PE20211496A1 - Nuevo compuesto que presenta actividad inhibidora de enteropeptidasa - Google Patents
Nuevo compuesto que presenta actividad inhibidora de enteropeptidasaInfo
- Publication number
- PE20211496A1 PE20211496A1 PE2020001822A PE2020001822A PE20211496A1 PE 20211496 A1 PE20211496 A1 PE 20211496A1 PE 2020001822 A PE2020001822 A PE 2020001822A PE 2020001822 A PE2020001822 A PE 2020001822A PE 20211496 A1 PE20211496 A1 PE 20211496A1
- Authority
- PE
- Peru
- Prior art keywords
- unsubstituted
- compounds
- independently
- substituted alkyl
- substituted
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 229940122632 Enteropeptidase inhibitor Drugs 0.000 title 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 3
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical group NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 abstract 2
- 230000003287 optical effect Effects 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 1
- 108010013369 Enteropeptidase Proteins 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Chemical group CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 150000003973 alkyl amines Chemical class 0.000 abstract 1
- 150000001408 amides Chemical group 0.000 abstract 1
- 150000001409 amidines Chemical group 0.000 abstract 1
- 150000001720 carbohydrates Chemical class 0.000 abstract 1
- 235000014633 carbohydrates Nutrition 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 230000001079 digestive effect Effects 0.000 abstract 1
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Chemical group CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 abstract 1
- 230000002496 gastric effect Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic 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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
- C07D277/82—Nitrogen atoms
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Diabetes (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)
- Hematology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
La presente invencion se refiere a compuestos de formula quimica 1, un isomero optico, o sal farmaceuticamente aceptable de los mismos; donde Het es un grupo mono o diheterociclico de 4 a 10 miembros que tiene uno o dos heteroatomos seleccionados del grupo que consiste en N, O y S; una linea de puntos representa la presencia o ausencia de un enlace, A1, A2, A3, A4 y A5 son cada uno independientemente C o N; Q es O o N; R1 y R6 son cada uno independientemente H, un alquilo no sustituido o sustituido, o R1 y R6 junto con el atomo de nitrogeno al que estan unidos forman un anillo heterociclico de 5 a 7 miembros no sustituido o sustituido; R2 es hidrogeno o un alquilo no sustituido o sustituido; R3 y R4 son cada uno independientemente H, halogeno o un alquilo no sustituido o sustituido; y R5 es amidina, guanidina, amida, o una alquilamina no sustituida o sustituida. La invencion tambien se refiere a composiciones farmaceuticas que comprenden los compuestos de formula quimica 1, el isomero optico o la sal farmaceuticamente aceptable de los mismos. Los compuestos de la presente invencion muestran actividad inhibitoria de la enzima enteropeptidasa, actuando a nivel gastrointestinal, por lo cual reduce la capacidad digestiva de proteinas, lipidos e hidratos de carbono siendo util para prevenir y tratar enfermedades metabolicas tales como obesidad, diabetes mellitus o hiperlipidemia, entre otras.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20180053315 | 2018-05-09 | ||
| KR20180053316 | 2018-05-09 | ||
| PCT/KR2019/005997 WO2019216742A1 (ko) | 2018-05-09 | 2019-05-08 | 엔테로펩디아제 억제 활성을 나타내는 신규 화합물 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211496A1 true PE20211496A1 (es) | 2021-08-11 |
Family
ID=68468129
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2020001822A PE20211496A1 (es) | 2018-05-09 | 2019-05-08 | Nuevo compuesto que presenta actividad inhibidora de enteropeptidasa |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US11447480B2 (es) |
| EP (1) | EP3778577B1 (es) |
| JP (1) | JP7199774B2 (es) |
| KR (1) | KR102325422B1 (es) |
| CN (1) | CN112105604B (es) |
| AU (1) | AU2019265268C1 (es) |
| BR (1) | BR112020022790A2 (es) |
| CA (1) | CA3099268C (es) |
| CL (1) | CL2020002887A1 (es) |
| CO (1) | CO2020014186A2 (es) |
| DK (1) | DK3778577T3 (es) |
| IL (1) | IL278435B1 (es) |
| JO (1) | JOP20200282A1 (es) |
| MX (1) | MX2020011960A (es) |
| PE (1) | PE20211496A1 (es) |
| PH (1) | PH12020551900A1 (es) |
| RU (1) | RU2768755C1 (es) |
| SG (1) | SG11202011083PA (es) |
| UA (1) | UA126099C2 (es) |
| WO (1) | WO2019216742A1 (es) |
| ZA (1) | ZA202007260B (es) |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9201956D0 (sv) * | 1992-06-25 | 1992-06-25 | Kabi Pharmacia Ab | Novel nicotinicacid esters |
| DE10228132A1 (de) * | 2002-06-24 | 2004-01-22 | Arzneimittelwerk Dresden Gmbh | Amide cyclischer Aminosäuren als PDE 4 Inhibitoren |
| CA2514573A1 (en) * | 2003-01-27 | 2004-08-12 | Astellas Pharma Inc. | Thiazole derivatives and their use as vap-1 inhibitors |
| DE602004028907D1 (de) * | 2003-02-06 | 2010-10-14 | Bristol Myers Squibb Co | Als kinaseinhibitoren geeignete verbindungen auf thiazolylbasis |
| JP4808616B2 (ja) * | 2003-07-30 | 2011-11-02 | ゼノン・ファーマシューティカルズ・インコーポレイテッド | ピリダジン誘導体および治療剤としてのその用途 |
| JP2008528585A (ja) * | 2005-01-26 | 2008-07-31 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| WO2008124393A1 (en) | 2007-04-04 | 2008-10-16 | Irm Llc | Benzothiazole derivatives and their use as protein kinase inhibitors |
| US8304547B2 (en) | 2007-10-24 | 2012-11-06 | Astellas Pharma Inc. | Azolecarboxamide compound or salt thereof |
| CA2728095A1 (en) | 2008-07-17 | 2010-01-21 | Asahi Kasei Pharma Corporation | Pyrazole-containing tricyclic compounds as antagonists of an ep1 receptor |
| 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 |
| JP5959116B2 (ja) | 2011-06-07 | 2016-08-02 | Ｅａファーマ株式会社 | ヘテロ環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 |
| JP6634070B2 (ja) * | 2015-03-27 | 2020-01-22 | 武田薬品工業株式会社 | 縮合複素環化合物 |
| ES2903528T3 (es) * | 2016-10-10 | 2022-04-04 | Dong A Socio Holdings Co Ltd | Compuestos de heteroarilo y su uso como inhibidores de MER |
-
2019
- 2019-05-08 UA UAA202007104A patent/UA126099C2/uk unknown
- 2019-05-08 EP EP19800582.9A patent/EP3778577B1/en active Active
- 2019-05-08 CN CN201980031203.8A patent/CN112105604B/zh active Active
- 2019-05-08 DK DK19800582.9T patent/DK3778577T3/da active
- 2019-05-08 PE PE2020001822A patent/PE20211496A1/es unknown
- 2019-05-08 SG SG11202011083PA patent/SG11202011083PA/en unknown
- 2019-05-08 JP JP2020562707A patent/JP7199774B2/ja active Active
- 2019-05-08 WO PCT/KR2019/005997 patent/WO2019216742A1/ko unknown
- 2019-05-08 US US17/054,084 patent/US11447480B2/en active Active
- 2019-05-08 MX MX2020011960A patent/MX2020011960A/es unknown
- 2019-05-08 JO JOP/2020/0282A patent/JOP20200282A1/ar unknown
- 2019-05-08 BR BR112020022790-0A patent/BR112020022790A2/pt active Search and Examination
- 2019-05-08 CA CA3099268A patent/CA3099268C/en active Active
- 2019-05-08 AU AU2019265268A patent/AU2019265268C1/en active Active
- 2019-05-08 IL IL278435A patent/IL278435B1/en unknown
- 2019-05-08 RU RU2020136431A patent/RU2768755C1/ru active
- 2019-05-08 KR KR1020190053818A patent/KR102325422B1/ko active IP Right Grant
-
2020
- 2020-11-06 CL CL2020002887A patent/CL2020002887A1/es unknown
- 2020-11-09 PH PH12020551900A patent/PH12020551900A1/en unknown
- 2020-11-12 CO CONC2020/0014186A patent/CO2020014186A2/es unknown
- 2020-11-20 ZA ZA2020/07260A patent/ZA202007260B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2019216742A1 (ko) | 2019-11-14 |
| ZA202007260B (en) | 2022-07-27 |
| MX2020011960A (es) | 2021-01-15 |
| CN112105604B (zh) | 2024-01-09 |
| AU2019265268A1 (en) | 2020-12-17 |
| AU2019265268C1 (en) | 2022-08-04 |
| UA126099C2 (uk) | 2022-08-10 |
| CA3099268C (en) | 2023-03-07 |
| CL2020002887A1 (es) | 2021-05-14 |
| EP3778577A1 (en) | 2021-02-17 |
| KR20190129009A (ko) | 2019-11-19 |
| US11447480B2 (en) | 2022-09-20 |
| IL278435A (es) | 2021-03-01 |
| AU2019265268B2 (en) | 2022-04-28 |
| JP7199774B2 (ja) | 2023-01-06 |
| EP3778577B1 (en) | 2023-08-30 |
| EP3778577A4 (en) | 2021-03-31 |
| IL278435B1 (en) | 2024-02-01 |
| CN112105604A (zh) | 2020-12-18 |
| KR102325422B1 (ko) | 2021-11-11 |
| JP2021521260A (ja) | 2021-08-26 |
| JOP20200282A1 (ar) | 2020-11-08 |
| SG11202011083PA (en) | 2020-12-30 |
| DK3778577T3 (da) | 2023-09-25 |
| US20210284634A1 (en) | 2021-09-16 |
| CO2020014186A2 (es) | 2020-11-30 |
| PH12020551900A1 (en) | 2021-05-31 |
| RU2768755C1 (ru) | 2022-03-24 |
| CA3099268A1 (en) | 2019-11-14 |
| BR112020022790A2 (pt) | 2021-02-02 |
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