AR072900A1 - Agentes terapeuticos derivados de pirazolo[3,4-d]pirimidina - Google Patents
Agentes terapeuticos derivados de pirazolo[3,4-d]pirimidinaInfo
- Publication number
- AR072900A1 AR072900A1 ARP090102973A ARP090102973A AR072900A1 AR 072900 A1 AR072900 A1 AR 072900A1 AR P090102973 A ARP090102973 A AR P090102973A AR P090102973 A ARP090102973 A AR P090102973A AR 072900 A1 AR072900 A1 AR 072900A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- pyridyl
- ring
- pyrazolo
- pyrimidin
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61P3/06—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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Agentes terapéuticos derivados de pirazolo[3,4-d]pirimidina util en el tratamiento o prevencion de una enfermedad o afeccion médica mediada por glucoquinasa (GLK o GK), que conduce a una reduccion del umbral de glucosa para la secrecion de insulina, diabetes tipo 2 y obesidad. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable del mismo en donde A y B son cada uno N o CR6, siempre que al menos uno de A y B sea CR6; X es C o N; Y es CH o N; Z es C o N; en donde X, Y y Z se seleccionan de forma tal que al menos dos de X, Y y Z son N, el anillo que los contiene es aromático y ningun átomo de N del anillo está cuaternizado; R1 es alquilo C1-6, arilo, arilalquilo C1-6, o HET-1, en donde el arilo, arilalquilo C1-6 y HET-1 están opcionalmente sustituidos por uno, dos, o tres grupos que se seleccionan independientemente de halo, alquilo C1-4, alcoxi C1-4, trifluorometilo, alquil C1-6tio, alquil C1-6sulfinilo, alquil C1-6sulfonilo, ciano, carboxi, alcoxi C1-6carbonilo, carbamoilo, N-alquil C1-4carbamoilo, N,N-dialquil C1-4carbamoilo, aminosulfonilo, alquil C1-6aminosulfonilo, dialquil C1-6aminosulfonilo, alcanoil C1-4amino, hidroxialquilo C1-4, alcoxi C1-4-alquilo C1-4, alquil C1-4S(O)p-alquilo C1-4, aminoalquilo C1-4, alquil C1-4-aminoalquilo C1-4, dialquil C1-4-aminoalquilo C1-4, alcoxi C1-6-carbonilalquilo C1-4, alquil C1-6-sulfoniloxi, cicloalquil C3-6-sulfonilo, alquil C1-6-sulfonilamino, azetidinilcarbonilo, pirrolidinilcarbonilo y HET-3A; en donde HET-1 es un anillo heteroarilo unido a C de 5 o 6 miembros, o un sistema de anillos bicíclico fusionado de formula -D-E, en donde el anillo D está unido a Z y es un anillo arilo o heteroarilo de 6 miembros y un anillo E es un anillo heteroarilo, heterociclilo o cicloalquilo de 5 o 6 miembros que está fusionado al anillo D en cualquier posicion disponible; R2 es alquilo C1-6 opcionalmente sustituido por uno o dos hidroxi o por uno de los siguientes: carboxi, carbamoilo, N,N-dialquil C1-4carbamoilo, alcoxi C1-6carbonilo, un grupo -N(R7)COR8 o un grupo NR9R10; o R2 es un grupo -(CHR4)n-P-Q en donde n es 1, 2, 3 o 4; P es un enlazante que se selecciona de O, SO2, CONH y NHCO; Q se selecciona de alquilo C1-6, cicloalquilo C3-6 y un heterociclilo de 4, 5 o 6 miembros (en donde dicho anillo heterociclilo contiene 1, 2 o 3 heteroátomos que se seleccionan independientemente de O, N y S, siempre que no haya enlaces O-O, S-S ni O-S en donde un átomo de C disponible en el anillo puede oxidarse para convertirse en un