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 US5912251A (en) | 1998-01-17 | 1998-01-17 | Metabolically inert anti-inflammatory and anti-tumor antifolates |
| US09/008,613 | 1998-01-17 | ||
| 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 |
|---|---|---|---|---|
| AU2002306824B2 (en) * | 2001-04-04 | 2007-10-25 | Bionumerik Pharmaceuticals, Inc. | Process for coupling amino acids to an antifolate scaffold |
| 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 |
| JP2008512490A (ja) * | 2004-09-08 | 2008-04-24 | チェルシー・セラピューティクス，インコーポレイテッド | 異常細胞増殖および炎症の障害を治療するための代謝的に不活性な葉酸拮抗剤 |
| JP2010516694A (ja) * | 2007-01-19 | 2010-05-20 | チェルシー・セラピューティクス，インコーポレイテッド | 新規な伝統的葉酸拮抗剤 |
| KR20100132061A (ko) * | 2008-04-07 | 2010-12-16 | 첼시 쎄라퓨틱스, 인코포레이티드 | 항엽산제 화합물의 결정 염 형태 및 이의 제조 방법 |
| 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 |
| MX2012000437A (es) * | 2009-07-08 | 2012-02-21 | Chelsea Therapeutics Inc | Polimorfos cristalinos estables de la sal dipotasica de acido (s)-2-{2,4-diamono-quizolin-6-il)-etil]-benzoilamino}-4-metilen-p entanodioico. |
| 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 |
| CN121177507A (zh) | 2016-08-12 | 2025-12-23 | L.E.A.F.控股集团公司 | α和γ-D聚谷氨酸化抗叶酸剂及其用途 |
| EP3749318A4 (en) | 2018-02-07 | 2022-07-06 | L.E.A.F Holdings Group LLC | GAMMA-POLYGLUTAMATED RALTITREXED AND ITS USES |
| US12310966B2 (en) | 2018-02-07 | 2025-05-27 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated aminopterin and uses thereof |
| US12220431B2 (en) | 2018-02-07 | 2025-02-11 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated antifolates and uses thereof |
| EP3749319A4 (en) | 2018-02-07 | 2022-06-22 | L.E.A.F Holdings Group LLC | TETRAHYDROFOLATES ALPHA POLYGLUTAMATE AND THEIR USES |
| EP3749314A4 (en) | 2018-02-07 | 2022-02-23 | L.E.A.F Holdings Group LLC | ALPHA-POLYGLUTAMATE METHOTREXATE AND ITS USES |
| WO2019157121A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated lometrexol and uses thereof |
| WO2019157145A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated pemetrexed and uses thereof |
| CA3090389A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated raltitrexed and uses thereof |
| WO2019157129A1 (en) | 2018-02-07 | 2019-08-15 | L.E.A.F. Holdings Group Llc | Alpha polyglutamated pralatrexate and uses thereof |
| CN111867593A (zh) | 2018-02-07 | 2020-10-30 | L.E.A.F.控股集团公司 | α聚谷氨酸化抗叶酸剂及其用途 |
| JP7491572B2 (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ペメトレキセドおよびその使用 |
| WO2019160735A1 (en) | 2018-02-14 | 2019-08-22 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated tetrahydrofolates and uses thereof |
| WO2019160734A1 (en) | 2018-02-14 | 2019-08-22 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated lometrexol and uses thereof |
| CA3090753A1 (en) | 2018-02-14 | 2019-08-22 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated pralatrexate and uses thereof |
| JP7462950B2 (ja) | 2018-02-14 | 2024-04-08 | 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 | ガンマポリグルタミン酸化メトトレキセートおよびその使用 |
| US12350271B2 (en) | 2018-02-14 | 2025-07-08 | L.E.A.F. Holdings Group Llc | Gamma polyglutamated aminopterin 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 |
| US5073554A (en) * | 1990-01-18 | 1991-12-17 | Nair Madhavan G | Two non-polyglutamatable antifolates |
| US4996207A (en) * | 1990-01-18 | 1991-02-26 | Nair Madhavan G | Three new non-polyglutamatable deazaaminopterins |
| 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 EP EP05004632A patent/EP1535911A1/en not_active Withdrawn
- 1999-01-13 WO PCT/US1999/000948 patent/WO1999036409A1/en not_active Ceased
- 1999-01-13 DE DE69940881T patent/DE69940881D1/de not_active Expired - Lifetime
- 1999-01-13 JP JP2000540125A patent/JP4854850B2/ja not_active Expired - Lifetime
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