CN103119047B - 三环类蛋白酶体活性增强化合物 - Google Patents
三环类蛋白酶体活性增强化合物 Download PDFInfo
- Publication number
- CN103119047B CN103119047B CN201180045618.4A CN201180045618A CN103119047B CN 103119047 B CN103119047 B CN 103119047B CN 201180045618 A CN201180045618 A CN 201180045618A CN 103119047 B CN103119047 B CN 103119047B
- Authority
- CN
- China
- Prior art keywords
- amyloidosis
- disease
- proteasome
- alkyl
- usp14
- 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
- 0 CC1(C)*C(C(C2)=C(C)N=NN=C2C=C)=CC=C(*)***1 Chemical compound CC1(C)*C(C(C2)=C(C)N=NN=C2C=C)=CC=C(*)***1 0.000 description 1
- PGGINYVNLNKQRD-UHFFFAOYSA-N CN(C1CC1)c1ncnc2c1c(CCCC1)c1[s]2 Chemical compound CN(C1CC1)c1ncnc2c1c(CCCC1)c1[s]2 PGGINYVNLNKQRD-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/12—Ophthalmic agents for cataracts
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- A61P7/06—Antianaemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Ophthalmology & Optometry (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Psychology (AREA)
- Dermatology (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36717310P | 2010-07-23 | 2010-07-23 | |
| US61/367,173 | 2010-07-23 | ||
| PCT/US2011/044999 WO2012012712A2 (en) | 2010-07-23 | 2011-07-22 | Tricyclic proteasome activity enhancing compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103119047A CN103119047A (zh) | 2013-05-22 |
| CN103119047B true CN103119047B (zh) | 2016-06-15 |
Family
ID=45497483
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180045618.4A Expired - Fee Related CN103119047B (zh) | 2010-07-23 | 2011-07-22 | 三环类蛋白酶体活性增强化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US8933087B2 (enExample) |
| EP (1) | EP2595993B1 (enExample) |
| JP (1) | JP6042331B2 (enExample) |
| CN (1) | CN103119047B (enExample) |
| AU (1) | AU2011281015B2 (enExample) |
| CA (1) | CA2808432C (enExample) |
| WO (1) | WO2012012712A2 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102844313B (zh) * | 2010-01-28 | 2016-10-05 | 哈佛大学校长及研究员协会 | 提高蛋白酶体活性的组合物和方法 |
| WO2012012712A2 (en) | 2010-07-23 | 2012-01-26 | President And Fellows Of Harvard College | Tricyclic proteasome activity enhancing compounds |
| EP2663312B1 (en) | 2011-01-10 | 2017-10-11 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| US9556166B2 (en) | 2011-05-12 | 2017-01-31 | Proteostasis Therapeutics, Inc. | Proteostasis regulators |
| CN104582705A (zh) | 2012-01-10 | 2015-04-29 | 林伯士艾瑞斯公司 | 白介素-1受体相关激酶(irak)抑制剂和其用途 |
| WO2013112651A2 (en) | 2012-01-25 | 2013-08-01 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating compounds |
| CN104902959A (zh) | 2012-07-11 | 2015-09-09 | 林伯士艾瑞斯公司 | Irak抑制剂和其用途 |
| EP2872144A4 (en) * | 2012-07-11 | 2015-12-02 | Nimbus Iris Inc | IRAQ INHIBITOR AND USES THEREOF |
| JP2016504365A (ja) | 2012-12-28 | 2016-02-12 | アメリカ合衆国 | Usp1/uaf1デユビキチナーゼ複合体阻害剤及びその使用 |
| AU2014205577A1 (en) | 2013-01-10 | 2015-05-28 | Nimbus Iris, Inc. | IRAK inhibitors and uses thereof |
| WO2014116228A1 (en) | 2013-01-25 | 2014-07-31 | President And Fellows Of Harvard College | Usp14 inhibitors for treating or preventing viral infections |
| WO2014145576A2 (en) | 2013-03-15 | 2014-09-18 | Northwestern University | Substituted pyrrolo(2,3-d)pyrimidines for the treatment of cancer |
| EP3049086A4 (en) | 2013-09-27 | 2017-02-22 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003037898A1 (en) * | 2001-10-31 | 2003-05-08 | Bayer Healthcare Ag | Pyrimido [4,5-b] indole derivatives |
| CN1522258A (zh) * | 2001-04-30 | 2004-08-18 | 新的4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶化合物 | |
| WO2007061764A2 (en) * | 2005-11-22 | 2007-05-31 | Merck & Co., Inc. | Tricyclic compounds useful as inhibitors of kinases |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3577420A (en) * | 1968-01-05 | 1971-05-04 | Pfizer | Certain 4-aminofuro(2,3-d)pyrimidines |
| GB1570494A (en) * | 1975-11-28 | 1980-07-02 | Ici Ltd | Thienopyrimidine derivatives and their use as pesticides |
| DD245666A1 (de) | 1985-09-20 | 1987-05-13 | Univ Halle Wittenberg | Verfahren zur herstellung von 4-aminosubstituierten thieno 2,3-d-pyrimidin-2-ylessigsaeureestern |
| JPH01313480A (ja) | 1988-06-14 | 1989-12-18 | Nippon Soda Co Ltd | ピリミジン誘導体、その製造方法及び農園芸用殺菌剤 |
| AU7890598A (en) * | 1996-12-27 | 1998-07-31 | Yoshitomi Pharmaceutical Industries, Ltd. | Fused pyrimidine compounds and medicinal use thereof |
| KR20010105399A (ko) | 1999-03-30 | 2001-11-28 | 쓰끼하시 다미까따 | 티에노피리미딘 화합물 및 그의 염, 및 그들의 제조 방법 |
| EP1175421A1 (en) | 1999-04-30 | 2002-01-30 | Neurogen Corporation | 9H-PYRIMIDO[4,5-b]INDOLE DERIVATIVES: CRF1 SPECIFIC LIGANDS |
| JP2002105082A (ja) | 2000-09-29 | 2002-04-10 | Nippon Soda Co Ltd | 縮合チエノピリミジン化合物、その塩及び製造法 |
| DE10064994A1 (de) | 2000-12-23 | 2002-07-04 | Merck Patent Gmbh | Sulfamidothienopyrimidine |
| JP2004517940A (ja) | 2001-01-31 | 2004-06-17 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフトング | ピラゾロ[4,3−d]ピリミジンおよびニトレートまたはチエノピリミジンおよびニトレートを含む医薬製剤 |
| DE10148883A1 (de) | 2001-10-04 | 2003-04-10 | Merck Patent Gmbh | Pyrimidinderivate |
| JP2003137886A (ja) * | 2001-10-31 | 2003-05-14 | Bayer Ag | ピリミド[4,5−b]インドール |
| US7199119B2 (en) | 2002-10-31 | 2007-04-03 | Amgen Inc. | Antiinflammation agents |
| ES2217956B1 (es) | 2003-01-23 | 2006-04-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de 4-aminotieno(2,3-d)pirimidin-6-carbonitrilo. |
| JP4677518B2 (ja) * | 2003-03-31 | 2011-04-27 | エピックス デラウェア, インコーポレイテッド | 新規ピペリジニルアミノ−チエノ[2,3−d]ピリミジン化合物 |
| US7612078B2 (en) * | 2003-03-31 | 2009-11-03 | Epix Delaware, Inc. | Piperidinylamino-thieno[2,3-D] pyrimidine compounds |
| US7960400B2 (en) | 2007-08-27 | 2011-06-14 | Duquesne University Of The Holy Ghost | Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof |
| US7982035B2 (en) | 2007-08-27 | 2011-07-19 | Duquesne University Of The Holy Spirit | Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof |
| WO2009033581A1 (en) | 2007-09-14 | 2009-03-19 | Bayer Schering Pharma Aktiengesellschaft | Substituted tricyclic compounds and methods of use thereof |
| US20100227853A1 (en) | 2008-04-18 | 2010-09-09 | Trustees Of Boston College | Inhibitors of cyclic amp phosphodiesterases |
| US8507502B2 (en) | 2008-11-10 | 2013-08-13 | National Health Research Institutes | Fused bicyclic and tricyclic pyrimidine compounds as tyrosine kinase inhibitors |
| KR20110136819A (ko) | 2009-02-27 | 2011-12-21 | 시가 테크놀로지스, 인크. | 뎅기 바이러스 감염의 치료 및 예방을 위한 티에노피리딘 유도체 |
| CN102844313B (zh) | 2010-01-28 | 2016-10-05 | 哈佛大学校长及研究员协会 | 提高蛋白酶体活性的组合物和方法 |
| WO2012012712A2 (en) | 2010-07-23 | 2012-01-26 | President And Fellows Of Harvard College | Tricyclic proteasome activity enhancing compounds |
| TW201219401A (en) | 2010-09-14 | 2012-05-16 | Lexicon Pharmaceuticals Inc | Bicyclic inhibitors of Notum Pectinacetylesterase and methods of their use |
| CN103261205B (zh) | 2010-11-12 | 2015-08-19 | 姚雪彪 | 动点马达蛋白cenp-e小分子抑制剂syntelin及其应用 |
| EP2663312B1 (en) | 2011-01-10 | 2017-10-11 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CN104582705A (zh) | 2012-01-10 | 2015-04-29 | 林伯士艾瑞斯公司 | 白介素-1受体相关激酶(irak)抑制剂和其用途 |
-
2011
- 2011-07-22 WO PCT/US2011/044999 patent/WO2012012712A2/en not_active Ceased
- 2011-07-22 CN CN201180045618.4A patent/CN103119047B/zh not_active Expired - Fee Related
- 2011-07-22 AU AU2011281015A patent/AU2011281015B2/en not_active Ceased
- 2011-07-22 EP EP11810459.5A patent/EP2595993B1/en not_active Not-in-force
- 2011-07-22 CA CA2808432A patent/CA2808432C/en not_active Expired - Fee Related
- 2011-07-22 US US13/811,129 patent/US8933087B2/en active Active
- 2011-07-22 JP JP2013520880A patent/JP6042331B2/ja not_active Expired - Fee Related
-
2014
- 2014-12-17 US US14/572,927 patent/US9981981B2/en active Active
-
2018
- 2018-05-21 US US15/984,937 patent/US20180265519A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1522258A (zh) * | 2001-04-30 | 2004-08-18 | 新的4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶化合物 | |
| WO2003037898A1 (en) * | 2001-10-31 | 2003-05-08 | Bayer Healthcare Ag | Pyrimido [4,5-b] indole derivatives |
| WO2007061764A2 (en) * | 2005-11-22 | 2007-05-31 | Merck & Co., Inc. | Tricyclic compounds useful as inhibitors of kinases |
Non-Patent Citations (2)
| Title |
|---|
| Synthesis and study of antiproliferative activity of novel thienopyrimidines on glioblastoma cells;Stéphane Pédeboscq等;《European Journal of Medicinal Chemistry》;20100601;第45卷(第6,1期);第2473-2479页 * |
| Thieno[2,3-d]pyrimidine als Glutamatantagonisten;D.BRIEL等;《DIE PHARMAZIE》;20081101;第63卷(第1期);第823-826页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20160039839A1 (en) | 2016-02-11 |
| CN103119047A (zh) | 2013-05-22 |
| WO2012012712A3 (en) | 2012-05-31 |
| US20130210845A1 (en) | 2013-08-15 |
| AU2011281015A1 (en) | 2013-03-07 |
| JP6042331B2 (ja) | 2016-12-14 |
| EP2595993A2 (en) | 2013-05-29 |
| US8933087B2 (en) | 2015-01-13 |
| CA2808432C (en) | 2019-06-04 |
| AU2011281015B2 (en) | 2015-09-24 |
| CA2808432A1 (en) | 2012-01-26 |
| EP2595993A4 (en) | 2014-01-08 |
| EP2595993B1 (en) | 2018-04-18 |
| WO2012012712A2 (en) | 2012-01-26 |
| US20180265519A1 (en) | 2018-09-20 |
| US9981981B2 (en) | 2018-05-29 |
| JP2013532662A (ja) | 2013-08-19 |
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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 | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20160615 Termination date: 20200722 |