AR046297A1 - DPP INHIBITORS - IV METHODS TO PREPARE THEM AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AS ACTIVE AGENTS - Google Patents
DPP INHIBITORS - IV METHODS TO PREPARE THEM AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AS ACTIVE AGENTSInfo
- Publication number
- AR046297A1 AR046297A1 ARP040103780A ARP040103780A AR046297A1 AR 046297 A1 AR046297 A1 AR 046297A1 AR P040103780 A ARP040103780 A AR P040103780A AR P040103780 A ARP040103780 A AR P040103780A AR 046297 A1 AR046297 A1 AR 046297A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- pharmaceutical compositions
- methods
- active agents
- independently
- Prior art date
Links
- 239000013543 active substance Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000004417 unsaturated alkyl group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 abstract 1
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 231100000252 nontoxic Toxicity 0.000 abstract 1
- 230000003000 nontoxic effect Effects 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- 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
- C07D417/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/06—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 only aliphatic carbon atoms
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K31/4245—Oxadiazoles
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Diabetes (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente se refiere a compuestos a base de pirrolidina que presentan actividad inhibitoria de la dipeptidilpeptidasa-IV, métodos para prepararlos y composiciones farmacéuticas que los contienen como agentes activos. Reivindicación 1: Un compuesto a base de pirrolidina de fórmula (1) donde: A es un sustituyente seleccionado del grupo de fórmulas (2), donde, R4 es cada uno independientemente H, alquilo opcionalmente sustituido lineal, ramificado o cíclico, saturado o insaturado, un anillo aromático o heteroaromático opcionalmente sustituido, o heterociclo opcionalmente sustituido, y X es O ó S; B es un compuesto de fórmula (3) donde R5 y R6 son cada uno independientemente H, alquilo opcionalmente sustituido lineal, ramificado o cíclico, saturado o insaturado; anillo aromático o heteroaromático opcionalmente sustituido, heterociclo opcionalmente sustituido; o R5 y R6 juntos se unen para formar un ciclo o heterociclo opcionalmente sustituido; n es 0, 1 ó 2; R3 es H, o alquilo C1-4; Y es C, O ó S; con la condición que Y es C, R1 y R2 son cada uno independientemente H o halógeno, y donde Y es O ó S, R1 y R2 no se encuentran presentes, o una sal no tóxica farmacéuticamente aceptable, éster fisiológicamente hidrolizable, hidrato, solvato, isómero o profármaco de los mismos.This refers to pyrrolidine-based compounds that have dipeptidylpeptidase-IV inhibitory activity, methods for preparing them and pharmaceutical compositions containing them as active agents. Claim 1: A pyrrolidine-based compound of formula (1) wherein: A is a substituent selected from the group of formulas (2), wherein, R 4 is each independently H, optionally substituted linear, branched or cyclic, saturated or unsaturated alkyl , an optionally substituted aromatic or heteroaromatic ring, or optionally substituted heterocycle, and X is O or S; B is a compound of formula (3) wherein R5 and R6 are each independently H, optionally substituted linear, branched or cyclic, saturated or unsaturated alkyl; optionally substituted aromatic or heteroaromatic ring, optionally substituted heterocycle; or R5 and R6 together to form an optionally substituted cycle or heterocycle; n is 0, 1 or 2; R3 is H, or C1-4 alkyl; Y is C, O or S; with the proviso that Y is C, R1 and R2 are each independently H or halogen, and where Y is O or S, R1 and R2 are not present, or a pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate, solvate , isomer or prodrug thereof.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20030072977 | 2003-10-20 | ||
| KR20030072962 | 2003-10-20 | ||
| KR20040036439 | 2004-05-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR046297A1 true AR046297A1 (en) | 2005-11-30 |
Family
ID=34468332
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040103780A AR046297A1 (en) | 2003-10-20 | 2004-10-19 | DPP INHIBITORS - IV METHODS TO PREPARE THEM AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AS ACTIVE AGENTS |
Country Status (4)
| Country | Link |
|---|---|
| KR (1) | KR20050037973A (en) |
| AR (1) | AR046297A1 (en) |
| TW (1) | TW200519105A (en) |
| WO (1) | WO2005037828A1 (en) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DOP2006000008A (en) | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | COMBINED THERAPY FOR THE TREATMENT OF DIABETES AND RELATED AFFECTIONS AND FOR THE TREATMENT OF AFFECTIONS THAT IMPROVE THROUGH AN INCREASE IN THE BLOOD CONCENTRATION OF GLP-1 |
| WO2006090244A1 (en) * | 2005-02-22 | 2006-08-31 | Glenmark Pharmaceuticals S.A. | New adamantane derivatives as dipeptidyl, peptidase iv inhibitors, processes for their preparation, and pharmaceutical compositions containing them |
| GB0515323D0 (en) | 2005-07-26 | 2005-08-31 | Electrophoretics Ltd | Mass labels |
| GB0526291D0 (en) | 2005-12-23 | 2006-02-01 | Prosidion Ltd | Therapeutic method |
| PE20071221A1 (en) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | GPR119 RECEPTOR AGONISTS IN METHODS TO INCREASE BONE MASS AND TO TREAT OSTEOPOROSIS AND OTHER CONDITIONS CHARACTERIZED BY LOW BONE MASS, AND COMBINED THERAPY RELATED TO THESE AGONISTS |
| KR20090004950A (en) | 2006-04-12 | 2009-01-12 | 프로비오드룩 아게 | Enzyme inhibitor |
| WO2008055945A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| ATE554085T1 (en) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | NEW INHIBITORS OF GLUTAMINYL CYCLASE |
| EP2143443B1 (en) | 2007-04-03 | 2014-11-19 | Mitsubishi Tanabe Pharma Corporation | A combination of dipeptidyl peptidase iv inhibitor and sweetener for use in the treatment of obesity |
| JP5667440B2 (en) | 2007-04-18 | 2015-02-12 | プロビオドルグ エージー | Thiourea derivatives as glutaminyl cyclase inhibitors |
| EP2025674A1 (en) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituted tetra hydro naphthalines, method for their manufacture and their use as drugs |
| US8338450B2 (en) | 2007-09-21 | 2012-12-25 | Lupin Limited | Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors |
| CL2008003653A1 (en) | 2008-01-17 | 2010-03-05 | Mitsubishi Tanabe Pharma Corp | Use of a glucopyranosyl-derived sglt inhibitor and a selected dppiv inhibitor to treat diabetes; and pharmaceutical composition. |
| EP2146210A1 (en) | 2008-04-07 | 2010-01-20 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY |
| ES2653563T3 (en) * | 2009-01-09 | 2018-02-07 | Orchid Pharma Limited | Dipeptidyl peptidases IV inhibitors |
| GB2483614B (en) | 2009-06-18 | 2014-12-03 | Lupin Ltd | 2-Amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo- ethanoyl derivatives as potent dpp-iv inhibitors |
| AR077642A1 (en) | 2009-07-09 | 2011-09-14 | Arena Pharm Inc | METABOLISM MODULATORS AND THE TREATMENT OF DISORDERS RELATED TO THE SAME |
| CN102695546B (en) | 2009-09-11 | 2014-09-10 | 前体生物药物股份公司 | Heterocylcic derivatives as inhibitors of glutaminyl cyclase |
| WO2011107494A1 (en) | 2010-03-03 | 2011-09-09 | Sanofi | Novel aromatic glycoside derivatives, medicaments containing said compounds, and the use thereof |
| US9181233B2 (en) | 2010-03-03 | 2015-11-10 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| US8269019B2 (en) | 2010-03-10 | 2012-09-18 | Probiodrug Ag | Inhibitors |
| JP2013523819A (en) | 2010-04-06 | 2013-06-17 | アリーナ ファーマシューティカルズ， インコーポレイテッド | GPR119 receptor modulators and treatment of disorders related thereto |
| JP5945532B2 (en) | 2010-04-21 | 2016-07-05 | プロビオドルグ エージー | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| WO2011157827A1 (en) | 2010-06-18 | 2011-12-22 | Sanofi | Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| EP2619198A1 (en) | 2010-09-22 | 2013-07-31 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| EP2766349B1 (en) | 2011-03-08 | 2016-06-01 | Sanofi | Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof |
| US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| WO2012120055A1 (en) | 2011-03-08 | 2012-09-13 | Sanofi | Di- and tri-substituted oxathiazine derivates, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| WO2012120056A1 (en) | 2011-03-08 | 2012-09-13 | Sanofi | Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof |
| US8530670B2 (en) | 2011-03-16 | 2013-09-10 | Probiodrug Ag | Inhibitors |
| US20140018371A1 (en) | 2011-04-01 | 2014-01-16 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| US20140066369A1 (en) | 2011-04-19 | 2014-03-06 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| WO2012145603A1 (en) | 2011-04-22 | 2012-10-26 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| US20140051714A1 (en) | 2011-04-22 | 2014-02-20 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| WO2012170702A1 (en) | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013055910A1 (en) | 2011-10-12 | 2013-04-18 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2014064215A1 (en) | 2012-10-24 | 2014-05-01 | INSERM (Institut National de la Santé et de la Recherche Médicale) | TPL2 KINASE INHIBITORS FOR PREVENTING OR TREATING DIABETES AND FOR PROMOTING β-CELL SURVIVAL |
| WO2014074668A1 (en) | 2012-11-08 | 2014-05-15 | Arena Pharmaceuticals, Inc. | Modulators of gpr119 and the treatment of disorders related thereto |
| EP3267994A4 (en) | 2015-03-09 | 2018-10-31 | Intekrin Therapeutics, Inc. | Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy |
| US10426818B2 (en) | 2015-03-24 | 2019-10-01 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Method and pharmaceutical composition for use in the treatment of diabetes |
| SG11201909046XA (en) | 2017-04-03 | 2019-10-30 | Coherus Biosciences Inc | PPARγ AGONIST FOR TREATMENT OF PROGRESSIVE SUPRANUCLEAR PALSY |
| PL3461819T3 (en) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4126277A1 (en) * | 1991-08-08 | 1993-02-11 | Cassella Ag | HYDANTO DERIVATIVES |
| JP2669579B2 (en) * | 1991-10-23 | 1997-10-29 | エーザイ株式会社 | Oxazolidone derivatives |
| US6159938A (en) * | 1994-11-21 | 2000-12-12 | Cortech, Inc. | Serine protease inhibitors comprising α-keto heterocycles |
| DE69926919D1 (en) * | 1998-12-18 | 2005-09-29 | Bristol Myers Squibb Pharma Co | N-UREIDOALKYLPIPERIDINES AS MODULATORS OF THE ACTIVITY OF CHEMOKIN RECEPTORS |
| CZ20013577A3 (en) * | 1999-04-09 | 2002-07-17 | Basf Aktiengesellschaft | Inhibitors of complement proteases with low molecular weight |
-
2004
- 2004-10-04 TW TW093129981A patent/TW200519105A/en unknown
- 2004-10-19 AR ARP040103780A patent/AR046297A1/en not_active Application Discontinuation
- 2004-10-20 KR KR1020040083793A patent/KR20050037973A/en not_active Ceased
- 2004-10-20 WO PCT/KR2004/002679 patent/WO2005037828A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| TW200519105A (en) | 2005-06-16 |
| WO2005037828A1 (en) | 2005-04-28 |
| KR20050037973A (en) | 2005-04-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |