JP2002509139A5 - - Google Patents
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- Publication number
- JP2002509139A5 JP2002509139A5 JP2000540125A JP2000540125A JP2002509139A5 JP 2002509139 A5 JP2002509139 A5 JP 2002509139A5 JP 2000540125 A JP2000540125 A JP 2000540125A JP 2000540125 A JP2000540125 A JP 2000540125A JP 2002509139 A5 JP2002509139 A5 JP 2002509139A5
- Authority
- JP
- Japan
- Prior art keywords
- deoxy
- amino
- acceptable salt
- pharmacologically acceptable
- diluent
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 description 37
- 239000003085 diluting agent Substances 0.000 description 30
- 239000008194 pharmaceutical composition Substances 0.000 description 26
- 239000003937 drug carrier Substances 0.000 description 25
- 206010028980 Neoplasm Diseases 0.000 description 16
- 231100000252 nontoxic Toxicity 0.000 description 15
- 230000003000 nontoxic effect Effects 0.000 description 15
- 206010061218 Inflammation Diseases 0.000 description 10
- 239000013566 allergen Substances 0.000 description 10
- 239000002246 antineoplastic agent Substances 0.000 description 10
- 208000006673 asthma Diseases 0.000 description 10
- 230000006472 autoimmune response Effects 0.000 description 10
- 208000035269 cancer or benign tumor Diseases 0.000 description 10
- 239000003814 drug Substances 0.000 description 10
- 230000004054 inflammatory process Effects 0.000 description 10
- 238000004519 manufacturing process Methods 0.000 description 10
- 239000000126 substance Substances 0.000 description 9
- 230000003432 anti-folate effect Effects 0.000 description 6
- 229940127074 antifolate Drugs 0.000 description 6
- 239000004052 folic acid antagonist Substances 0.000 description 6
- 230000004044 response Effects 0.000 description 6
- 208000027866 inflammatory disease Diseases 0.000 description 5
- 230000002401 inhibitory effect Effects 0.000 description 5
- RCCMXKJGURLWPB-BYPYZUCNSA-N 4-methylene-L-glutamic acid Chemical group OC(=O)[C@@H](N)CC(=C)C(O)=O RCCMXKJGURLWPB-BYPYZUCNSA-N 0.000 description 4
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 3
- 159000000000 sodium salts Chemical group 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/008,613 | 1998-01-17 | ||
| US09/008,613 US5912251A (en) | 1998-01-17 | 1998-01-17 | Metabolically inert anti-inflammatory and anti-tumor antifolates |
| PCT/US1999/000948 WO1999036409A1 (en) | 1998-01-17 | 1999-01-13 | Metabolically inert anti-inflammatory and anti-tumor antifolates |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002509139A JP2002509139A (ja) | 2002-03-26 |
| JP2002509139A5 true JP2002509139A5 (https=) | 2007-01-11 |
| JP4854850B2 JP4854850B2 (ja) | 2012-01-18 |
Family
ID=21732611
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000540125A Expired - Lifetime JP4854850B2 (ja) | 1998-01-17 | 1999-01-13 | 代謝的に不活性な抗炎症性および抗腫瘍性葉酸拮抗剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US5912251A (https=) |
| EP (2) | EP1062209B1 (https=) |
| JP (1) | JP4854850B2 (https=) |
| DE (1) | DE69940881D1 (https=) |
| WO (1) | WO1999036409A1 (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5079969B2 (ja) * | 2001-04-04 | 2012-11-21 | バイオニューメリック・ファーマスーティカルズ・インコーポレイテッド | 葉酸拮抗剤骨格へのアミノ酸のカップリング方法 |
| GB0219897D0 (en) * | 2002-08-27 | 2002-10-02 | Melacure Therapeutics Ab | Pharmaceutically active compounds |
| US7563590B2 (en) * | 2002-08-30 | 2009-07-21 | Cypress Bioscience Inc. | Methods of quantifying methotrexate metabolites |
| US20040092739A1 (en) * | 2002-11-13 | 2004-05-13 | Zejun Xiao | Process for synthesizing antifolates |
| US7060825B2 (en) * | 2003-07-25 | 2006-06-13 | Bionumerik Pharmaceuticals, Inc. | Process for synthesizing 6-quinazolinyl-ethyl-benzoyl and related antifolates |
| US20050032807A1 (en) * | 2003-08-06 | 2005-02-10 | Rosenwald Lindsay A. | Methods of treating inflammatory diseases with ammonium salts of ornitihine derivatives |
| EP1791544A4 (en) * | 2004-09-08 | 2007-09-12 | Chelsea Therapeutics Inc | CHINAZOLINE DERIVATIVES AS METABOLIC INERT ANTIFOLATE |
| BRPI0806632A2 (pt) * | 2007-01-19 | 2011-09-06 | Chelsea Therapeutics Inc | composto, composição farmacêutica, método para o tratamento de uma condição selecionada a partir do grupo constituìdo de proliferação celular anormal, inflamação, asma e artrite |
| WO2009126637A1 (en) * | 2008-04-07 | 2009-10-15 | Chelsea Therapeutics, Inc. | Antifolate compositions |
