CN102648177B - 同时基于三取代的1h-吡咯和芳香族及杂芳族间隔基的新型组蛋白脱乙酰基酶抑制剂 - Google Patents
同时基于三取代的1h-吡咯和芳香族及杂芳族间隔基的新型组蛋白脱乙酰基酶抑制剂 Download PDFInfo
- Publication number
- CN102648177B CN102648177B CN201080052814.XA CN201080052814A CN102648177B CN 102648177 B CN102648177 B CN 102648177B CN 201080052814 A CN201080052814 A CN 201080052814A CN 102648177 B CN102648177 B CN 102648177B
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- Prior art keywords
- pyrrole
- carbonyl
- phenyl
- benzyl
- carboxamide
- 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.)
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- 0 C*[C@@](C)C(c1ccc(C*C(C2*(C3CC3)C(c3ccccc3)=CC2c(cc2)cc(N)c2N)=O)cc1)=O Chemical compound C*[C@@](C)C(c1ccc(C*C(C2*(C3CC3)C(c3ccccc3)=CC2c(cc2)cc(N)c2N)=O)cc1)=O 0.000 description 6
- PRGIDXCMQOBJCD-UHFFFAOYSA-N ONC(c1ccc(CNC(c([nH]c(-c2ccccc2)c2)c2-c(cc2)ccc2F)=O)[o]1)=O Chemical compound ONC(c1ccc(CNC(c([nH]c(-c2ccccc2)c2)c2-c(cc2)ccc2F)=O)[o]1)=O PRGIDXCMQOBJCD-UHFFFAOYSA-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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D405/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09382193.2 | 2009-10-02 | ||
| ES09382193.2 | 2009-10-02 | ||
| EP09382193A EP2305643A1 (en) | 2009-10-02 | 2009-10-02 | New histone deacetylase inhibitors based simultaneously on trisubstituted 1h-pyrroles and aromatic and heteroaromatic spacers |
| PCT/EP2010/064653 WO2011039353A1 (en) | 2009-10-02 | 2010-10-01 | New histone deacetylase inhibitors based simultaneously on trisubstituted 1h-pyrroles and aromatic and heteroaromatic spacers |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102648177A CN102648177A (zh) | 2012-08-22 |
| CN102648177B true CN102648177B (zh) | 2015-01-07 |
Family
ID=41716282
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080052814.XA Active CN102648177B (zh) | 2009-10-02 | 2010-10-01 | 同时基于三取代的1h-吡咯和芳香族及杂芳族间隔基的新型组蛋白脱乙酰基酶抑制剂 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8685992B2 (https=) |
| EP (2) | EP2305643A1 (https=) |
| JP (1) | JP5746185B2 (https=) |
| KR (1) | KR101754940B1 (https=) |
| CN (1) | CN102648177B (https=) |
| AU (1) | AU2010302572B2 (https=) |
| BR (1) | BR112012007411B8 (https=) |
| CA (1) | CA2776351C (https=) |
| ES (1) | ES2452868T3 (https=) |
| IL (1) | IL218995A (https=) |
| IN (1) | IN2012DN03129A (https=) |
| MX (1) | MX2012003988A (https=) |
| PL (1) | PL2483242T3 (https=) |
| PT (1) | PT2483242E (https=) |
| RU (1) | RU2549885C2 (https=) |
| WO (1) | WO2011039353A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2627324A4 (en) * | 2010-10-11 | 2014-05-07 | Univ Leland Stanford Junior | SUBSTITUTED BENZAMIDES AND USES THEREOF |
| US9878986B2 (en) | 2013-04-29 | 2018-01-30 | Chong Kun Dang Pharmaceutical Corp. | Compounds for selective histone deacetylase inhibitors, and pharmaceutical composition comprising the same |
| SG11201708622UA (en) | 2015-02-02 | 2017-11-29 | Forma Therapeutics Inc | 3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as hdac inhibitors |
| WO2016126726A1 (en) | 2015-02-02 | 2016-08-11 | Forma Therapeutics, Inc. | Bicyclic [4,6,0] hydroxamic acids as hdac6 inhibitors |
