EA014706B1 - КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 1-БЕНЗОИЛ-4-[2-[4-МЕТОКСИ-7-(3-МЕТИЛ-1H-1,2,4-ТРИАЗОЛ-1-ИЛ)-1-[(ФОСФОНОКСИ)МЕТИЛ]-1H-ПИРРОЛО[2,3-c]ПИРИДИН-3-ИЛ]-1,2-ДИОКСОЭТИЛ]ПИПЕРАЗИНА - Google Patents
КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 1-БЕНЗОИЛ-4-[2-[4-МЕТОКСИ-7-(3-МЕТИЛ-1H-1,2,4-ТРИАЗОЛ-1-ИЛ)-1-[(ФОСФОНОКСИ)МЕТИЛ]-1H-ПИРРОЛО[2,3-c]ПИРИДИН-3-ИЛ]-1,2-ДИОКСОЭТИЛ]ПИПЕРАЗИНА Download PDFInfo
- Publication number
- EA014706B1 EA014706B1 EA200801529A EA200801529A EA014706B1 EA 014706 B1 EA014706 B1 EA 014706B1 EA 200801529 A EA200801529 A EA 200801529A EA 200801529 A EA200801529 A EA 200801529A EA 014706 B1 EA014706 B1 EA 014706B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- crystalline form
- compound
- form according
- methyl
- temperature
- Prior art date
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- 239000003921 oil Substances 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N p-hydroxybenzoic acid propyl ester Natural products CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
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- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 description 1
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- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- WRIKHQLVHPKCJU-UHFFFAOYSA-N sodium bis(trimethylsilyl)amide Chemical compound C[Si](C)(C)N([Na])[Si](C)(C)C WRIKHQLVHPKCJU-UHFFFAOYSA-N 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
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- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical class OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 description 1
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- 238000012360 testing method Methods 0.000 description 1
- OSBSFAARYOCBHB-UHFFFAOYSA-N tetrapropylammonium Chemical compound CCC[N+](CCC)(CCC)CCC OSBSFAARYOCBHB-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
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| US75024705P | 2005-12-14 | 2005-12-14 | |
| PCT/US2006/047571 WO2007070589A2 (en) | 2005-12-14 | 2006-12-13 | Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1h-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine |
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| EA200801529A1 EA200801529A1 (ru) | 2009-02-27 |
| EA014706B1 true EA014706B1 (ru) | 2011-02-28 |
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| EA200801529A EA014706B1 (ru) | 2005-12-14 | 2006-12-13 | КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 1-БЕНЗОИЛ-4-[2-[4-МЕТОКСИ-7-(3-МЕТИЛ-1H-1,2,4-ТРИАЗОЛ-1-ИЛ)-1-[(ФОСФОНОКСИ)МЕТИЛ]-1H-ПИРРОЛО[2,3-c]ПИРИДИН-3-ИЛ]-1,2-ДИОКСОЭТИЛ]ПИПЕРАЗИНА |
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| EP (1) | EP1963342A2 (enExample) |
| JP (1) | JP5400387B2 (enExample) |
| KR (1) | KR20080077010A (enExample) |
| CN (1) | CN101365708B (enExample) |
| AU (1) | AU2006326432B2 (enExample) |
| BR (1) | BRPI0619851A2 (enExample) |
| CA (1) | CA2635717A1 (enExample) |
| EA (1) | EA014706B1 (enExample) |
| GE (1) | GEP20125413B (enExample) |
| IL (1) | IL191769A (enExample) |
| MY (1) | MY144293A (enExample) |
| NO (1) | NO20082477L (enExample) |
| NZ (2) | NZ568776A (enExample) |
| UA (1) | UA94928C2 (enExample) |
| WO (1) | WO2007070589A2 (enExample) |
| ZA (1) | ZA200805063B (enExample) |
