AR099833A1 - Compuesto amídico como antagonista del receptor ep4 - Google Patents
Compuesto amídico como antagonista del receptor ep4Info
- Publication number
- AR099833A1 AR099833A1 ARP150100875A ARP150100875A AR099833A1 AR 099833 A1 AR099833 A1 AR 099833A1 AR P150100875 A ARP150100875 A AR P150100875A AR P150100875 A ARP150100875 A AR P150100875A AR 099833 A1 AR099833 A1 AR 099833A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- receptor
- salt
- pharmaceutical composition
- antagonistic action
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 239000005557 antagonist Substances 0.000 title 1
- 101150109738 Ptger4 gene Proteins 0.000 abstract 3
- -1 amide compound Chemical class 0.000 abstract 3
- 230000003042 antagnostic effect Effects 0.000 abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 208000007342 Diabetic Nephropathies Diseases 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 2
- 208000020832 chronic kidney disease Diseases 0.000 abstract 2
- 208000022831 chronic renal failure syndrome Diseases 0.000 abstract 2
- 239000013078 crystal Substances 0.000 abstract 2
- 208000033679 diabetic kidney disease Diseases 0.000 abstract 2
- LKEYBJRFBJOLBQ-AWEZNQCLSA-N 4-[(1S)-1-[[4-bromo-2-(isoquinolin-3-ylmethyl)-5-methylpyrazole-3-carbonyl]amino]ethyl]benzoic acid Chemical compound BrC=1C(=NN(C=1C(=O)N[C@@H](C)C1=CC=C(C(=O)O)C=C1)CC=1N=CC2=CC=CC=C2C=1)C LKEYBJRFBJOLBQ-AWEZNQCLSA-N 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid group Chemical group C(C1=CC=CC=C1)(=O)O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 238000000113 differential scanning calorimetry Methods 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se presenta un compuesto que es útil como ingrediente activo de una composición farmacéutica, por ejemplo, una composición farmacéutica para tratar la insuficiencia renal crónica y/o la nefropatía diabética. Se han llevado a cabo extensos estudios sobre un compuesto con una acción antagonista del receptor EP4 y han encontrado que un compuesto amídico o una sal del mismo exhibe una acción antagonista del receptor EP4, completando de esa manera la presente. El compuesto amídico o una sal del mismo tiene acción antagonista del receptor EP4 y se lo puede utilizar como ingrediente activo de una composición farmacéutica para prevenir y/o tratar diversas enfermedades relacionadas con el EP4, por ejemplo, la insuficiencia renal crónica y/o la nefropatía diabética. Reivindicación 1: Ácido 4-[(1S)-1-({[4-bromo-1-(isoquinolin-3-ilmetil)-3-metil-1H-pirazol-5-il]carbonil}amino)etil]benzoico o una sal del mismo. Reivindicación 3: El compuesto de acuerdo con la reivindicación 2, que es un cristal de metansulfonato de ácido 4-[(1S)-1-({[4-bromo-1-(isoquinolin-3-ilmetil)-3-metil-1H-pirazol-5-iI]carbonil}amino)etil]benzoico. Reivindicación 4: El compuesto de acuerdo con la reivindicación 3, que es un cristal con una temperatura de inicio de un pico endotérmico en el análisis de DSC de 192ºC y con picos a 2q (º) = 4,7, 9,5, 12,0, 13,2, 13,7, 15,3, 18,8, 20,3, 20,9 y 22,8 en la difracción de rayos X en polvo utilizando Cu como tubo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2014064590 | 2014-03-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR099833A1 true AR099833A1 (es) | 2016-08-24 |
Family
ID=54195532