| US20180251425A1 (en) * | 2015-08-17 | 2018-09-06 | University Of Mysore | 2,3,5 trisubstituted pyrrole derivatives as topoisomerase inhibitors and therapeutic uses thereof |
| EP3472131B1 (en) | 2016-06-17 | 2020-02-19 | Forma Therapeutics, Inc. | 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors |
| CN107793375A (zh) * | 2016-08-31 | 2018-03-13 | 中国科学院上海药物研究所 | 一类芳基2,2’‑串联双噻唑类化合物及其制备方法和用途 |
| EP3318256A1 (en) * | 2016-11-08 | 2018-05-09 | Quimatryx, S.L | Compounds for the treatment of autoimmune diseases |
| GB201708457D0 (en) | 2017-05-26 | 2017-07-12 | Univ Oxford Innovation Ltd | Inhibitors of metallo-beta-lactamases |
| CN110938055A (zh) * | 2018-09-21 | 2020-03-31 | 华东师范大学 | 六元环甲酰胺类化合物及其合成方法和应用 |
| KR20220012243A (ko) | 2019-04-17 | 2022-02-03 | 퀴마트리스 에스.엘. | 히스톤 디아세틸라제 억제제로서의 1,3,4-옥사디아졸 유도체 |
| CN112225737B (zh) * | 2020-12-11 | 2021-04-09 | 北京鑫开元医药科技有限公司 | 具有hdac抑制活性的化合物、制备方法、组合物及用途 |
| CN112516142B (zh) * | 2020-12-11 | 2021-10-15 | 北京华氏精恒医药科技有限公司 | 一种具有hdac抑制活性的药物组合物、制备方法及其用途 |
| CN116813560A (zh) * | 2022-03-28 | 2023-09-29 | 上海科技大学 | 三唑酰胺类化合物及其制备方法和用途 |
| CN114558004B (zh) * | 2022-03-29 | 2023-08-11 | 奎马特里克斯有限公司 | Qtx125药物制剂 |
| CN114634489B (zh) * | 2022-04-19 | 2023-07-04 | 奎马特里克斯有限公司 | 结晶形式 |
| CN114652715B (zh) | 2022-04-29 | 2023-04-25 | 奎马特里克斯有限公司 | 联合疗法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006108864A2 (en) * | 2005-04-15 | 2006-10-19 | Dominion Pharmakine S.L. | New nitrogenated trans-stilbene analogs, method for the obtention and medical applications thereof |
| CN101351444A (zh) * | 2005-12-27 | 2009-01-21 | 巴斯克国家大学 | 具有组蛋白脱乙酰基酶抑制活性的新颖的吡咯衍生物 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA76977C2 (en) * | 2001-03-02 | 2006-10-16 | Icos Corp | Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers |
| PT1673349E (pt) | 2003-09-22 | 2010-09-28 | S Bio Pte Ltd | Derivados benzimidazole: preparação e aplicações farmacêuticas |
| MXPA06005915A (es) * | 2003-12-05 | 2006-06-27 | Warner Lambert Co | N-alquil pirroles como inhibidores de la hmg-coa reductasa. |
| US7754717B2 (en) * | 2005-08-15 | 2010-07-13 | Amgen Inc. | Bis-aryl amide compounds and methods of use |
| BRPI0817897A2 (pt) * | 2007-11-02 | 2019-09-24 | Methylgene Inc | composto, composição, e, métodos de inibição da atividade hdac, e de tratamento de uma doença responsiva a um inibidor de atividade hdac |
-
2009
- 2009-10-02 EP EP09382193A patent/EP2305643A1/en not_active Withdrawn
-
2010
- 2010-10-01 BR BR112012007411A patent/BR112012007411B8/pt active IP Right Grant
- 2010-10-01 PL PL10763676T patent/PL2483242T3/pl unknown
- 2010-10-01 PT PT107636763T patent/PT2483242E/pt unknown
- 2010-10-01 RU RU2012117885/04A patent/RU2549885C2/ru not_active IP Right Cessation
- 2010-10-01 ES ES10763676.3T patent/ES2452868T3/es active Active
- 2010-10-01 WO PCT/EP2010/064653 patent/WO2011039353A1/en not_active Ceased
- 2010-10-01 JP JP2012531445A patent/JP5746185B2/ja active Active
- 2010-10-01 EP EP10763676.3A patent/EP2483242B1/en active Active
- 2010-10-01 CA CA2776351A patent/CA2776351C/en active Active
- 2010-10-01 AU AU2010302572A patent/AU2010302572B2/en active Active
- 2010-10-01 IN IN3129DEN2012 patent/IN2012DN03129A/en unknown
- 2010-10-01 CN CN201080052814.XA patent/CN102648177B/zh active Active
- 2010-10-01 MX MX2012003988A patent/MX2012003988A/es active IP Right Grant
- 2010-10-01 US US13/499,839 patent/US8685992B2/en active Active
- 2010-10-01 KR KR1020127011407A patent/KR101754940B1/ko active Active
-
2012
- 2012-04-02 IL IL218995A patent/IL218995A/en not_active IP Right Cessation
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006108864A2 (en) * | 2005-04-15 | 2006-10-19 | Dominion Pharmakine S.L. | New nitrogenated trans-stilbene analogs, method for the obtention and medical applications thereof |
| CN101351444A (zh) * | 2005-12-27 | 2009-01-21 | 巴斯克国家大学 | 具有组蛋白脱乙酰基酶抑制活性的新颖的吡咯衍生物 |
Also Published As
| Publication number | Publication date |
|---|---|
| PT2483242E (pt) | 2014-03-17 |
| HK1173450A1 (en) | 2013-05-16 |
| KR20120091176A (ko) | 2012-08-17 |
| BR112012007411B1 (pt) | 2020-12-15 |
| US8685992B2 (en) | 2014-04-01 |
| CN102648177A (zh) | 2012-08-22 |
| EP2483242B1 (en) | 2013-12-11 |
| WO2011039353A1 (en) | 2011-04-07 |
| RU2549885C2 (ru) | 2015-05-10 |
| JP5746185B2 (ja) | 2015-07-08 |
| BR112012007411B8 (pt) | 2021-05-25 |
| IL218995A0 (en) | 2012-06-28 |
| IN2012DN03129A (https=) | 2015-09-18 |
| JP2013506637A (ja) | 2013-02-28 |
| US20120196885A1 (en) | 2012-08-02 |
| EP2305643A1 (en) | 2011-04-06 |
| IL218995A (en) | 2016-11-30 |
| PL2483242T3 (pl) | 2014-05-30 |
| RU2012117885A (ru) | 2013-11-10 |
| ES2452868T3 (es) | 2014-04-03 |
| KR101754940B1 (ko) | 2017-07-06 |
| CA2776351A1 (en) | 2011-04-07 |
| EP2483242A1 (en) | 2012-08-08 |
| AU2010302572A1 (en) | 2012-05-17 |
| BR112012007411A2 (pt) | 2016-12-06 |
| CA2776351C (en) | 2017-10-31 |
| AU2010302572B2 (en) | 2016-10-20 |
| MX2012003988A (es) | 2012-07-23 |
| AU2010302572A8 (en) | 2012-05-24 |
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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 | ||
| CI01 | Publication of corrected invention patent application |
Correction item: Priority Correct: 09382193.2 20091002 EP False: 09382193.2 20091002 ES Number: 34 Volume: 28 |
|
| CI02 | Correction of invention patent application |
Correction item: Priority Correct: 09382193.2 20091002 EP False: 09382193.2 20091002 ES Number: 34 Page: The title page Volume: 28 |
|
| ERR | Gazette correction |
Free format text: CORRECT: PRIORITY DATA; FROM: 09382193.2 20091002 ES TO: 09382193.2 20091002 EP |
|
| RECT | Rectification | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20220218 Address after: San Sebastian Patentee after: Quematrix Co.,Ltd. Patentee after: University PAIS VASCO Address before: San Sebastian Patentee before: IKERCHEM, S.L. Patentee before: University PAIS VASCO |
|
| TR01 | Transfer of patent right | ||
| EE01 | Entry into force of recordation of patent licensing contract |
Application publication date: 20120822 Assignee: Hongxing Xianghe (Taicang) Biotechnology Co.,Ltd. Assignor: Quematrix Co.,Ltd.|University PAIS VASCO Contract record no.: X2022990000430 Denomination of invention: Novel histone deacetylase inhibitors based on trisubstituted 1H pyrrole and aromatic and heteroaromatic spacers Granted publication date: 20150107 License type: Exclusive License Record date: 20220725 |
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| EE01 | Entry into force of recordation of patent licensing contract |