AR076433A1 - Sales inhibidoras de cdk - Google Patents
Sales inhibidoras de cdkInfo
- Publication number
- AR076433A1 AR076433A1 ARP100101427A ARP100101427A AR076433A1 AR 076433 A1 AR076433 A1 AR 076433A1 AR P100101427 A ARP100101427 A AR P100101427A AR P100101427 A ARP100101427 A AR P100101427A AR 076433 A1 AR076433 A1 AR 076433A1
- Authority
- AR
- Argentina
- Prior art keywords
- salts
- hydrochloride
- cdk inhibitor
- crystalline
- malate
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title abstract 5
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 title abstract 2
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 title abstract 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 4
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 abstract 2
- AEMRFAOFKBGASW-UHFFFAOYSA-M Glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 abstract 2
- JVTAAEKCZFNVCJ-REOHCLBHSA-N L-lactic acid Chemical compound C[C@H](O)C(O)=O JVTAAEKCZFNVCJ-REOHCLBHSA-N 0.000 abstract 2
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 abstract 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 2
- 229910019142 PO4 Inorganic materials 0.000 abstract 2
- WNLRTRBMVRJNCN-UHFFFAOYSA-L adipate(2-) Chemical compound [O-]C(=O)CCCCC([O-])=O WNLRTRBMVRJNCN-UHFFFAOYSA-L 0.000 abstract 2
- 229940116871 l-lactate Drugs 0.000 abstract 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 abstract 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 abstract 2
- 239000010452 phosphate Substances 0.000 abstract 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 abstract 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000012458 free base Substances 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- QYRFJLLXPINATB-UHFFFAOYSA-N hydron;2,4,5,6-tetrafluorobenzene-1,3-diamine;dichloride Chemical compound Cl.Cl.NC1=C(F)C(N)=C(F)C(F)=C1F QYRFJLLXPINATB-UHFFFAOYSA-N 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- -1 salts fumarate Chemical class 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Communicable Diseases (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Virology (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Forma(s) cristalina(s) de sales solubles en agua y de la base libre de un inhibidor de cdk. Estas sales cristalinas son, por ejemplo, fumarato, L-malato, maleato, succinato, adipato, malonato, glicolato, fosfato, mesilato, L-lactato, clorhidrato, di-clorhidrato y tri-clorhidrato. Hidratos y polimorfos de estas formas de sales, un proceso para su preparacion, su utilidad en terapia y las composiciones farmacéuticas que las contienen, también se reivindican y describen en la presente solicitud. Reivindicacion 1: Sales y sus formas cristalinas del compuesto 125, caracterizadas porque tienen la formula (1) seleccionadas entre las sales fumarato, L-malato, maleato, succinato, adipato, malonato, glicolato, fosfato, mesilato y L-lactato.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09159030 | 2009-04-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR076433A1 true AR076433A1 (es) | 2011-06-08 |
Family
ID=42199163
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101427A AR076433A1 (es) | 2009-04-29 | 2010-04-28 | Sales inhibidoras de cdk |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8586598B2 (es) |
| EP (1) | EP2424868B1 (es) |
| JP (1) | JP5801285B2 (es) |
| CN (1) | CN102428086B (es) |
| AR (1) | AR076433A1 (es) |
| ES (1) | ES2660146T3 (es) |
| TW (1) | TW201043631A (es) |
| WO (1) | WO2010125004A1 (es) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2591191C2 (ru) * | 2011-01-26 | 2016-07-10 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Трициклические пирроло производные, способ их получения и их применение в качестве ингибиторов киназы |
| JP5925808B2 (ja) * | 2011-01-26 | 2016-05-25 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | 三環式誘導体、これらの調製方法およびこれらのキナーゼ阻害剤としての使用 |
| TR201902875T4 (tr) | 2013-10-18 | 2019-03-21 | Univ Health Network | Plk-4 inhibitörünün tuz ve kristal formları. |
| MX368767B (es) | 2014-04-07 | 2019-10-15 | Netherlands Translational Res Center B V | (5,6-dihidro)pirimido[4,5-e]indolizinas. |
| JP7038675B2 (ja) | 2016-03-11 | 2022-03-18 | ステルス バイオセラピューティクス インコーポレイテッド | 結晶塩形態 |
| CN107216340B (zh) * | 2016-03-22 | 2021-05-04 | 中国科学院上海药物研究所 | 一种dppiv抑制剂的盐型及其制备方法 |
| CN107216339B (zh) * | 2016-03-22 | 2021-05-04 | 中国科学院上海药物研究所 | 一种dppiv抑制剂马来酸盐的多晶型及其制备方法 |
| CN110914287A (zh) | 2017-04-05 | 2020-03-24 | 隐形生物治疗公司 | Boc-d-arg-dmt-lys-(boc)-phe-nh2的结晶盐形式 |
| US10676506B2 (en) | 2018-01-26 | 2020-06-09 | Stealth Biotherapeutics Corp. | Crystalline bis- and tris-hydrochloride salt of elamipretide |
| EP3747880B1 (en) * | 2018-01-29 | 2023-05-03 | Xuanzhu Biopharmaceutical Co., Ltd. | Crystal form targeting cdk4/6 kinase inhibitor |
| CN110092775B (zh) * | 2018-01-29 | 2021-09-10 | 轩竹生物科技有限公司 | 靶向cdk4/6激酶抑制剂的晶型 |
| CN109632555B (zh) * | 2018-12-28 | 2021-07-27 | 上海新黄河制药有限公司 | 一种富马酸福莫特罗无定型含量的动态蒸汽吸附分析方法 |
| BR112021021106A2 (pt) | 2019-04-24 | 2021-12-14 | Univ Health Network | Forma cristalina s4 do inibidor plk4 fumarato (ir,2s)-(e)-2-(3-(4-((cis-2,6-dimetilmorfolino)metil)estiril)-1h-imidazol-6-il)-5'-metoxiespiro[ciclopropano-1,3'-indolin]-2'ona |
| CN112010839B (zh) * | 2019-05-31 | 2022-06-17 | 轩竹生物科技股份有限公司 | 靶向丝/苏氨酸激酶抑制剂的晶型 |
| ES3048697T3 (en) * | 2019-09-30 | 2025-12-11 | Univ Mainz | Cdk4/6 inhibitors for the treatment of psoriasis |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | 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 |
| WO2025255438A1 (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 |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030100594A1 (en) * | 2001-08-10 | 2003-05-29 | Pharmacia Corporation | Carbonic anhydrase inhibitor |
| ME00142B (me) * | 2003-05-22 | 2010-10-10 | Nerviano Medical Sciences Srl | Derivati pirazolo-hinazolina, postupci za njihovo dobijanje i njihova upotreba kao inhibitora kinaze |
| WO2007090794A1 (en) | 2006-02-10 | 2007-08-16 | Nerviano Medical Sciences S.R.L. | Combinations comprising a cdk inhibitor and a growth factor antibody or anti-mitotic |
| EP2019101A1 (en) * | 2007-07-26 | 2009-01-28 | GPC Biotech AG | Pyrazol[3,4-d]pyrimidin-4-one useful as Kinase Inhibitor |
| MX2010003269A (es) * | 2007-09-25 | 2010-08-02 | Bayer Healthcare Llc | Derivados de pirrolotriazina utiles para tratar cancer a traves de la inhibicion de la aurora quinasa. |
| US8022216B2 (en) * | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
| CN102105151B (zh) * | 2008-07-29 | 2013-12-18 | 内尔维阿诺医学科学有限公司 | Cdk抑制剂在治疗神经胶质瘤中的应用 |
| CN102105152B (zh) * | 2008-07-29 | 2012-10-17 | 内尔维阿诺医学科学有限公司 | 包含cdks抑制剂和抗肿瘤剂的治疗组合 |
| CN102223885B (zh) * | 2008-11-24 | 2013-04-03 | 内尔维阿诺医学科学有限公司 | 用于治疗间皮瘤的cdk抑制剂 |
| EP2408776B1 (en) * | 2009-03-20 | 2014-01-08 | Nerviano Medical Sciences S.r.l. | Use of a kinase inhibitor for the treatment of thymoma |
-
2010
- 2010-04-23 US US13/265,918 patent/US8586598B2/en active Active
- 2010-04-23 JP JP2012507696A patent/JP5801285B2/ja active Active
- 2010-04-23 WO PCT/EP2010/055463 patent/WO2010125004A1/en not_active Ceased
- 2010-04-23 EP EP10715240.7A patent/EP2424868B1/en active Active
- 2010-04-23 CN CN201080018865.0A patent/CN102428086B/zh active Active
- 2010-04-23 ES ES10715240.7T patent/ES2660146T3/es active Active
- 2010-04-27 TW TW099113232A patent/TW201043631A/zh unknown
- 2010-04-28 AR ARP100101427A patent/AR076433A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP5801285B2 (ja) | 2015-10-28 |
| CN102428086B (zh) | 2014-08-20 |
| CN102428086A (zh) | 2012-04-25 |
| TW201043631A (en) | 2010-12-16 |
| US8586598B2 (en) | 2013-11-19 |
| ES2660146T3 (es) | 2018-03-21 |
| WO2010125004A1 (en) | 2010-11-04 |
| JP2012525345A (ja) | 2012-10-22 |
| EP2424868B1 (en) | 2018-01-10 |
| EP2424868A1 (en) | 2012-03-07 |
| HK1169408A1 (en) | 2013-01-25 |
| US20120041007A1 (en) | 2012-02-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |