AR081178A1 - Derivados de heterociclos de nitrogeno, la preparacion y la aplicacion de los mismos en terapias de enfermedades mediadas por la inhibicion de scd-1. - Google Patents
Derivados de heterociclos de nitrogeno, la preparacion y la aplicacion de los mismos en terapias de enfermedades mediadas por la inhibicion de scd-1.Info
- Publication number
- AR081178A1 AR081178A1 ARP110101348A ARP110101348A AR081178A1 AR 081178 A1 AR081178 A1 AR 081178A1 AR P110101348 A ARP110101348 A AR P110101348A AR P110101348 A ARP110101348 A AR P110101348A AR 081178 A1 AR081178 A1 AR 081178A1
- Authority
- AR
- Argentina
- Prior art keywords
- phenyl
- triazine
- trifluoromethyl
- fluoro
- branched
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
- C07D241/18—Oxygen or sulfur atoms
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
- C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
- C07D253/06—1,2,4-Triazines
- C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
- C07D253/07—1,2,4-Triazines having 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se proveen además, un método para su preparación, composiciones farmacéuticas que los contienen y su uso para el tratamiento de enfermedades mediadas por la inhibición de la enzima SCD-1. Reivindicación 1: Compuestos que tienen la fórmula general 1 en la cual R1 representa uno o una pluralidad de grupos tales como: trifluorometilo, halógeno tal como F, CI, Br, nitro, alquilo C1-4 de cadena recta o ramificada, trifluorometoxi, acetilo; A representa un grupo de fórmula (2) en la cual si n=m=1, X representa -CH2- o -CH Me-, E representa CH, y D representa oxígeno o -NH-, o E representa nitrógeno, y D representa C=Q o CH2; si n=m=0, X representa -CH2- y E representa -CH-, D representa -OCH2-, si n=1 y m=0, X representa -CH2- y E representa -CH-, D representa oxígeno, o A representa un grupo de fórmula (3); R representa nitrógeno; T-U representa C=C, V representa N, W representa C=O, R2 representa Br, CI o H, R3=H y R4 representa un alquilo C1-7 de cadena recta o ramificada o radical alquenilo, o, T-U representa N=C, V-W representa C=N, R2 no representa un sustituyente, en donde R3=H y R4 representa hidrógeno o un metilo o un fenilo, opcionalmente sustituido por uno o una pluralidad de grupos tales como trifluorometilo, OMe, metilo o halógeno tal como F, CI, Br excluyendo los compuestos 3-[4-(3-fluoro-bencil)-piperazin-1-il]-5-(4-trifluorometil-fenil)-[1,2,4]triazina, 3-[4-(3-Cloro-fenoxi)-piperidin-1-il]-5-(4-fluoro-fenil )- [1,2,4]triazina, 3-[4-(4-fluoro-fenoxi)-piperidin-1-il]-5-(4-fluoro-fenil)-[1,2,4]triazina, 5-(2,6-Dimetoxi-fenil)-3-(4-m-toliloxi-piperidin-1-il)-[1,2,4]triazina, o R3=Me y R4 representa hidrógeno o un metilo o un fenilo, opcionalmente sustituido por uno o una pluralidad de grupos tales como trifluorometilo, OMe, halógeno tal como F, CI, Br o metilo, o R3 y R4 simultáneamente representan fenilo o furano o piridilo, o R3 y R4 representan -(CH2)4-, o R representa C; T-U representa C=N, V representa N, W representa C=O, R2=H, R3 no representa un sustituyente y R4 representa un alquilo C1-7 de cadena recta o ramificada o radical alquenilo, o TR2 representa C=O, U representa N, R3 representa un alquilo C1-7 de cadena recta o ramificada o radical alquenilo, V-W representa N=CH, R4 no representa un sustituyente, junto con los diversos isómeros y mezclas de los mismos en cualquiera de las proporciones, y las sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR1052943A FR2958935B1 (fr) | 2010-04-19 | 2010-04-19 | Derives d'heterocycles azotes, leur preparation et leur application en therapeutique humaine |
Publications (1)
Publication Number | Publication Date |
---|---|
AR081178A1 true AR081178A1 (es) | 2012-07-04 |
Family
ID=42651470
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110101348A AR081178A1 (es) | 2010-04-19 | 2011-04-19 | Derivados de heterociclos de nitrogeno, la preparacion y la aplicacion de los mismos en terapias de enfermedades mediadas por la inhibicion de scd-1. |
Country Status (6)
Country | Link |
---|---|
US (1) | US8962837B2 (es) |
EP (1) | EP2560963B1 (es) |
AR (1) | AR081178A1 (es) |
FR (1) | FR2958935B1 (es) |
TW (1) | TW201202213A (es) |
WO (1) | WO2011131593A1 (es) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2997024B1 (en) * | 2013-05-17 | 2018-03-28 | Boehringer Ingelheim International GmbH | Pyrrolidine derivatives, pharmaceutical compositions and uses thereof |
MY176401A (en) | 2014-04-24 | 2020-08-05 | Mitsubishi Tanabe Pharma Corp | Novel disubstituted 1,2,4-triazine compound |
US11970486B2 (en) | 2016-10-24 | 2024-04-30 | Janssen Pharmaceutica Nv | Compounds and uses thereof |
EP3566055A4 (en) | 2017-01-06 | 2020-12-02 | Yumanity Therapeutics, Inc. | TREATMENT METHODS FOR NEUROLOGICAL DISORDERS |
EP3700934A4 (en) | 2017-10-24 | 2021-10-27 | Yumanity Therapeutics, Inc. | COMPOUNDS AND USES OF THESE COMPOUNDS |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7759348B2 (en) | 2003-07-30 | 2010-07-20 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives and their use as therapeutic agents |
CA2664849A1 (en) * | 2006-10-20 | 2008-04-24 | Merck Frosst Canada Ltd. | Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
AR064965A1 (es) * | 2007-01-26 | 2009-05-06 | Merck Frosst Canada Inc | Derivados de azacicloalcanos como inhibidores de estearoil - coenzima a delta -9 desaturasa |
US8242286B2 (en) * | 2007-08-08 | 2012-08-14 | Medicis Pharmaceutical Corporation | Phenoxy-pyrrolidine derivative and its use and compositions |
FR2933979B1 (fr) | 2008-07-15 | 2012-08-24 | Pf Medicament | Derives de triazines et uraciles, leur preparation et leur application en therapeutique humaine |
-
2010
- 2010-04-19 FR FR1052943A patent/FR2958935B1/fr active Active
-
2011
- 2011-04-15 EP EP11714629.0A patent/EP2560963B1/fr active Active
- 2011-04-15 US US13/642,025 patent/US8962837B2/en active Active
- 2011-04-15 WO PCT/EP2011/056066 patent/WO2011131593A1/fr active Application Filing
- 2011-04-18 TW TW100113367A patent/TW201202213A/zh unknown
- 2011-04-19 AR ARP110101348A patent/AR081178A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
EP2560963A1 (fr) | 2013-02-27 |
FR2958935A1 (fr) | 2011-10-21 |
WO2011131593A1 (fr) | 2011-10-27 |
EP2560963B1 (fr) | 2016-10-05 |
FR2958935B1 (fr) | 2012-06-22 |
US20130040928A1 (en) | 2013-02-14 |
US8962837B2 (en) | 2015-02-24 |
TW201202213A (en) | 2012-01-16 |
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