AR072352A1 - Compuestos de oximetilen arilo y usos de estos - Google Patents
Compuestos de oximetilen arilo y usos de estosInfo
- Publication number
- AR072352A1 AR072352A1 ARP090101153A ARP090101153A AR072352A1 AR 072352 A1 AR072352 A1 AR 072352A1 AR P090101153 A ARP090101153 A AR P090101153A AR P090101153 A ARP090101153 A AR P090101153A AR 072352 A1 AR072352 A1 AR 072352A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- elements
- substituted
- aryl
- Prior art date
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
-
- 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
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
-
- 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- 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
-
- 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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Reivindicacion 1: Un método para tratar la diabetes que comprende la administracion a un paciente que lo necesita de un compuesto de la formula (1) y un inhibidor de DPP IV, en donde, D se elige del grupo que consiste en O, S y NR8; X, Y, y Z se eligen en forma independiente del grupo que consiste en O, N, NR8, S y CR3, y por lo menos uno entre X, Y, y Z es O, N, NR8 o S; J, K, T y U se eligen, cada uno en forma independiente, del grupo que consiste en C, CH y N; el subíndice p es un entero que fluctua entre 0 y 4; el subíndice q es un entero que fluctua entre 0 y 4; R1 es un elemento elegido del grupo que consiste en H, alquilo C1-10, alquilo C1-10 sustituido, cicloalquilo C3-7, alquenilo C2-10, alquinilo C2-10, -X1-CORa, -X1-CO2Ra, -X1-CONRaRb, -SO2Ra, un grupo heterociclo de 4 a 7 elementos, arilo y un grupo heteroarilo de 5 a 10 elementos, en donde cada uno de dichos grupos cicloalquilo, grupo heterociclo, grupo arilo y grupo heteroarilo se sustituye en forma opcional por entre 1 a 4 sustituyentes elegidos en forma independiente entre halo, alquilo C1-10, alquilo C1-10 sustituido, cicloalquilo C3-7, alquenilo C2-10, alquinilo C2-10, arilo, heteroarilo, -CN, -NRaCORb, -NRaCONRaRb, -NO2, -ORa, -NRaRb, -CORa, -CO2Ra, -CONRaRb, -S(O)mRa, NRaS(O)2Rb, y -SO2NRaRb, u opcionalmente Ra y Rb se combinan para formar un anillo de 4, 5 o 6 elementos, y X1 se elige del grupo que consiste en un enlace, alqueno C2-6, alquino C2-6, -C(O)- y -C(O)-(CH2)1-4-, en donde las porciones alifáticas de X1 son opcionalmente sustituidas por uno a tres elementos elegidos entre halogeno, alquilo C1-4, alquilo C1-4 sustituido y haloalquilo C1-4; cada R2 es un elemento elegido en forma independiente del grupo que consiste en halogeno, alquilo C1-5, alquilo C1-5 sustituido, cicloalquilo C3-7, -CORa, -CO2Ra, -CONRaRb, -ORa, -NRaRb, -NRaCORb, -SORaRb, -SO2Ra y -SO2NRaRb, y, en donde cuando el subíndice q es 2 y R2 es alquilo o alquilo sustituido, los dos elementos R2 se pueden ciclar opcionalmente para formar un anillo; R3 es un elemento elegido del grupo que consiste en hidrogeno, halogeno, alquilo C1-4 y haloalquilo C1-4; cada R7 es elegido en forma independiente del grupo que consiste en halo, alquilo C1-10, alquilo C1-10 sustituido, cicloalquilo C3-7, alquenilo C2-10, alquinilo C2-10, -CN, -NO2, -ORa, -NRaRb, -CORa, -CO2Ra, -CONRaRb, -NRaCORb, -NRaCO2Rb, -NRaCONRaRb, -S(O)mRa, -NRaS(O)mRb, -SO2NRaRb, un grupo heterociclo de 4 a 7 elementos, arilo y un grupo heteroarilo de 5 a 10 elementos, en donde cada uno de dichos grupos heterociclos, dichos grupos arilo y heteroarilo son opcionalmente sustituidos por uno a cuatro sustituyentes elegidos en forma independiente entre halo, oxo, alquilo C1-4, haloalquilo C1-4, cicloalquilo C3-7, -CN, -NO2, -ORa, -NRaRb, -CORa, -CO2Ra, -CONRaRb, -NRaCORb, -NRaCO2Rb, -NRaCONRaRb, -S(O)mRa, -NRaSO2Rb y -SO2NRaRb y, en donde el subíndice m es un entero que fluctua entre 0 y 2, u opcionalmente Ra y Rb se combinan para formar un anillo de 4, 4 o 6 elementos; R8 es un elemento elegido en forma independiente del grupo que consiste en hidrogeno, alquilo C1-4 y haloalquilo C1-4; y cada Ra y Rb es elegido en forma independiente del grupo que consiste en hidrogeno, alquilo C1-10, haloalquilo C1-10, cicloalquilo C3-10, heterociclilo, alquenilo C2-10, alquinilo C2-10, arilo, heteroarilo de 5 a 6 elementos y arilalquilo C1-4; y, en donde las porciones alifáticas de cada uno de dichos Ra y Rb se sustituye en forma opcional por entre uno y tres elementos elegidos del grupo que consiste en halo, -ORn, -OCORn, -OC(O)N(Rn)2, -SRn, -S(O)Rn, -S(O)2Rn, -S(O)2N(Rn)2, -NRnS(O)2Rn, -C(O)N(Rn)2, -C(O)Rn, -NRnC(O)Rn, -NRnC(O)N(Rn)2, -CO2Rn, -NRnCO2Rn, -CN, -NO2, -N(Rn)2 y -NRnS(O)2N(Rn)2, en donde cada Rn es, en forma independiente, hidrogeno o un alquilo C1-6 no sustituido; y, en donde las porciones arilo y heteroarilo se sustituyen opcionalmente por entre uno y tres elementos elegidos entre halogeno, -ORm, -OC(O)N(Rm)2, -SRm, -S(O)Rm, -S(O)2Rm, -S(O)2N(Rm)2, -NRmS(O)2Rm, -C(O)N(Rm)2, -C(O)Rm, -NRmC(O)Rm, -NRmC(O)N(Rm)2, -CO2Rm, -NRmCO2Rm, -CN, -NO2, -N(Rm)2 y -NRmS(O)2N(Rm)2, en donde cada Rm es, en forma independiente, hidrogeno o un alquilo C1-6 no sustituido; o una sal o éster farmacéuticamente aceptable de estos; y, en donde el peso molecular de dicho compuesto es inferior a 1200. Reivindicacion 3: El método de la reivindicacion 2, en donde dicho compuesto de la formula (1) es un compuesto de la formula (2) o una sal farmacéuticamente aceptable de estos. Reivindicacion 4: El método de la reivindicacion 1, en donde dicho inhibidor de DPP-IV se selecciona a partir del grupo que consiste en sitagliptina, vildagliptina, denagliptina, saxagliptina y alogliptina. Reivindicacion 37: Uso de (a) un compuesto de formula (1) de acuerdo con la reivindicacion 1 y (b) un inhibidor de DPP-IV, en la preparacion de un medicamento para utilizarse en: tratamiento de diabetes, reducir los niveles de glucosa en la sangre; reducir los niveles de insulina en la sangre, aumentar los niveles de incretina en la sangre; reducir los niveles de triglicéridos en la sangre; y/o aumentar la produccion de insulina dependiente de la glucosa.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4119608P | 2008-03-31 | 2008-03-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR072352A1 true AR072352A1 (es) | 2010-08-25 |
Family
ID=40668739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090101153A AR072352A1 (es) | 2008-03-31 | 2009-03-31 | Compuestos de oximetilen arilo y usos de estos |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20090270404A1 (es) |
| EP (1) | EP2280704B1 (es) |
| JP (1) | JP5711655B2 (es) |
| KR (1) | KR20100134659A (es) |
| CN (1) | CN102026636B (es) |
| AR (1) | AR072352A1 (es) |
| AU (1) | AU2009231906A1 (es) |
| BR (1) | BRPI0909469A2 (es) |
| CA (1) | CA2719507C (es) |
| CL (1) | CL2009000782A1 (es) |
| DK (1) | DK2280704T3 (es) |
| ES (1) | ES2543358T3 (es) |
| HK (1) | HK1153946A1 (es) |
| IL (1) | IL208230A0 (es) |
| MX (1) | MX2010010562A (es) |
| PL (1) | PL2280704T3 (es) |
| SM (1) | SMP201000118B (es) |
| TW (1) | TW201002705A (es) |
| WO (1) | WO2009123992A1 (es) |
| ZA (1) | ZA201006687B (es) |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| DOP2006000008A (es) * | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1 |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| NZ619413A (en) | 2006-05-04 | 2015-08-28 | Boehringer Ingelheim Int | Polymorphs of a dpp-iv enzyme inhibitor |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| US7638541B2 (en) | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| US8183381B2 (en) * | 2007-07-19 | 2012-05-22 | Metabolex Inc. | N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders |
| CL2008002427A1 (es) | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende 1-cloro-4-(b-d-glucopiranos-1-il)-2-[4-((s)-tetrahidrofurano-3-iloxi)bencil]-benceno combinado con 1-[(4-metilquinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(r)-aminopiperidin-1-il)xantina; y su uso para tratar diabetes mellitus tipo 2. |
| AR071175A1 (es) | 2008-04-03 | 2010-06-02 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un inhibidor de la dipeptidil-peptidasa-4 (dpp4) y un farmaco acompanante |
| 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 |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| RU2011113823A (ru) | 2008-09-10 | 2012-10-20 | БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) | Комбинированная терапия, предназначенная для лечения диабета и связанных с ним состояний |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| AU2009316786A1 (en) * | 2008-11-19 | 2010-05-27 | Merck Sharp & Dohme Corp. | Inhibitors of diacylglycerol acyltransferase |
| US20110160222A1 (en) * | 2008-11-26 | 2011-06-30 | Metabolex, Inc. | Modulators of glucose homeostasis for the treatment of diabetes and metabolic disorders |
| JP2012512848A (ja) | 2008-12-23 | 2012-06-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 有機化合物の塩の形態 |
| AR074990A1 (es) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina |
| PL2395983T3 (pl) | 2009-02-13 | 2020-09-07 | Boehringer Ingelheim International Gmbh | Kompozycja farmaceutyczna zawierająca inhibitor sglt2, inhibitor dpp-iv i ewentualnie dalszy środek przeciwcukrzycowy oraz jej zastosowania |
| PE20120399A1 (es) * | 2009-06-05 | 2012-04-24 | Pfizer | Derivados del l-(piperidin-4-il)-pirazol como moduladores de gpr 119 |
| WO2010149685A1 (en) | 2009-06-24 | 2010-12-29 | Boehringer Ingelheim International Gmbh | New compounds, pharmaceutical composition and methods relating thereto |
| MX2011013648A (es) | 2009-06-24 | 2012-03-06 | Boehringer Ingelheim Int | Nuevos compuestos, composiciones farmaceuticas y metodos relacionados con ellos. |
| US8410127B2 (en) | 2009-10-01 | 2013-04-02 | Metabolex, Inc. | Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts |
| JP2013512229A (ja) | 2009-11-27 | 2013-04-11 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 遺伝子型が同定された糖尿病患者のリナグリプチン等のｄｄｐ−ｉｖ阻害薬による治療 |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
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- 2009-03-30 MX MX2010010562A patent/MX2010010562A/es not_active Application Discontinuation
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- 2009-03-30 US US12/414,639 patent/US20090270404A1/en not_active Abandoned
- 2009-03-30 CL CL2009000782A patent/CL2009000782A1/es unknown
- 2009-03-30 BR BRPI0909469A patent/BRPI0909469A2/pt not_active Application Discontinuation
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- 2009-03-30 CN CN200980110894.7A patent/CN102026636B/zh not_active Expired - Fee Related
- 2009-03-30 WO PCT/US2009/038847 patent/WO2009123992A1/en active Application Filing
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| BRPI0909469A2 (pt) | 2015-12-29 |
| IL208230A0 (en) | 2010-12-30 |
| US20090270404A1 (en) | 2009-10-29 |
| SMP201000118B (it) | 2011-09-09 |
| HK1153946A1 (en) | 2012-04-20 |
| CL2009000782A1 (es) | 2010-04-30 |
| ZA201006687B (en) | 2011-12-28 |
| JP2011516428A (ja) | 2011-05-26 |
| CN102026636A (zh) | 2011-04-20 |
| KR20100134659A (ko) | 2010-12-23 |
| TW201002705A (en) | 2010-01-16 |
| JP5711655B2 (ja) | 2015-05-07 |
| CN102026636B (zh) | 2014-07-16 |
| EP2280704B1 (en) | 2015-05-13 |
| CA2719507A1 (en) | 2009-10-08 |
| WO2009123992A1 (en) | 2009-10-08 |
| CA2719507C (en) | 2018-03-27 |
| MX2010010562A (es) | 2010-12-07 |
| DK2280704T3 (en) | 2015-06-29 |
| EP2280704A1 (en) | 2011-02-09 |
| PL2280704T3 (pl) | 2015-10-30 |
| ES2543358T3 (es) | 2015-08-18 |
| AU2009231906A1 (en) | 2009-10-08 |
| SMAP201000118A (it) | 2011-01-19 |
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