AU2010227245B2 - Fused pyrimidine-dione derivatives as TRPA1 modulators - Google Patents
Fused pyrimidine-dione derivatives as TRPA1 modulators Download PDFInfo
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- AU2010227245B2 AU2010227245B2 AU2010227245A AU2010227245A AU2010227245B2 AU 2010227245 B2 AU2010227245 B2 AU 2010227245B2 AU 2010227245 A AU2010227245 A AU 2010227245A AU 2010227245 A AU2010227245 A AU 2010227245A AU 2010227245 B2 AU2010227245 B2 AU 2010227245B2
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- Prior art keywords
- mmol
- acetamide
- thiazol
- dioxo
- tetrahydro
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- 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
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
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- A—HUMAN NECESSITIES
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- 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
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-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Otolaryngology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (21)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN665MU2009 | 2009-03-23 | ||
| IN665/MUM/2009 | 2009-03-23 | ||
| US17135509P | 2009-04-21 | 2009-04-21 | |
| US61/171,355 | 2009-04-21 | ||
| IN2211MU2009 | 2009-09-23 | ||
| IN2212/MUM/2009 | 2009-09-23 | ||
| IN2212MU2009 | 2009-09-23 | ||
| IN2211/MUM/2009 | 2009-09-23 | ||
| US25194409P | 2009-10-15 | 2009-10-15 | |
| US61/251,944 | 2009-10-15 | ||
| US25326309P | 2009-10-20 | 2009-10-20 | |
| US61/253,263 | 2009-10-20 | ||
| IN2892MU2009 | 2009-12-15 | ||
| IN2891MU2009 | 2009-12-15 | ||
| IN2892/MUM/2009 | 2009-12-15 | ||
| IN2891/MUM/2009 | 2009-12-15 | ||
| US29446310P | 2010-01-12 | 2010-01-12 | |
| US61/294,463 | 2010-01-12 | ||
| US30024110P | 2010-02-01 | 2010-02-01 | |
| US61/300,241 | 2010-02-01 | ||
| PCT/IB2010/000553 WO2010109287A1 (en) | 2009-03-23 | 2010-03-17 | Fused pyrimidine-dione derivatives as trpa1 modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| AU2010227245A1 AU2010227245A1 (en) | 2011-09-22 |
| AU2010227245A2 AU2010227245A2 (en) | 2011-10-27 |
| AU2010227245B2 true AU2010227245B2 (en) | 2015-09-10 |
Family
ID=42780198
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2010227245A Ceased AU2010227245B2 (en) | 2009-03-23 | 2010-03-17 | Fused pyrimidine-dione derivatives as TRPA1 modulators |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9000159B2 (enExample) |
| EP (2) | EP2411393B1 (enExample) |
| JP (1) | JP5657638B2 (enExample) |
| KR (1) | KR20110132575A (enExample) |
| CN (1) | CN102361873B (enExample) |
| AP (1) | AP3280A (enExample) |
| AU (1) | AU2010227245B2 (enExample) |
| BR (1) | BRPI1013559A2 (enExample) |
| CA (1) | CA2756518A1 (enExample) |
| CL (2) | CL2011002315A1 (enExample) |
| DK (1) | DK2411393T3 (enExample) |
| EA (1) | EA023857B1 (enExample) |
| ES (2) | ES2456515T3 (enExample) |
| IL (1) | IL215178A (enExample) |
| MX (1) | MX2011009824A (enExample) |
| PE (1) | PE20120774A1 (enExample) |
| PL (1) | PL2411393T3 (enExample) |
| PT (1) | PT2411393E (enExample) |
| SG (1) | SG174402A1 (enExample) |
| SI (1) | SI2411393T1 (enExample) |
| UA (1) | UA108069C2 (enExample) |
| WO (1) | WO2010109287A1 (enExample) |
| ZA (1) | ZA201107648B (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008019357A2 (en) | 2006-08-07 | 2008-02-14 | Ironwood Pharmaceuticals, Inc. | Indole compounds |
| EA023857B1 (ru) | 2009-03-23 | 2016-07-29 | Гленмарк Фармасеутикалс С.А. | Сочлененные производные пиримидиндионов в качестве модуляторов trpa1 |
| JP5694560B2 (ja) | 2010-12-20 | 2015-04-01 | グレンマーク ファーマシューティカルズ, エセ.アー. | Trpa1アンタゴニストとしての2−アミノ−4−アリールチアゾール化合物 |
| AR084433A1 (es) | 2010-12-22 | 2013-05-15 | Ironwood Pharmaceuticals Inc | Inhibidores de la faah y composiciones farmaceuticas que los contienen |
| EP2520566A1 (en) | 2011-05-06 | 2012-11-07 | Orion Corporation | New Pharmaceutical Compounds |
| CN103826637A (zh) | 2011-06-13 | 2014-05-28 | 格兰马克药品股份有限公司 | 使用trpa1拮抗剂治疗呼吸疾患 |
| US20140107113A1 (en) | 2011-06-22 | 2014-04-17 | Glenmark Pharmaceuticals S.A. | Pharmaceutical composition comprising a trpa1 antagonist and a beta-2 agonist |
| WO2012176105A1 (en) | 2011-06-22 | 2012-12-27 | Glenmark Pharmaceuticals Sa | Pharmaceutical composition comprising a trpa1 antagonist and a leukotriene receptor antagonist |
| WO2013014597A1 (en) | 2011-07-25 | 2013-01-31 | Glenmark Pharmaceuticals Sa | Pharmaceutical composition comprising a trpa1 antagonist and a steroid |
| CN103265543A (zh) | 2011-08-09 | 2013-08-28 | 丘比斯特药物股份有限公司 | 抑制瞬时受体电位离子通道trpa1 |
| EP2787991A1 (en) | 2011-12-05 | 2014-10-15 | Glenmark Pharmaceuticals S.A. | Pharmaceutical composition comprising a trpa1 antagonist and an anticholinergic agent |
| JP6182072B2 (ja) | 2012-01-17 | 2017-08-16 | Eaファーマ株式会社 | 複素環アミド誘導体及びそれを含有する医薬 |
| NZ701721A (en) | 2012-06-08 | 2016-03-31 | Glenmark Pharmaceuticals Sa | Amides of 2-amino-4-arylthiazole compounds and their salts |
| NZ706989A (en) | 2012-10-01 | 2018-07-27 | Orion Corp | N-prop-2-ynyl carboxamide derivatives and their use as trpa1 antagonists |
| US9394308B2 (en) | 2013-01-18 | 2016-07-19 | Merck Sharp & Dohme Corp. | Inhibiting the transient receptor potential A1 ion channel |
| US9532988B2 (en) | 2013-10-15 | 2017-01-03 | Glenmark Pharmaceuticals S.A. | Pharmaceutical composition comprising a TRPA1 antagonist and an analgesic agent |
| CN104884457B (zh) * | 2013-10-30 | 2016-12-07 | 上海恒瑞医药有限公司 | 吡唑并嘧啶酮类或吡咯并三嗪酮类衍生物、其制备方法及其在医药上的应用 |
