AU2014205642B2 - Pyrido- or pyrrolo-fused pyrimidine derivatives as autotaxin inhibitors for treating pain - Google Patents
Pyrido- or pyrrolo-fused pyrimidine derivatives as autotaxin inhibitors for treating pain Download PDFInfo
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- AU2014205642B2 AU2014205642B2 AU2014205642A AU2014205642A AU2014205642B2 AU 2014205642 B2 AU2014205642 B2 AU 2014205642B2 AU 2014205642 A AU2014205642 A AU 2014205642A AU 2014205642 A AU2014205642 A AU 2014205642A AU 2014205642 B2 AU2014205642 B2 AU 2014205642B2
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- Prior art keywords
- dihydro
- equiv
- mmoles
- ylamino
- inden
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- 208000002193 Pain Diseases 0.000 title claims description 21
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- 108050004000 Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 Proteins 0.000 title description 32
- 239000003112 inhibitor Substances 0.000 title description 10
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title description 3
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- 238000011282 treatment Methods 0.000 claims description 22
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- 201000008482 osteoarthritis Diseases 0.000 claims description 14
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- YZXSXEOZLIJTDE-UHFFFAOYSA-N tert-butyl n-[2-[2-(2,3-dihydro-1h-inden-2-ylamino)-7,8-dihydro-5h-pyrido[4,3-d]pyrimidin-6-yl]-2-oxoethyl]-n-[2-(2h-triazol-4-yl)ethyl]carbamate Chemical compound C1CC2=NC(NC3CC4=CC=CC=C4C3)=NC=C2CN1C(=O)CN(C(=O)OC(C)(C)C)CCC1=CNN=N1 YZXSXEOZLIJTDE-UHFFFAOYSA-N 0.000 description 1
- ZFYXKMPUMSUPJS-UHFFFAOYSA-N tert-butyl n-[3-[2-(2,3-dihydro-1h-inden-2-ylamino)-7,8-dihydro-5h-pyrido[4,3-d]pyrimidin-6-yl]-3-oxopropyl]carbamate Chemical compound C1C2=CC=CC=C2CC1NC1=NC=C(CN(C(=O)CCNC(=O)OC(C)(C)C)CC2)C2=N1 ZFYXKMPUMSUPJS-UHFFFAOYSA-N 0.000 description 1
- KURGIGSAAKEWFW-UHFFFAOYSA-N tert-butyl n-but-3-ynyl-n-[2-[2-(2,3-dihydro-1h-inden-2-ylamino)-5,7-dihydropyrrolo[3,4-d]pyrimidin-6-yl]-2-oxoethyl]carbamate Chemical compound C1C2=CC=CC=C2CC1NC1=NC=C2CN(C(=O)CN(CCC#C)C(=O)OC(C)(C)C)CC2=N1 KURGIGSAAKEWFW-UHFFFAOYSA-N 0.000 description 1
- ZVQXQPNJHRNGID-UHFFFAOYSA-N tetramethylsuccinonitrile Chemical compound N#CC(C)(C)C(C)(C)C#N ZVQXQPNJHRNGID-UHFFFAOYSA-N 0.000 description 1
- 238000010257 thawing Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 229910052723 transition metal Inorganic materials 0.000 description 1
- 150000003624 transition metals Chemical class 0.000 description 1
- 238000005292 vacuum distillation Methods 0.000 description 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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]
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Epidemiology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361751363P | 2013-01-11 | 2013-01-11 | |
| US61/751,363 | 2013-01-11 | ||
| US201361777201P | 2013-03-12 | 2013-03-12 | |
| US61/777,201 | 2013-03-12 | ||
| PCT/US2014/010400 WO2014110000A1 (en) | 2013-01-11 | 2014-01-07 | Pyrido- or pyrrolo-fused pyrimidine derivatives as autotaxin inhibitors for treating pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2014205642A1 AU2014205642A1 (en) | 2015-07-02 |
| AU2014205642B2 true AU2014205642B2 (en) | 2016-02-25 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2014205642A Ceased AU2014205642B2 (en) | 2013-01-11 | 2014-01-07 | Pyrido- or pyrrolo-fused pyrimidine derivatives as autotaxin inhibitors for treating pain |
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| Country | Link |
|---|---|
| US (1) | US8969555B2 (enExample) |
| EP (1) | EP2943494B1 (enExample) |
| JP (1) | JP6285461B2 (enExample) |
| KR (1) | KR101757997B1 (enExample) |
| CN (1) | CN104903327B (enExample) |
| AU (1) | AU2014205642B2 (enExample) |
| BR (1) | BR112015015812A2 (enExample) |
| CA (1) | CA2893253C (enExample) |
| EA (1) | EA025106B1 (enExample) |
| ES (1) | ES2636248T3 (enExample) |
| MX (1) | MX2015008971A (enExample) |
| TW (1) | TWI499591B (enExample) |
| WO (1) | WO2014110000A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201500356A (zh) * | 2013-04-12 | 2015-01-01 | Lilly Co Eli | 二氫吡啶并嘧啶化合物 |
| WO2015077503A1 (en) | 2013-11-22 | 2015-05-28 | Pharmakea, Inc. | Autotaxin inhibitor compounds |
| US9051320B1 (en) | 2014-08-18 | 2015-06-09 | Pharmakea, Inc. | Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor |
| GB201501870D0 (en) | 2015-02-04 | 2015-03-18 | Cancer Rec Tech Ltd | Autotaxin inhibitors |
| GB201502020D0 (en) | 2015-02-06 | 2015-03-25 | Cancer Rec Tech Ltd | Autotaxin inhibitory compounds |
| AU2016268250B2 (en) | 2015-05-27 | 2020-08-27 | Sabre Therapeutics Llc | Autotaxin inhibitors and uses thereof |
| US10118904B2 (en) | 2015-06-05 | 2018-11-06 | Vertex Pharmaceuticals Incorporated | Triazoles for the treatment of Demyelinating Diseases |
| WO2018106641A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Pyrazoles for the treatment of demyelinating diseases |
| WO2018106643A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Heterocyclic azoles for the treatment of demyelinating diseases |
| WO2018106646A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Aminotriazoles for the treatment of demyelinating diseases |
| US10961242B2 (en) | 2017-05-17 | 2021-03-30 | Legochem Biosciences, Inc. | Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same |
| KR101798840B1 (ko) | 2017-05-17 | 2017-11-17 | 주식회사 레고켐 바이오사이언스 | 신규 오토탁신 저해 화합물 및 이를 함유하는 약제학적 조성물 |
| EP3805234B1 (en) * | 2018-05-24 | 2024-09-04 | Guangzhou Henovcom Bioscience Co., Ltd. | Aromatic heterocyclic compound, and pharmaceutical composition and use thereof |
| CA3106641A1 (en) * | 2018-07-16 | 2020-01-23 | The Scripps Research Institute | Opioid haptens, conjugates, vaccines, and methods of generating antibodies |
| CN111518101B (zh) * | 2019-02-01 | 2022-07-29 | 武汉人福创新药物研发中心有限公司 | 吡咯并嘧啶衍生物及其用途 |
| CA3149062A1 (en) * | 2019-09-06 | 2021-03-11 | Xuejun Zhang | Pyrimidine compound and preparation method therefor |
| WO2021055612A1 (en) * | 2019-09-17 | 2021-03-25 | BIAL-BioTech Investments, Inc. | Substituted imidazole carboxamides and their use in the treatment of medical disorders |
| WO2021088957A1 (zh) * | 2019-11-07 | 2021-05-14 | 广州市恒诺康医药科技有限公司 | 芳杂环化合物、其药物组合物及其应用 |
| AU2020402940A1 (en) * | 2019-12-11 | 2022-06-02 | Sichuan Haisco Pharmaceutical Co., Ltd. | Nitrogen-containing heterocyclic autotaxin inhibitor, and composition containing same and use thereof |
| CN113943296B (zh) * | 2020-07-16 | 2025-07-04 | 武汉人福创新药物研发中心有限公司 | 吡咯并嘧啶衍生物及其应用 |
| CN113943295B (zh) * | 2020-07-16 | 2025-08-12 | 武汉人福创新药物研发中心有限公司 | 吡咯并嘧啶类化合物及其用途 |
| CN113999236B (zh) * | 2020-07-28 | 2025-06-10 | 武汉人福创新药物研发中心有限公司 | 含氮杂环化合物的盐及其盐的固体形式、药物组合物和用途 |
