CN102333773B - 盐皮质激素受体拮抗剂及使用方法 - Google Patents
盐皮质激素受体拮抗剂及使用方法 Download PDFInfo
- Publication number
- CN102333773B CN102333773B CN201080009314.8A CN201080009314A CN102333773B CN 102333773 B CN102333773 B CN 102333773B CN 201080009314 A CN201080009314 A CN 201080009314A CN 102333773 B CN102333773 B CN 102333773B
- Authority
- CN
- China
- Prior art keywords
- compound
- solid
- added
- stirred
- pharmaceutically acceptable
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- BWHDSMWDRPOGPA-VXGBXAGGSA-N C=[Br]c(cc1)cc([N+]([O-])=O)c1N[C@H](C1)CN2[C@H]1COCC2 Chemical compound C=[Br]c(cc1)cc([N+]([O-])=O)c1N[C@H](C1)CN2[C@H]1COCC2 BWHDSMWDRPOGPA-VXGBXAGGSA-N 0.000 description 1
- OCLZOKUGIXLYJZ-HTQZYQBOSA-N CC(C)(C)OC(N(C1)[C@@H](CO)C[C@H]1N)=O Chemical compound CC(C)(C)OC(N(C1)[C@@H](CO)C[C@H]1N)=O OCLZOKUGIXLYJZ-HTQZYQBOSA-N 0.000 description 1
- KTWPMWMLNYHUIJ-DTWKUNHWSA-N C[C@@H](C[C@@H]1[IH](OC)=O)CN1C(OC(C)(C)C)=O Chemical compound C[C@@H](C[C@@H]1[IH](OC)=O)CN1C(OC(C)(C)C)=O KTWPMWMLNYHUIJ-DTWKUNHWSA-N 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N Cc(cc1)ccc1S(O)(=O)=O Chemical compound Cc(cc1)ccc1S(O)(=O)=O JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- CZHIJMGMBQCQDA-ISGJEAITSA-N O=C1N([C@H](C2)CN3[C@H]2COCC3)c(ccc(/C=C2/c(ccc(F)c3)c3OCc3ccccc23)c2)c2N1 Chemical compound O=C1N([C@H](C2)CN3[C@H]2COCC3)c(ccc(/C=C2/c(ccc(F)c3)c3OCc3ccccc23)c2)c2N1 CZHIJMGMBQCQDA-ISGJEAITSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15957809P | 2009-03-12 | 2009-03-12 | |
| US61/159,578 | 2009-03-12 | ||
| PCT/US2010/026138 WO2010104721A1 (en) | 2009-03-12 | 2010-03-04 | Mineralocorticoid receptor antagonist and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102333773A CN102333773A (zh) | 2012-01-25 |
| CN102333773B true CN102333773B (zh) | 2014-04-16 |
Family
ID=42139981
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080009314.8A Expired - Fee Related CN102333773B (zh) | 2009-03-12 | 2010-03-04 | 盐皮质激素受体拮抗剂及使用方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8658638B2 (https=) |
| EP (1) | EP2406252B1 (https=) |
| JP (1) | JP5570536B2 (https=) |
| KR (1) | KR101312179B1 (https=) |
| CN (1) | CN102333773B (https=) |
| AU (1) | AU2010222902B2 (https=) |
| BR (1) | BRPI1009257A2 (https=) |
| CA (1) | CA2751901C (https=) |
| EA (1) | EA019179B1 (https=) |
| ES (1) | ES2542001T3 (https=) |
| MX (1) | MX2011009506A (https=) |
| WO (1) | WO2010104721A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI431010B (zh) | 2007-12-19 | 2014-03-21 | Lilly Co Eli | 礦皮質素受體拮抗劑及使用方法 |
| MX367404B (es) | 2014-06-30 | 2019-08-20 | Astrazeneca Ab | Amidas de benzoxazinona como moduladores del receptor de mineralocorticoides. |
| JP6835836B2 (ja) | 2015-10-13 | 2021-02-24 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 脈絡膜血管新生の処置のための方法及び医薬組成物 |
| EP3490606B8 (en) | 2016-07-26 | 2024-04-10 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Antagonist of mineralocorticoid receptor for the treatment of osteoarthritis |
| JP7697961B2 (ja) | 2020-03-11 | 2025-06-24 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 対象が中心性漿液性脈絡網膜症を有するか、または有する危険性があるかどうかを決定する方法。 |
| US20240366632A1 (en) | 2021-08-31 | 2024-11-07 | Institut National de la Santé et de la Recherche Médicale | Methods for the treatment of ocular rosacea |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004052847A2 (en) * | 2002-06-26 | 2004-06-24 | Eli Lilly And Company | Tricyclic steroid hormone nuclear receptor modulators |
| WO2005066161A1 (en) * | 2003-12-19 | 2005-07-21 | Eli Lilly And Company | Tricyclic steroid hormone nuclear receptor modulators |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI431010B (zh) * | 2007-12-19 | 2014-03-21 | Lilly Co Eli | 礦皮質素受體拮抗劑及使用方法 |
-
2010
- 2010-03-04 AU AU2010222902A patent/AU2010222902B2/en not_active Ceased
- 2010-03-04 EA EA201171125A patent/EA019179B1/ru not_active IP Right Cessation
- 2010-03-04 KR KR1020117021231A patent/KR101312179B1/ko not_active Expired - Fee Related
- 2010-03-04 CA CA2751901A patent/CA2751901C/en not_active Expired - Fee Related
- 2010-03-04 BR BRPI1009257A patent/BRPI1009257A2/pt not_active IP Right Cessation
- 2010-03-04 ES ES10707770.3T patent/ES2542001T3/es active Active
- 2010-03-04 EP EP20100707770 patent/EP2406252B1/en not_active Not-in-force
- 2010-03-04 US US13/203,518 patent/US8658638B2/en not_active Expired - Fee Related
- 2010-03-04 WO PCT/US2010/026138 patent/WO2010104721A1/en not_active Ceased
- 2010-03-04 MX MX2011009506A patent/MX2011009506A/es active IP Right Grant
- 2010-03-04 JP JP2011554083A patent/JP5570536B2/ja not_active Expired - Fee Related
- 2010-03-04 CN CN201080009314.8A patent/CN102333773B/zh not_active Expired - Fee Related
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004052847A2 (en) * | 2002-06-26 | 2004-06-24 | Eli Lilly And Company | Tricyclic steroid hormone nuclear receptor modulators |
| CN1665780A (zh) * | 2002-06-26 | 2005-09-07 | 伊莱利利公司 | 三环甾类激素核受体调节剂 |
| WO2005066161A1 (en) * | 2003-12-19 | 2005-07-21 | Eli Lilly And Company | Tricyclic steroid hormone nuclear receptor modulators |
| CN1918151A (zh) * | 2003-12-19 | 2007-02-21 | 伊莱利利公司 | 三环甾类激素核受体调节剂 |
Non-Patent Citations (2)
| Title |
|---|
| Salt Selection and Optimization Procedures for Pharmaceutical New Chemical Entities;Richard J.Bastin,etc;《Organic Process Research and Development》;20001231(第4期);第427-435页 * |
| Salt selection for basic drugs;Philip L.Gould;《International Journal of Pharmaceutics》;19861231;第33卷;第201-217页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EA019179B1 (ru) | 2014-01-30 |
| EP2406252A1 (en) | 2012-01-18 |
| AU2010222902A1 (en) | 2011-08-11 |
| JP5570536B2 (ja) | 2014-08-13 |
| CN102333773A (zh) | 2012-01-25 |
| ES2542001T3 (es) | 2015-07-29 |
| US20110312954A1 (en) | 2011-12-22 |
| US8658638B2 (en) | 2014-02-25 |
| CA2751901A1 (en) | 2010-09-16 |
| CA2751901C (en) | 2013-08-06 |
| AU2010222902B2 (en) | 2013-04-18 |
| EA201171125A1 (ru) | 2012-02-28 |
| KR101312179B1 (ko) | 2013-09-26 |
| BRPI1009257A2 (pt) | 2016-03-08 |
| JP2012520302A (ja) | 2012-09-06 |
| EP2406252B1 (en) | 2015-05-20 |
| MX2011009506A (es) | 2011-09-28 |
| WO2010104721A1 (en) | 2010-09-16 |
| KR20110124305A (ko) | 2011-11-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20140416 Termination date: 20190304 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |