RU2014101626A - Полиморфы 2-амид 1-({4-метил-5-[2-(2, 2, 2-трифтор-1, 1-диметил-этил)-пиридин-4-ил]тиазол-2-ил}амида) (s)-пирролидин-1, 2-дикарбоновой кислоты - Google Patents
Полиморфы 2-амид 1-({4-метил-5-[2-(2, 2, 2-трифтор-1, 1-диметил-этил)-пиридин-4-ил]тиазол-2-ил}амида) (s)-пирролидин-1, 2-дикарбоновой кислоты Download PDFInfo
- Publication number
- RU2014101626A RU2014101626A RU2014101626/04A RU2014101626A RU2014101626A RU 2014101626 A RU2014101626 A RU 2014101626A RU 2014101626/04 A RU2014101626/04 A RU 2014101626/04A RU 2014101626 A RU2014101626 A RU 2014101626A RU 2014101626 A RU2014101626 A RU 2014101626A
- Authority
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- Russia
- Prior art keywords
- cancer
- powder
- compound
- degrees
- polymorph
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- OAWXZFGKDDFTGS-BYPYZUCNSA-N (2s)-pyrrolidine-1,2-dicarboxylic acid Chemical compound OC(=O)[C@@H]1CCCN1C(O)=O OAWXZFGKDDFTGS-BYPYZUCNSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 30
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 12
- 239000000843 powder Substances 0.000 claims abstract 8
- 150000003839 salts Chemical class 0.000 claims abstract 4
- 239000012453 solvate Substances 0.000 claims abstract 4
- 206010028980 Neoplasm Diseases 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 201000011510 cancer Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 2
- 108091007960 PI3Ks Proteins 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 230000009826 neoplastic cell growth Effects 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010048832 Colon adenoma Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000012609 Cowden disease Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000008770 Multiple Hamartoma Syndrome Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 1
- 208000009621 actinic keratosis Diseases 0.000 claims 1
- 201000005188 adrenal gland cancer Diseases 0.000 claims 1
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 201000008275 breast carcinoma Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 201000002758 colorectal adenoma Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 208000014899 intrahepatic bile duct cancer Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000003747 lymphoid leukemia Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 210000003800 pharynx Anatomy 0.000 claims 1
- 208000037244 polycythemia vera Diseases 0.000 claims 1
- 208000003476 primary myelofibrosis Diseases 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 206010046885 vaginal cancer Diseases 0.000 claims 1
- 208000013139 vaginal neoplasm Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161499222P | 2011-06-21 | 2011-06-21 | |
| US61/499,222 | 2011-06-21 | ||
| PCT/EP2012/061756 WO2012175522A1 (en) | 2011-06-21 | 2012-06-19 | Polymorphs of (s)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2014101626A true RU2014101626A (ru) | 2015-07-27 |
Family
ID=46319784
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2014101626/04A RU2014101626A (ru) | 2011-06-21 | 2012-06-19 | Полиморфы 2-амид 1-({4-метил-5-[2-(2, 2, 2-трифтор-1, 1-диметил-этил)-пиридин-4-ил]тиазол-2-ил}амида) (s)-пирролидин-1, 2-дикарбоновой кислоты |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9006270B2 (enExample) |
| EP (1) | EP2723733A1 (enExample) |
| JP (1) | JP2014517049A (enExample) |
| KR (1) | KR20140033432A (enExample) |
| CN (1) | CN103619840B (enExample) |
| BR (1) | BR112013032687A2 (enExample) |
| CA (1) | CA2839621A1 (enExample) |
| IN (1) | IN2014DN00145A (enExample) |
| MX (1) | MX2013014887A (enExample) |
| RU (1) | RU2014101626A (enExample) |
| WO (1) | WO2012175522A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY192644A (en) | 2009-11-27 | 2022-08-29 | Genzyme Corp | An amorphous and a crystalline form of genz 112638 hemitartrate as inhibitor of glucosylceramide synthase |
| CN104244949A (zh) * | 2012-03-30 | 2014-12-24 | 诺华股份有限公司 | 用于治疗神经母细胞瘤、尤文氏肉瘤或横纹肌肉瘤的化合物 |
| DK3076969T3 (da) * | 2013-12-06 | 2021-11-22 | Novartis Ag | Doseringsregime for en alfa-isoform-selektiv phosphatidylinositol-3-kinase-hæmmer |
| EP3200772B1 (en) * | 2014-10-03 | 2022-08-03 | Novartis AG | Pharmaceutical compositions comprising alpelisib |
| EP3956330A4 (en) | 2019-04-18 | 2023-01-18 | The Johns Hopkins University | SUBSTITUTED 2-AMINO-PYRAZOLYL-[1,2,4]TRIAZOLO[1,5A]PYRIDINE DERIVATIVES AND THEIR USE |
| CN112961090A (zh) * | 2019-12-13 | 2021-06-15 | 武汉九州钰民医药科技有限公司 | 合成Alpelisib的关键中间体及其制备方法 |
| CN110964005A (zh) * | 2019-12-16 | 2020-04-07 | 武汉九州钰民医药科技有限公司 | 一种Alpelisib的制备工艺 |
| CN111057051A (zh) * | 2019-12-16 | 2020-04-24 | 武汉九州钰民医药科技有限公司 | PI3K抑制剂Alpelisib的新合成方法 |
| JP7649637B2 (ja) | 2020-10-06 | 2025-03-21 | エルジー ディスプレイ カンパニー リミテッド | 伝送装置及び表示システム |
| IL301817A (en) | 2020-10-13 | 2023-06-01 | Univ Johns Hopkins | Modified 4-([4,2,1]triazolo[5,1-a]pyridin-6-yl)thiophene-2-carboxamide histories and their use |
| WO2022234408A1 (en) * | 2021-05-03 | 2022-11-10 | Novartis Ag | Alpelisib formulation |
| CN116925023B (zh) * | 2023-07-18 | 2025-11-21 | 江苏桐孚高新材料有限公司 | 2-全氟烷基-4h-吡喃-4-酮衍生物的改进合成方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY29149A1 (es) * | 2004-10-07 | 2006-05-31 | Boehringer Ingelheim Int | Tiazolil-dihidro-indazoles |
| JP2009535386A (ja) * | 2006-05-03 | 2009-10-01 | アストラゼネカ アクチボラグ | チアゾール誘導体および抗腫瘍剤としてのその使用 |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| AR082418A1 (es) * | 2010-08-02 | 2012-12-05 | Novartis Ag | Formas cristalinas de 1-(4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il)-amida de 2-amida del acido (s)-pirrolidin-1,2-dicarboxilico |
-
2012
- 2012-06-19 JP JP2014516316A patent/JP2014517049A/ja active Pending
- 2012-06-19 MX MX2013014887A patent/MX2013014887A/es not_active Application Discontinuation
- 2012-06-19 CN CN201280030432.6A patent/CN103619840B/zh not_active Expired - Fee Related
- 2012-06-19 IN IN145DEN2014 patent/IN2014DN00145A/en unknown
- 2012-06-19 KR KR1020137033590A patent/KR20140033432A/ko not_active Withdrawn
- 2012-06-19 WO PCT/EP2012/061756 patent/WO2012175522A1/en not_active Ceased
- 2012-06-19 EP EP12728285.3A patent/EP2723733A1/en not_active Withdrawn
- 2012-06-19 RU RU2014101626/04A patent/RU2014101626A/ru not_active Application Discontinuation
- 2012-06-19 US US14/127,027 patent/US9006270B2/en not_active Expired - Fee Related
- 2012-06-19 CA CA2839621A patent/CA2839621A1/en not_active Abandoned
- 2012-06-19 BR BR112013032687A patent/BR112013032687A2/pt not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| KR20140033432A (ko) | 2014-03-18 |
| CA2839621A1 (en) | 2012-12-27 |
| US20140171470A1 (en) | 2014-06-19 |
| WO2012175522A1 (en) | 2012-12-27 |
| JP2014517049A (ja) | 2014-07-17 |
| BR112013032687A2 (pt) | 2016-08-30 |
| MX2013014887A (es) | 2014-02-17 |
| CN103619840B (zh) | 2016-01-20 |
| AU2012274141A1 (en) | 2013-12-12 |
| US9006270B2 (en) | 2015-04-14 |
| EP2723733A1 (en) | 2014-04-30 |
| IN2014DN00145A (enExample) | 2015-05-22 |
| CN103619840A (zh) | 2014-03-05 |
| AU2012274141B2 (en) | 2015-12-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20170213 |