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150100875A AR099833A1 (es) | 2014-03-26 | 2015-03-25 | Compuesto amídico como antagonista del receptor ep4 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10106523B2 (es) |
| EP (1) | EP3124480B1 (es) |
| JP (1) | JP6428763B2 (es) |
| KR (1) | KR20160138098A (es) |
| CN (1) | CN106132945B (es) |
| AR (1) | AR099833A1 (es) |
| CA (1) | CA2943778A1 (es) |
| ES (1) | ES2684334T3 (es) |
| MX (1) | MX368098B (es) |
| PL (1) | PL3124480T3 (es) |
| PT (1) | PT3124480T (es) |
| RU (1) | RU2684906C2 (es) |
| TW (1) | TW201623277A (es) |
| WO (1) | WO2015147020A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| AU2018269666B2 (en) | 2017-05-18 | 2022-02-03 | Idorsia Pharmaceuticals Ltd | Phenyl derivatives as PGE2 receptor modulators |
| EP3625224B1 (en) | 2017-05-18 | 2021-08-04 | Idorsia Pharmaceuticals Ltd | N-substituted indole derivatives |
| CA3063788A1 (en) | 2017-05-18 | 2018-11-22 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives |
| KR102612649B1 (ko) | 2017-05-18 | 2023-12-11 | 이도르시아 파마슈티컬스 리미티드 | Pge2 수용체 조절제로서의 벤조푸란 및 벤조티오페논 유도체 |
| US11839613B2 (en) | 2017-05-18 | 2023-12-12 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives as PGE2 receptor modulators |
| KR20230107228A (ko) | 2020-11-13 | 2023-07-14 | 오노 야꾸힝 고교 가부시키가이샤 | Ep4 길항약과 면역 체크포인트 저해 물질의 병용에 의한 암 치료 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003233297A1 (en) * | 2002-05-23 | 2003-12-12 | Theratechnologies Inc | Antagonistic peptides of prostaglandin e2 receptor subtype ep4 |
| JP5259592B2 (ja) | 2006-08-11 | 2013-08-07 | メルク カナダ インコーポレイテッド | Ｅｐ４受容体リガンドとしてのチオフェンカルボキサミド誘導体 |
| US20110028463A1 (en) * | 2007-07-03 | 2011-02-03 | Astellas Pharma Inc. | Amide compounds |
| ES2518919T3 (es) | 2008-05-14 | 2014-11-05 | Astellas Pharma Inc. | Derivados del ácido 4-(Indol-7-ilcarbonilaminometil)ciclohexanocarboxílico como antagonistas del receptor EP4 útiles para el tratamiento de la insuficiencia renal crónica o la nefropatía diabética |
| CN103097358B (zh) | 2010-09-21 | 2015-04-08 | 卫材R&D管理有限公司 | 药物组合物 |
| WO2012103071A2 (en) | 2011-01-25 | 2012-08-02 | Eisai R&D Management Co., Ltd. | Compounds and compositions |
-
2015
- 2015-03-24 TW TW104109378A patent/TW201623277A/zh unknown
- 2015-03-25 JP JP2016510404A patent/JP6428763B2/ja not_active Expired - Fee Related
- 2015-03-25 CA CA2943778A patent/CA2943778A1/en not_active Abandoned
- 2015-03-25 ES ES15770149.1T patent/ES2684334T3/es active Active
- 2015-03-25 AR ARP150100875A patent/AR099833A1/es unknown
- 2015-03-25 CN CN201580016273.8A patent/CN106132945B/zh active Active
- 2015-03-25 PL PL15770149T patent/PL3124480T3/pl unknown
- 2015-03-25 RU RU2016141650A patent/RU2684906C2/ru active
- 2015-03-25 EP EP15770149.1A patent/EP3124480B1/en active Active
- 2015-03-25 MX MX2016012318A patent/MX368098B/es active IP Right Grant
- 2015-03-25 WO PCT/JP2015/059026 patent/WO2015147020A1/ja active Application Filing
- 2015-03-25 PT PT15770149T patent/PT3124480T/pt unknown
- 2015-03-25 KR KR1020167027923A patent/KR20160138098A/ko active IP Right Grant
- 2015-03-25 US US15/127,574 patent/US10106523B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US10106523B2 (en) | 2018-10-23 |
| TW201623277A (zh) | 2016-07-01 |
| PL3124480T3 (pl) | 2018-10-31 |
| US20180030030A1 (en) | 2018-02-01 |
| EP3124480A4 (en) | 2017-11-22 |
| KR20160138098A (ko) | 2016-12-02 |
| WO2015147020A1 (ja) | 2015-10-01 |
| RU2016141650A3 (es) | 2018-11-12 |
| MX368098B (es) | 2019-09-19 |
| JP6428763B2 (ja) | 2018-11-28 |
| CN106132945A (zh) | 2016-11-16 |
| EP3124480B1 (en) | 2018-07-11 |
| CN106132945B (zh) | 2019-04-26 |
| CA2943778A1 (en) | 2015-10-01 |
| RU2684906C2 (ru) | 2019-04-16 |
| JPWO2015147020A1 (ja) | 2017-04-13 |
| MX2016012318A (es) | 2017-02-23 |
| EP3124480A1 (en) | 2017-02-01 |
| ES2684334T3 (es) | 2018-10-02 |
| RU2016141650A (ru) | 2018-04-27 |
| PT3124480T (pt) | 2018-10-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR099833A1 (es) | Compuesto amídico como antagonista del receptor ep4 | |
| CL2016002072A1 (es) | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer | |
| CY1119490T1 (el) | Παραγωγα πυραζολοπυρρολιδινης και η χρηση τους στην θεραπεια νοσηματων | |
| TR201901312T4 (tr) | Mcl-1 proteinini inhibe eden tetrahidronaftalen türevleri. | |
| CL2019001565A1 (es) | Composición farmacéutica para prevenir o tratar el cáncer, comprendiendo el polímorfo cristalino del hexoxido tetraarsénico. | |
| CR20140472A (es) | Composicion herbicida que comprende como ingrediente activo un compuesto de uracilo | |
| CL2019002464A1 (es) | Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. | |
| DOP2015000274A (es) | Compuestos químicos | |
| CL2015000578A1 (es) | Compuesto n-(2-(6-fluoro-1-h-indol-3-il)etil)-3-(2,2,3,3-tetrafluoropropoxi)bencilamina o su sal, antagonista del receptor 5-ht6; composicion farmaceutica; uso en el tratamiento de la enfermedad de alzheimer. | |
| CL2013002053A1 (es) | Compuestos derivados de heterociclicos, antagonistas del receptor de glucagon; composicion farmaceutica que lo comprende y su uso en el tratamiento de diabetes y enfermedades metabolicas. pct | |
| DOP2015000197A (es) | Sales de derivados de 2-amino-1-hidroxietil-8-hidroxiquinolin-2(1h)-ona que tienen actividad agonista del receptor ¿2 adrenérgico así como actividad antagonista del receptor muscarínico m3. | |
| HN2010002030A (es) | Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 | |
| MX2015016344A (es) | Derivados de imidazo-pirrolidinona y su uso en el tratamiento de enfermedades. | |
| DOP2015000170A (es) | Compuestos químicos | |
| CL2015002608A1 (es) | Compuesto de amino-pirazol y usos medicinales relacionados. | |
| BR112015030387A2 (pt) | compostos de pirazol como moduladores de fshr e usos dos mesmos | |
| ECSP16008797A (es) | Derivados de heterobicicloaril como inhibidores rorc2 y métodos de uso de los mismos | |
| AR128459A2 (es) | Composición farmacéutica sólida comprimida por rodillo y el proceso para su fabricación | |
| CR20160460A (es) | Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y trastornos relacionados | |
| IL240949B (en) | Aqueous pharmaceutical formulation for use in the treatment of type 1 or type 2 juvenile diabetes | |
| CL2015003195A1 (es) | Derivados de purina como agonistas del receptor cb2. | |
| MX2015012528A (es) | Inhibidores macrociclicos de cinasa inducibles por sal. | |
| CL2014002845A1 (es) | Compuestos derivados de pirazol inhibidores de sglt1; metodo para tratar la diabetes; composicion farmaceutica; uso del compuesto para el tratamiento de la diabetes tipo 1 y tipo 2. | |
| CR20150267A (es) | 6-((s)-1-{1-[5-(2-hidroxi-etoxi)-piridin-2-il] 1h-pirazol-3-il}-etil)-3h-1,3-benzotiazol-2-ona como un antagonista del receptor ampa dependiente de tarp-gamma 8 | |
| EA201692276A1 (ru) | Комбинации тиотропия бромида, формотерола и будесонида для лечения хобл |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |