylalkoxy-substituted quinolone inhibitors of PDE4 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078142A1 true AR078142A1 (es) | 2011-10-19 |
Family
ID=43989737
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100103047A AR078142A1 (es) | 2009-08-19 | 2010-08-19 | Compuestos inhibidores heteroarilicos biciclicos de pde4, las composiciones farmaceuticas que los contienen y el uso de los mismos para la preparacion de medicamentos. |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US8138205B2 (es) |
| EP (1) | EP2467376A4 (es) |
| JP (1) | JP2013502432A (es) |
| KR (1) | KR20120051071A (es) |
| CN (1) | CN102686578A (es) |
| AR (1) | AR078142A1 (es) |
| AU (1) | AU2010344165A1 (es) |
| BR (1) | BR112012003738A2 (es) |
| CA (1) | CA2770767A1 (es) |
| CO (1) | CO6612202A2 (es) |
| MX (1) | MX2012001695A (es) |
| TW (1) | TW201111363A (es) |
| UY (1) | UY32849A (es) |
| WO (1) | WO2011093924A1 (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2657093A1 (en) | 2006-07-07 | 2008-01-10 | Steven P. Govek | Bicyclic heteroaryl inhibitors of pde4 |
| US8138205B2 (en) * | 2006-07-07 | 2012-03-20 | Kalypsys, Inc. | Heteroarylalkoxy-substituted quinolone inhibitors of PDE4 |
| MX2012003693A (es) * | 2009-10-01 | 2012-04-19 | Alcon Res Ltd | Composiciones de olopatadine y usos de las mismas. |
| US20130116279A1 (en) * | 2011-11-07 | 2013-05-09 | Kalypsys, Inc. | Bicyclic heteroaryl inhibitors of pde4 |
| MD20150071A2 (ro) | 2013-02-19 | 2016-02-29 | Pfizer Inc. | Compuşi azabenzimidazolici ca inhibitori ai PDE4 izoenzimelor pentru tratamentul tulburărilor SNC şi altor afecţiuni |
| US10131669B2 (en) | 2014-07-24 | 2018-11-20 | Pfizer Inc. | Pyrazolopyrimidine compounds |
| HUE044040T2 (hu) | 2014-08-06 | 2019-09-30 | Pfizer | Imidazopiridazin vegyületek |
| 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 |
| CN106916104B (zh) * | 2017-02-28 | 2019-08-27 | 牡丹江医学院 | 用于治疗结肠炎的药物 |
| CN117187343B (zh) * | 2023-09-06 | 2024-11-01 | 青岛大学 | 一种磷酸二酯酶抑制剂的高通量筛选方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU639529B2 (en) | 1987-03-04 | 1993-07-29 | Higuchi, Yoshinari | Carbostyril derivatives and salts thereof and anti-arrhythmic agents containing the carbostyril derivatives |
| CA2091172C (en) * | 1990-09-07 | 1997-05-20 | Adriano Afonso | Antiviral compounds and antihypertensive compounds |
| DE69231679T2 (de) | 1991-04-03 | 2001-10-31 | Korea Research Institute Of Chemical Technology, Daejeon | 2-chinolinonderivate, verfahren zu deren herstellung und diese enthaltende fungizide und insektizide |
| US5412401A (en) * | 1991-04-12 | 1995-05-02 | Abekas Video Systems, Inc. | Digital video effects generator |
| IT1296985B1 (it) | 1997-12-19 | 1999-08-03 | Zambon Spa | Derivati benzazinici inibitori della fosfodiesterasi 4 |
| PL211125B1 (pl) | 2000-09-11 | 2012-04-30 | Novartis Vaccines & Diagnostic | Pochodne chinolinonu jako inhibitory kinazy tyrozynowej, kompozycje je zawierające i ich zastosowanie |
| US20030028018A1 (en) * | 2000-09-11 | 2003-02-06 | Chiron Coporation | Quinolinone derivatives |
| JP2002371078A (ja) | 2001-06-12 | 2002-12-26 | Sankyo Co Ltd | キノリン誘導体及びキノロン誘導体 |
