AR086958A1 - Antagonistas de trpv4 - Google Patents
Antagonistas de trpv4Info
- Publication number
- AR086958A1 AR086958A1 ARP120102143A ARP120102143A AR086958A1 AR 086958 A1 AR086958 A1 AR 086958A1 AR P120102143 A ARP120102143 A AR P120102143A AR P120102143 A ARP120102143 A AR P120102143A AR 086958 A1 AR086958 A1 AR 086958A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- het
- halo
- hydrogen
- independently
- Prior art date
Links
- 102000003567 TRPV4 Human genes 0.000 title abstract 2
- 101150098315 TRPV4 gene Proteins 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 11
- 125000001475 halogen functional group Chemical group 0.000 abstract 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- AHHWIHXENZJRFG-UHFFFAOYSA-N oxetane Chemical compound C1COC1 AHHWIHXENZJRFG-UHFFFAOYSA-N 0.000 abstract 2
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 2
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 abstract 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 abstract 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical group O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- -1 tetrahydrofurfuryl Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P1/10—Laxatives
-
- 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
- A61P1/12—Antidiarrhoeals
-
- 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
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
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- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
-
- 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]
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- 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
-
- 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
- A61P31/04—Antibacterial agents
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- 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
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- 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
- A61P7/10—Antioedematous agents; Diuretics
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- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
- C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
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- 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
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Otolaryngology (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente se refiere a análogos de espirocarbamato, a composiciones farmacéuticas que los contienen y a su uso como antagonistas de TRPV4.Reivindicación 1: Un compuesto de fórmula (1), en la que: R1 es hidrógeno, alquilo C1-3, CH2OH, CH2-O-CH3, CH2OCH2Ph, CH2CN, CN, halo o C(O)OCH3; R2 es independientemente hidrógeno, CN, CF3, halo, SO2-alquilo C1-3, alquilo C1-3 o CºCH; R3 es hidrógeno, alquilo C1-2, CF3 u OH; R4 es hidrógeno, halo o alquilo C1-3; X es CR4 o N; A es (CH2)n-Het; o A es (CH2)n-(CRaRb)-(CH2)m-Het; Ra es hidrógeno o alquilo C1-3, en el que el alquilo C1-3 puede estar sustituido adicionalmente con uno o más halos; Rb es alquilo C1-3; o Ra y Rb, junto con el átomo de carbono al que están unidos, forma un grupo cicloalquilo C3-6; uno o más de los átomos de carbono en el grupo cicloalquilo C3-6 formado por Ra y Rb pueden estar reemplazados con oxígeno para formar un oxetano, tetrahidrofurilo o tetrahidropiranilo; uno de los átomos de carbono en el grupo cicloalquilo C3-6 formado por Ra y Rb, puede estar reemplazado con nitrógeno para formar un grupo pirrolidinilo o piperidinilo; Het es seleccionado del grupo de fórmulas (2), en la que Het puede estar sustituido con dos o tres sustituyentes seleccionados entre: halo, alquilo C1-5, CN, CH2F, CHF2, CF3, cicloalquilo C3-6, (CH2)n-O-alquilo C1-3, (CH2)n-fenilo, (CH2)n-piridilo, pirimidinilo, pirazinilo, CH(CH3)-O-alquilo C1-3, CH(OH)-alquilo C1-5, C(CH3)2-R5, C(O)N(CH3)p, N(alquilo C1-3)p, NH2, C(O)NH2, oxetano, oxetano-CH3, tetrahidrofurfurilo, tetrahidropiranilo, morfolinilo o pirazolilo; en la que el sustituyente fenilo, pirazolilo, y piridilo en el Het puede estar adicionalmente sustituido con uno o dos sustituyentes seleccionados entre: halo, CN, OCH3, alquilo C1-3 o CF3; y el sustituyente alquilo C1-5 y cicloalquilo C3-6 en el Het puede estar adicionalmente sustituido con CN u OH; R5 es CN, O-alquilo C1-4, (CH2)m-OH, (CH2)p-O-C(O)-O-alquilo C1-5 ó O-(CH2)p-O-R6; R6 es alquilo C1-4 o P(O)2(CH3)2; n es independientemente 0, 1 ó 2; m es independientemente 0, 1 ó 2; p es independientemente 1 ó 2; e y es 1, 2 ó 3; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161498110P | 2011-06-17 | 2011-06-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR086958A1 true AR086958A1 (es) | 2014-02-05 |
Family
ID=47558389
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120102143A AR086958A1 (es) | 2011-06-17 | 2012-06-15 | Antagonistas de trpv4 |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US9187464B2 (es) |
| EP (2) | EP2721016B1 (es) |
| JP (1) | JP5969017B2 (es) |
| KR (1) | KR101870003B1 (es) |
| CN (1) | CN103732583B (es) |
| AR (1) | AR086958A1 (es) |
| AU (1) | AU2012284540B2 (es) |
| BR (1) | BR112013032391B1 (es) |
| CA (1) | CA2839743C (es) |
| CL (1) | CL2013003602A1 (es) |
| CO (1) | CO6821953A2 (es) |
| CR (1) | CR20130671A (es) |
| CY (1) | CY1117792T1 (es) |
| DK (1) | DK2721016T3 (es) |
| DO (1) | DOP2013000307A (es) |
| EA (1) | EA023616B1 (es) |
| ES (2) | ES2688733T3 (es) |
| HR (1) | HRP20160539T1 (es) |
| HU (1) | HUE029594T2 (es) |
| IL (1) | IL229872A (es) |
| JO (1) | JO3154B1 (es) |
| MA (1) | MA35184B1 (es) |
| ME (1) | ME02416B (es) |
| MX (1) | MX337440B (es) |
| MY (1) | MY173521A (es) |
| PE (1) | PE20141943A1 (es) |
| PH (1) | PH12013502463A1 (es) |
| PL (1) | PL2721016T3 (es) |
| PT (1) | PT2721016E (es) |
| RS (1) | RS54858B1 (es) |
| SG (1) | SG195106A1 (es) |
| SI (1) | SI2721016T1 (es) |
| SM (1) | SMT201600150B (es) |
| TW (1) | TWI538912B (es) |
| UA (1) | UA113963C2 (es) |
| UY (1) | UY34138A (es) |
| WO (1) | WO2013012500A1 (es) |
| ZA (1) | ZA201308816B (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5969016B2 (ja) | 2011-06-17 | 2016-08-10 | グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ | Ｔｒｐｖ４拮抗薬 |
| JP5969015B2 (ja) * | 2011-06-17 | 2016-08-10 | グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ | Ｔｒｐｖ４拮抗薬 |
| EP2832731A4 (en) | 2012-03-27 | 2015-08-19 | Shionogi & Co | AROMATIC HETEROCYCLIC CHAIN 5-CORE DERIVED DERIVATIVE HAVING TRPV4 INHIBITORY ACTIVITY |
| 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 |
| AU2017266562A1 (en) * | 2016-05-19 | 2018-11-15 | Glaxosmithkline Intellectual Property (No.2) Limited | TRPV4 antagonist |
| US10968209B2 (en) | 2016-05-19 | 2021-04-06 | Glaxosmithkline Intellectual Property (No.2) Limited | TRPV4 antagonist |
| EP3519413A1 (en) | 2016-10-03 | 2019-08-07 | Janssen Pharmaceutica NV | Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors |
| WO2018185701A1 (en) | 2017-04-06 | 2018-10-11 | Glaxosmithkline Intellectual Property (No.2) Limited | Trpv4 antagonists as antitussive agents |
| CA3081424A1 (en) * | 2017-11-01 | 2019-05-09 | Bristol-Myers Squibb Company | Spirocyclic compounds as farnesoid x receptor modulators |
| WO2021170811A1 (en) | 2020-02-27 | 2021-09-02 | Glaxosmithkline Intellectual Property (No.2) Limited | Method of treating eye disease using trpv4 antagonists |
| MX2022013607A (es) | 2020-04-30 | 2022-11-16 | Raqualia Pharma Inc | Derivados de la pirimidina-4(3h)-ona como antagonistas de trpv4. |
| CN111704613B (zh) * | 2020-06-23 | 2021-07-06 | 中国人民解放军军事科学院军事医学研究院 | 咪唑类衍生物及其作为trpv4抑制剂的用途 |
| KR20230041680A (ko) * | 2020-07-16 | 2023-03-24 | 라퀄리아 파마 인코포레이티드 | 안구 질환 치료제로서의 trpv4 억제제 |
| IL318209A (en) | 2022-07-08 | 2025-03-01 | Actio Biosciences Inc | Medical compounds and methods |
| WO2024217429A1 (zh) * | 2023-04-18 | 2024-10-24 | 河北乌图药业有限公司 | 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用 |
| CN120641413A (zh) * | 2023-04-18 | 2025-09-12 | 河北乌图药业有限公司 | 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用 |
| CN121175303A (zh) * | 2023-04-18 | 2025-12-19 | 河北乌图药业有限公司 | 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用 |
| CN120225516A (zh) * | 2023-04-18 | 2025-06-27 | 河北乌图药业有限公司 | 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用 |
| CN119855818A (zh) * | 2023-04-18 | 2025-04-18 | 河北乌图药业有限公司 | 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用 |
| WO2025014818A1 (en) * | 2023-07-07 | 2025-01-16 | Actio Biosciences, Inc. | Solid forms of gsk2798745, a trpv4 antagonist |
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| US6673797B1 (en) * | 1998-05-26 | 2004-01-06 | Chugai Seiyaku Kabushiki Kaisha | Heterocyclic indole derivatives and mono- or diazaindole derivatives |
| EP1644358A2 (en) * | 2003-07-16 | 2006-04-12 | Neurogen Corporation | Biaryl piperazinyl-pyridine analogues |
| CN101346375B (zh) * | 2005-11-23 | 2013-04-10 | 阿罗斯药物有限责任公司 | 调节门离子通道用组合物和方法 |
| WO2007067756A2 (en) | 2005-12-08 | 2007-06-14 | Amphora Discovery Corporation | Certain chemical entities, compositions, and methods for modulating trpv1 |
| AU2006327181A1 (en) * | 2005-12-22 | 2007-06-28 | Hydra Biosciences, Inc. | TRPA1 inhibitors for treating pain |
| TW200819457A (en) * | 2006-08-30 | 2008-05-01 | Actelion Pharmaceuticals Ltd | Spiro antibiotic derivatives |
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| GB0707934D0 (en) * | 2007-04-24 | 2007-05-30 | Glaxo Group Ltd | Chemical compounds |
| WO2009023539A2 (en) * | 2007-08-09 | 2009-02-19 | Abbott Laboratories | Tetrahydropyridine carboxamide derivatives as trpvl antagonists |
| TW200944520A (en) * | 2008-01-29 | 2009-11-01 | Glaxo Group Ltd | Spiro compounds as NPY Y5 receptor antagonists |
| WO2010011914A1 (en) | 2008-07-25 | 2010-01-28 | Smithkline Beecham Corporation | Trpv4 antagonists |
| JP2012006837A (ja) * | 2008-09-30 | 2012-01-12 | Mochida Pharmaceut Co Ltd | ２−インドールアクリルアミド類縁体 |
| EP2605658B1 (en) * | 2010-08-18 | 2016-03-23 | Merck Sharp & Dohme Corp. | Spiroxazolidinone compounds |
| JP5969016B2 (ja) * | 2011-06-17 | 2016-08-10 | グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ | Ｔｒｐｖ４拮抗薬 |
| JP5969015B2 (ja) * | 2011-06-17 | 2016-08-10 | グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ | Ｔｒｐｖ４拮抗薬 |
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