| CN103755705B (zh) * | 2014-02-17 | 2017-02-15 | 上海佰特因医药科技有限公司 | 一种天然产物四甲基尿酸的全合成方法 |
| JP6667092B2 (ja) * | 2014-08-11 | 2020-03-18 | ハイドラ・バイオサイエンシーズ・リミテッド・ライアビリティ・カンパニーHydra Biosciences, LLC | ピロロ[3,2−d]ピリミジン−2,4(3H,5H)−ジオン誘導体 |
| WO2016042501A1 (en) | 2014-09-16 | 2016-03-24 | Glenmark Pharmaceuticals S.A. | Trpa1 antagonist for the treatment of pain associated to diabetic neuropathic pain |
| CN105001170A (zh) * | 2015-07-13 | 2015-10-28 | 佛山市赛维斯医药科技有限公司 | 末端腈基取代的三氮唑亚砜类化合物、其制备方法及其用途 |
| WO2017060488A1 (en) | 2015-10-09 | 2017-04-13 | Almirall, S.A. | New trpa1 antagonists |
| WO2017064068A1 (en) | 2015-10-14 | 2017-04-20 | Almirall, S.A. | New trpa1 antagonists |
| WO2019020102A1 (zh) * | 2017-07-28 | 2019-01-31 | 江苏恒瑞医药股份有限公司 | 一种嘧啶酮并杂芳基类衍生物的制备方法及其中间体 |
| CN109422749B (zh) * | 2017-08-21 | 2023-01-24 | 重庆医药工业研究院有限责任公司 | 一种抑制单羧酸转运蛋白的嘧啶二酮衍生物 |
| US10710994B2 (en) | 2018-03-19 | 2020-07-14 | Genentech, Inc. | Oxadiazole transient receptor potential channel inhibitors |
| CN108558836A (zh) * | 2018-05-14 | 2018-09-21 | 东南大学 | 一类具有双重作用机制的dpp-4抑制剂及其用途 |
| WO2023096915A1 (en) * | 2021-11-24 | 2023-06-01 | Slap Pharmaceuticals Llc | Multicyclic compounds |
| MX2024009581A (es) * | 2022-02-03 | 2024-08-13 | De Shaw Res Llc | Compuestos de uracilo n3-sustituidos como inhibidores de trpa1. |
| JP2025510646A (ja) * | 2022-03-14 | 2025-04-15 | スラップ ファーマシューティカルズ エルエルシー | 多環式化合物 |
| CN114656472B (zh) * | 2022-04-27 | 2023-07-04 | 成都施贝康生物医药科技有限公司 | 吡唑并嘧啶类化合物、异构体或盐及其制备方法和用途 |
| CN114656473B (zh) * | 2022-04-27 | 2023-09-29 | 成都施贝康生物医药科技有限公司 | 吡咯并嘧啶类化合物、异构体或盐及其制备方法和用途 |
| CN114656480B (zh) * | 2022-04-27 | 2024-01-26 | 成都施贝康生物医药科技有限公司 | 噻吩并嘧啶类化合物、异构体或盐及其制备方法和用途 |
| CN118373832B (zh) * | 2023-01-20 | 2025-01-28 | 深圳晶蛋生物医药科技有限公司 | 大环类化合物、其药物组合物及其应用 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007073505A2 (en) * | 2005-12-22 | 2007-06-28 | Hydra Biosciences, Inc. | Trpa1 inhibitors for treating pain |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2248231A1 (de) | 1972-10-02 | 1974-04-11 | Basf Ag | 3-aminoisothiazolo eckige klammer auf 3,4-d eckige klammer zu pyrimidine |
| SE9701398D0 (sv) * | 1997-04-15 | 1997-04-15 | Astra Pharma Prod | Novel compounds |
| ES2193839B1 (es) | 2001-06-22 | 2005-02-16 | Almirall Prodesfarma, S.A. | Nuevos derivados de 6-fenildihidropirrolpirimidindiona. |
| AU2003253165A1 (en) | 2002-08-13 | 2004-02-25 | Warner-Lambert Company Llc | Pyrimidine fused bicyclic metalloproteinase inhibitors |
| AU2003290066A1 (en) | 2002-12-18 | 2004-07-09 | Novartis Ag | Anktm1, a cold-activated trp-like channel expressed in nociceptive neurons |
| JP2007522214A (ja) * | 2004-02-11 | 2007-08-09 | スミスクライン・ビーチャム・コーポレイション | Pthアゴニスト |
| US20070196866A1 (en) | 2004-03-13 | 2007-08-23 | Irm Llc | Modulators of ion channel trpa1 |
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