| WO2022022569A1 (zh) * | 2020-07-28 | 2022-02-03 | 武汉人福创新药物研发中心有限公司 | 含氮杂环化合物的固体形式及其药物组合物和用途 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012085167A1 (en) * | 2010-12-22 | 2012-06-28 | Merz Pharma Gmbh & Co. Kgaa | Metabotropic glutamate receptor modulators |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1071301A (en) * | 1999-11-01 | 2001-05-14 | Eli Lilly And Company | Pharmaceutical compounds |
| WO2003104230A1 (ja) | 2002-06-07 | 2003-12-18 | 協和醱酵工業株式会社 | 二環性ピリミジン誘導体 |
| DE102004020908A1 (de) * | 2004-04-28 | 2005-11-17 | Grünenthal GmbH | Substituierte 5,6,7,8,-Tetrahydro-pyrido[4,3-d]pyrimidin-2-yl- und 5,6,7,8,-Tetrahydro-chinazolin-2-yl-Verbindungen |
| WO2006119504A2 (en) * | 2005-05-04 | 2006-11-09 | Renovis, Inc. | Fused heterocyclic compounds, and compositions and uses thereof |
| SG171809A1 (en) * | 2008-12-01 | 2011-07-28 | Merck Patent Gmbh | 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer |
| WO2012009258A2 (en) * | 2010-07-13 | 2012-01-19 | Edward Roberts | Peptidomimetic galanin receptor modulators |
| JP2013536200A (ja) | 2010-08-20 | 2013-09-19 | アミラ ファーマシューティカルス，インコーポレーテッド | オートタキシン阻害剤およびその使用 |
| WO2013054185A1 (en) * | 2011-10-13 | 2013-04-18 | Pfizer, Inc. | Pyrimidine and pyridine derivatives useful in therapy |
| EP2771325B1 (en) * | 2011-10-28 | 2017-06-28 | Inhibitaxin Limited | Pyridazine derivatives useful in therapy |
| TW201520219A (zh) * | 2013-03-12 | 2015-06-01 | Lilly Co Eli | 咪唑並吡啶化合物 |
| TW201500356A (zh) * | 2013-04-12 | 2015-01-01 | Lilly Co Eli | 二氫吡啶并嘧啶化合物 |
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2013
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2014
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- 2014-01-07 CN CN201480004482.6A patent/CN104903327B/zh not_active Expired - Fee Related
- 2014-01-07 WO PCT/US2014/010400 patent/WO2014110000A1/en not_active Ceased
- 2014-01-07 JP JP2015552726A patent/JP6285461B2/ja not_active Expired - Fee Related
- 2014-01-07 ES ES14702336.0T patent/ES2636248T3/es active Active
- 2014-01-07 EP EP14702336.0A patent/EP2943494B1/en active Active
- 2014-01-07 CA CA2893253A patent/CA2893253C/en not_active Expired - Fee Related
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- 2014-01-07 KR KR1020157018295A patent/KR101757997B1/ko not_active Expired - Fee Related
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- 2014-01-07 BR BR112015015812A patent/BR112015015812A2/pt not_active IP Right Cessation
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012085167A1 (en) * | 2010-12-22 | 2012-06-28 | Merz Pharma Gmbh & Co. Kgaa | Metabotropic glutamate receptor modulators |
Also Published As
| Publication number | Publication date |
|---|---|
| ES2636248T3 (es) | 2017-10-05 |
| EA201591098A1 (ru) | 2015-11-30 |
| KR20150092761A (ko) | 2015-08-13 |
| KR101757997B1 (ko) | 2017-07-13 |
| JP6285461B2 (ja) | 2018-02-28 |
| WO2014110000A1 (en) | 2014-07-17 |
| EP2943494B1 (en) | 2017-02-22 |
| EA025106B1 (ru) | 2016-11-30 |
| US8969555B2 (en) | 2015-03-03 |
| CN104903327B (zh) | 2016-09-07 |
| CN104903327A (zh) | 2015-09-09 |
| CA2893253C (en) | 2017-11-28 |
| EP2943494A1 (en) | 2015-11-18 |
| TWI499591B (zh) | 2015-09-11 |
| JP2016505010A (ja) | 2016-02-18 |
| MX2015008971A (es) | 2015-09-28 |
| US20140200231A1 (en) | 2014-07-17 |
| CA2893253A1 (en) | 2014-07-17 |
| AU2014205642A1 (en) | 2015-07-02 |
| BR112015015812A2 (pt) | 2017-07-11 |
| TW201437209A (zh) | 2014-10-01 |
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| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |