BR112015014839A2 - forma cristalina do composto utilizado como antagonista do receptor de mineralocorticóide e método para a sua preparação - Google Patents
forma cristalina do composto utilizado como antagonista do receptor de mineralocorticóide e método para a sua preparaçãoInfo
- Publication number
- BR112015014839A2 BR112015014839A2 BR112015014839A BR112015014839A BR112015014839A2 BR 112015014839 A2 BR112015014839 A2 BR 112015014839A2 BR 112015014839 A BR112015014839 A BR 112015014839A BR 112015014839 A BR112015014839 A BR 112015014839A BR 112015014839 A2 BR112015014839 A2 BR 112015014839A2
- Authority
- BR
- Brazil
- Prior art keywords
- preparation
- crystalline form
- receptor antagonist
- compound used
- mineralocorticoid receptor
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title abstract 9
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 238000000034 method Methods 0.000 title abstract 6
- 229940083712 aldosterone antagonist Drugs 0.000 title abstract 4
- 239000013078 crystal Substances 0.000 abstract 4
- 239000003814 drug Substances 0.000 abstract 4
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 abstract 3
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 abstract 2
- 206010061481 Renal injury Diseases 0.000 abstract 2
- 229940079593 drug Drugs 0.000 abstract 2
- 230000002265 prevention Effects 0.000 abstract 2
- UXHQLGLGLZKHTC-CUNXSJBXSA-N 4-[(3s,3ar)-3-cyclopentyl-7-(4-hydroxypiperidine-1-carbonyl)-3,3a,4,5-tetrahydropyrazolo[3,4-f]quinolin-2-yl]-2-chlorobenzonitrile Chemical compound C1CC(O)CCN1C(=O)C1=CC=C(C=2[C@@H]([C@H](C3CCCC3)N(N=2)C=2C=C(Cl)C(C#N)=CC=2)CC2)C2=N1 UXHQLGLGLZKHTC-CUNXSJBXSA-N 0.000 abstract 1
- -1 4-hydroxypiperidine-1-carbonyl Chemical group 0.000 abstract 1
- 208000037806 kidney injury Diseases 0.000 abstract 1
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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/40—Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/50—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
- C07D215/60—N-oxides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
abstract the present invention belongs to the technical field of medicines, and relates to a crystal form of a compound used as a mineralocorticoid receptor antagonist and a preparation method therefor, and in particular, to a method for preparing a compound 2-chloro-4-[(3s,3ar)-3-cyclopentyl-7-(4-hydroxypiperidin-1-carbonyl)-3,3a,4,5-tetrahydro-2h-pyrazolo[3,4-f]quinolin-2-yl]benzonitrile of formula (1); a crystal form thereof, a preparation method for the crystal form, and the use of the crystal form in the preparation of drugs for the treatment and/or prevention of renal injury or cardiovascular diseases. formula (1) ______________________________________________________________ resumo patente de invenção: "forma cristalina do composto utilizado como antagonista do receptor de mineralocorticóide e método para a sua preparação". a presente invenção pertence ao campo técnico de medicamentos, e refere-se a uma forma cristalina de um composto utilizado como um antagonista do receptor de mineralocorticóide e um método para a sua preparação, e em particular, a um método para a preparação de um composto 2-cloro-4-[(3s,3ar)-3-ciclopentil-7-(4-hidroxipiperidina-1-carbonil)-3,3a,4,5-tetraidro-2h-pirazol[3,4-f]quinolina-2-il]benzonitrila de fórmula (i), a uma forma cristalina deste, a um método de preparação para a forma cristalina, e ao uso da forma cristalina na preparação de medicamentos para o tratamento e/ou prevenção da lesão renal ou de doenças cardiovasculares.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210563636.8 | 2012-12-22 | ||
| CN201210563636 | 2012-12-22 | ||
| PCT/CN2013/090252 WO2014094664A1 (zh) | 2012-12-22 | 2013-12-23 | 作为盐皮质激素受体拮抗剂的化合物的晶型及其制备方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112015014839A2 true BR112015014839A2 (pt) | 2017-07-11 |
| BR112015014839B1 BR112015014839B1 (pt) | 2022-09-06 |
Family
ID=50977609
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112015014839-5A BR112015014839B1 (pt) | 2012-12-22 | 2013-12-23 | Forma cristalina do composto utilizado como antagonista do receptor de mineralocorticoide, seus usos, seu processo de preparação e composição farmacêutica |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9809589B2 (pt) |
| EP (2) | EP2937348B1 (pt) |
| JP (6) | JP2016503041A (pt) |
| KR (1) | KR101737883B1 (pt) |
| CN (1) | CN105026391B (pt) |
| AU (1) | AU2013362400B2 (pt) |
| BR (1) | BR112015014839B1 (pt) |
| CA (1) | CA2895968C (pt) |
| ES (1) | ES2897496T3 (pt) |
| HK (2) | HK1212676A1 (pt) |
| IL (1) | IL239581B (pt) |
| MX (1) | MX360889B (pt) |
| NZ (1) | NZ709361A (pt) |
| RU (1) | RU2622105C2 (pt) |
| SG (1) | SG11201504928XA (pt) |
| WO (1) | WO2014094664A1 (pt) |
| ZA (1) | ZA201504485B (pt) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX360889B (es) * | 2012-12-22 | 2018-11-20 | Kbp Biosciences Co Ltd | Forma cristalina de un compuesto usado como un antagonista del receptor mineralocorticoide y metodo de preparacion de la misma. |
| CU24569B1 (es) * | 2016-09-24 | 2022-01-13 | Kbp Biosciences Co Ltd | Composición farmacéutica como antagonista del receptor de mineralocorticoides |
| JP7291426B2 (ja) * | 2019-03-01 | 2023-06-15 | 山東亨利醫藥科技有限責任公司 | 縮合三環式化合物を調製するための方法、及びその中間体 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5245716B1 (pt) * | 1970-07-10 | 1977-11-17 | ||
| CN85101404A (zh) * | 1985-05-16 | 1987-01-17 | 帝人株式会社 | 头孢菌素衍生物的生产过程 |
| JPH04235188A (ja) * | 1990-06-19 | 1992-08-24 | Takeda Chem Ind Ltd | ペネム化合物の結晶、その製造方法および抗菌剤 |
| DE4235133A1 (de) * | 1992-10-19 | 1994-04-21 | Bayer Ag | Kristallines (R)-(-)-2-Cycloheptyl-N-methylsulfonyl-[4-(2-chinolinyl-methoxy)-phenyl]-acetamid |
| JP3623531B2 (ja) * | 1993-06-07 | 2005-02-23 | ビーエーエスエフ アクチェンゲゼルシャフト | 結晶質ｌ−アスコルビン酸−２−燐酸エステルマグネシウム塩の製造法 |
| EP0847647B1 (en) * | 1996-06-28 | 2003-03-12 | Koninklijke Philips Electronics N.V. | Method and arrangement for transmitting teletext pages |
| WO1998009969A1 (en) | 1996-09-05 | 1998-03-12 | Astra Pharmaceuticals Ltd. | Novel aryl-pyridazines |
| NZ540081A (en) * | 2002-11-22 | 2008-03-28 | Active Biotech Ab | Pyrazoloquinolines with immunomodulating activity |
| JPWO2006101082A1 (ja) * | 2005-03-21 | 2008-09-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピリミジン化合物の結晶、非晶質および製造方法 |
| DE102007054497B3 (de) * | 2007-11-13 | 2009-07-23 | Sanofi-Aventis Deutschland Gmbh | Neue kristalline Diphenylazetidinonhydrate und Verfahren zu deren Herstellung |
| CN102372710A (zh) * | 2010-08-18 | 2012-03-14 | 山东轩竹医药科技有限公司 | 作为盐皮质激素受体拮抗剂的并环类化合物 |
| SI2623498T1 (sl) * | 2010-09-30 | 2016-03-31 | Toyama Chemical Co., Ltd. | Natrijeva sol 6-fluoro-3-hidroksi-2-pirazinkarboksamida |
| MX360889B (es) * | 2012-12-22 | 2018-11-20 | Kbp Biosciences Co Ltd | Forma cristalina de un compuesto usado como un antagonista del receptor mineralocorticoide y metodo de preparacion de la misma. |
-
2013
- 2013-12-23 MX MX2015008193A patent/MX360889B/es active IP Right Grant
- 2013-12-23 KR KR1020157019924A patent/KR101737883B1/ko active IP Right Grant
- 2013-12-23 US US14/653,933 patent/US9809589B2/en active Active
- 2013-12-23 RU RU2015130222A patent/RU2622105C2/ru active
- 2013-12-23 SG SG11201504928XA patent/SG11201504928XA/en unknown
- 2013-12-23 AU AU2013362400A patent/AU2013362400B2/en active Active
- 2013-12-23 ES ES13864994T patent/ES2897496T3/es active Active
- 2013-12-23 BR BR112015014839-5A patent/BR112015014839B1/pt active IP Right Grant
- 2013-12-23 JP JP2015548180A patent/JP2016503041A/ja active Pending
- 2013-12-23 WO PCT/CN2013/090252 patent/WO2014094664A1/zh active Application Filing
- 2013-12-23 CN CN201380066871.7A patent/CN105026391B/zh active Active
- 2013-12-23 NZ NZ709361A patent/NZ709361A/en unknown
- 2013-12-23 CA CA2895968A patent/CA2895968C/en active Active
- 2013-12-23 EP EP13864994.2A patent/EP2937348B1/en active Active
- 2013-12-23 EP EP21194531.6A patent/EP3954688A1/en active Pending
-
2015
- 2015-06-22 ZA ZA2015/04485A patent/ZA201504485B/en unknown
- 2015-06-22 IL IL239581A patent/IL239581B/en active IP Right Grant
-
2016
- 2016-01-15 HK HK16100440.8A patent/HK1212676A1/zh unknown
- 2016-05-03 HK HK16105012.5A patent/HK1217019A1/zh unknown
-
2017
- 2017-07-04 JP JP2017131078A patent/JP2017165787A/ja active Pending
-
2019
- 2019-02-05 JP JP2019018876A patent/JP2019065057A/ja active Pending
-
2020
- 2020-04-16 JP JP2020073415A patent/JP6986197B6/ja active Active
-
2021
- 2021-11-02 JP JP2021179425A patent/JP2022009922A/ja active Pending
-
2023
- 2023-11-17 JP JP2023195879A patent/JP2024009114A/ja active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B06I | Publication of requirement cancelled [chapter 6.9 patent gazette] |
Free format text: ANULADA A PUBLICACAO CODIGO 6.6.1 NA RPI NO 2462 DE 13/03/2018 POR TER SIDO INDEVIDA. |
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| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
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| B06T | Formal requirements before examination [chapter 6.20 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 23/12/2013, OBSERVADAS AS CONDICOES LEGAIS |
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| B25G | Requested change of headquarter approved |
Owner name: KBP BIOSCIENCES CO., LTD. (CN) |
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| B25A | Requested transfer of rights approved |
Owner name: KBP BIOSCIENCES PTE. LTD. (SG) |