| US6822097B1 (en) | 2002-02-07 | 2004-11-23 | Amgen, Inc. | Compounds and methods of uses |
| US7144896B2 (en) * | 2002-03-18 | 2006-12-05 | Merck Frosst Canada Ltd. | Hetero-bridge substituted 8-arylquinoline pde4 inhibitors |
| KR20050037585A (ko) | 2002-08-23 | 2005-04-22 | 카이론 코포레이션 | 벤지미다졸 퀴놀리논 및 그들의 사용 |
| AU2005216904B2 (en) | 2004-02-20 | 2010-11-25 | Novartis Vaccines And Diagnostics, Inc. | Modulation of inflammatory and metastatic processes |
| WO2005116009A1 (en) * | 2004-05-18 | 2005-12-08 | Schering Corporation | Substituted 2-quinolyl-oxazoles useful as pde4 inhibitors |
| DK1809622T3 (da) | 2004-09-22 | 2010-11-08 | Janssen Pharmaceutica Nv | Inhibitorer af interaktionen mellem MDM2 og P53 |
| US8048889B2 (en) * | 2005-03-29 | 2011-11-01 | Xtl Biopharmaceuticals Ltd. | 3,4-disubstituted coumarin and quinolone compounds |
| WO2007036743A2 (en) | 2005-09-30 | 2007-04-05 | Argenta Discovery Limited | Quinolines and their therapeutic use |
| US8138205B2 (en) * | 2006-07-07 | 2012-03-20 | Kalypsys, Inc. | Heteroarylalkoxy-substituted quinolone inhibitors of PDE4 |
| CA2657093A1 (en) * | 2006-07-07 | 2008-01-10 | Steven P. Govek | Bicyclic heteroaryl inhibitors of pde4 |
-
2009
- 2009-08-19 US US12/544,185 patent/US8138205B2/en not_active Expired - Fee Related
-
2010
- 2010-08-19 CN CN201080043000XA patent/CN102686578A/zh active Pending
- 2010-08-19 EP EP10844912A patent/EP2467376A4/en not_active Withdrawn
- 2010-08-19 AR ARP100103047A patent/AR078142A1/es unknown
- 2010-08-19 CA CA2770767A patent/CA2770767A1/en not_active Abandoned
- 2010-08-19 BR BR112012003738A patent/BR112012003738A2/pt not_active IP Right Cessation
- 2010-08-19 WO PCT/US2010/045997 patent/WO2011093924A1/en not_active Ceased
- 2010-08-19 AU AU2010344165A patent/AU2010344165A1/en not_active Abandoned
- 2010-08-19 KR KR1020127006729A patent/KR20120051071A/ko not_active Withdrawn
- 2010-08-19 MX MX2012001695A patent/MX2012001695A/es active IP Right Grant
- 2010-08-19 TW TW099127743A patent/TW201111363A/zh unknown
- 2010-08-19 UY UY0001032849A patent/UY32849A/es not_active Application Discontinuation
- 2010-08-19 JP JP2012525683A patent/JP2013502432A/ja active Pending
-
2012
- 2012-02-10 US US13/370,756 patent/US20130045975A1/en not_active Abandoned
- 2012-02-17 CO CO12028570A patent/CO6612202A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011093924A1 (en) | 2011-08-04 |
| BR112012003738A2 (pt) | 2019-09-24 |
| TW201111363A (en) | 2011-04-01 |
| JP2013502432A (ja) | 2013-01-24 |
| CO6612202A2 (es) | 2013-02-01 |
| EP2467376A1 (en) | 2012-06-27 |
| CA2770767A1 (en) | 2011-08-04 |
| CN102686578A (zh) | 2012-09-19 |
| US8138205B2 (en) | 2012-03-20 |
| US20100081646A1 (en) | 2010-04-01 |
| EP2467376A4 (en) | 2013-01-16 |
| KR20120051071A (ko) | 2012-05-21 |
| AU2010344165A1 (en) | 2012-03-01 |
| MX2012001695A (es) | 2012-07-23 |
| US20130045975A1 (en) | 2013-02-21 |
| UY32849A (es) | 2011-03-31 |
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Legal Events
| Date | Code | Title | Description |
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| FB | Suspension of granting procedure |