WO2010035220A1 - Pyrazolo pyridine derivatives as nadph oxidase inhibitors - Google Patents

Pyrazolo pyridine derivatives as nadph oxidase inhibitors Download PDF

Info

Publication number
WO2010035220A1
WO2010035220A1 PCT/IB2009/054155 IB2009054155W WO2010035220A1 WO 2010035220 A1 WO2010035220 A1 WO 2010035220A1 IB 2009054155 W IB2009054155 W IB 2009054155W WO 2010035220 A1 WO2010035220 A1 WO 2010035220A1
Authority
WO
WIPO (PCT)
Prior art keywords
optionally substituted
pyrazolo
pyridine
dione
methyl
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/IB2009/054155
Other languages
English (en)
French (fr)
Inventor
Patrick Page
Mike Orchard
Benoît Laleu
Francesca Gaggini
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Calliditas Therapeutics Suisse SA
Original Assignee
Genkyotex SA
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
Priority to HK11113467.4A priority Critical patent/HK1159092B/xx
Priority to ES09815761.3T priority patent/ES2561210T3/es
Priority to EP09815761.3A priority patent/EP2342203B1/en
Priority to AU2009298007A priority patent/AU2009298007B2/en
Priority to CN200980133736.3A priority patent/CN102137862B/zh
Priority to BRPI0919331A priority patent/BRPI0919331A2/pt
Priority to CA2737538A priority patent/CA2737538C/en
Priority to US13/120,438 priority patent/US8455486B2/en
Priority to JP2011527465A priority patent/JP5750372B2/ja
Priority to RU2011116232/04A priority patent/RU2548022C2/ru
Application filed by Genkyotex SA filed Critical Genkyotex SA
Priority to KR1020117006133A priority patent/KR101716511B1/ko
Publication of WO2010035220A1 publication Critical patent/WO2010035220A1/en
Priority to IL211891A priority patent/IL211891B/en
Anticipated expiration legal-status Critical
Priority to US13/755,617 priority patent/US9006238B2/en
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/435—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
    • A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • 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
    • A61P25/28—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • A61P37/08—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
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Definitions

  • alkoxy Ci-C 6 alkyl refers to Ci-C 6 alkyl groups having an alkoxy substituent, including methoxyethyl and the like.
  • alkoxycarbonyl refers to the group -C(O)OR where R includes "Ci-C 6 alkyl",
  • halogen refers to fluoro, chloro, bromo and iodo atoms.
  • compositions of this invention may also be liquid formulations, including, but not limited to, aqueous or oily suspensions, solutions, emulsions, syrups, and elixirs.
  • Liquid forms suitable for oral administration may include a suitable aqueous or non-aqueous vehicle with buffers, suspending and dispensing agents, colorants, flavors and the like.
  • the compositions may also be formulated as a dry product for reconstitution with water or other suitable vehicle before use.
  • Such liquid preparations may contain additives, including, but not limited to, suspending agents, emulsifying agents, non-aqueous vehicles and preservatives.
  • compositions of this invention may also be formulated as suppositories, which may contain suppository bases including, but not limited to, cocoa butter or glycerides.
  • Compositions of this invention may also be formulated for inhalation, which may be in a form including, but not limited to, a solution, suspension, or emulsion that may be administered as a dry powder or in the form of an aerosol using a propellant, such as dichlorodifiuoromethane or trichlorofluoromethane.
  • compositions of this invention may also be formulated as a depot preparation, which may be administered by implantation or by intramuscular injection.
  • the compositions may be formulated with suitable polymeric or hydrophobic materials (as an emulsion in an acceptable oil, for example), ion exchange resins, or as sparingly soluble derivatives (as a sparingly soluble salt, for example).
  • compositions of this invention may also be formulated as a liposome preparation.
  • the liposome preparation can comprise liposomes which penetrate the cells of interest or the stratum corneum, and fuse with the cell membrane, resulting in delivery of the contents of the liposome into the cell.
  • Other suitable formulations can employ niosomes.
  • Niosomes are lipid vesicles similar to liposomes, with membranes consisting largely of non-ionic lipids, some forms of which are effective for transporting compounds across the stratum corneum.
  • the compounds of this invention can also be administered in sustained release forms or from sustained release drug delivery systems. A description of representative sustained release materials can also be found in the incorporated materials in Remington 's Pharmaceutical Sciences.
  • the invention provides a use of a pyrazolo pyridine derivative according to Formula (I) wherein G 1 , G 2 , G3, G 4 and G5 are as defined in the detailed description as well as pharmaceutically acceptable salts and pharmaceutically active derivative thereof for the preparation of a pharmaceutical composition for the treatment or prophylaxis of a disease or condition selected from cardiovascular disorders, respiratory disorders, metabolism disorders, skin disorders, bone disorders, neuroinflammatory and/or neurodegenerative disorders, kidney diseases, reproduction disorders, diseases affecting the eye and/or the lens and/or conditions affecting the inner ear, inflammatory disorders, liver diseases, pain, cancers, allergic disorders, traumatisms, septic, hemorrhagic and anaphylactic shock, disorders of the gastrointestinal system, angiogenesis, angiogenesis- dependent conditions and other diseases and disorders associated with Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
  • a disease or condition selected from cardiovascular disorders, respiratory disorders, metabolism disorders, skin disorders, bone
  • Pyrazolo pyridine derivatives according to Formula (I), whereby the substituents G 1 , G 2 , G3, G 4 and G5 are as above defined, may be prepared in four to five chemical steps, from custom made or commercially available substituted hydrazine derivatives according to Formula (VI), acetone dicarboxylate derivatives according to Formula (V), primary amine derivatives according to Formula (II) and acyl chloride derivatives according to Formula (DC), following the synthetic protocol outlined in Scheme 2 above.
  • a 24 hour time point is monitored.
  • the animals are controlled for an additional week without treatment in order to monitor the compound withdrawal.
  • the animals are treated once a day for a period of two weeks by gavage with a special needle adapted for gavage at 5 ml/kg.
  • They are acclimated for two days and further trained during one week.
  • the blood pressure is measured in awaken rats by tail- cuff plethysmography (Codas 6, Kent). Animals are included into groups after training for several days and if SBP variability was ⁇ 40mm Hg, i.e. +/- 20 mm Hg. Baseline measurements were performed at least on two days before the experiment. Before the beginning of the experiment, animals are randomized in order to constitute homogeneous groups.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
PCT/IB2009/054155 2008-09-23 2009-09-22 Pyrazolo pyridine derivatives as nadph oxidase inhibitors Ceased WO2010035220A1 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
JP2011527465A JP5750372B2 (ja) 2008-09-23 2009-09-22 Ｎａｄｐｈオキシダーゼインヒビターとしてのピラゾロピリジン誘導体
EP09815761.3A EP2342203B1 (en) 2008-09-23 2009-09-22 Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
AU2009298007A AU2009298007B2 (en) 2008-09-23 2009-09-22 Pyrazolo pyridine derivatives as NADPH Oxidase inhibitors
CN200980133736.3A CN102137862B (zh) 2008-09-23 2009-09-22 作为nadph氧化酶抑制剂的吡唑并吡啶衍生物
BRPI0919331A BRPI0919331A2 (pt) 2008-09-23 2009-09-22 derivados de pirazolo piridina, composições farmacêuticas e métodos associados
CA2737538A CA2737538C (en) 2008-09-23 2009-09-22 Pyrazolo pyridine derivatives as nadph oxidase inhibitors
US13/120,438 US8455486B2 (en) 2008-09-23 2009-09-22 Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
HK11113467.4A HK1159092B (en) 2008-09-23 2009-09-22 Pyrazolo pyridine derivatives as nadph oxidase inhibitors
ES09815761.3T ES2561210T3 (es) 2008-09-23 2009-09-22 Derivados de piridina pirazolo como inhibidores de la NADPH oxidasa
RU2011116232/04A RU2548022C2 (ru) 2008-09-23 2009-09-22 Пиразолопиридиновые производные как ингибиторы надфн-оксидазы
KR1020117006133A KR101716511B1 (ko) 2008-09-23 2009-09-22 Ｎａｄｐｈ 옥시다아제 억제제로서 피라졸로 피리딘 유도체
IL211891A IL211891B (en) 2008-09-23 2011-03-23 Pyrazolo pyridine derivatives, preparations containing them and their uses
US13/755,617 US9006238B2 (en) 2008-09-23 2013-01-31 Pyrazolo pyridine derivatives as NADPH oxidase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20080164849 EP2166009A1 (en) 2008-09-23 2008-09-23 Pyrazolo pyridine derivatives as nadph oxidase inhibitors
EP08164849.5 2008-09-23

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/120,438 A-371-Of-International US8455486B2 (en) 2008-09-23 2009-09-22 Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US13/755,617 Continuation US9006238B2 (en) 2008-09-23 2013-01-31 Pyrazolo pyridine derivatives as NADPH oxidase inhibitors

Publications (1)

Publication Number Publication Date
WO2010035220A1 true WO2010035220A1 (en) 2010-04-01

Family

ID=40299403

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2009/054155 Ceased WO2010035220A1 (en) 2008-09-23 2009-09-22 Pyrazolo pyridine derivatives as nadph oxidase inhibitors

Country Status (12)

Country Link
US (2) US8455486B2 (enExample)
EP (2) EP2166009A1 (enExample)
JP (1) JP5750372B2 (enExample)
KR (1) KR101716511B1 (enExample)
CN (1) CN102137862B (enExample)
AU (1) AU2009298007B2 (enExample)
BR (1) BRPI0919331A2 (enExample)
CA (1) CA2737538C (enExample)
ES (1) ES2561210T3 (enExample)
IL (1) IL211891B (enExample)
RU (1) RU2548022C2 (enExample)
WO (1) WO2010035220A1 (enExample)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8288432B2 (en) 2007-03-28 2012-10-16 Genkyotex Sa Tetrahydroindole derivatives as NADPH oxidase inhibitors
US8389518B2 (en) 2007-03-22 2013-03-05 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US8455485B2 (en) 2008-09-23 2013-06-04 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US8481562B2 (en) 2008-09-23 2013-07-09 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US8865758B2 (en) 2010-02-18 2014-10-21 Genkyotex Sa Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
US9096588B2 (en) 2008-09-23 2015-08-04 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US9394306B2 (en) 2009-09-28 2016-07-19 Genkyotex Sa Pyrazoline dione derivatives as NADPH oxidase inhibitors
US9687490B2 (en) 2012-10-24 2017-06-27 Glucox Biotech Ab Triazine derivatives for the treatment of conditions associated with nicotinamide adenine dinucleotide phosphate oxidase
WO2018203298A1 (en) 2017-05-04 2018-11-08 Glenmark Pharmaceuticals S.A. Substituted bicyclic heterocyclic compounds as nadph oxidase inhibitors
US10173988B2 (en) 2015-02-16 2019-01-08 Glucox Biotech Ab N2-(3,4-dimethylphenyl)-6-((4-(p-tolyl)piperazin-1-yl)methyl)-1,3,5-triazine-2,4-diamine
EP3479843A1 (en) 2017-11-01 2019-05-08 GenKyoTex Suisse SA Use of nox inhibitors for treatment of cancer
US11896719B2 (en) 2022-01-24 2024-02-13 Calliditas Therapeutics Ab Pharmaceutical compositions

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140212891A1 (en) * 2013-01-29 2014-07-31 Amina El Jamali Compositions and Methods Using NOX5
EP3551047A1 (en) 2016-12-07 2019-10-16 Progenity, Inc. Gastrointestinal tract detection methods, devices and systems
WO2019246317A1 (en) 2018-06-20 2019-12-26 Progenity, Inc. Treatment of a disease or condition in a tissue originating from the endoderm
CN116726362A (zh) 2018-11-19 2023-09-12 比奥拉治疗股份有限公司 用生物治疗剂治疗疾病的方法和装置
CN115666704B (zh) 2019-12-13 2025-09-26 比特比德科有限责任公司 用于将治疗剂递送至胃肠道的可摄取装置

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1505068A1 (en) 2002-04-23 2005-02-09 Shionogi & Co., Ltd. PYRAZOLO (1,5-a) PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
EP2002835A1 (en) * 2007-06-04 2008-12-17 GenKyo Tex Pyrazolo pyridine derivatives as NADPH oxidase inhibitors

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3391407A (en) * 1966-08-15 1968-07-09 William A. Waters Helmet
US3931407A (en) 1973-03-01 1976-01-06 American Hoechst Corporation Method of treatment with and compositions containing condensed pyrroles bearing an N-phenyl substituent
DE3728278A1 (de) 1986-12-17 1988-06-23 Bayer Ag Herbizide und fungizide mittel auf basis von substituierten pyrazolin-5-on derivaten
DE19518082A1 (de) * 1995-05-17 1996-11-21 Merck Patent Gmbh 4(-Arylaminomethylen)-2,4-dihydropyrazol-3-one
US5763496A (en) 1995-11-27 1998-06-09 The Research Foundation Of State University Of New York Prevention of atherosclerosis using NADPH oxidase inhibitors
TW432073B (en) 1995-12-28 2001-05-01 Pfizer Pyrazolopyridine compounds
WO1998037068A1 (en) * 1997-02-21 1998-08-27 Bristol-Myers Squibb Company Benzoic acid derivatives and related compounds as antiarrhythmic agents
IL144468A0 (en) 2000-07-27 2002-05-23 Pfizer Prod Inc Use of growth hormone secretagogues for improvement of functional health status
JP4196678B2 (ja) 2001-04-26 2008-12-17 味の素株式会社 複素環化合物
EP1291017A3 (en) 2001-09-10 2003-07-02 Warner-Lambert Company Use of statins to inhibit formation of osteoclasts
WO2004005267A2 (en) 2002-07-03 2004-01-15 Janssen Pharmaceutica, N.V. Heteroaryl compounds useful in treating inflammatory disorders
EP1603543A4 (en) 2003-02-28 2009-03-04 Florey Howard Inst THERAPEUTIC COMPOSITIONS
US20070082910A1 (en) 2003-04-08 2007-04-12 Mitsubishi Pharma Corporation Specific nad(p)h oxidase inhibitor
TW200533356A (en) 2004-02-24 2005-10-16 Mitsubishi Pharma Corp Fused pyridazine derivatives
JP2007529496A (ja) * 2004-03-19 2007-10-25 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 抗菌剤としてのイミダゾピリジン及びイミダゾピリミジン誘導体
EP1809601B1 (en) 2004-10-04 2014-09-10 Manfredi, John Compounds for alzheimer's disease
FR2882654B1 (fr) 2005-03-01 2007-04-27 Servier Lab Utilisation de derives de la diosmetine pour le traitement et la prevention des pathologies thrombotiques
US7759337B2 (en) 2005-03-03 2010-07-20 Amgen Inc. Phthalazine compounds and methods of use
US20070014739A1 (en) 2005-07-14 2007-01-18 Eldridge Gary R Compositions and methods for controlling biofilms and bacterial infections
DE102005048897A1 (de) 2005-10-12 2007-04-19 Sanofi-Aventis Deutschland Gmbh Diacylindazol-derivate als Inhibitoren von Lipasen und Phospholipasen
JP2009532501A (ja) * 2006-04-04 2009-09-10 ミリアド ジェネティクス， インコーポレイテッド 疾患および障害のための化合物
EP2000176A1 (en) 2007-06-04 2008-12-10 GenKyo Tex Tetrahydroindole derivatives as NADPH Oxidase inhibitors
PE20091093A1 (es) 2007-12-03 2009-08-25 Takeda Pharmaceutical Compuesto heterociclico que contiene nitrogeno y su uso
US20090163452A1 (en) 2007-12-20 2009-06-25 Schwartz Janice B Compositions and methods for lowering serum cholesterol
FR2929276B1 (fr) 2008-04-01 2010-04-23 Servier Lab Nouveaux derives de diosmetine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP2165707A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2166010A1 (en) 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2166008A1 (en) * 2008-09-23 2010-03-24 Genkyo Tex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
EP2305679A1 (en) 2009-09-28 2011-04-06 GenKyoTex SA Pyrazoline dione derivatives as nadph oxidase inhibitors
WO2011085293A1 (en) 2010-01-08 2011-07-14 Beth Israel Deaconess Medical Center Methods and compositions for the treatment of migraine headaches
EP2361911A1 (en) 2010-02-18 2011-08-31 GenKyoTex SA Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
EP2361912A1 (en) 2010-02-18 2011-08-31 GenKyoTex SA Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
CN102014373B (zh) 2010-11-22 2015-04-01 中兴通讯股份有限公司 一种激活配置的方法及装置
EP2591782A1 (en) 2011-11-11 2013-05-15 Johann Wolfgang Goethe-Universität Nadph oxidase 4 inhibitors and use thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1505068A1 (en) 2002-04-23 2005-02-09 Shionogi & Co., Ltd. PYRAZOLO (1,5-a) PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
EP2002835A1 (en) * 2007-06-04 2008-12-17 GenKyo Tex Pyrazolo pyridine derivatives as NADPH oxidase inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CHENG ET AL., GENE, vol. 16, no. 269, 16 December 2000 (2000-12-16), pages 131 - 40
LETO ET AL., ANTIOXID REDOX SIGNAL, vol. 8, no. 9-10, 2006, pages 1549 - 61

Cited By (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8389518B2 (en) 2007-03-22 2013-03-05 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US9073919B2 (en) 2007-03-22 2015-07-07 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US8288432B2 (en) 2007-03-28 2012-10-16 Genkyotex Sa Tetrahydroindole derivatives as NADPH oxidase inhibitors
US10772891B2 (en) 2008-09-23 2020-09-15 Genkyotex Suisse Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US8455485B2 (en) 2008-09-23 2013-06-04 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US8481562B2 (en) 2008-09-23 2013-07-09 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US8940760B2 (en) 2008-09-23 2015-01-27 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US9012449B2 (en) 2008-09-23 2015-04-21 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US9096588B2 (en) 2008-09-23 2015-08-04 Genkyotex Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US9974791B2 (en) 2008-09-23 2018-05-22 Genkyotex Suisse Sa Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
US9394306B2 (en) 2009-09-28 2016-07-19 Genkyotex Sa Pyrazoline dione derivatives as NADPH oxidase inhibitors
US8865758B2 (en) 2010-02-18 2014-10-21 Genkyotex Sa Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
US9687490B2 (en) 2012-10-24 2017-06-27 Glucox Biotech Ab Triazine derivatives for the treatment of conditions associated with nicotinamide adenine dinucleotide phosphate oxidase
US10173988B2 (en) 2015-02-16 2019-01-08 Glucox Biotech Ab N2-(3,4-dimethylphenyl)-6-((4-(p-tolyl)piperazin-1-yl)methyl)-1,3,5-triazine-2,4-diamine
WO2018203298A1 (en) 2017-05-04 2018-11-08 Glenmark Pharmaceuticals S.A. Substituted bicyclic heterocyclic compounds as nadph oxidase inhibitors
EP3479843A1 (en) 2017-11-01 2019-05-08 GenKyoTex Suisse SA Use of nox inhibitors for treatment of cancer
WO2019086579A1 (en) 2017-11-01 2019-05-09 Genkyotex Suisse Sa Use of nox inhibitors for treatment of cancer
US12011436B2 (en) 2017-11-01 2024-06-18 Calliditas Therapeutics Suisse Sa Use of NOX inhibitors for treatment of cancer
US11896719B2 (en) 2022-01-24 2024-02-13 Calliditas Therapeutics Ab Pharmaceutical compositions
US12171883B2 (en) 2022-01-24 2024-12-24 Calliditas Therapeutics Ab Pharmaceutical compositions
US12171882B2 (en) 2022-01-24 2024-12-24 Calliditas Therapeutics Ab Pharmaceutical compositions
US12311057B2 (en) 2022-01-24 2025-05-27 Calliditas Therapeutics Ab Pharmaceutical compositions

Also Published As

Publication number Publication date
CN102137862B (zh) 2014-07-02
IL211891A0 (en) 2011-06-30
RU2548022C2 (ru) 2015-04-10
KR101716511B1 (ko) 2017-03-14
EP2166009A1 (en) 2010-03-24
IL211891B (en) 2018-01-31
US9006238B2 (en) 2015-04-14
AU2009298007A1 (en) 2010-04-01
CA2737538C (en) 2019-04-23
HK1159092A1 (en) 2012-07-27
US8455486B2 (en) 2013-06-04
JP5750372B2 (ja) 2015-07-22
US20130158027A1 (en) 2013-06-20
RU2011116232A (ru) 2012-10-27
CA2737538A1 (en) 2010-04-01
JP2012502980A (ja) 2012-02-02
BRPI0919331A2 (pt) 2015-12-29
EP2342203B1 (en) 2015-11-04
KR20110060901A (ko) 2011-06-08
EP2342203A1 (en) 2011-07-13
CN102137862A (zh) 2011-07-27
ES2561210T3 (es) 2016-02-25
AU2009298007B2 (en) 2014-02-06
US20110178082A1 (en) 2011-07-21

Similar Documents

Publication Publication Date Title
AU2009298004B2 (en) Pyrazolo Pyridine Compounds as NADPH Oxidase Inhibitors
EP2349261B1 (en) Pyrazolo pyridine derivatives as nadph oxidase inhibitors
AU2009298007B2 (en) Pyrazolo pyridine derivatives as NADPH Oxidase inhibitors
DK2860179T3 (en) Pyrazolopyridine derivatives as NADPH oxidase inhibitors
EP2536723A1 (en) Pyrazolo piperidine derivatives as nadph oxidase inhibitors
HK1193974B (en) Pyrazolo pyridine derivatives as nadph oxidase inhibitors
HK1208452B (en) Pyrazolo pyridine derivatives as nadph oxidase inhibitors

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 200980133736.3

Country of ref document: CN

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 09815761

Country of ref document: EP

Kind code of ref document: A1

ENP Entry into the national phase

Ref document number: 20117006133

Country of ref document: KR

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 2737538

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 1165/KOLNP/2011

Country of ref document: IN

ENP Entry into the national phase

Ref document number: 2011527465

Country of ref document: JP

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 2009298007

Country of ref document: AU

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 13120438

Country of ref document: US

ENP Entry into the national phase

Ref document number: 2009298007

Country of ref document: AU

Date of ref document: 20090922

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 2009815761

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 2011116232

Country of ref document: RU

ENP Entry into the national phase

Ref document number: PI0919331

Country of ref document: BR

Kind code of ref document: A2

Effective date: 20110323