BR112022019628A2 - Composto da fórmula (i), enantiômero único, composição farmacêutica, processo para a preparação desta, método para o tratamento de uma condição ou distúrbio mediado pela atividade antagonista do receptor de trpv4 em um animal incluindo um humano, uso de um composto e composto representado pela fórmula (i-d) - Google Patents
Composto da fórmula (i), enantiômero único, composição farmacêutica, processo para a preparação desta, método para o tratamento de uma condição ou distúrbio mediado pela atividade antagonista do receptor de trpv4 em um animal incluindo um humano, uso de um composto e composto representado pela fórmula (i-d)Info
- Publication number
- BR112022019628A2 BR112022019628A2 BR112022019628A BR112022019628A BR112022019628A2 BR 112022019628 A2 BR112022019628 A2 BR 112022019628A2 BR 112022019628 A BR112022019628 A BR 112022019628A BR 112022019628 A BR112022019628 A BR 112022019628A BR 112022019628 A2 BR112022019628 A2 BR 112022019628A2
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- formula
- treatment
- preparing
- human
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 102000003567 TRPV4 Human genes 0.000 title abstract 3
- 101150098315 TRPV4 gene Proteins 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 230000000694 effects Effects 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 230000001404 mediated effect Effects 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000002464 receptor antagonist Substances 0.000 title abstract 2
- 229940044551 receptor antagonist Drugs 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical class O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 abstract 2
- 208000027866 inflammatory disease Diseases 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
-
- 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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]
-
- 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
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- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
COMPOSTO DA FÓRMULA (I), ENANTIÔMERO ÚNICO, COMPOSIÇÃO FARMACÊUTICA, PROCESSO PARA A PREPARAÇÃO DESTA, MÉTODO PARA O TRATAMENTO DE UMA CONDIÇÃO OU DISTÚRBIO MEDIADO PELA ATIVIDADE ANTAGONISTA DO RECEPTOR DE TRPV4 EM UM ANIMAL INCLUINDO UM HUMANO, USO DE UM COMPOSTO E COMPOSTO REPRESENTADO PELA FÓRMULA (I-D). Esta invenção se refere a derivados de pirimidin-4(3H)-ona que atuam como moduladores do receptor TRPV4. A presente invenção também se refere a processos para a preparação de novos derivados de pirimidin-4(3H)-ona e ao seu uso no tratamento de uma ampla gama de doenças, síndromes e distúrbios, em particular para o tratamento de doenças ou distúrbios inflamatórios, dolorosos e urológicos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202063017891P | 2020-04-30 | 2020-04-30 | |
PCT/JP2021/017277 WO2021221169A1 (en) | 2020-04-30 | 2021-04-30 | Pyrimidin-4(3h)-one derivatives as trpv4 antagonists |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112022019628A2 true BR112022019628A2 (pt) | 2022-11-16 |
Family
ID=78332043
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112022019628A BR112022019628A2 (pt) | 2020-04-30 | 2021-04-30 | Composto da fórmula (i), enantiômero único, composição farmacêutica, processo para a preparação desta, método para o tratamento de uma condição ou distúrbio mediado pela atividade antagonista do receptor de trpv4 em um animal incluindo um humano, uso de um composto e composto representado pela fórmula (i-d) |
Country Status (10)
Country | Link |
---|---|
US (1) | US20230339934A1 (pt) |
EP (1) | EP4142874A4 (pt) |
JP (1) | JP2023523469A (pt) |
KR (1) | KR20230005227A (pt) |
CN (1) | CN115427409A (pt) |
BR (1) | BR112022019628A2 (pt) |
CA (1) | CA3180132A1 (pt) |
MX (1) | MX2022013607A (pt) |
TW (1) | TW202206430A (pt) |
WO (1) | WO2021221169A1 (pt) |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2139896A1 (en) * | 2007-03-23 | 2010-01-06 | Pfizer Limited | Pyrimido [4, 5-d]azepine derivatives as 5-ht2c agonists |
JP5819397B2 (ja) | 2010-03-23 | 2015-11-24 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーGlaxoSmithKline LLC | Trpv4拮抗薬 |
WO2011119704A1 (en) * | 2010-03-23 | 2011-09-29 | Glaxosmithkline Llc | Trpv4 antagonists |
JO3154B1 (ar) | 2011-06-17 | 2017-09-20 | Glaxosmithkline Llc | عوامل مضادة لـ trpv4 |
ES2571409T3 (es) | 2011-06-17 | 2016-05-25 | Glaxosmithkline Intellectual Property (No 2) Ltd | Antagonistas espiro-cíclicos de TRPV4 |
ES2595606T3 (es) | 2011-06-17 | 2017-01-02 | Glaxosmithkline Intellectual Property (No. 2) Limited | Antagonistas TRPV4 |
WO2013146754A1 (ja) | 2012-03-27 | 2013-10-03 | 塩野義製薬株式会社 | Trpv4阻害活性を有する芳香族複素5員環誘導体 |
WO2015046193A1 (ja) * | 2013-09-25 | 2015-04-02 | 塩野義製薬株式会社 | Trpv4阻害活性を有する芳香族複素環式アミン誘導体 |
TW201825458A (zh) | 2016-09-20 | 2018-07-16 | 英商葛蘭素史克智慧財產(第二)有限公司 | Trpv4拮抗劑 |
US11260049B2 (en) | 2016-09-20 | 2022-03-01 | Glaxosmithkline Intellectual Property (No. 2) Limited | TRPV4 antagonists |
US10590077B2 (en) | 2016-09-20 | 2020-03-17 | Glaxosmithkline Intellectual Property Development Limited | TRPV4 antagonists |
JP7195067B2 (ja) | 2018-06-20 | 2022-12-23 | 花王株式会社 | ロズマリン酸誘導体又はその塩 |
-
2021
- 2021-04-30 US US17/921,203 patent/US20230339934A1/en active Pending
- 2021-04-30 JP JP2022566153A patent/JP2023523469A/ja active Pending
- 2021-04-30 CN CN202180029570.1A patent/CN115427409A/zh active Pending
- 2021-04-30 CA CA3180132A patent/CA3180132A1/en active Pending
- 2021-04-30 BR BR112022019628A patent/BR112022019628A2/pt unknown
- 2021-04-30 MX MX2022013607A patent/MX2022013607A/es unknown
- 2021-04-30 EP EP21796562.3A patent/EP4142874A4/en active Pending
- 2021-04-30 KR KR1020227040115A patent/KR20230005227A/ko active Search and Examination
- 2021-04-30 TW TW110115811A patent/TW202206430A/zh unknown
- 2021-04-30 WO PCT/JP2021/017277 patent/WO2021221169A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
CA3180132A1 (en) | 2021-10-30 |
MX2022013607A (es) | 2022-11-16 |
KR20230005227A (ko) | 2023-01-09 |
EP4142874A4 (en) | 2024-05-22 |
WO2021221169A1 (en) | 2021-11-04 |
US20230339934A1 (en) | 2023-10-26 |
EP4142874A1 (en) | 2023-03-08 |
TW202206430A (zh) | 2022-02-16 |
JP2023523469A (ja) | 2023-06-05 |
CN115427409A (zh) | 2022-12-02 |
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