BRPI0922642B8 - formas polimórficas de sal de cloridrato de 3-(1-{3-[5-(1-metil-piperidin-4-ilmetóxi)-pirimidin-2-il]-benzil}-6-oxo-1,6-di-hidro-piridazin-3-il)-benzonitrila,seus processos de fabricação, composição farmacêutica, medicamento, e kit - Google Patents
formas polimórficas de sal de cloridrato de 3-(1-{3-[5-(1-metil-piperidin-4-ilmetóxi)-pirimidin-2-il]-benzil}-6-oxo-1,6-di-hidro-piridazin-3-il)-benzonitrila,seus processos de fabricação, composição farmacêutica, medicamento, e kitInfo
- Publication number
- BRPI0922642B8 BRPI0922642B8 BRPI0922642A BRPI0922642A BRPI0922642B8 BR PI0922642 B8 BRPI0922642 B8 BR PI0922642B8 BR PI0922642 A BRPI0922642 A BR PI0922642A BR PI0922642 A BRPI0922642 A BR PI0922642A BR PI0922642 B8 BRPI0922642 B8 BR PI0922642B8
- Authority
- BR
- Brazil
- Prior art keywords
- ylmethoxy
- pyridazin
- benzonitrile
- oxo
- benzyl
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 3
- 239000003814 drug Substances 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 150000003839 salts Chemical group 0.000 title 1
- AHYMHWXQRWRBKT-UHFFFAOYSA-N tepotinib Chemical compound C1CN(C)CCC1COC1=CN=C(C=2C=C(CN3C(C=CC(=N3)C=3C=C(C=CC=3)C#N)=O)C=CC=2)N=C1 AHYMHWXQRWRBKT-UHFFFAOYSA-N 0.000 title 1
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Substances N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 abstract 2
- 239000013078 crystal Substances 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 238000012986 modification Methods 0.000 abstract 2
- 230000004048 modification Effects 0.000 abstract 2
- 230000004963 pathophysiological condition Effects 0.000 abstract 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 abstract 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 abstract 1
- 230000033228 biological regulation Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000004962 physiological condition Effects 0.000 abstract 1
- 230000000644 propagated effect Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 230000019491 signal transduction Effects 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
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- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P5/00—Drugs for disorders of the endocrine system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Ophthalmology & Optometry (AREA)
- Reproductive Health (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
formas polimórficas de sal de cloridrato de 3-(1-{3-[5-(1 metil- piperidin-4-ilmetóxi)-priridin-2-il]-benzil}-6-oxo-1,6-di-hidro-piridazin-3-il)-benzonitrila e processos de fabricação do mesmo. a presente invenção refere-se a solvatos de cloridrato de 3-(1-{3-[5-(1-metil-pepiridin-4-ilmetóxi)-primidin-2-il]-benzil}-6-oxo-1,6-di-hidro-piridazin-3-il)-benzonitrila e modificações cristalinas dos mesmos. a presente invenção também refere-se a processos de fabricações destas modificações cristalinas, bem como seu uso no tratamento e/ou profilaxia de condições fisiológicas e/ou patofisiológicas, que são causadas, mediadas e/ou propagadas pela inibição, regulação e/ou modulação de transdução de sinal de quinases, em particular pela inibição de tirosina quinases, por exemplo, condições patofisiológicas tais como câncer.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09000140 | 2009-01-08 | ||
