JP2010506942A - Ｃｈｋ１阻害剤の組成物 - Google Patents
Ｃｈｋ１阻害剤の組成物 Download PDFInfo
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- JP2010506942A JP2010506942A JP2009533425A JP2009533425A JP2010506942A JP 2010506942 A JP2010506942 A JP 2010506942A JP 2009533425 A JP2009533425 A JP 2009533425A JP 2009533425 A JP2009533425 A JP 2009533425A JP 2010506942 A JP2010506942 A JP 2010506942A
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- alkylene
- cancer
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- alkyl
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Classifications
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B82—NANOTECHNOLOGY
- B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
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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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
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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
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| PCT/US2007/080150 WO2008067027A2 (en) | 2006-10-20 | 2007-10-02 | Compositions of chkl inhibitors and cyclodextrin |
Publications (2)
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| JP2010506942A true JP2010506942A (ja) | 2010-03-04 |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014526512A (ja) * | 2011-09-18 | 2014-10-06 | ユーロ−セルティーク エス．エイ． | 医薬組成物 |
| JP2017155023A (ja) * | 2016-03-04 | 2017-09-07 | ジェイファーマ株式会社 | Ｌａｔ１阻害活性を有する芳香族アミノ酸誘導体を含有する注射剤 |
| JP2018203747A (ja) * | 2012-04-13 | 2018-12-27 | エル アンド エフ リサーチ，リミテッド ライアビリティー カンパニー | シクロデキストリンを使用するための方法 |
| JP2023026562A (ja) * | 2017-05-03 | 2023-02-24 | サイデックス・ファーマシューティカルズ・インコーポレイテッド | シクロデキストリン及びブスルファンを含有する組成物 |
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|---|---|---|---|---|
| US11020363B2 (en) | 2009-05-29 | 2021-06-01 | Cydex Pharmaceuticals, Inc. | Injectable nitrogen mustard compositions comprising a cyclodextrin derivative and methods of making and using the same |
| JP5914328B2 (ja) | 2009-05-29 | 2016-05-11 | サイデックス・ファーマシューティカルズ・インコーポレイテッド | シクロデキストリン誘導体を含む注射用メルファラン組成物並びにその製造及び使用方法 |
| GB201008005D0 (en) | 2010-05-13 | 2010-06-30 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| PH12014500547A1 (en) | 2011-10-03 | 2014-04-21 | Respivert Ltd | 1-pyrazolyl-3-(-4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 map kinase inhibitors |
| EP2578582A1 (en) | 2011-10-03 | 2013-04-10 | Respivert Limited | 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors |
| TWI573792B (zh) | 2012-02-01 | 2017-03-11 | 歐陸斯迪公司 | 新穎治療劑 |
| US9993460B2 (en) | 2013-07-26 | 2018-06-12 | Race Oncology Ltd. | Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof |
| JP6586098B2 (ja) | 2014-02-14 | 2019-10-02 | レスピバート・リミテツド | キナーゼ阻害剤としてのピラゾリル尿素 |
| GB201409488D0 (en) | 2014-05-28 | 2014-07-09 | Euro Celtique Sa | Pharmaceutical composition |
| GB201409485D0 (en) | 2014-05-28 | 2014-07-09 | Euro Celtique Sa | Pharmaceutical composition |
| GB201409471D0 (en) | 2014-05-28 | 2014-07-09 | Euro Celtique Sa | Pharmaceutical composition |
| US9890564B2 (en) * | 2014-10-28 | 2018-02-13 | Sargent Manufacturing Company | Interconnected lock with direct drive for adjustable deadbolt to latchbolt spacing |
| US20200000840A1 (en) * | 2016-03-20 | 2020-01-02 | Asdera Llc | Use of cyclodextrins to reduce endocytosis in malignant and neurodegenerative disorders |
| WO2018068832A1 (en) | 2016-10-11 | 2018-04-19 | Euro-Celtique S.A. | Hodgkin lymphoma therapy |
| GB201709403D0 (en) | 2017-06-13 | 2017-07-26 | Euro Celtique Sa | Compounds for treating sarcoma |
| GB201709402D0 (en) | 2017-06-13 | 2017-07-26 | Euro Celtique Sa | Compounds for treating t-pll |
| GB201709405D0 (en) | 2017-06-13 | 2017-07-26 | Euro Celtique Sa | Compounds for treating ovarian cancer |
| GB201709406D0 (en) | 2017-06-13 | 2017-07-26 | Euro-Cletique S A | Compounds for treating TNBC |
| WO2019067269A2 (en) | 2017-09-28 | 2019-04-04 | Asdera Llc | USE OF CYCLODEXTRINS IN DISEASES AND DISORDERS INVOLVING PHOSPHOLIPID DISRUPTION |
| CN109078005B (zh) * | 2018-08-07 | 2021-11-26 | 江苏领航生物科技有限公司 | 一种白消安组合物及其制备方法和应用 |
| EP3897625A1 (en) | 2018-12-18 | 2021-10-27 | Mundipharma International Corporation Limited | Compounds for treating lymphoma or a t-cell malignant disease |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2024246220A1 (en) * | 2023-05-31 | 2024-12-05 | Institut National de la Santé et de la Recherche Médicale | Methods and compositions for treating lung cancer |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025217307A1 (en) | 2024-04-09 | 2025-10-16 | Revolution Medicines, Inc. | Methods for predicting response to a ras(on) inhibitor and combination therapies |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61500788A (ja) * | 1983-12-21 | 1986-04-24 | ヤンセン・フア−マセウテイカ・エヌ・ヴエ− | 水に不安定なまたは僅かに溶解性の薬物を含有する医薬調製物およびその製造方法 |
| JPH029825A (ja) * | 1988-03-29 | 1990-01-12 | Univ Florida | 非経口投与用薬剤組成物 |
| JP2003522207A (ja) * | 1998-02-23 | 2003-07-22 | サイクロプス・イーエイチエフ | 高エネルギーシクロデキストリン複合体 |
| WO2005040106A1 (en) * | 2003-10-23 | 2005-05-06 | Amorepacific Corporation | Thiourea derivative-containing pharmaceutical composition having improved solubility and bioavailability |
| JP2005536471A (ja) * | 2002-05-31 | 2005-12-02 | アストラゼネカ アクチボラグ | 即時放出性医薬製剤 |
| WO2006105262A1 (en) * | 2005-03-29 | 2006-10-05 | Icos Corporation | HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHKl |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU193933B (en) * | 1984-06-08 | 1987-12-28 | Nitrokemia Ipartelepek | Herbicide or plant growth stimulating agent comprising beta-cyclodextrin complex of benzolsulphonylurea derivative and process for preparing the active substances |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| GB9001987D0 (en) | 1990-01-29 | 1990-03-28 | Janssen Pharmaceutica Nv | Improved cyclodextrin based erythropietin formulation |
| US5602112A (en) | 1992-06-19 | 1997-02-11 | Supergen, Inc. | Pharmaceutical formulation |
| US6046177A (en) | 1997-05-05 | 2000-04-04 | Cydex, Inc. | Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations |
| WO2002007772A2 (en) * | 2000-07-24 | 2002-01-31 | Boehringer Ingelheim Pharmaceuticals, Inc. | Improved oral dosage formulations |
| UA76977C2 (en) | 2001-03-02 | 2006-10-16 | Icos Corp | Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers |
| CA2454913A1 (en) * | 2001-08-20 | 2003-02-27 | Boehringer Ingelheim Pharmaceuticals, Inc. | Parenteral formulations of 1-(5-tert-butyl-2-p-tolyl-2h-pryrazol-3-yl)-3-¬4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl|-urea and a cyclodextrin |
| WO2005027907A1 (en) * | 2003-09-17 | 2005-03-31 | Icos Corporation | Use of chk1 inhibitors to control cell proliferation |
| CN1813739A (zh) | 2005-11-25 | 2006-08-09 | 王颖 | 一种注射用盐酸纳美芬冻干粉针制剂 |
-
2007
- 2007-10-02 CN CN2007800390301A patent/CN101528215B/zh not_active Expired - Fee Related
- 2007-10-02 BR BRPI0717460-8A2A patent/BRPI0717460A2/pt not_active IP Right Cessation
- 2007-10-02 MY MYPI20091558 patent/MY150649A/en unknown
- 2007-10-02 KR KR1020117017995A patent/KR20110098009A/ko not_active Ceased
- 2007-10-02 EP EP07871106A patent/EP2063879A2/en not_active Withdrawn
- 2007-10-02 AU AU2007325576A patent/AU2007325576B2/en not_active Ceased
- 2007-10-02 KR KR1020097007975A patent/KR20090065537A/ko not_active Ceased
- 2007-10-02 JP JP2009533425A patent/JP2010506942A/ja active Pending
- 2007-10-02 CA CA2673483A patent/CA2673483C/en not_active Expired - Fee Related
- 2007-10-02 NZ NZ575394A patent/NZ575394A/en not_active IP Right Cessation
- 2007-10-02 US US12/442,529 patent/US8455471B2/en not_active Expired - Fee Related
- 2007-10-02 UA UAA200903745A patent/UA95310C2/ru unknown
- 2007-10-02 MX MX2009004214A patent/MX2009004214A/es active IP Right Grant
- 2007-10-02 EA EA200900571A patent/EA200900571A1/ru unknown
- 2007-10-02 WO PCT/US2007/080150 patent/WO2008067027A2/en not_active Ceased
-
2009
- 2009-03-20 CR CR10680A patent/CR10680A/es unknown
- 2009-03-26 IL IL197869A patent/IL197869A/en not_active IP Right Cessation
- 2009-04-17 TN TNP2009000146A patent/TN2009000146A1/fr unknown
- 2009-04-17 ZA ZA200902670A patent/ZA200902670B/xx unknown
- 2009-04-17 CO CO09039148A patent/CO6180503A2/es not_active Application Discontinuation
- 2009-04-20 SV SV2009003227A patent/SV2009003227A/es unknown
- 2009-04-20 NO NO20091544A patent/NO20091544L/no not_active Application Discontinuation
- 2009-05-07 MA MA31850A patent/MA30872B1/fr unknown
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61500788A (ja) * | 1983-12-21 | 1986-04-24 | ヤンセン・フア−マセウテイカ・エヌ・ヴエ− | 水に不安定なまたは僅かに溶解性の薬物を含有する医薬調製物およびその製造方法 |
| JPH029825A (ja) * | 1988-03-29 | 1990-01-12 | Univ Florida | 非経口投与用薬剤組成物 |
| JP2003522207A (ja) * | 1998-02-23 | 2003-07-22 | サイクロプス・イーエイチエフ | 高エネルギーシクロデキストリン複合体 |
| JP2005536471A (ja) * | 2002-05-31 | 2005-12-02 | アストラゼネカ アクチボラグ | 即時放出性医薬製剤 |
| WO2005040106A1 (en) * | 2003-10-23 | 2005-05-06 | Amorepacific Corporation | Thiourea derivative-containing pharmaceutical composition having improved solubility and bioavailability |
| JP2007509137A (ja) * | 2003-10-23 | 2007-04-12 | 株式會社アモーレパシフィック | 溶解性及び生体内利用率が改善されたチオウレア誘導体含有の医薬用組成物 |
| WO2006105262A1 (en) * | 2005-03-29 | 2006-10-05 | Icos Corporation | HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHKl |
| JP2008535830A (ja) * | 2005-03-29 | 2008-09-04 | イコス・コーポレイション | Ｃｈｋ１阻害に有用なヘテロアリール尿素誘導体 |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014526512A (ja) * | 2011-09-18 | 2014-10-06 | ユーロ−セルティーク エス．エイ． | 医薬組成物 |
| JP2018039848A (ja) * | 2011-09-18 | 2018-03-15 | ユーロ−セルティーク エス．エイ． | 医薬組成物 |
| JP2018203747A (ja) * | 2012-04-13 | 2018-12-27 | エル アンド エフ リサーチ，リミテッド ライアビリティー カンパニー | シクロデキストリンを使用するための方法 |
| US10980828B2 (en) | 2012-04-13 | 2021-04-20 | L & F Research LLC | Method of using cyclodextrin |
| JP2017155023A (ja) * | 2016-03-04 | 2017-09-07 | ジェイファーマ株式会社 | Ｌａｔ１阻害活性を有する芳香族アミノ酸誘導体を含有する注射剤 |
| JP2023026562A (ja) * | 2017-05-03 | 2023-02-24 | サイデックス・ファーマシューティカルズ・インコーポレイテッド | シクロデキストリン及びブスルファンを含有する組成物 |
| JP7597778B2 (ja) | 2017-05-03 | 2024-12-10 | サイデックス・ファーマシューティカルズ・インコーポレイテッド | シクロデキストリン及びブスルファンを含有する組成物 |
Also Published As
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|---|---|
| ZA200902670B (en) | 2010-06-30 |
| CR10680A (es) | 2009-10-13 |
| WO2008067027A3 (en) | 2009-04-16 |
| KR20090065537A (ko) | 2009-06-22 |
| EP2063879A2 (en) | 2009-06-03 |
| MY150649A (en) | 2014-02-14 |
| UA95310C2 (ru) | 2011-07-25 |
| AU2007325576A1 (en) | 2008-06-05 |
| BRPI0717460A2 (pt) | 2013-12-24 |
| KR20110098009A (ko) | 2011-08-31 |
| CA2673483C (en) | 2014-04-08 |
| IL197869A (en) | 2013-11-28 |
| AU2007325576B2 (en) | 2013-01-10 |
| US8455471B2 (en) | 2013-06-04 |
| NZ575394A (en) | 2012-01-12 |
| EA200900571A1 (ru) | 2009-12-30 |
| CA2673483A1 (en) | 2008-06-05 |
| SV2009003227A (es) | 2010-02-04 |
| CN101528215B (zh) | 2011-10-19 |
| MX2009004214A (es) | 2009-05-11 |
| WO2008067027A2 (en) | 2008-06-05 |
| CN101528215A (zh) | 2009-09-09 |
| MA30872B1 (fr) | 2009-11-02 |
| US20100022512A1 (en) | 2010-01-28 |
| TN2009000146A1 (en) | 2010-10-18 |
| NO20091544L (no) | 2009-06-10 |
| CO6180503A2 (es) | 2010-07-19 |
| IL197869A0 (en) | 2009-12-24 |
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