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| RU2663466C1 (ru) * | 2017-03-20 | 2018-08-06 | Общество с ограниченной ответственностью "МБА-групп" | Композиция для профилактики и/или лечения вич-инфекции |
| RU2778508C1 (ru) * | 2021-03-31 | 2022-08-22 | Общество с ограниченной ответственностью «29 февраля» | Кристаллическая форма моноэтаноламин 3'-[(2Z)-2-[1-(3,4-диметилфенил)-1,5-дигидро-3-метил-5-оксо-4Н-пиразол-4-илиден]гидразино]-2'-гидрокси-[1,1'-бифенил]-3-карбоновой кислоты |
| US12180185B2 (en) | 2018-11-15 | 2024-12-31 | Hk Inno.N Corporation | Compound as protein kinase inhibitor, and pharmaceutical composition comprising thereof |
| US12365665B2 (en) | 2019-04-30 | 2025-07-22 | Beijing Tide Pharmaceutical Co., Ltd. | Solid form of diaminopyrimidine compound or hydrate thereof, preparation method therefor, and application thereof |
| US12384774B2 (en) | 2019-06-06 | 2025-08-12 | Genfleet Therapeutics (Shanghai) Inc. | Polymorph of CDK9 inhibitor and preparation method for polymorph and use thereof |
| US12419877B2 (en) | 2013-11-15 | 2025-09-23 | Akebia Therapeutics, Inc. | Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof |
| US12479839B2 (en) | 2019-08-06 | 2025-11-25 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Crystalline form of ATR inhibitor and use thereof |
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| US20040110785A1 (en) * | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| US7745625B2 (en) * | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| ES2389478T3 (es) * | 2008-06-25 | 2012-10-26 | Bristol-Myers Squibb Company | Derivados de dicetopiperidina como inhibidores de la fijación del VIH |
| CN102131810B (zh) * | 2008-06-25 | 2014-02-26 | 百时美施贵宝公司 | 作为抗hiv剂的二酮稠合的吡咯并哌啶类和吡咯并哌嗪类 |
| JP5638527B2 (ja) * | 2008-09-04 | 2014-12-10 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｈｉｖ結合阻害剤の最適な送達のための安定な医薬組成物 |
| US8912195B2 (en) | 2010-12-02 | 2014-12-16 | Bristol-Myers Squibb Company | Alkyl amides as HIV attachment inhibitors |
| PT2670751E (pt) * | 2011-01-31 | 2015-07-29 | Bristol Myers Squibb Co | Métodos de fabrico de um composto profármaco inibidor da fixação do vih e intermediários |
| EP2696937B1 (en) | 2011-04-12 | 2017-05-17 | VIIV Healthcare UK (No.5) Limited | Thioamide, amidoxime and amidrazone derivatives as hiv attachment inhibitors |
| EP2751118B1 (en) | 2011-08-29 | 2016-10-12 | Bristol-Myers Squibb Company | Spiro bicyclic diamine derivatives as hiv attachment inhibitors |
| WO2013033061A1 (en) | 2011-08-29 | 2013-03-07 | Bristol-Myers Squibb Company | Fused bicyclic diamine derivatives as hiv attachment inhibitors |
| WO2013138436A1 (en) | 2012-03-14 | 2013-09-19 | Bristol-Myers Squibb Company | Cyclolic hydrazine derivatives as hiv attachment inhibitors |
| EP2895471B1 (en) | 2012-08-09 | 2016-11-23 | VIIV Healthcare UK (No.5) Limited | Piperidine amide derivatives as hiv attachment inhibitors |
| US9655888B2 (en) | 2012-08-09 | 2017-05-23 | VIIV Healthcare UK (No.5) Limited | Tricyclic alkene derivatives as HIV attachment inhibitors |
| WO2019006393A1 (en) | 2017-06-29 | 2019-01-03 | G1 Therapeutics, Inc. | Morphic forms of git38 and methods of manufacture thereof |
| WO2020219524A1 (en) | 2019-04-24 | 2020-10-29 | Elanco Us Inc. | A 7h-pyrrolo[2,3-d]pyrimidine jak-inhibitor |
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| US20050209246A1 (en) * | 2004-03-15 | 2005-09-22 | Yasutsugu Ueda | Prodrugs of piperazine and substituted piperidine antiviral agents |
