CA2471265C - Pyrimidotriazines as phosphatase inhibitors - Google Patents
Pyrimidotriazines as phosphatase inhibitors Download PDFInfo
- Publication number
- CA2471265C CA2471265C CA2471265A CA2471265A CA2471265C CA 2471265 C CA2471265 C CA 2471265C CA 2471265 A CA2471265 A CA 2471265A CA 2471265 A CA2471265 A CA 2471265A CA 2471265 C CA2471265 C CA 2471265C
- Authority
- CA
- Canada
- Prior art keywords
- ylmethyl
- diamine
- pyrimido
- triazine
- lower alkyl
- 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.)
- Expired - Fee Related
Links
- 239000003112 inhibitor Substances 0.000 title description 3
- 102000004160 Phosphoric Monoester Hydrolases Human genes 0.000 title description 2
- 108090000608 Phosphoric Monoester Hydrolases Proteins 0.000 title description 2
- QNQCJTHZJJOUGL-UHFFFAOYSA-N pyrimido[5,4-d]triazine Chemical class N1=NN=CC2=NC=NC=C21 QNQCJTHZJJOUGL-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 67
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- 125000000217 alkyl group Chemical group 0.000 claims description 35
- 125000003545 alkoxy group Chemical group 0.000 claims description 28
- 125000001475 halogen functional group Chemical group 0.000 claims description 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 20
- 125000001624 naphthyl group Chemical group 0.000 claims description 19
- 125000003118 aryl group Chemical group 0.000 claims description 18
- 125000004171 alkoxy aryl group Chemical group 0.000 claims description 16
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 16
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- 125000004093 cyano group Chemical group *C#N 0.000 claims description 15
- 239000008103 glucose Substances 0.000 claims description 15
- 238000000034 method Methods 0.000 claims description 15
- 150000003839 salts Chemical class 0.000 claims description 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 13
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- 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
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Plant Substances (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34393701P | 2001-12-27 | 2001-12-27 | |
| US60/343,937 | 2001-12-27 | ||
| US39911002P | 2002-07-26 | 2002-07-26 | |
| US60/399,110 | 2002-07-26 | ||
| PCT/EP2002/014771 WO2003055883A1 (en) | 2001-12-27 | 2002-12-27 | Pyrimidotriazines as phosphatase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2471265A1 CA2471265A1 (en) | 2003-07-10 |
| CA2471265C true CA2471265C (en) | 2010-02-09 |
Family
ID=26993696
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2471265A Expired - Fee Related CA2471265C (en) | 2001-12-27 | 2002-12-27 | Pyrimidotriazines as phosphatase inhibitors |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US6642381B2 (enExample) |
| EP (1) | EP1467996B1 (enExample) |
| JP (1) | JP4188839B2 (enExample) |
| KR (1) | KR100601769B1 (enExample) |
| CN (1) | CN100402530C (enExample) |
| AT (1) | ATE311388T1 (enExample) |
| AU (1) | AU2002367190B2 (enExample) |
| BR (1) | BR0215395A (enExample) |
| CA (1) | CA2471265C (enExample) |
| DE (1) | DE60207759T2 (enExample) |
| ES (1) | ES2252554T3 (enExample) |
| JO (1) | JO2242B1 (enExample) |
| MX (1) | MXPA04006266A (enExample) |
| PA (1) | PA8562901A1 (enExample) |
| PE (1) | PE20030896A1 (enExample) |
| PL (1) | PL371180A1 (enExample) |
| TW (1) | TW200306313A (enExample) |
| UY (1) | UY27606A1 (enExample) |
| WO (1) | WO2003055883A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2002342859B2 (en) * | 2001-10-30 | 2007-07-26 | Merck Serono Sa | Oxindole hydrazide modulators of protein tyrosine phosphatases (PTPS) |
| DE60327097D1 (de) * | 2002-11-18 | 2009-05-20 | Hoffmann La Roche | Diazinopyrimidine und ihre verwendung als proteinkinaseinhibitoren |
| WO2004071448A2 (en) * | 2003-02-12 | 2004-08-26 | Transtech Pharma Inc. | Substituted azole derivatives as inhibitors of protein tyrosine phosphatases |
| CN1747936A (zh) * | 2003-02-12 | 2006-03-15 | 特兰斯泰克制药公司 | 作为治疗试剂的取代吡咯衍生物 |
| CN1922151A (zh) * | 2004-02-12 | 2007-02-28 | 特兰斯泰克制药公司 | 取代的吡咯衍生物、组合物和使用方法 |
