CA2548035A1 - Cdk2 antagonists as short form c-maf transcription factor antagonists for treatment of glaucoma - Google Patents
Cdk2 antagonists as short form c-maf transcription factor antagonists for treatment of glaucoma Download PDFInfo
- Publication number
- CA2548035A1 CA2548035A1 CA002548035A CA2548035A CA2548035A1 CA 2548035 A1 CA2548035 A1 CA 2548035A1 CA 002548035 A CA002548035 A CA 002548035A CA 2548035 A CA2548035 A CA 2548035A CA 2548035 A1 CA2548035 A1 CA 2548035A1
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- Prior art keywords
- maf
- glaucoma
- antagonist
- purvalanol
- composition
- 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.)
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
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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
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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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
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- Public Health (AREA)
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- Animal Behavior & Ethology (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Ophthalmology & Optometry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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| US53180103P | 2003-12-22 | 2003-12-22 | |
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| PCT/US2004/042930 WO2005063252A1 (en) | 2003-12-22 | 2004-12-21 | Cdk2 antagonists as short form c-maf transcription factor antagonists for treatment of glaucoma |
Publications (1)
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| CA2548035A1 true CA2548035A1 (en) | 2005-07-14 |
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| CA002548035A Abandoned CA2548035A1 (en) | 2003-12-22 | 2004-12-21 | Cdk2 antagonists as short form c-maf transcription factor antagonists for treatment of glaucoma |
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| JP (1) | JP2007515426A (https=) |
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| AU (1) | AU2004308938B2 (https=) |
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| CA (1) | CA2548035A1 (https=) |
| MX (1) | MXPA06007062A (https=) |
| RU (1) | RU2370267C2 (https=) |
| TW (1) | TW200526224A (https=) |
| UY (1) | UY28660A1 (https=) |
| WO (1) | WO2005063252A1 (https=) |
| ZA (1) | ZA200604576B (https=) |
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| CA2548146A1 (en) * | 2003-12-22 | 2005-07-14 | Alcon, Inc. | Agents for treatment of diabetic retinopathy and drusen formation in macular degeneration |
| MXPA06006980A (es) * | 2003-12-22 | 2006-12-14 | Alcon Inc | Agentes para tratamiento de retinopatia glaucomatosa y neuropatia optica. |
| US20050222127A1 (en) * | 2004-03-30 | 2005-10-06 | Alcon, Inc. | Use of Rho kinase inhibitors in the treatment of hearing loss, tinnitus and improving body balance |
| US20060115870A1 (en) * | 2004-03-30 | 2006-06-01 | Alcon, Inc. | High throughput assay for human Rho kinase activity |
| US20080096238A1 (en) * | 2004-03-30 | 2008-04-24 | Alcon, Inc. | High throughput assay for human rho kinase activity with enhanced signal-to-noise ratio |
| DK2444807T3 (da) * | 2006-11-01 | 2014-08-11 | Ventana Med Syst Inc | Mono- og dinitropyrazolhaptenkonjugater |
| WO2008079980A1 (en) * | 2006-12-22 | 2008-07-03 | Alcon Research, Ltd. | Inhibitors of protein kinase c-delta for the treatment of glaucoma |
| US7682789B2 (en) * | 2007-05-04 | 2010-03-23 | Ventana Medical Systems, Inc. | Method for quantifying biomolecules conjugated to a nanoparticle |
| EP2167963B1 (en) | 2007-05-23 | 2019-04-17 | Ventana Medical Systems, Inc. | Polymeric carriers for immunohistochemistry and in situ hybridization |
| WO2009149013A2 (en) | 2008-06-05 | 2009-12-10 | Ventana Medical Systems, Inc. | Compositions comprising nanomaterials and method for using such compositions for histochemical processes |
| USPP22463P3 (en) * | 2010-02-16 | 2012-01-17 | Menachem Bornstein | Gypsophila plant named ‘Pearl Blossom’ |
| EP3517630B1 (en) | 2010-10-06 | 2022-01-19 | Institució Catalana de Recerca i Estudis Avançats | Method for the diagnosis, prognosis and treatment of breast cancer metastasis |
| EP2650682A1 (en) | 2012-04-09 | 2013-10-16 | Fundació Privada Institut de Recerca Biomèdica | Method for the prognosis and treatment of cancer metastasis |
| EP3467124A1 (en) | 2012-06-06 | 2019-04-10 | Fundació Institut de Recerca Biomèdica IRB (Barcelona) | Method for the diagnosis, prognosis and treatment of lung cancer metastasis |
| US10119171B2 (en) | 2012-10-12 | 2018-11-06 | Inbiomotion S.L. | Method for the diagnosis, prognosis and treatment of prostate cancer metastasis |
| KR101872965B1 (ko) | 2012-10-12 | 2018-06-29 | 인바이오모션 에스.엘. | Ｃ―ｍａｆ를 이용하는 전립선암 전이의 진단, 예후 및 치료 방법 |
| JP6577873B2 (ja) | 2013-03-15 | 2019-09-18 | フンダシオ、インスティトゥト、デ、レセルカ、ビオメディカ（イエレベ、バルセロナ）Ｆｕｎｄａｃｉｏ Ｉｎｓｔｉｔｕｔ Ｄｅ Ｒｅｃｅｒｃａ Ｂｉｏｍｅｄｉｃａ （Ｉｒｂ Ｂａｒｃｅｌｏｎａ） | がんの転移の予後診断および処置のための方法 |
| WO2014184679A2 (en) | 2013-03-15 | 2014-11-20 | Inbiomotion S.L. | Method for the prognosis and treatment of renal cell carcinoma metastasis |
| CA2903306A1 (en) | 2013-03-15 | 2014-09-18 | Fundacio Institut De Recerca Biomedica (Irb Barcelona) | Method for the diagnosis, prognosis and treatment of metastatic cancer |
| TR201907389T4 (tr) | 2013-10-09 | 2019-06-21 | Fundacio Inst De Recerca Biomedica Irb Barcelona | Meme kanserinden kaynaklanan metastazlı kemik kanserinin prognozu ve tedavisine yönelik yöntem. |
| AU2017271385B2 (en) | 2016-05-25 | 2023-10-05 | Inbiomotion S.L. | Therapeutic treatment of breast cancer based on c-MAF status |
| MX2020005182A (es) | 2017-11-22 | 2020-08-17 | Inbiomotion Sl | Tratamiento terapeutico del cancer de mama basado en el estado del c-maf. |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4456757A (en) * | 1981-03-20 | 1984-06-26 | Asahi Kasei Kogyo Kabushiki Kaisha | Isoquinolinesulfonyl derivatives and process for the preparation thereof |
| US4678783B1 (en) * | 1983-11-04 | 1995-04-04 | Asahi Chemical Ind | Substituted isoquinolinesulfonyl compounds |
| US4959389A (en) * | 1987-10-19 | 1990-09-25 | Speiser Peter P | Pharmaceutical preparation for the treatment of psoriatic arthritis |
| US5124154A (en) * | 1990-06-12 | 1992-06-23 | Insite Vision Incorporated | Aminosteroids for ophthalmic use |
| JP3193301B2 (ja) * | 1995-09-14 | 2001-07-30 | 麒麟麦酒株式会社 | 生理活性タンパク質ｐ１６０ |
| US5906819A (en) * | 1995-11-20 | 1999-05-25 | Kirin Beer Kabushiki Kaisha | Rho target protein Rho-kinase |
| US5681854A (en) * | 1995-11-22 | 1997-10-28 | Alcon Laboratories, Inc. | Use of aliphatic carboxylic acid derivatives in ophthalmic disorders |
| ATE289815T1 (de) * | 1995-12-21 | 2005-03-15 | Alcon Lab Inc | Verwendung von substituierten isochinolinsulfonyl-verbindungen zur herstellung eines medikaments für die behandlung von glaukom und okularer ischämie |
| ES2205166T3 (es) * | 1996-02-02 | 2004-05-01 | D. Western Therapeutics Institute | Derivados de isoquinolina y medicamento. |
| US6586425B2 (en) * | 1996-02-21 | 2003-07-01 | Wisconsin Alumni Research Foundation | Cytoskeletal active agents for glaucoma therapy |
| US5798380A (en) * | 1996-02-21 | 1998-08-25 | Wisconsin Alumni Research Foundation | Cytoskeletal active agents for glaucoma therapy |
| BR9711154A (pt) * | 1996-08-12 | 1999-08-17 | Yoshitomi Pharmaceutical | Agente farmac-utico contendo inibidor cinase rho |
| US5759787A (en) * | 1996-08-26 | 1998-06-02 | Tularik Inc. | Kinase assay |
| US6255485B1 (en) * | 1997-08-07 | 2001-07-03 | The Regents Of The University Of California | Purine inhibitors of protein kinases, G proteins and polymerases |