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| US12419877B2 (en) | 2013-11-15 | 2025-09-23 | Akebia Therapeutics, Inc. | Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof |
| RU2663466C1 (ru) * | 2017-03-20 | 2018-08-06 | Общество с ограниченной ответственностью "МБА-групп" | Композиция для профилактики и/или лечения вич-инфекции |
| US12180185B2 (en) | 2018-11-15 | 2024-12-31 | Hk Inno.N Corporation | Compound as protein kinase inhibitor, and pharmaceutical composition comprising thereof |
| RU2844681C2 (ru) * | 2018-12-06 | 2025-08-05 | Ле Лаборатуар Сервье | Новые кристаллические формы mcl-1 ингибитора, способ их получения и содержащие их фармацевтические композиции |
| RU2843869C2 (ru) * | 2019-04-24 | 2025-07-21 | Эланко Юс Инк. | Ингибиторы jak на основе 7h-пирроло[2,3-d]пиримидина |
| RU2844833C2 (ru) * | 2019-04-30 | 2025-08-07 | Бэйцзин Тайд Фармасьютикл Ко., Лтд. | Твердая форма диаминопиримидина или его гидрата, способ ее получения и ее применение |
| US12365665B2 (en) | 2019-04-30 | 2025-07-22 | Beijing Tide Pharmaceutical Co., Ltd. | Solid form of diaminopyrimidine compound or hydrate thereof, preparation method therefor, and application thereof |
| RU2825215C2 (ru) * | 2019-05-31 | 2024-08-21 | Хёндэ Фарм Ко., Лтд. | Новая кристаллическая форма производного 3-(4-(бензилокси)фенил)гекс-4-иновой кислоты |
| US12384774B2 (en) | 2019-06-06 | 2025-08-12 | Genfleet Therapeutics (Shanghai) Inc. | Polymorph of CDK9 inhibitor and preparation method for polymorph and use thereof |
| RU2832707C2 (ru) * | 2019-08-06 | 2024-12-27 | Уси Байосити Байофармасьютикс Ко., Лтд. | Кристаллическая форма ингибитора atr и ее применение |
| US12479839B2 (en) | 2019-08-06 | 2025-11-25 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Crystalline form of ATR inhibitor and use thereof |
| RU2847971C2 (ru) * | 2019-12-05 | 2025-10-15 | Ле Лаборатуар Сервье | Новые кристаллические формы mcl-1 ингибитора, способ их получения и содержащие их фармацевтические композиции |
| RU2829609C1 (ru) * | 2020-07-02 | 2024-11-01 | Гуанчжоу Хэлсквест Фармасьютикалс Ко., Лтд. | Кристаллы алкинилсодержащего соединения, его соли и сольвата, способ его получения и пути применения |
| RU2778508C1 (ru) * | 2021-03-31 | 2022-08-22 | Общество с ограниченной ответственностью «29 февраля» | Кристаллическая форма моноэтаноламин 3'-[(2Z)-2-[1-(3,4-диметилфенил)-1,5-дигидро-3-метил-5-оксо-4Н-пиразол-4-илиден]гидразино]-2'-гидрокси-[1,1'-бифенил]-3-карбоновой кислоты |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1963342A2 (en) | 2008-09-03 |
| IL191769A0 (en) | 2008-12-29 |
| WO2007070589A2 (en) | 2007-06-21 |
| MY144293A (en) | 2011-08-29 |
| GEP20125413B (en) | 2012-03-12 |
| JP2009521414A (ja) | 2009-06-04 |
| CA2635717A1 (en) | 2007-06-21 |
| US20070155702A1 (en) | 2007-07-05 |
| US7851476B2 (en) | 2010-12-14 |
| JP5400387B2 (ja) | 2014-01-29 |
| KR20080077010A (ko) | 2008-08-20 |
| CN101365708B (zh) | 2012-12-12 |
| AU2006326432A1 (en) | 2007-06-21 |
| BRPI0619851A2 (pt) | 2011-10-25 |
| CN101365708A (zh) | 2009-02-11 |
| NO20082477L (no) | 2008-09-05 |
| EA200801529A1 (ru) | 2009-02-27 |
| ZA200805063B (en) | 2009-10-28 |
| NZ568776A (en) | 2011-06-30 |
| WO2007070589A3 (en) | 2007-09-27 |
| IL191769A (en) | 2011-08-31 |
| NZ592684A (en) | 2012-07-27 |
| AU2006326432B2 (en) | 2012-07-12 |
| UA94928C2 (en) | 2011-06-25 |
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