| US20100260825A1 (en) * | 2009-04-13 | 2010-10-14 | Nair Madhavan G | Antifolates for the treatment of cardiovascular, inflammatory, neoplastic, autoimmune and related diseases in sublingual dosage units, film strips, or skin patches |
| AU2010270596A1 (en) * | 2009-07-08 | 2012-02-02 | Chelsea Therapeutics, Inc. | Stable crystalline polymorphs of the dipotassium salt of (S) -2- {4- [2- (2, 4-diamino-quinazolin-6-yl) -ethyl] -benzoylamino} -4-methylene-pentanedioic acid |
| AU2010315152A1 (en) | 2009-11-06 | 2012-06-14 | Chelsea Therapeutics, Inc. | Enzyme inhibiting compounds |
| US20110237609A1 (en) * | 2010-03-29 | 2011-09-29 | Chelsea Therapeutics, Inc. | Antifolate compositions |
| WO2012078708A1 (en) | 2010-12-07 | 2012-06-14 | Chelsea Therapeutics, Inc. | Combination comprising methotrexate and an antifolate compound |
| WO2018031968A1 (en) | 2016-08-12 | 2018-02-15 | L.E.A.F. Holdings Group Llc | Alpha and gamma-d polyglutamated antifolates and uses thereof |
| CN120939250A (zh) | 2016-08-12 | 2025-11-14 | L.E.A.F.控股集团公司 | 聚谷氨酸化抗叶酸剂及其用途 |
| JP7491573B2 (ja) | 2018-02-07 | 2024-05-28 | エル．イー．エー．エフ． ホールディングス グループ エルエルシー | アルファポリグルタミン酸化メトトレキセートおよびその使用 |
| WO2019157123A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated aminopterin and uses thereof |
| US12246015B2 (en) | 2018-02-07 | 2025-03-11 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated raltitrexed and uses thereof |
| US12220431B2 (en) | 2018-02-07 | 2025-02-11 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated antifolates and uses thereof |
| WO2019157129A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated pralatrexate and uses thereof |
| CA3090500A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated antifolates and uses thereof |
| EP3749311A4 (en) | 2018-02-07 | 2022-07-06 | L.E.A.F Holdings Group LLC | PEMETREXED POLYGLUTAMATE GAMMA COMPOSITIONS AND THEIR USES |
| US12239734B2 (en) | 2018-02-07 | 2025-03-04 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated raltitrexed and uses thereof |
| WO2019157121A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated lometrexol and uses thereof |
| CN111954531A (zh) | 2018-02-07 | 2020-11-17 | L.E.A.F.控股集团公司 | α聚谷氨酸化培美曲塞及其用途 |
| EP3749319A4 (en) | 2018-02-07 | 2022-06-22 | L.E.A.F Holdings Group LLC | TETRAHYDROFOLATES ALPHA POLYGLUTAMATE AND THEIR USES |
| CN111936145A (zh) | 2018-02-14 | 2020-11-13 | L.E.A.F.控股集团公司 | γ聚谷氨酸化氨甲蝶呤及其用途 |
| EP3752157A4 (en) | 2018-02-14 | 2022-07-06 | L.E.A.F Holdings Group LLC | GAMMA-POLYGLUTAMATED LOMETREXOLE AND USES THEREOF |
| WO2019160732A1 (en) | 2018-02-14 | 2019-08-22 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated aminopterin and uses thereof |
| EP3752156A4 (en) | 2018-02-14 | 2021-10-27 | L.E.A.F Holdings Group LLC | GAMMA-POLYGLUTAMIZED PRALATREXATE AND USES THEREOF |
| US12048766B2 (en) | 2018-02-14 | 2024-07-30 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated tetrahydrofolates and uses thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8607683D0 (en) * | 1986-03-27 | 1986-04-30 | Ici Plc | Anti-tumor agents |
| US4818753A (en) * | 1987-09-18 | 1989-04-04 | Sri International | Synthesis and method of use for 2, 4 diaminoquinazoline |
| JP2830008B2 (ja) * | 1988-04-01 | 1998-12-02 | 武田薬品工業株式会社 | 縮合ピリミジン誘導体 |
| US4996207A (en) * | 1990-01-18 | 1991-02-26 | Nair Madhavan G | Three new non-polyglutamatable deazaaminopterins |
| US5073554A (en) * | 1990-01-18 | 1991-12-17 | Nair Madhavan G | Two non-polyglutamatable antifolates |
| US5550128A (en) * | 1994-09-09 | 1996-08-27 | Nair; Madhavan G. | Enantiomers of gamma methylene 10-deaza aminopterin and process for preparing the same |
| US5593999A (en) * | 1995-06-07 | 1997-01-14 | Nair; Madhavan G. | Non-classical folate analogue inhibitors of glycinamide ribonucleotide formyltransferase (GARFT) |
-
1998
- 1998-01-17 US US09/008,613 patent/US5912251A/en not_active Expired - Lifetime
-
1999
- 1999-01-13 EP EP99903128A patent/EP1062209B1/en not_active Expired - Lifetime
- 1999-01-13 WO PCT/US1999/000948 patent/WO1999036409A1/en not_active Ceased
- 1999-01-13 JP JP2000540125A patent/JP4854850B2/ja not_active Expired - Lifetime
- 1999-01-13 EP EP05004632A patent/EP1535911A1/en not_active Withdrawn
- 1999-01-13 DE DE69940881T patent/DE69940881D1/de not_active Expired - Lifetime
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