AR116019A1 - Derivados de guanidinobenzoilo como inhibidores de enteropeptidasa - Google Patents
Derivados de guanidinobenzoilo como inhibidores de enteropeptidasaInfo
- Publication number
- AR116019A1 AR116019A1 ARP190102423A ARP190102423A AR116019A1 AR 116019 A1 AR116019 A1 AR 116019A1 AR P190102423 A ARP190102423 A AR P190102423A AR P190102423 A ARP190102423 A AR P190102423A AR 116019 A1 AR116019 A1 AR 116019A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- substituents
- optionally
- alkyl group
- integer
- Prior art date
Links
- 102100029727 Enteropeptidase Human genes 0.000 title abstract 2
- 108010013369 Enteropeptidase Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- -1 GUANIDINOBENZOYL Chemical class 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 101100294115 Caenorhabditis elegans nhr-4 gene Proteins 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical group OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000542 sulfonic acid group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
- C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
- C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Child & Adolescent Psychology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Se proveen compuestos derivados de guanidinbenzoil éster como inhibidores de enteropeptidasa y un medicamento que lo comprende para el tratamiento de la obesidad y de la diabetes mellitus. Reivindicación 1: Un compuesto representado por la fórmula (1) o una sal del mismo, caracterizado porque cada símbolo tiene el siguiente significado: R¹: H, halógeno, un grupo C₁₋₆ alquilo que opcionalmente tiene uno o más sustituyentes, o un grupo C₁₋₆ alcoxi que opcionalmente tiene uno o más sustituyentes; R²: H o un grupo C₁₋₆ alquilo opcionalmente sustituido con un grupo carboxilo; R³: un grupo C₁₋₈ alquilo que tiene un sustituyente seleccionado entre el grupo que consiste en un grupo carboxilo, un grupo ácido sulfónico, y un grupo ácido fosfórico y opcionalmente está sustituido adicionalmente con un sustituyente seleccionado entre el grupo que consiste en un grupo carboxilo, NHR⁴ y un grupo hidroxi; R⁴: H o un grupo C₁₋₆ alquilo que opcionalmente tiene uno o más sustituyentes; n: un entero entre 0 y 2; X: una unión o NH; Y: **-C(=O)O- o **-OC(=O)- (donde** se une al anillo benceno sustituido con un grupo guanidino o un grupo carbomimidoilo); Qᵃ y Qᵇ: iguales o diferentes, -(CH₂)ₘO-*, -(CH₂)ₘNR⁵-, -(CH₂)ₘNR⁵C(=O)-*, -C(=O)NR⁵-*, -S-*, o -SO₂-* (donde * se une a Z); R⁵: H o un grupo C₁₋₆ alquilo que opcionalmente tiene uno o más sustituyentes; m: es un entero entre 0 y 6; Z: -[(CR⁶ᵃR⁶ᵇ)q-A]ʳ-(CR⁷ᵃR⁷ᵇ)ₛ-; A: O, S, SO₂, NR⁸, -C(=O)-, -OC(=O)-, -C(=O)O-, -NR⁸C(=O)-, o C(=O)-NR⁸; R⁶ᵃ, R⁶ᵇ, R⁷ᵃ y R⁷ᵇ: iguales o diferentes, H, halógeno, un grupo hidroxi, o un grupo C₁₋₆ alquilo que opcionalmente tiene uno o más sustituyentes, o un grupo C₁₋₆ alcoxi que opcionalmente tiene uno o más sustituyentes; R⁸: H o un grupo C₁₋₆ alquilo que opcionalmente tiene uno o más sustituyentes; q: un entero entre 1 y 6; r: un entero entre 0 y 50; y s: un entero entre 1 y 6.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2018157901 | 2018-08-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR116019A1 true AR116019A1 (es) | 2021-03-25 |
Family
ID=69644539
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190102423A AR116019A1 (es) | 2018-08-27 | 2019-08-26 | Derivados de guanidinobenzoilo como inhibidores de enteropeptidasa |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20210403420A1 (es) |
| EP (1) | EP3650440A4 (es) |
| JP (1) | JP6773938B2 (es) |
| AR (1) | AR116019A1 (es) |
| TW (1) | TW202024028A (es) |
| WO (1) | WO2020045326A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2019088270A1 (ja) | 2017-11-02 | 2020-12-03 | 宇部興産株式会社 | 蛋白分解酵素の双頭型阻害剤 |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1072649C (zh) | 1995-09-13 | 2001-10-10 | 武田药品工业株式会社 | 苯并氧杂吖庚因化合物,其生产方法和用途 |
| AR035016A1 (es) | 1999-08-25 | 2004-04-14 | Takeda Chemical Industries Ltd | Composicion de azol promotor de produccion/secrecion de neurotrofina, compuesto prodroga del mismo, composicion farmaceutica que lo comprende y uso del mismo para preparar esta ultima. |
