RS54858B1 - Antagonisti trpv4 - Google Patents
Antagonisti trpv4Info
- Publication number
- RS54858B1 RS54858B1 RS20160417A RSP20160417A RS54858B1 RS 54858 B1 RS54858 B1 RS 54858B1 RS 20160417 A RS20160417 A RS 20160417A RS P20160417 A RSP20160417 A RS P20160417A RS 54858 B1 RS54858 B1 RS 54858B1
- Authority
- RS
- Serbia
- Prior art keywords
- 3alkyl
- het
- halo
- hydrogen
- 5alkyl
- Prior art date
Links
- 101150098315 TRPV4 gene Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 8
- 125000001475 halogen functional group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- -1 SO2C1-3alkyl 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
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 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
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [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
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 229910052698 phosphorus Inorganic materials 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000003373 pyrazinyl 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
- 125000001412 tetrahydropyranyl group 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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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
- A61P9/04—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)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Otolaryngology (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Communicable Diseases (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Jedinjenje Formule (I):naznačeno time, što suR1 je vodonik, C1-3alkil, CH2OH, CH2-O-CH3, CH2OCH2Ph, CH2CN, CN, halo ili C(0)OCH3;R2 je nezavisno vodonik, CN, CF3, halo, SO2C1-3alkil, C1-3alkil ili C=CH;R3 je vodonik, C1-2alkil, CF3 ili OH;R4 je vodonik, halo ili C1-3alkil;X je CR4 ili N;A je (CH2)n-Het; iliA je (CH2)n-(CRaRb)-(CH2)m-Het;Ra je vodonik ili C1-3alkil, pri čemu ovaj C1-3alkil može biti još supstituisan, sa jedan ili više halo;Rb je C1-3alkil;ili, Ra i Rb zajedno sa atomom ugljenika za koji su vezani, formiraju neku C3-6ciklolalkil grupu;ili, jedan ili više atoma ugljenika u ovoj C3-6ciklolalkil grupi, formiranoj sa Ra i Rb, može biti zamenjen sa kiseonikom, formirajući neku oksetan, tetrahidrofuril ili tetrahidropiranil grupu;ili, jedan ili više atoma ugljenika u ovoj C3-6ciklolalkil grupi, formiranoj sa Ra i Rb, može biti zamenjen sa azotom, formirajući neku pirolidinil ili piperidnil grupu;Het je:gde Het može biti supstituisan sa jednim, dva ili tri supstituenta koji se biraju između: halo, C1-5alkil, CN, CH2F, CHF2, CF3, C3-6cikloalkil, (CH2)n-O-C1-3alkil, (CH2)n-fenil, (CH2)n-piridil, pirimidinil, pirazinil, CH(CH3)-O-C1-3alkil, CH(OH)-C1-5alkil, C(CH3)2 - R5, C(O)N(CH3)P, N(C1-3alkil)p, NH2, C(O)NH2, oksetan, oksetan-CH3, tetrahidrofuril, tetrahidropiranil, morfolinil, ili pirazolil; pri čemu ovaj fenil, pirazolil i piridil supstituent na Het može biti još supstituisan sa jednim ili dva supstituenta koji se biraju između: halo, CN, OCH3, C1-3alkil ili CF3;a ovaj C1-5alkil i C3-6cikloalkil supstituent na Het može biti još supstituisan sa CN ili OH;R5 je CN, O-C1-4alkil, (CH2)m-OH, (CH2)p-O-C(O)-O-C1-5alkil, ili O-(CH2)p-O-R6;R6 je C1-4alkil ili P(O)2(CH3)2;n je nezavisno 0, 1 ili 2;m je nezavisno 0, 1 ili 2;p je nezavisno 1 ili 2; iy je1,2 ili 3;ili neka njegova farmaceutski prihvatljiva so.Prijava sadrži još 16 patentnih zahteva.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161498110P | 2011-06-17 | 2011-06-17 | |
| EP12814591.9A EP2721016B1 (en) | 2011-06-17 | 2012-06-15 | Trpv4 antagonists |
| PCT/US2012/042622 WO2013012500A1 (en) | 2011-06-17 | 2012-06-15 | Trpv4 antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RS54858B1 true RS54858B1 (sr) | 2016-10-31 |
Family
ID=47558389
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RS20160417A RS54858B1 (sr) | 2011-06-17 | 2012-06-15 | Antagonisti trpv4 |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US9187464B2 (sr) |
| EP (2) | EP2721016B1 (sr) |
| JP (1) | JP5969017B2 (sr) |
| KR (1) | KR101870003B1 (sr) |
| CN (1) | CN103732583B (sr) |
| AR (1) | AR086958A1 (sr) |
| AU (1) | AU2012284540B2 (sr) |
| BR (1) | BR112013032391B1 (sr) |
| CA (1) | CA2839743C (sr) |
| CL (1) | CL2013003602A1 (sr) |
| CO (1) | CO6821953A2 (sr) |
| CR (1) | CR20130671A (sr) |
| CY (1) | CY1117792T1 (sr) |
| DK (1) | DK2721016T3 (sr) |
| DO (1) | DOP2013000307A (sr) |
| EA (1) | EA023616B1 (sr) |
| ES (2) | ES2569193T3 (sr) |
| HK (1) | HK1195068A1 (sr) |
| HR (1) | HRP20160539T1 (sr) |
| HU (1) | HUE029594T2 (sr) |
| IL (1) | IL229872A (sr) |
| JO (1) | JO3154B1 (sr) |
| MA (1) | MA35184B1 (sr) |
| ME (1) | ME02416B (sr) |
| MX (1) | MX337440B (sr) |
| MY (1) | MY173521A (sr) |
| PE (1) | PE20141943A1 (sr) |
| PL (1) | PL2721016T3 (sr) |
| PT (1) | PT2721016E (sr) |
| RS (1) | RS54858B1 (sr) |
| SG (1) | SG195106A1 (sr) |
| SI (1) | SI2721016T1 (sr) |
| SM (1) | SMT201600150B (sr) |
| TW (1) | TWI538912B (sr) |
| UA (1) | UA113963C2 (sr) |
| UY (1) | UY34138A (sr) |
| WO (1) | WO2013012500A1 (sr) |
| ZA (1) | ZA201308816B (sr) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2595606T3 (es) * | 2011-06-17 | 2017-01-02 | Glaxosmithkline Intellectual Property (No. 2) Limited | Antagonistas TRPV4 |
| US9487507B2 (en) | 2011-06-17 | 2016-11-08 | Glaxosmithkline Intellectual Property (No. 2) Limited | TRPV4 antagonists |
| 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 |
| US10968209B2 (en) | 2016-05-19 | 2021-04-06 | Glaxosmithkline Intellectual Property (No.2) Limited | TRPV4 antagonist |
| WO2017199199A1 (en) | 2016-05-19 | 2017-11-23 | 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 |
| MX2020004400A (es) * | 2017-11-01 | 2020-08-06 | Bristol Myers Squibb Co | Compuestos espirociclicos como moduladores del receptor farnesoide x. |
| 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 |
| CN115776890A (zh) * | 2020-07-16 | 2023-03-10 | 拉夸里亚创药株式会社 | 作为眼病治疗剂的trpv4抑制剂 |
| TW202409024A (zh) | 2022-07-08 | 2024-03-01 | 美商愛克堤歐生物科學公司 | 治療性化合物及方法 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69942801D1 (de) * | 1998-05-26 | 2010-11-11 | Chugai Pharmaceutical Co Ltd | Heterozyklische indolderivate und mono- oder diazaindol-derivate |
| EP1644358A2 (en) * | 2003-07-16 | 2006-04-12 | Neurogen Corporation | Biaryl piperazinyl-pyridine analogues |
| CA2630617C (en) * | 2005-11-23 | 2014-03-25 | Painceptor Pharma Corporation | Compositions and methods for modulating gated ion channels |
| WO2007067756A2 (en) | 2005-12-08 | 2007-06-14 | Amphora Discovery Corporation | Certain chemical entities, compositions, and methods for modulating trpv1 |
| TWI610684B (zh) * | 2005-12-22 | 2018-01-11 | 海卓勒生物科學公司 | 用於調節ｔｒｐａ１功能之化合物 |
| TW200819457A (en) * | 2006-08-30 | 2008-05-01 | Actelion Pharmaceuticals Ltd | Spiro antibiotic derivatives |
| WO2008092891A1 (en) * | 2007-02-01 | 2008-08-07 | Glaxo Group Limited | 1-oxa-3-azaspiro(4.5)decan-2-one derivatives for the treatment of eating disorders |
| 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 |
| EP2312947B1 (en) * | 2008-07-25 | 2014-01-01 | GlaxoSmithKline LLC | 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 |
| WO2012024183A1 (en) * | 2010-08-18 | 2012-02-23 | Merck Sharp & Dohme Corp. | Spiroxazolidinone compounds |
| ES2595606T3 (es) * | 2011-06-17 | 2017-01-02 | Glaxosmithkline Intellectual Property (No. 2) Limited | Antagonistas TRPV4 |
| US9487507B2 (en) * | 2011-06-17 | 2016-11-08 | Glaxosmithkline Intellectual Property (No. 2) Limited | TRPV4 antagonists |
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