| US20080125403A1 (en) | 2004-04-02 | 2008-05-29 | Merck & Co., Inc. | Method of Treating Men with Metabolic and Anthropometric Disorders |
| CA2637024C (en) | 2006-01-30 | 2013-05-14 | Transtech Pharma, Inc. | Substituted imidazole derivatives, compositions, and methods of use as ptpase inhibitors |
| WO2008151257A2 (en) | 2007-06-04 | 2008-12-11 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
| US8034782B2 (en) | 2008-07-16 | 2011-10-11 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| EP2810951B1 (en) | 2008-06-04 | 2017-03-15 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| WO2010083645A1 (en) * | 2009-01-21 | 2010-07-29 | Shanghai Targetdrug Co., Ltd | PYRIMIDO[5,4-e][1,2,4]TRIAZINES AND USES THEREOF |
| WO2012027331A1 (en) | 2010-08-27 | 2012-03-01 | Ironwood Pharmaceuticals, Inc. | Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| US9486433B2 (en) | 2012-10-12 | 2016-11-08 | Mochida Pharmaceuticals Co. Ltd. | Compositions and methods for treating non-alcoholic steatohepatitis |
| US9708367B2 (en) | 2013-03-15 | 2017-07-18 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase and their uses |
| AU2014235209B2 (en) | 2013-03-15 | 2018-06-14 | Bausch Health Ireland Limited | Guanylate cyclase receptor agonists combined with other drugs |
| US9889108B2 (en) | 2013-03-15 | 2018-02-13 | Mochida Pharmaceutical Co., Ltd. | Compositions and methods for treating non-alcoholic steatohepatitis |
| US10441560B2 (en) | 2013-03-15 | 2019-10-15 | Mochida Pharmaceutical Co., Ltd. | Compositions and methods for treating non-alcoholic steatohepatitis |
| CN105764916B (zh) | 2013-06-05 | 2021-05-18 | 博士医疗爱尔兰有限公司 | 鸟苷酸环化酶c的超纯激动剂、制备和使用所述激动剂的方法 |
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| US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| GB0022079D0 (en) | 2000-09-08 | 2000-10-25 | Inst Of Molecul & Cell Biology | Novel protein tyrosine phosphatase inhibitor |
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2002
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- 2002-12-24 PA PA20028562901A patent/PA8562901A1/es unknown
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- 2002-12-26 UY UY27606A patent/UY27606A1/es not_active Application Discontinuation
- 2002-12-26 JO JO2002137A patent/JO2242B1/en active
- 2002-12-27 EP EP02805774A patent/EP1467996B1/en not_active Expired - Lifetime
- 2002-12-27 CN CNB028264223A patent/CN100402530C/zh not_active Expired - Fee Related
- 2002-12-27 DE DE60207759T patent/DE60207759T2/de not_active Expired - Lifetime
- 2002-12-27 WO PCT/EP2002/014771 patent/WO2003055883A1/en not_active Ceased
- 2002-12-27 ES ES02805774T patent/ES2252554T3/es not_active Expired - Lifetime
- 2002-12-27 JP JP2003556413A patent/JP4188839B2/ja not_active Expired - Fee Related
- 2002-12-27 KR KR1020047010017A patent/KR100601769B1/ko not_active Expired - Fee Related
- 2002-12-27 AT AT02805774T patent/ATE311388T1/de not_active IP Right Cessation
- 2002-12-27 BR BR0215395-5A patent/BR0215395A/pt not_active IP Right Cessation
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- 2002-12-27 MX MXPA04006266A patent/MXPA04006266A/es active IP Right Grant
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Also Published As
| Publication number | Publication date |
|---|---|
| UY27606A1 (es) | 2003-06-30 |
| KR20040068981A (ko) | 2004-08-02 |
| BR0215395A (pt) | 2004-12-07 |
| PE20030896A1 (es) | 2003-11-05 |
| MXPA04006266A (es) | 2004-09-27 |
| EP1467996B1 (en) | 2005-11-30 |
| JO2242B1 (en) | 2004-10-07 |
| AU2002367190A1 (en) | 2003-07-15 |
| TW200306313A (en) | 2003-11-16 |
| ATE311388T1 (de) | 2005-12-15 |
| WO2003055883A1 (en) | 2003-07-10 |
| AU2002367190B2 (en) | 2006-10-05 |
| CN1610683A (zh) | 2005-04-27 |
| PA8562901A1 (es) | 2003-07-28 |
| CN100402530C (zh) | 2008-07-16 |
| US20030153756A1 (en) | 2003-08-14 |
| JP2005517677A (ja) | 2005-06-16 |
| DE60207759D1 (de) | 2006-01-05 |
| EP1467996A1 (en) | 2004-10-20 |
| JP4188839B2 (ja) | 2008-12-03 |
| CA2471265A1 (en) | 2003-07-10 |
| DE60207759T2 (de) | 2006-08-03 |
| PL371180A1 (en) | 2005-06-13 |
| KR100601769B1 (ko) | 2006-07-19 |
| US6642381B2 (en) | 2003-11-04 |
| ES2252554T3 (es) | 2006-05-16 |
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