| US20030187023A1 (en) | 2000-07-17 | 2003-10-02 | Keiji Kubo | Sulfone derivatives, process for their production and use thereof |
| NZ540381A (en) | 2002-11-01 | 2007-11-30 | Takeda Pharmaceutical | 5-membered aromatic heterocycle derivatives as prophylactic and therapeutic agents for treating neuropathy |
| EP1559422B1 (en) | 2002-11-08 | 2014-04-30 | Takeda Pharmaceutical Company Limited | Receptor function controlling agent |
| AU2003284596A1 (en) | 2002-11-22 | 2004-06-18 | Takeda Pharmaceutical Company Limited | Imidazole derivative, process for producing the same, and use |
| EP1630152A4 (en) | 2003-05-30 | 2009-09-23 | Takeda Pharmaceutical | CONDENSED CYCLIC COMPOUND |
| WO2005030740A1 (ja) | 2003-09-30 | 2005-04-07 | Takeda Pharmaceutical Company Limited | チアゾリン誘導体およびその用途 |
| US7820673B2 (en) | 2003-12-17 | 2010-10-26 | Takeda Pharmaceutical Company Limited | Urea derivative, process for producing the same, and use |
| EP1697339A1 (en) | 2003-12-25 | 2006-09-06 | Takeda Pharmaceutical Company Limited | 3-(4-benzyloxyphenyl)propanoic acid derivatives |
| WO2005063725A1 (ja) | 2003-12-26 | 2005-07-14 | Takeda Pharmaceutical Company Limited | フェニルプロパン酸誘導体 |
| JP4875978B2 (ja) | 2004-03-15 | 2012-02-15 | 武田薬品工業株式会社 | アミノフェニルプロパン酸誘導体 |
| JP4859665B2 (ja) | 2004-03-30 | 2012-01-25 | 武田薬品工業株式会社 | アルコキシフェニルプロパン酸誘導体 |
| TWI396686B (zh) | 2004-05-21 | 2013-05-21 | Takeda Pharmaceutical | 環狀醯胺衍生物、以及其製品和用法 |
| WO2006112549A1 (ja) | 2005-04-20 | 2006-10-26 | Takeda Pharmaceutical Company Limited | 縮合複素環化合物 |
| US8153694B2 (en) | 2005-07-29 | 2012-04-10 | Takeda Pharmaceutical Company Limited | Cyclopropanecarboxylic acid compound |
| JPWO2007013694A1 (ja) | 2005-07-29 | 2009-02-12 | 武田薬品工業株式会社 | フェノキシアルカン酸化合物 |
| RU2008108984A (ru) | 2005-08-10 | 2009-09-20 | Такеда Фармасьютикал Компани Лимитед (Jp) | Терапевтический агент от диабета |
| JP2007063225A (ja) | 2005-09-01 | 2007-03-15 | Takeda Chem Ind Ltd | イミダゾピリジン化合物 |
| US7732626B2 (en) | 2006-06-27 | 2010-06-08 | Takeda Pharmaceutical Company Limited | Fused cyclic compounds |
| WO2008047821A1 (en) | 2006-10-18 | 2008-04-24 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound |
| CN101573357B (zh) | 2006-10-19 | 2013-01-23 | 武田药品工业株式会社 | 吲哚化合物 |
| WO2008093639A1 (ja) | 2007-01-29 | 2008-08-07 | Takeda Pharmaceutical Company Limited | ピラゾール化合物 |
| MX2009008103A (es) | 2007-02-09 | 2009-08-18 | Takeda Pharmaceutical | Compuestos anulares fusionados como agonistas parciales de prar-gamma. |
| US8318746B2 (en) | 2007-04-27 | 2012-11-27 | Takeda Pharmaceutical Company Limited | Nitrogen-containing five-membered heterocyclic compound |
| WO2008156757A1 (en) | 2007-06-19 | 2008-12-24 | Takeda Pharmaceutical Company Limited | Indazole compounds for activating glucokinase |
| WO2011071048A1 (ja) * | 2009-12-07 | 2011-06-16 | 味の素株式会社 | ヘテロアリールカルボン酸エステル誘導体 |
| US9346776B2 (en) | 2014-02-13 | 2016-05-24 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound |
| US9428470B2 (en) * | 2014-02-13 | 2016-08-30 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| WO2016104630A1 (ja) * | 2014-12-26 | 2016-06-30 | 武田薬品工業株式会社 | 縮合複素環化合物 |
| WO2016158788A1 (ja) * | 2015-03-27 | 2016-10-06 | 武田薬品工業株式会社 | 縮合複素環化合物 |
| JPWO2019088270A1 (ja) * | 2017-11-02 | 2020-12-03 | 宇部興産株式会社 | 蛋白分解酵素の双頭型阻害剤 |
-
2019
- 2019-08-26 US US16/641,971 patent/US20210403420A1/en not_active Abandoned
- 2019-08-26 JP JP2020506388A patent/JP6773938B2/ja not_active Expired - Fee Related
- 2019-08-26 AR ARP190102423A patent/AR116019A1/es unknown
- 2019-08-26 TW TW108130417A patent/TW202024028A/zh unknown
- 2019-08-26 WO PCT/JP2019/033215 patent/WO2020045326A1/ja not_active Ceased
- 2019-08-26 EP EP19842579.5A patent/EP3650440A4/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| US20210403420A1 (en) | 2021-12-30 |
| EP3650440A4 (en) | 2020-11-25 |
| WO2020045326A1 (ja) | 2020-03-05 |
| JP6773938B2 (ja) | 2020-10-21 |
| TW202024028A (zh) | 2020-07-01 |
| JPWO2020045326A1 (ja) | 2020-09-24 |
| EP3650440A1 (en) | 2020-05-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |