CA2511818A1 - Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders - Google Patents
Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders Download PDFInfo
- Publication number
- CA2511818A1 CA2511818A1 CA002511818A CA2511818A CA2511818A1 CA 2511818 A1 CA2511818 A1 CA 2511818A1 CA 002511818 A CA002511818 A CA 002511818A CA 2511818 A CA2511818 A CA 2511818A CA 2511818 A1 CA2511818 A1 CA 2511818A1
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- Prior art keywords
- protein
- compound
- phosphate
- natural ligand
- proteins
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- QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 description 1
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 description 1
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- 230000001988 toxicity Effects 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
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- 235000011178 triphosphate Nutrition 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 229960004528 vincristine Drugs 0.000 description 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 description 1
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Classifications
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- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P7/06—Antianaemics
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- A—HUMAN NECESSITIES
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- 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
- 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
- C07D417/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Transplantation (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43757202P | 2002-12-30 | 2002-12-30 | |
| US60/437,572 | 2002-12-30 | ||
| PCT/US2003/041630 WO2004062664A1 (en) | 2002-12-30 | 2003-12-30 | Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2511818A1 true CA2511818A1 (en) | 2004-07-29 |
Family
ID=32713206
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002511818A Abandoned CA2511818A1 (en) | 2002-12-30 | 2003-12-30 | Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7432292B2 (enExample) |
| EP (1) | EP1594497B1 (enExample) |
| JP (1) | JP4611751B2 (enExample) |
| AT (1) | ATE432074T1 (enExample) |
| AU (2) | AU2003300447B2 (enExample) |
| CA (1) | CA2511818A1 (enExample) |
| DE (1) | DE60327811D1 (enExample) |
| WO (1) | WO2004062664A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005509616A (ja) * | 2001-10-16 | 2005-04-14 | センジェント・セラピューティクス・インク | チロシンホスファターゼに対する有機硫黄阻害剤 |
| AU2004210711B2 (en) * | 2003-02-12 | 2010-07-08 | Transtech Pharma, Inc. | Substituted azole derivatives as therapeutic agents |
| WO2005035551A2 (en) | 2003-10-08 | 2005-04-21 | Incyte Corporation | Inhibitors of proteins that bind phosphorylated molecules |
| WO2005080346A1 (en) * | 2004-02-12 | 2005-09-01 | Transtech Pharma, Inc. | Substituted azole derivatives, compositions, and methods of use |
| US20060135773A1 (en) * | 2004-06-17 | 2006-06-22 | Semple Joseph E | Trisubstituted nitrogen modulators of tyrosine phosphatases |
| WO2006017124A2 (en) * | 2004-07-09 | 2006-02-16 | Cengent Therapeutics, Inc. | Oxygen/nitrogen heterocycle inhibitors of tyrosine phosphatases |
| WO2006028970A1 (en) | 2004-09-02 | 2006-03-16 | Cengent Therapeutics, Inc. | Derivatives of thiazole and thiadiazole inhibitors of tyrosine phosphatases |
| EP1728790A1 (en) | 2005-06-01 | 2006-12-06 | Max-Delbrück-Centrum Für Molekulare Medizin | Shp-2 inhibitors, pharmaceutical compositions comprising them and their use for treating phosphatase-mediated diseases |
| UA94724C2 (en) * | 2005-12-08 | 2011-06-10 | Новартис Аг | Thiadiazolidinone derivatives as antidiabetic agents |
| EP1963294B1 (en) * | 2005-12-08 | 2012-10-10 | Novartis AG | 1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (ptpase) |
| RU2008127253A (ru) * | 2005-12-08 | 2010-01-20 | Новартис АГ (CH) | 1,1,3-триоксо-1,2,5-тиадиазолидины и их применение в качестве ингибиторов птфаз |
| UA94921C2 (en) * | 2005-12-08 | 2011-06-25 | Новартис Аг | 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors |
| EP1991544B1 (en) * | 2006-01-30 | 2018-08-15 | vTv Therapeutics LLC | Substituted imidazole derivatives and their use as ptpase inhibitors |
| JP2009532379A (ja) * | 2006-03-31 | 2009-09-10 | ノバルティス アクチエンゲゼルシャフト | ＰＴＰａｓｅのチアジアゾリジノン阻害剤 |
| WO2010011666A2 (en) * | 2008-07-21 | 2010-01-28 | University Of South Florida | Indoline scaffold shp-2 inhibitors and cancer treatment method |
| EP2552451A1 (en) * | 2010-03-29 | 2013-02-06 | Novartis Forschungsstiftung, Zweigniederlassung Friedrich Miescher Institute For Biomedical Research | Protein tyrosine phosphatase, non-receptor type 11 (ptpn11) and tumor initiating cells |
| WO2012041524A1 (en) | 2010-10-01 | 2012-04-05 | Max-Delbrück-Centrum Für Molekulare Medizin (Mdc) | Hydrazonopyrazolones as protein tyrosine phosphatase inhibitors |
| EP2717911A1 (en) * | 2011-06-06 | 2014-04-16 | Novartis Forschungsstiftung, Zweigniederlassung | Protein tyrosine phosphatase, non-receptor type 11 (ptpn11) and triple-negative breast cancer |
| CN103087166B (zh) * | 2011-10-31 | 2014-03-05 | 中国科学院微生物研究所 | 一种钾氢泵蛋白及其编码基因和它们的应用 |
| US9844535B2 (en) | 2013-07-03 | 2017-12-19 | Indiana University Research And Technology Corporation | SHP2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using SHP2 inhibitors |
| TWI888352B (zh) * | 2018-06-21 | 2025-07-01 | 美商嘉來克生命科學有限責任公司 | 蛋白質酪胺酸磷酸酯酶抑制劑及其使用方法 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US555609A (en) * | 1896-03-03 | Yarn-dyeing machine | ||
| US4952397A (en) * | 1985-06-17 | 1990-08-28 | Merck & Co., Inc. | 2-quaternary heteroarylalkylthio carbapenems having an acid moiety substituent |
| US5550139A (en) * | 1994-01-03 | 1996-08-27 | The Wichita State University | Serine protease inhibitors |
| US5512576A (en) | 1994-12-02 | 1996-04-30 | Sterling Winthrop Inc. | 2-substituted 1,2,5,-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof |
| US5494925A (en) * | 1994-12-02 | 1996-02-27 | Sterling Winthrop Inc. | 2-heterocyclyloxymethyl and 2-heterocyclylthiomethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof |
| US5556909A (en) | 1994-12-02 | 1996-09-17 | Sanofi Winthrop Inc. | Substituted 2-arylcarbonyloxymethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives and compositions and method of use thereof |
| US5750546A (en) | 1994-12-02 | 1998-05-12 | Sanofi Winthrop, Inc. | 2-(2, 3, 5, 6-tetrafluoro-4-pyridyl)-1, 2, 5-thiadiazolidin-3-one 1, 1-dioxides and compositions and method of use thereof |
| US5541168A (en) | 1994-12-02 | 1996-07-30 | Sterling Winthrop Inc. | Substituted 2-(phosphinyloxymethyl)-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof |
| ATE534637T1 (de) * | 2002-04-03 | 2011-12-15 | Novartis Ag | 5-substituierte 1,1-dioxo- 1,2,5 thiazolidin-3- onderivate als ptpase 1b hemmer |
| GB0227813D0 (en) * | 2002-11-29 | 2003-01-08 | Astrazeneca Ab | Chemical compounds |
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2003
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- 2003-12-30 WO PCT/US2003/041630 patent/WO2004062664A1/en not_active Ceased
- 2003-12-30 US US10/749,121 patent/US7432292B2/en not_active Expired - Fee Related
- 2003-12-30 AT AT03815258T patent/ATE432074T1/de not_active IP Right Cessation
- 2003-12-30 EP EP03815258A patent/EP1594497B1/en not_active Expired - Lifetime
- 2003-12-30 JP JP2004566641A patent/JP4611751B2/ja not_active Expired - Fee Related
- 2003-12-30 CA CA002511818A patent/CA2511818A1/en not_active Abandoned
- 2003-12-30 DE DE60327811T patent/DE60327811D1/de not_active Expired - Lifetime
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2009
- 2009-12-03 AU AU2009243502A patent/AU2009243502A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2006514960A (ja) | 2006-05-18 |
| AU2003300447B2 (en) | 2009-09-03 |
| AU2009243502A1 (en) | 2009-12-24 |
| DE60327811D1 (de) | 2009-07-09 |
| AU2003300447A1 (en) | 2004-08-10 |
| EP1594497B1 (en) | 2009-05-27 |
| US20040167187A1 (en) | 2004-08-26 |
| WO2004062664A1 (en) | 2004-07-29 |
| US7432292B2 (en) | 2008-10-07 |
| ATE432074T1 (de) | 2009-06-15 |
| JP4611751B2 (ja) | 2011-01-12 |
| EP1594497A1 (en) | 2005-11-16 |
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