JOP20200282A1 - مركب جديد ينطوي على نشاط مثبط للإنتيروببتيداز - Google Patents
مركب جديد ينطوي على نشاط مثبط للإنتيروببتيدازInfo
- Publication number
- JOP20200282A1 JOP20200282A1 JOP/2020/0282A JOP20200282A JOP20200282A1 JO P20200282 A1 JOP20200282 A1 JO P20200282A1 JO P20200282 A JOP20200282 A JO P20200282A JO P20200282 A1 JOP20200282 A1 JO P20200282A1
- Authority
- JO
- Jordan
- Prior art keywords
- novel compound
- inhibitory activity
- enteropeptidase
- compound
- compound exhibiting
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 102100029727 Enteropeptidase Human genes 0.000 title abstract 3
- 108010013369 Enteropeptidase Proteins 0.000 title abstract 3
- 230000002401 inhibitory effect Effects 0.000 title abstract 3
- 230000001747 exhibiting effect Effects 0.000 title abstract 2
- 208000030159 metabolic disease Diseases 0.000 abstract 3
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 2
- 208000008589 Obesity Diseases 0.000 abstract 2
- 206010012601 diabetes mellitus Diseases 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 235000020824 obesity Nutrition 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 208000016097 disease of metabolism Diseases 0.000 abstract 1
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229940043274 prophylactic drug Drugs 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 229940126585 therapeutic drug Drugs 0.000 abstract 1
- 230000001225 therapeutic effect Effects 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)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
يتعلق الاختراع الحالي بمركب جديد ينطوي على نشاط مثبط للإنتيروببتيداز، وملح مقبول صيدلانيًا منه، وتركيبة صيدلانية للوقاية من الأمراض الأيضية وعلاجها مثل السمنة أو داء السكري أو فرط دهون الدم أو ما إلى ذلك، والتي تشتمل على المركب أو الملح المقبول صيدلانيًا، وطريقة للوقاية من المرض الأيضي أو علاجه باستخدام المركب الجديد المشار إليه أعلاه. ينطوي المركب وفقًا للاختراع الحالي على نشاط تثبيطي ممتاز ضد الإنتيروببتيداز، وبالتالي لا يتم امتصاصه في الجسم، ولكن يتم إخراجه خارج الجسم. مع ذلك، نظرًا لأنه لا يتم تفريغ الدهون فحسب بل والبروتينات أيضًا، فإنه ينطوي على آثار جانبية طفيفة مثل البراز الدهني، ولا يظهر أثره إلا في السبيل المعوي، ومن ثم ينطوي على القليل من الآثار الجانبية مثل الاكتئاب، كما أنه مفيد للغاية كعقار علاجي أو وقائي لمختلف الأمراض الأيضية مثل السمنة وداء السكري وفرط دهون الدم.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20180053316 | 2018-05-09 | ||
| KR20180053315 | 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 |
|---|---|
| JOP20200282A1 true JOP20200282A1 (ar) | 2020-11-08 |
Family
ID=68468129
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2020/0282A JOP20200282A1 (ar) | 2018-05-09 | 2019-05-08 | مركب جديد ينطوي على نشاط مثبط للإنتيروببتيداز |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US11447480B2 (ar) |
| EP (1) | EP3778577B1 (ar) |
| JP (1) | JP7199774B2 (ar) |
| KR (1) | KR102325422B1 (ar) |
| CN (1) | CN112105604B (ar) |
| AU (1) | AU2019265268C1 (ar) |
| BR (1) | BR112020022790A2 (ar) |
| CA (1) | CA3099268C (ar) |
| CL (1) | CL2020002887A1 (ar) |
| CO (1) | CO2020014186A2 (ar) |
| DK (1) | DK3778577T3 (ar) |
| IL (1) | IL278435B1 (ar) |
| JO (1) | JOP20200282A1 (ar) |
| MX (1) | MX2020011960A (ar) |
| PE (1) | PE20211496A1 (ar) |
| PH (1) | PH12020551900A1 (ar) |
| RU (1) | RU2768755C1 (ar) |
| SG (1) | SG11202011083PA (ar) |
| UA (1) | UA126099C2 (ar) |
| WO (1) | WO2019216742A1 (ar) |
| ZA (1) | ZA202007260B (ar) |
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 |
| US7335658B2 (en) * | 2003-07-30 | 2008-02-26 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives and their use as therapeutic agents |
| WO2006081172A2 (en) * | 2005-01-26 | 2006-08-03 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| WO2008124393A1 (en) | 2007-04-04 | 2008-10-16 | Irm Llc | Benzothiazole derivatives and their use as protein kinase inhibitors |
| EP2206707B1 (en) * | 2007-10-24 | 2014-07-23 | Astellas Pharma Inc. | Azolecarboxamide compound or salt thereof |
| JPWO2010007943A1 (ja) | 2008-07-17 | 2012-01-05 | 旭化成ファーマ株式会社 | 含窒素複素環化合物 |
| ES2532201T3 (es) * | 2009-12-07 | 2015-03-25 | Ajinomoto Co., Inc. | Derivado de éster de ácido heteroarilcarboxílico |
| 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 |
| JPWO2016104630A1 (ja) | 2014-12-26 | 2017-10-05 | 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 |
| US10913730B2 (en) * | 2016-10-10 | 2021-02-09 | Dong-A Socio Holdings Co., Ltd. | Heteroaryl compounds and their use as Mer inhibitors |
-
2019
- 2019-05-08 UA UAA202007104A patent/UA126099C2/uk unknown
- 2019-05-08 JP JP2020562707A patent/JP7199774B2/ja active Active
- 2019-05-08 DK DK19800582.9T patent/DK3778577T3/da active
- 2019-05-08 IL IL278435A patent/IL278435B1/en unknown
- 2019-05-08 WO PCT/KR2019/005997 patent/WO2019216742A1/ko unknown
- 2019-05-08 CA CA3099268A patent/CA3099268C/en active Active
- 2019-05-08 JO JOP/2020/0282A patent/JOP20200282A1/ar unknown
- 2019-05-08 EP EP19800582.9A patent/EP3778577B1/en active Active
- 2019-05-08 AU AU2019265268A patent/AU2019265268C1/en active Active
- 2019-05-08 KR KR1020190053818A patent/KR102325422B1/ko active IP Right Grant
- 2019-05-08 CN CN201980031203.8A patent/CN112105604B/zh active Active
- 2019-05-08 RU RU2020136431A patent/RU2768755C1/ru active
- 2019-05-08 US US17/054,084 patent/US11447480B2/en active Active
- 2019-05-08 MX MX2020011960A patent/MX2020011960A/es unknown
- 2019-05-08 SG SG11202011083PA patent/SG11202011083PA/en unknown
- 2019-05-08 BR BR112020022790-0A patent/BR112020022790A2/pt active Search and Examination
- 2019-05-08 PE PE2020001822A patent/PE20211496A1/es unknown
-
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 |
|---|---|
| PH12020551900A1 (en) | 2021-05-31 |
| CL2020002887A1 (es) | 2021-05-14 |
| WO2019216742A1 (ko) | 2019-11-14 |
| PE20211496A1 (es) | 2021-08-11 |
| IL278435A (ar) | 2021-03-01 |
| KR102325422B1 (ko) | 2021-11-11 |
| MX2020011960A (es) | 2021-01-15 |
| AU2019265268C1 (en) | 2022-08-04 |
| CN112105604B (zh) | 2024-01-09 |
| JP7199774B2 (ja) | 2023-01-06 |
| EP3778577A4 (en) | 2021-03-31 |
| BR112020022790A2 (pt) | 2021-02-02 |
| JP2021521260A (ja) | 2021-08-26 |
| AU2019265268B2 (en) | 2022-04-28 |
| EP3778577B1 (en) | 2023-08-30 |
| CA3099268C (en) | 2023-03-07 |
| SG11202011083PA (en) | 2020-12-30 |
| CN112105604A (zh) | 2020-12-18 |
| KR20190129009A (ko) | 2019-11-19 |
| US11447480B2 (en) | 2022-09-20 |
| ZA202007260B (en) | 2022-07-27 |
| IL278435B1 (en) | 2024-02-01 |
| DK3778577T3 (da) | 2023-09-25 |
| US20210284634A1 (en) | 2021-09-16 |
| CA3099268A1 (en) | 2019-11-14 |
| EP3778577A1 (en) | 2021-02-17 |
| AU2019265268A1 (en) | 2020-12-17 |
| CO2020014186A2 (es) | 2020-11-30 |
| RU2768755C1 (ru) | 2022-03-24 |
| UA126099C2 (uk) | 2022-08-10 |
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