| US6573044B1 (en) * | 1997-08-07 | 2003-06-03 | The Regents Of The University Of California | Methods of using chemical libraries to search for new kinase inhibitors |
| US6441033B1 (en) * | 1997-12-22 | 2002-08-27 | Alcon Manufacturing, Ltd. | 11β-fluoro 15β-hydroxy PGF2α analogs as FP receptor antagonists |
| US6274338B1 (en) * | 1998-02-24 | 2001-08-14 | President And Fellows Of Harvard College | Human c-Maf compositions and methods of use thereof |
| GB9806739D0 (en) * | 1998-03-28 | 1998-05-27 | Univ Newcastle Ventures Ltd | Cyclin dependent kinase inhibitors |
| US20010041174A1 (en) * | 1998-11-24 | 2001-11-15 | Najam Sharif | Use of implanted encapsulated cells expressing glutamate transporter proteins for the treatment of neurodegenerative diseases |
| BR9916327A (pt) * | 1998-12-17 | 2001-09-18 | Hoffmann La Roche | Oxindóis de 4-alquenila (e alquinila) como inibidores de cinases dependentes de ciclina, em particular, cdk2 |
| US6020383A (en) * | 1999-01-11 | 2000-02-01 | Eastman Chemicals Company | Method for reducing blood cholesterol and/or blood triglycerides |
| US6103756A (en) * | 1999-08-11 | 2000-08-15 | Vitacost Inc. | Ocular orally ingested composition for prevention and treatment of individuals |
| US6573299B1 (en) * | 1999-09-20 | 2003-06-03 | Advanced Medical Instruments | Method and compositions for treatment of the aging eye |
| WO2002002190A2 (en) * | 2000-07-05 | 2002-01-10 | Johns Hopkins School Of Medicine | Prevention and treatment of neurodegenerative diseases by glutathione and phase ii detoxification enzymes |
| WO2002012250A2 (en) * | 2000-08-09 | 2002-02-14 | Agouron Pharmaceuticals, Inc. | Pyrazole-thiazole compounds, pharmaceutical compositions containing them, and methods of their use for inhibiting cyclin-dependent kinases |
| GB0030727D0 (en) * | 2000-12-15 | 2001-01-31 | Lumitech Uk Ltd | Methods and kits for detecting kinase activity |
| US6756063B2 (en) * | 2001-03-29 | 2004-06-29 | Zoltan Laboratories, Llc | Methods and compositions for the treatment of human and animal cancers |
| US6884816B2 (en) * | 2001-08-31 | 2005-04-26 | Alcon, Inc. | Hydroxy substituted fused naphthyl-azoles and fused indeno-azoles and their use for the treatment of glaucoma |
| TW201041580A (en) * | 2001-09-27 | 2010-12-01 | Alcon Inc | Inhibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma |
| US20030219846A1 (en) * | 2002-02-28 | 2003-11-27 | Pfizer Inc. | Assay for activity of the ActRIIB kinase |
| US7351407B2 (en) * | 2002-04-30 | 2008-04-01 | Alcon, Inc. | Agents which regulate, inhibit, or modulate the activity and/or expression of connective tissue growth factor (CTGF) as a unique means to both lower intraocular pressure and treat glaucomatous retinopathies/optic neuropathies |
| US7196090B2 (en) * | 2002-07-25 | 2007-03-27 | Warner-Lambert Company | Kinase inhibitors |
| CN100497302C (zh) * | 2002-09-05 | 2009-06-10 | 神经研究公司 | 二芳基脲衍生物和它们作为氯通道阻滞剂的用途 |
| US6747025B1 (en) * | 2002-11-27 | 2004-06-08 | Allergan, Inc. | Kinase inhibitors for the treatment of disease |
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- 2004-11-26 AR ARP040104413A patent/AR046728A1/es not_active Application Discontinuation
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| AU2004308938B2 (en) | 2011-06-23 |
| ZA200604576B (en) | 2007-11-28 |
| JP2007515426A (ja) | 2007-06-14 |
| RU2006126638A (ru) | 2008-01-27 |
| RU2370267C2 (ru) | 2009-10-20 |
| UY28660A1 (es) | 2005-07-29 |
| EP1696928A1 (en) | 2006-09-06 |
| TW200526224A (en) | 2005-08-16 |
| AR046728A1 (es) | 2005-12-21 |
| MXPA06007062A (es) | 2006-09-04 |
| AU2004308938A1 (en) | 2005-07-14 |
| KR20060110301A (ko) | 2006-10-24 |
| BRPI0418033A (pt) | 2007-04-17 |
| WO2005063252A1 (en) | 2005-07-14 |
| US20050159432A1 (en) | 2005-07-21 |
| CN1886138A (zh) | 2006-12-27 |
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