PE20161396A1 - Compuesto heterociclico - Google Patents
Compuesto heterociclicoInfo
- Publication number
- PE20161396A1 PE20161396A1 PE2016001481A PE2016001481A PE20161396A1 PE 20161396 A1 PE20161396 A1 PE 20161396A1 PE 2016001481 A PE2016001481 A PE 2016001481A PE 2016001481 A PE2016001481 A PE 2016001481A PE 20161396 A1 PE20161396 A1 PE 20161396A1
- Authority
- PE
- Peru
- Prior art keywords
- carbamimidamidobenzoyl
- oxazole
- dihydro
- oxy
- carboxymethyl
- Prior art date
Links
- 150000002391 heterocyclic compounds Chemical class 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- KVQMAUMDMPEQBA-HXUWFJFHSA-N (5R)-5-(carboxymethyl)-3-[3-[4-(diaminomethylideneamino)benzoyl]oxyphenyl]-4H-1,2-oxazole-5-carboxylic acid Chemical compound N(C(=N)N)C1=CC=C(C(=O)OC=2C=C(C=CC2)C2=NO[C@@](C2)(C(=O)O)CC(=O)O)C=C1 KVQMAUMDMPEQBA-HXUWFJFHSA-N 0.000 abstract 1
- KVQMAUMDMPEQBA-FQEVSTJZSA-N (5S)-5-(carboxymethyl)-3-[3-[4-(diaminomethylideneamino)benzoyl]oxyphenyl]-4H-1,2-oxazole-5-carboxylic acid Chemical compound N(C(=N)N)C1=CC=C(C(=O)OC=2C=C(C=CC2)C2=NO[C@](C2)(C(=O)O)CC(=O)O)C=C1 KVQMAUMDMPEQBA-FQEVSTJZSA-N 0.000 abstract 1
- 102100029727 Enteropeptidase Human genes 0.000 abstract 1
- 108010013369 Enteropeptidase Proteins 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 150000001555 benzenes Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- 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
- A61K31/42—Oxazoles
-
- 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- 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
-
- 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
-
- 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
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se refiere a compuestos heterociclicos de formula (I) o sales de los mismos, donde A es un anillo de benceno opcionalmente sustituido; L1 y L2 son enlaces o grupos C1-C3 alquileno lineales opcionalmente sustituidos. Son compuestos preferidos: acido (5R)-3-(3-((4-Carbamimidamidobenzoil) oxi) fenil)-5-(carboximetil)-4,5-dihidro-1,2-oxazol-5-carboxilico; acido (5S)-3-(3-((4-Carbamimidamidobenzoil) oxi) fenil)-5-(carboximetil)-4,5-dihidro-1,2-oxazol-5-carboxilico; entre otros. Dichos compuestos son inhibidores de la enteropeptidasa, siendo utiles en el tratamiento o profilaxis de obesidad, diabetes mellitus, entre otros
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2014025944 | 2014-02-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20161396A1 true PE20161396A1 (es) | 2017-01-10 |
Family
ID=52589730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016001481A PE20161396A1 (es) | 2014-02-13 | 2015-02-12 | Compuesto heterociclico |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US9428470B2 (es) |
| EP (1) | EP3105228B1 (es) |
| JP (1) | JP6458054B2 (es) |
| KR (1) | KR20160113299A (es) |
| CN (1) | CN106170487A (es) |
| AR (1) | AR099399A1 (es) |
| AU (1) | AU2015216439A1 (es) |
| BR (1) | BR112016018548A2 (es) |
| CA (1) | CA2939675A1 (es) |
| CL (1) | CL2016002023A1 (es) |
| CR (1) | CR20160368A (es) |
| EA (1) | EA201691624A1 (es) |
| EC (1) | ECSP16067163A (es) |
| IL (1) | IL247018A0 (es) |
| MA (1) | MA39247B1 (es) |
| MX (1) | MX2016010561A (es) |
| PE (1) | PE20161396A1 (es) |
| PH (1) | PH12016501614A1 (es) |
| SG (1) | SG11201606176YA (es) |
| TW (1) | TW201609677A (es) |
| UY (1) | UY35995A (es) |
| WO (1) | WO2015122188A1 (es) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TR201809418T4 (tr) | 2013-03-13 | 2018-07-23 | Takeda Pharmaceuticals Co | Guanidinobenzoik asit ester bileşiği. |
| PL3104939T3 (pl) | 2014-02-10 | 2024-09-30 | Fred Hutchinson Cancer Center | Leczenie jodkiem sodu zawału serca i urazu niedokrwiennego |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| PH12020552066A1 (en) | 2014-02-13 | 2022-05-11 | Incyte Corp | Cyclopropylamines as lsd1 inhibitors |
| US9346776B2 (en) | 2014-02-13 | 2016-05-24 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound |
| RS59534B1 (sr) | 2014-02-13 | 2019-12-31 | Incyte Corp | Ciklopropilamini kao lsd1 inhibitori |
| US9428470B2 (en) * | 2014-02-13 | 2016-08-30 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| JP2018080109A (ja) * | 2015-03-16 | 2018-05-24 | 武田薬品工業株式会社 | 治療剤 |
| 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 |
| EP3626720A1 (en) | 2015-04-03 | 2020-03-25 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| MX389824B (es) | 2015-08-12 | 2025-03-20 | Incyte Holdings Corp | Sales de un inhibidor de dimetilasa 1 especifica para lisina (lsd1). |
| KR20200075867A (ko) | 2017-11-02 | 2020-06-26 | 우베 고산 가부시키가이샤 | 단백 분해 효소의 쌍두형 저해제 |
| PE20211496A1 (es) | 2018-05-09 | 2021-08-11 | Lg Chemical Ltd | Nuevo compuesto que presenta actividad inhibidora de enteropeptidasa |
| AR116019A1 (es) * | 2018-08-27 | 2021-03-25 | Scohia Pharma Inc | Derivados de guanidinobenzoilo como inhibidores de enteropeptidasa |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| SG11202103984WA (en) * | 2018-10-23 | 2021-05-28 | Japan Science & Tech Agency | PPARd activator |
| US20220281866A1 (en) | 2019-07-19 | 2022-09-08 | Janssen Pharmaceutica Nv | 5,8-disubstituted-[1,2,4]triazolo[1,5-a]pyridinyl and 5,8-disubstituted-imidazo[1,2-a]pyridine derivatives useful as inhibitors of enteropeptidase |
| JP7327788B2 (ja) * | 2019-08-06 | 2023-08-16 | 学校法人福岡大学 | 糖化産物生成抑制剤及び医薬組成物 |
| WO2021137932A1 (en) * | 2019-11-04 | 2021-07-08 | Faraday Pharmaceuticals, Inc. | Use of iodide compounds for the treatment and prevention of chemotherapy-associated cachexia and cardiotoxicity |
| WO2021166899A1 (ja) * | 2020-02-17 | 2021-08-26 | 宇部興産株式会社 | インクレチン様物質と組み合わせて使用するための消化管プロテアーゼ阻害剤を含む薬剤 |
| CN111803652B (zh) * | 2020-08-04 | 2021-09-14 | 南通康是美生物科技有限公司 | 治疗痤疮的化合物在制备治疗痤疮的药物组合物或化妆品组合物中的用途 |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
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| US9428470B2 (en) | 2014-02-13 | 2016-08-30 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| RS59534B1 (sr) | 2014-02-13 | 2019-12-31 | Incyte Corp | Ciklopropilamini kao lsd1 inhibitori |
| PH12020552066A1 (en) | 2014-02-13 | 2022-05-11 | Incyte Corp | Cyclopropylamines as lsd1 inhibitors |
| US9346776B2 (en) | 2014-02-13 | 2016-05-24 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound |
-
2015
- 2015-02-11 US US14/619,464 patent/US9428470B2/en not_active Expired - Fee Related
- 2015-02-12 CA CA2939675A patent/CA2939675A1/en not_active Abandoned
- 2015-02-12 PE PE2016001481A patent/PE20161396A1/es not_active Application Discontinuation
- 2015-02-12 UY UY0001035995A patent/UY35995A/es not_active Application Discontinuation
- 2015-02-12 JP JP2016569124A patent/JP6458054B2/ja not_active Expired - Fee Related
- 2015-02-12 SG SG11201606176YA patent/SG11201606176YA/en unknown
- 2015-02-12 MA MA39247A patent/MA39247B1/fr unknown
- 2015-02-12 EP EP15706547.5A patent/EP3105228B1/en active Active
- 2015-02-12 AR ARP150100410A patent/AR099399A1/es unknown
- 2015-02-12 MX MX2016010561A patent/MX2016010561A/es unknown
- 2015-02-12 BR BR112016018548A patent/BR112016018548A2/pt not_active Application Discontinuation
- 2015-02-12 CN CN201580019434.9A patent/CN106170487A/zh active Pending
- 2015-02-12 EA EA201691624A patent/EA201691624A1/ru unknown
- 2015-02-12 CR CR20160368A patent/CR20160368A/es unknown
- 2015-02-12 KR KR1020167024873A patent/KR20160113299A/ko not_active Withdrawn
- 2015-02-12 US US15/117,539 patent/US10023544B2/en not_active Expired - Fee Related
- 2015-02-12 AU AU2015216439A patent/AU2015216439A1/en not_active Abandoned
- 2015-02-12 TW TW104104692A patent/TW201609677A/zh unknown
- 2015-02-12 WO PCT/JP2015/000640 patent/WO2015122188A1/en not_active Ceased
-
2016
- 2016-07-31 IL IL247018A patent/IL247018A0/en unknown
- 2016-08-10 CL CL2016002023A patent/CL2016002023A1/es unknown
- 2016-08-11 EC ECIEPI201667163A patent/ECSP16067163A/es unknown
- 2016-08-12 PH PH12016501614A patent/PH12016501614A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US10023544B2 (en) | 2018-07-17 |
| AU2015216439A1 (en) | 2016-08-11 |
| MX2016010561A (es) | 2016-11-16 |
| WO2015122188A1 (en) | 2015-08-20 |
| CN106170487A (zh) | 2016-11-30 |
| TW201609677A (zh) | 2016-03-16 |
| EA201691624A1 (ru) | 2017-05-31 |
| SG11201606176YA (en) | 2016-08-30 |
| IL247018A0 (en) | 2016-09-29 |
| AR099399A1 (es) | 2016-07-20 |
| EP3105228A1 (en) | 2016-12-21 |
| US20160347724A1 (en) | 2016-12-01 |
| EP3105228B1 (en) | 2018-09-26 |
| CR20160368A (es) | 2016-12-01 |
| CA2939675A1 (en) | 2015-08-20 |
| BR112016018548A2 (pt) | 2019-01-15 |
| JP6458054B2 (ja) | 2019-01-23 |
| US9428470B2 (en) | 2016-08-30 |
| ECSP16067163A (es) | 2017-10-31 |
| MA39247A1 (fr) | 2017-11-30 |
| MA39247B1 (fr) | 2018-04-30 |
| PH12016501614A1 (en) | 2017-02-06 |
| CL2016002023A1 (es) | 2017-03-24 |
| JP2017505823A (ja) | 2017-02-23 |
| KR20160113299A (ko) | 2016-09-28 |
| UY35995A (es) | 2015-08-31 |
| US20150225354A1 (en) | 2015-08-13 |
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