| EP09000140.5 | 2009-01-08 | ||
| PCT/EP2009/008684 WO2010078897A1 (en) | 2009-01-08 | 2009-12-04 | Novel polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0922642A2 BRPI0922642A2 (pt) | 2016-01-05 |
| BRPI0922642B1 BRPI0922642B1 (pt) | 2020-09-29 |
| BRPI0922642B8 true BRPI0922642B8 (pt) | 2021-05-25 |
Family
ID=41572530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0922642A BRPI0922642B8 (pt) | 2009-01-08 | 2009-12-04 | formas polimórficas de sal de cloridrato de 3-(1-{3-[5-(1-metil-piperidin-4-ilmetóxi)-pirimidin-2-il]-benzil}-6-oxo-1,6-di-hidro-piridazin-3-il)-benzonitrila,seus processos de fabricação, composição farmacêutica, medicamento, e kit |
Country Status (31)
| Country | Link |
|---|---|
| US (3) | US8710058B2 (pt) |
| EP (1) | EP2373640B1 (pt) |
| JP (2) | JP5719781B2 (pt) |
| KR (2) | KR101829595B1 (pt) |
| CN (1) | CN102272121B (pt) |
| AR (1) | AR074996A1 (pt) |
| AU (1) | AU2009336839B2 (pt) |
| BR (1) | BRPI0922642B8 (pt) |
| CA (4) | CA3097370A1 (pt) |
| CL (1) | CL2011001356A1 (pt) |
| CO (1) | CO6400191A2 (pt) |
| CY (1) | CY1115631T1 (pt) |
| DK (1) | DK2373640T3 (pt) |
| EA (1) | EA019342B1 (pt) |
| EC (1) | ECSP11011248A (pt) |
| ES (1) | ES2522629T3 (pt) |
| HR (1) | HRP20140908T1 (pt) |
| IL (1) | IL213829A0 (pt) |
| MX (3) | MX363852B (pt) |
| MY (1) | MY160017A (pt) |
| NZ (1) | NZ594404A (pt) |
| PE (2) | PE20120474A1 (pt) |
| PL (1) | PL2373640T3 (pt) |
| PT (1) | PT2373640E (pt) |
| SG (2) | SG10201504735QA (pt) |
| SI (1) | SI2373640T1 (pt) |
| SM (1) | SMT201400161B (pt) |
| TW (1) | TWI475997B (pt) |
| UA (1) | UA106220C2 (pt) |
| WO (1) | WO2010078897A1 (pt) |
| ZA (1) | ZA201105782B (pt) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2373640B1 (en) * | 2009-01-08 | 2014-07-30 | Merck Patent GmbH | Novel polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof |
| AU2013234767B2 (en) * | 2012-03-19 | 2017-02-23 | Merck Patent Gmbh | Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with other anti-tumor compounds |
| HRP20171295T1 (hr) * | 2012-11-02 | 2017-10-20 | Merck Patent Gmbh | Derivat 6-okso-1,6-dihidro-piridazina za upotrebu za liječenje hepatocelularnog karcinoma (hcc) |
| AU2014377079A1 (en) * | 2014-01-07 | 2016-08-18 | Merck Patent Gmbh | A 6-oxo-1,6-dihydro-pyridazine derivative for the use for the treatment of renal cell carcinoma (RCC) |
| CN106999493A (zh) | 2014-12-12 | 2017-08-01 | 默克专利股份公司 | 具有抗癌活性的6‑氧代‑1,6‑二氢‑哒嗪衍生物与egfr抑制剂的组合 |
| WO2016155655A1 (zh) | 2015-04-03 | 2016-10-06 | 上海瑛派药业有限公司 | Parp抑制剂固体药物剂型及其应用 |
| WO2016192831A1 (en) | 2015-05-29 | 2016-12-08 | Merck Patent Gmbh | Compositions of anions and cations with pharmacological activity |
| KR20180092096A (ko) | 2017-02-08 | 2018-08-17 | 에이비온 주식회사 | 트리아졸로 피라진 유도체의 신규한 다형체 및 이의 제조 방법 |
| EA039713B1 (ru) * | 2018-04-26 | 2022-03-03 | Фуцзянь Косантер Фармасьютикал Ко., Лтд. | Кристаллическая форма ингибитора c-met, его солевая форма и способ их получения |
| SI3996688T1 (sl) * | 2019-07-10 | 2024-01-31 | Merck Patent Gmbh | Farmacevtski preparat |
| CA3167676A1 (en) | 2020-01-21 | 2021-07-29 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Irak4 inhibitor crystal and preparation method therefor |
| WO2022063869A2 (en) | 2020-09-24 | 2022-03-31 | Merck Patent Gmbh | Compounds for the treatment of viral infections |
| KR102489160B1 (ko) | 2021-05-26 | 2023-01-18 | 주식회사 이노큐어테라퓨틱스 | 피페리딘디온 유도체 |
| WO2022250350A1 (ko) | 2021-05-26 | 2022-12-01 | 주식회사 이노큐어테라퓨틱스 | 피페리딘디온 유도체 |
| EP4346829A1 (en) | 2021-06-04 | 2024-04-10 | Merck Patent GmbH | Compounds for the treatment of glioblastoma |
| CN114394957B (zh) * | 2021-12-24 | 2023-05-09 | 武汉九州钰民医药科技有限公司 | Met抑制剂盐酸特泊替尼的制备方法 |
| KR20230155324A (ko) | 2022-05-03 | 2023-11-10 | 주식회사 이노큐어테라퓨틱스 | 피페리딘디온 유도체 |
| CN116768868B (zh) * | 2023-08-15 | 2023-12-08 | 云南省药物研究所 | 一种哒嗪酮硫代衍生物及其制备方法和应用 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7169932B2 (en) * | 2001-06-11 | 2007-01-30 | Pfizer Inc. | HIV protease inhibitors, compositions containing the same, their pharmaceutical uses, material for their synthesis |
| US7094909B2 (en) * | 2001-06-11 | 2006-08-22 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis |
| WO2005016345A1 (en) * | 2003-08-19 | 2005-02-24 | Boehringer Ingelheim International Gmbh | Multivitamin syrup for children or young adults |
| WO2005026114A1 (en) * | 2003-09-17 | 2005-03-24 | Pfizer Inc. | Hiv protease inhibitors, compositions containing the same and their pharmaceutical uses |
| TW200616634A (en) * | 2004-10-01 | 2006-06-01 | Bristol Myers Squibb Co | Crystalline forms and process for preparing spiro-hydantoin compounds |
| EP1805187A1 (en) * | 2004-10-21 | 2007-07-11 | Pfizer, Inc. | Inhibitors of hepatitis c virus protease, and compositions and treatments using the same |
| CN101052633A (zh) * | 2004-11-02 | 2007-10-10 | 辉瑞大药厂 | 制备吲唑化合物的方法 |
| KR20070058690A (ko) * | 2004-11-02 | 2007-06-08 | 화이자 인코포레이티드 | 인다졸 화합물의 제조방법 |
| DE102005057924A1 (de) * | 2005-12-05 | 2007-06-06 | Merck Patent Gmbh | Pyridazinonderivate |
| JP5291616B2 (ja) * | 2006-04-26 | 2013-09-18 | ジェネンテック， インコーポレイテッド | ホスホイノシチド３−キナーゼ抑制剤化合物およびその使用方法 |
| US7820812B2 (en) * | 2006-07-25 | 2010-10-26 | Abbott Laboratories | Methods of manufacturing crystalline forms of rapamycin analogs |
| US7812032B2 (en) * | 2006-07-25 | 2010-10-12 | Abbott Laboratories | Crystalline forms of rapamycin analogs |
| DE102007032507A1 (de) * | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
| EP2373640B1 (en) * | 2009-01-08 | 2014-07-30 | Merck Patent GmbH | Novel polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof |
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2009
- 2009-12-04 EP EP09764204.5A patent/EP2373640B1/en active Active
- 2009-12-04 DK DK09764204.5T patent/DK2373640T3/da active
- 2009-12-04 WO PCT/EP2009/008684 patent/WO2010078897A1/en not_active Ceased
- 2009-12-04 CA CA3097370A patent/CA3097370A1/en active Pending
- 2009-12-04 EA EA201101039A patent/EA019342B1/ru not_active IP Right Cessation
- 2009-12-04 KR KR1020177010801A patent/KR101829595B1/ko active Active
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