grupo carbonilo, un átomo de S disponible en el anillo puede oxidarse para convertirse en un grupo SO o SO2 y en donde opcionalmente hay un enlace doble en el anillo) y Q está opcionalmente sustituido en un átomo de C disponible por hidroxi o alcoxi C1-4; R3 es HET-2 en donde HET-2 es un anillo heteroarilo monocíclico unido a C de 5 o 6 miembros, que contiene un átomo de N en la posicion 2 y opcionalmente 1 o 2 heteroátomos del anillo adicionales que se seleccionan independientemente de O, N y S; o HET-2 es un anillo heteroarilo bicíclico unido a C de 8, 9 o 10 miembros que contiene un átomo de N en la posicion 2 con hasta cinco heteroátomos del anillo adicionales que se seleccionan independientemente de O, N y S; en donde HET-2 está opcionalmente sustituido en un átomo de C disponible, o en un átomo de N del anillo siempre que no quede de este modo cuaternizado, con 1 o 2 sustituyentes que se seleccionan independientemente de R11; cada R4 se selecciona independientemente de H, hidroxi, metilo y etilo; siempre que cuando n es > 1, entonces no más de dos grupos R4 son hidroxi; R5 es H, alcoxi C1-4 o alquilo C1-4; R6 es H, alcoxi C1-4 o alquilo C1-4; R7 es H, o alquilo C1-4; R8 es alquilo C1-4; R9 es H o alquilo C1-4 opcionalmente sustituido por hidroxi o metoxi; R10 es H o alquilo C1-4; o -NR9R10 forma una azetidina opcionalmente sustituida por hidroxi; R11 se selecciona independientemente de halo, alquilo C1-4, alcoxi C1-4, trifluorometilo, alquil C1-6tio, alquil C1-6sulfinilo, alquil C1-6sulfonilo, ciano, carboxi, alcoxi C1-6carbonilo, carbamoilo, N-alquil C1-4carbamoilo, N,N-dialquil C1-4carbamoilo, aminosulfonilo, alquil C1-6aminosulfonilo, dialquil C1-6aminosulfonilo, alcanoil C1-4amino, hidroxialquilo C1-4, alcoxi C1-4-alquilo C1-4, alquil C1-4S(O)p-alquilo C1-4 (en donde p es 0, 1 o 2), aminoalquilo C1-4, alquil C1-4-aminoalquilo C1-4, dialquil C1-4-aminoalquilo C1-4, alcoxi C1-6-carbonilalquilo C1-4, alquil C1-6-sulfoniloxi, cicloalquil C3-6-sulfonilo, alquil C1-6-sulfonilamino, azetidinilcarbonilo, pirrolidinilcarbonilo y HET-3; HET-3 y HET-3A son cada uno independientemente un anillo heteroarilo insustituido unido a C o N de 5 o 6 miembros que contiene 1, 2 o 3 heteroátomos del anillo que se seleccionan independientemente de O, N y S, o un anillo heterociclilo saturado insustituido unido a C o N de 4, 5 o 6 miembros que contiene un heteroátomo del anillo que se selecciona de O, N y S; L es S, O o NR12; y R12 es H o alquilo C1-4; pero excluyendo N-(5-cloro-2-piridinil)-2-[(1-fenil-1H-pirazolo[3,4-d]pirimidin-4-il)tio]propanamida; N-[1-(1-metiletil)-1H-pirazol-5-il]-2-[(1-fenil-1H-pirazolo[3,4-d]pirimidin-4-il)tio]propanamida; N-(5-(metil)isoxazol-3-il)-2-[[1-(4-fluorofenil)-1H-pirazolo[3,4-d]pirimidin-4-il]tio]butanamida; N-(5-(metil)isoxazol-3-il)-2-[[1-(4-fluorofenil)-1H-pirazolo[3,4-d]pirimidin-4-il]tio]propanamida; (2R)-2-[1-(3-cloro-2-piridil)pirazolo[4,5-e]pirimidin-4-il]oxi-5-hidroxi-N-(5-metil-2-piridil)pentanamida; (2R)-N-(5-cloro-2-piridil)-2-[1-(3-cloro-2-piridil)pirazolo[4,5-e]pirimidin-4-il]oxi-5-hidroxi-pentanamida; (2S)-2-[1-(3-cloro-2-piridil)pirazolo[4,5-e]pirimidin-4-il]oxi-N-(5-ciano-2-piridil)-3-[(1S)-2-hidroxi-1-metil-etoxi]propanamida; (2R)-2-[1-(2-clorofenil)pirazolo[4,5-e]pirimidin-4-il]oxi-N-(5-ciano-2-piridil)-3-(2-hidroxietoxi)propanamida; (2S)-N-(5-ciano-2-piridil)-2-[1-(2,5-dimetilfenil)pirazolo[4,5-e]pirimidin-4-il]oxi-3-(2-hidroxietoxi)-propanamida; (2S)-3-(2-hidroxietoxi)-N-(5-metil-2-piridil)-2-(9-fenilpurin-6-il)oxi-propanamida; (2R)-2-[1-(2-clorofenil)pirazolo[4,5-e]pirimidin-4-il]oxi-N-(5-fluoro-2-piridil)-3-(2-hidroxietoxi)propanamida; (2S)-N-(5-cloro-2-piridil)-2-[1-(3-cloro-2-piridil)pirazolo[4,5-e]pirimidin-4-il]oxi-3-[(2R)-2-hidroxipropoxi]propanamida; (2R)-N-(5-cloro-2-piridil)-2-[1-(3-cloro-2-piridil)pirazolo[4,5-e]pirimidin-4-il]oxi-3-[(2R)-2-hidroxipropoxi]propanamida; (2S)-2-[1-(3-cloro-2-piridil)-pirazolo[4,5-e]pirimidin-4-il]oxi-N-(5-ciano-2-piridil)-3-(3-hidroxiciclobutoxi)propanamida; y (2S)-N-(5-cloro-2-piridil)-2-[1-(3-cloro-2-piridil)pirazolo[4,5-e]pirimidin-4-il]oxi-3-(3-hidroxiciclobutoxi)propanamida.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US8591908P | 2008-08-04 | 2008-08-04 | |
US16804809P | 2009-04-09 | 2009-04-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR072900A1 true AR072900A1 (es) | 2010-09-29 |
Family
ID=41563374
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090102973A AR072900A1 (es) | 2008-08-04 | 2009-08-03 | Agentes terapeuticos derivados de pirazolo[3,4-d]pirimidina |
Country Status (23)
Country | Link |
---|---|
US (1) | US8143263B2 (es) |
EP (1) | EP2324028A2 (es) |
JP (1) | JP2011529955A (es) |
KR (1) | KR20110052676A (es) |
CN (1) | CN102171213A (es) |
AR (1) | AR072900A1 (es) |
AU (1) | AU2009278929B2 (es) |
BR (1) | BRPI0917589A2 (es) |
CA (1) | CA2732165A1 (es) |
CL (1) | CL2011000249A1 (es) |
CO (1) | CO6351730A2 (es) |
CR (1) | CR20110065A (es) |
DO (1) | DOP2011000047A (es) |
EA (1) | EA201100097A1 (es) |
EC (1) | ECSP11010809A (es) |
IL (1) | IL210778A0 (es) |
MX (1) | MX2011001333A (es) |
PE (1) | PE20110568A1 (es) |
SV (1) | SV2011003829A (es) |
TW (1) | TW201011026A (es) |
UY (1) | UY32032A (es) |
WO (1) | WO2010015849A2 (es) |
ZA (1) | ZA201101663B (es) |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW200600086A (en) * | 2004-06-05 | 2006-01-01 | Astrazeneca Ab | Chemical compound |
TW200714597A (en) * | 2005-05-27 | 2007-04-16 | Astrazeneca Ab | Chemical compounds |
TW200825060A (en) * | 2006-10-26 | 2008-06-16 | Astrazeneca Ab | Chemical compounds |
GB0902434D0 (en) * | 2009-02-13 | 2009-04-01 | Astrazeneca Ab | Chemical process |
GB0902406D0 (en) * | 2009-02-13 | 2009-04-01 | Astrazeneca Ab | Crystalline polymorphic form |
AR076220A1 (es) * | 2009-04-09 | 2011-05-26 | Astrazeneca Ab | Derivados de pirazol [4,5 - e] pirimidina |
AR076221A1 (es) * | 2009-04-09 | 2011-05-26 | Astrazeneca Ab | Derivado de pirazol [4,5-e] pirimidina y su uso para tratar diabetes y obesidad |
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 |
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 |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
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 |
CN103450124B (zh) * | 2013-08-30 | 2016-03-09 | 江苏九九久科技股份有限公司 | 决奈达隆合成方法 |
WO2016183519A1 (en) | 2015-05-14 | 2016-11-17 | The Regents Of The University Of California | Brassinosteroid mimetics |
EP3872068A1 (en) * | 2015-12-16 | 2021-09-01 | Nippon Soda Co., Ltd. | Arylazole compound and pest control agent |
CN106749263A (zh) * | 2016-11-13 | 2017-05-31 | 曹艳 | 一种别嘌醇衍生物及其在制备抗肿瘤药物中的用途 |
CN106361753A (zh) * | 2016-11-13 | 2017-02-01 | 曹艳 | 一种别嘌醇衍生物及其在制备抗肿瘤药物中的用途 |
CN106749264A (zh) * | 2016-11-13 | 2017-05-31 | 曹艳 | 一种别嘌醇衍生物及其在制备抗肿瘤药物中的用途 |
CN106749265A (zh) * | 2016-11-13 | 2017-05-31 | 曹艳 | 一种别嘌醇衍生物及其在制备抗肿瘤药物中的用途 |
EP3357928B1 (en) | 2017-02-03 | 2021-01-06 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Novel dyes with phosphinic acid, phosphinate, phosphonate and phosphonamidate substituents as auxochromic groups and methods for preparing the same |
CN108033966A (zh) * | 2018-01-05 | 2018-05-15 | 天津药明康德新药开发有限公司 | 7-叔丁基3-乙基8-甲基5,6二氢三唑并吡嗪3,7(8h)二甲酸基酯的合成方法 |
WO2020254553A1 (en) | 2019-06-19 | 2020-12-24 | Nmd Pharma A/S | Compounds for the treatment of neuromuscular disorders |
CN113185520A (zh) * | 2021-04-28 | 2021-07-30 | 山东鲁抗医药股份有限公司 | 替格瑞洛杂质b及其制备方法 |
Family Cites Families (99)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2750393A (en) | 1954-12-01 | 1956-06-12 | Sterling Drug Inc | Iodinated 5-henzamidotetrazoles and preparation thereof |
US2967194A (en) | 1958-05-15 | 1961-01-03 | Pennsalt Chemicals Corp | 4-trifluoromethylsalicylamides |
FR1526074A (fr) | 1967-03-22 | 1968-05-24 | Rech S Ind S O R I Soc D | Méthoxy-phényl-amino-2-thiazoles, leurs amides et leurs procédés de préparation |
FR2088019A1 (en) | 1970-05-08 | 1972-01-07 | Rabot Ets David | Esters of 2 and 6-substituted nicotinic acids - with vasomotor active |
GB1352415A (en) | 1970-05-03 | 1974-05-08 | Boots Co Ltd | Esters of substituted nicotine acids |
CS173097B1 (es) | 1972-12-01 | 1977-02-28 | ||
GB1400540A (en) | 1972-12-06 | 1975-07-16 | Smith Kline French Lab | Salicylamides and compositions thereof |
US4009174A (en) | 1972-12-08 | 1977-02-22 | The Boots Company Limited | Esters of substituted nicotinic acids |
GB1437800A (en) | 1973-08-08 | 1976-06-03 | Phavic Sprl | Derivatives of 2-benzamido-5-nitro-thiazoles |
GB1561350A (en) | 1976-11-05 | 1980-02-20 | May & Baker Ltd | Benzamide derivatives |
FR2344284A1 (fr) | 1976-03-17 | 1977-10-14 | Cerm Cent Europ Rech Mauvernay | Nouveaux composes tricycliques a cycle furannique et leur application comme antidepresseurs |
GB1588242A (en) | 1977-10-28 | 1981-04-23 | May & Baker Ltd | N-(tetrazol-5-yl)-salicylamide derivatives |
US4474792A (en) | 1979-06-18 | 1984-10-02 | Riker Laboratories, Inc. | N-Tetrazolyl benzamides and anti-allergic use thereof |
FR2493848B2 (fr) | 1980-11-07 | 1986-05-16 | Delalande Sa | Nouveaux derives des nor-tropane et granatane, leur procede de preparation et leur application en therapeutique |
JPS59139357A (ja) | 1983-01-28 | 1984-08-10 | Torii Yakuhin Kk | アミジン誘導体 |
JPS62142168A (ja) | 1985-10-16 | 1987-06-25 | Mitsubishi Chem Ind Ltd | チアゾ−ル誘導体及びそれを有効成分とするロイコトリエンきつ抗剤 |
CA1327358C (en) | 1987-11-17 | 1994-03-01 | Morio Fujiu | Fluoro cytidine derivatives |
JP2852659B2 (ja) | 1988-03-03 | 1999-02-03 | 富山化学工業株式会社 | ピペラジン誘導体およびその塩 |
DE3822449A1 (de) | 1988-07-02 | 1990-01-04 | Henkel Kgaa | Oxidationshaarfaerbemittel mit neuen kupplern |
GB9015764D0 (en) * | 1990-07-18 | 1990-09-05 | Fujisawa Pharmaceutical Co | Pyrazolopyridine compound and processes for preparation thereof |
US5258407A (en) | 1991-12-31 | 1993-11-02 | Sterling Winthrop Inc. | 3,4-disubstituted phenols-immunomodulating agents |
US5466715A (en) | 1991-12-31 | 1995-11-14 | Sterling Winthrop Inc. | 3,4-disubstituted phenols-immunomodulating agents |
US5273986A (en) | 1992-07-02 | 1993-12-28 | Hoffmann-La Roche Inc. | Cycloalkylthiazoles |
EP0619116A3 (en) | 1993-04-05 | 1994-11-23 | Hoechst Japan | Use of synthetic retinoids for osteopathy. |
GB9307527D0 (en) | 1993-04-13 | 1993-06-02 | Fujisawa Pharmaceutical Co | New venzamide derivatives,processes for the preparation thereof and pharmaceutical composition comprising the same |
US5661153A (en) | 1994-07-19 | 1997-08-26 | Japan Energy Corporation | 1-arylpyrimidine derivatives and pharmaceutical use thereof |
US5510478A (en) | 1994-11-30 | 1996-04-23 | American Home Products Corporation | 2-arylamidothiazole derivatives with CNS activity |
US5672750A (en) | 1994-12-16 | 1997-09-30 | Eastman Chemical Company | Preparation of aromatic amides from carbon monoxide, an amine and an aromatic chloride |
US5849735A (en) | 1995-01-17 | 1998-12-15 | American Cyanamid Company | Tricyclic benzazepine vasopressin antagonists |
US5712270A (en) | 1995-11-06 | 1998-01-27 | American Home Products Corporation | 2-arylamidothiazole derivatives with CNS activity |
ATE354577T1 (de) * | 1996-11-06 | 2007-03-15 | Basilea Pharmaceutica Ag | Vinylpyrrolidinon-cephalosporin-derivate |
AUPO395396A0 (en) | 1996-12-02 | 1997-01-02 | Fujisawa Pharmaceutical Co., Ltd. | Benzamide derivatives |
FR2757852B1 (fr) | 1996-12-31 | 1999-02-19 | Cird Galderma | Composes stilbeniques a groupement adamantyl, compositions les contenant et utilisations |
US6245817B1 (en) | 1997-02-14 | 2001-06-12 | Bayer Corporation | NPY5 receptor antagonists and methods for using same |
CA2251368A1 (en) | 1997-02-14 | 1998-08-20 | Bayer Corporation | Amide derivatives as selective neuropeptide y receptor antagonists |
DE69826286T2 (de) | 1997-06-27 | 2005-11-24 | Fujisawa Pharmaceutical Co., Ltd. | Derivate mit einem aromatischen ring |
KR20010014183A (ko) | 1997-06-27 | 2001-02-26 | Fujisawa Pharmaceutical Co | 술폰아미드 화합물 및 그의 의약 용도 |
US6613942B1 (en) | 1997-07-01 | 2003-09-02 | Novo Nordisk A/S | Glucagon antagonists/inverse agonists |
US6114483A (en) | 1997-08-27 | 2000-09-05 | E. I. Du Pont De Nemours And Company | Polymerization of olefins |
CA2309331A1 (en) | 1997-11-12 | 1999-05-20 | Institute Of Medicinal Molecular Design, Inc. | Agent acting on retinoid receptor |
GB9725298D0 (en) | 1997-11-28 | 1998-01-28 | Zeneca Ltd | Insecticidal thiazole derivatives |
AU759255B2 (en) | 1998-01-29 | 2003-04-10 | Amgen, Inc. | PPAR-gamma modulators |
DE19816780A1 (de) | 1998-04-16 | 1999-10-21 | Bayer Ag | Substituierte 2-Oxo-alkansäure-[2-(indol-3-yl)-ethyl]amide |
GB9811969D0 (en) | 1998-06-03 | 1998-07-29 | Celltech Therapeutics Ltd | Chemical compounds |
US6197798B1 (en) | 1998-07-21 | 2001-03-06 | Novartis Ag | Amino-benzocycloalkane derivatives |
JP4191825B2 (ja) | 1998-09-10 | 2008-12-03 | あすか製薬株式会社 | 5−アミノイソキサゾール誘導体 |
US6320050B1 (en) | 1999-03-29 | 2001-11-20 | Hoffmann-La Roche Inc. | Heteroaromatic glucokinase activators |
US6610846B1 (en) | 1999-03-29 | 2003-08-26 | Hoffman-La Roche Inc. | Heteroaromatic glucokinase activators |
RU2242469C2 (ru) | 1999-03-29 | 2004-12-20 | Ф.Хоффманн-Ля Рош Аг | Активаторы глюкокиназы |
AU1917201A (en) | 1999-11-18 | 2001-05-30 | Centaur Pharmaceuticals, Inc. | Amide therapeutics and methods for treating inflammatory bowel disease |
CA2401778C (en) | 2000-02-29 | 2010-12-21 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
EP1132381A1 (en) | 2000-03-08 | 2001-09-12 | Cermol S.A. | Ester derivatives of dimethylpropionic acid and pharmaceutical compositions containing them |
US6534651B2 (en) | 2000-04-06 | 2003-03-18 | Inotek Pharmaceuticals Corp. | 7-Substituted isoindolinone inhibitors of inflammation and reperfusion injury and methods of use thereof |
JP3788935B2 (ja) | 2000-05-03 | 2006-06-21 | エフ.ホフマン−ラ ロシュ アーゲー | アルキニルフェニルヘテロ芳香族グルコキナーゼ活性化物質 |
WO2002042270A1 (fr) | 2000-11-22 | 2002-05-30 | Yamanouchi Pharmaceutical Co., Ltd. | Derives de benzene substitues ou leurs sels |
BR0115999A (pt) | 2000-12-06 | 2003-09-30 | Hoffmann La Roche | Composto, composição farmacêutica que compreende o mesmo, sua utilização, processo para o tratamento profilático ou terapêutico de diabetes do tipo ii e processo para a preparação do composto |
CA2432713C (en) | 2000-12-22 | 2009-10-27 | Ishihara Sangyo Kaisha, Ltd. | Aniline derivatives or salts thereof and cytokine production inhibitors containing the same |
JPWO2002062775A1 (ja) | 2001-02-02 | 2004-06-10 | 山之内製薬株式会社 | 2−アシルアミノチアゾール誘導体又はその塩 |
SE0102300D0 (sv) | 2001-06-26 | 2001-06-26 | Astrazeneca Ab | Compounds |
SE0102299D0 (sv) | 2001-06-26 | 2001-06-26 | Astrazeneca Ab | Compounds |
PL368129A1 (en) | 2001-08-09 | 2005-03-21 | Ono Pharmaceutical Co, Ltd. | Carboxylic acid derivative compounds and drugs comprising these compounds as the active ingredient |
SE0102764D0 (sv) | 2001-08-17 | 2001-08-17 | Astrazeneca Ab | Compounds |
EP1336607A1 (en) | 2002-02-19 | 2003-08-20 | Novo Nordisk A/S | Amide derivatives as glucokinase activators |
DE10161765A1 (de) | 2001-12-15 | 2003-07-03 | Bayer Cropscience Gmbh | Substituierte Phenylderivate |
US6911545B2 (en) | 2001-12-19 | 2005-06-28 | Hoffman-La Roche Inc. | Crystals of glucokinase and methods of growing them |
CA2488161A1 (en) | 2002-03-26 | 2003-10-02 | Banyu Pharmaceutical Co., Ltd. | Novel aminobenzamide derivative |
EP1541563A4 (en) | 2002-07-10 | 2007-11-07 | Ono Pharmaceutical Co | ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE |
GB0226930D0 (en) | 2002-11-19 | 2002-12-24 | Astrazeneca Ab | Chemical compounds |
GB0226931D0 (en) | 2002-11-19 | 2002-12-24 | Astrazeneca Ab | Chemical compounds |
RU2330030C2 (ru) | 2003-02-26 | 2008-07-27 | Баниу Фармасьютикал Ко., Лтд. | Производные гетероарилкарбамоилбензола |
EP2385040A1 (en) | 2003-03-14 | 2011-11-09 | ONO Pharmaceutical Co., Ltd. | Nitrogen-containing heterocyclic derivatives and drugs containing the same as the active ingredient |
GB0325402D0 (en) | 2003-10-31 | 2003-12-03 | Astrazeneca Ab | Compounds |
CA2545711A1 (en) | 2003-11-13 | 2005-06-02 | Ambit Biosciences Corporation | Urea derivatives as kinase modulators |
EP1532980A1 (en) | 2003-11-24 | 2005-05-25 | Novo Nordisk A/S | N-heteroaryl indole carboxamides and analogues thereof, for use as glucokinase activators in the treatment of diabetes |
GB0327761D0 (en) | 2003-11-29 | 2003-12-31 | Astrazeneca Ab | Compounds |
GB0327760D0 (en) | 2003-11-29 | 2003-12-31 | Astrazeneca Ab | Compounds |
GB0328178D0 (en) | 2003-12-05 | 2004-01-07 | Astrazeneca Ab | Compounds |
EP1702919B1 (en) | 2003-12-29 | 2012-05-30 | Msd K.K. | Novel 2-heteroaryl-substituted benzimidazole derivative |
CA2554686A1 (en) | 2004-02-18 | 2005-09-01 | Astrazeneca Ab | Compounds |
RU2392275C2 (ru) | 2004-02-18 | 2010-06-20 | Астразенека Аб | Бензамидные производные и их применение в качестве активирующих глюкокиназу агентов |
TW200600086A (en) | 2004-06-05 | 2006-01-01 | Astrazeneca Ab | Chemical compound |
KR101231466B1 (ko) | 2004-09-13 | 2013-02-07 | 오노 야꾸힝 고교 가부시키가이샤 | 질소 함유 복소환 유도체 및 이들을 유효 성분으로 하는약제 |
BRPI0516595A (pt) | 2004-10-16 | 2008-09-23 | Astrazeneca Ab | processo para fabricar um composto, e, composto |
GB0423043D0 (en) | 2004-10-16 | 2004-11-17 | Astrazeneca Ab | Compounds |
GB0423044D0 (en) | 2004-10-16 | 2004-11-17 | Astrazeneca Ab | Compounds |
US8859581B2 (en) | 2005-04-25 | 2014-10-14 | Merck Patent Gmbh | Azaheterocyclic compounds as kinase inhibitors |
WO2006125958A1 (en) * | 2005-05-24 | 2006-11-30 | Astrazeneca Ab | 2-phenyl substituted imidazol [4 , 5b] pyridine/ pyrazine and purine derivatives as glucokinase modulators |
TW200714597A (en) | 2005-05-27 | 2007-04-16 | Astrazeneca Ab | Chemical compounds |
KR101346902B1 (ko) | 2005-07-09 | 2014-01-02 | 아스트라제네카 아베 | 당뇨병 치료에 있어 glk 활성화제로서 사용하기 위한헤테로아릴 벤즈아미드 유도체 |
US20080234273A1 (en) | 2005-07-09 | 2008-09-25 | Mckerrecher Darren | Heteroaryl Benzamide Derivatives for Use as Glk Activators in the Treatment of Diabetes |
US20110053910A1 (en) | 2005-07-09 | 2011-03-03 | Mckerrecher Darren | 2 -heterocyclyloxybenzoyl amino heterocyclyl compounds as modulators of glucokinase for the treatment of type 2 diabetes |
JP2009508832A (ja) | 2005-09-16 | 2009-03-05 | アストラゼネカ アクチボラグ | グルコキナーゼ活性化剤としてのヘテロ二環式化合物 |
TW200738621A (en) | 2005-11-28 | 2007-10-16 | Astrazeneca Ab | Chemical process |
CN101443322A (zh) | 2006-03-10 | 2009-05-27 | 小野药品工业株式会社 | 含氮杂环衍生物及含有该衍生物作为活性成分的药物 |
TW200825063A (en) | 2006-10-23 | 2008-06-16 | Astrazeneca Ab | Chemical compounds |
TW200825060A (en) | 2006-10-26 | 2008-06-16 | Astrazeneca Ab | Chemical compounds |
AU2007336016A1 (en) | 2006-12-21 | 2008-06-26 | Astrazeneca Ab | Novel crystalline compound useful as GLK activator |
GB0902434D0 (en) | 2009-02-13 | 2009-04-01 | Astrazeneca Ab | Chemical process |
GB0902406D0 (en) | 2009-02-13 | 2009-04-01 | Astrazeneca Ab | Crystalline polymorphic form |
-
2009
- 2009-08-03 EA EA201100097A patent/EA201100097A1/ru unknown
- 2009-08-03 EP EP09785441A patent/EP2324028A2/en not_active Withdrawn
- 2009-08-03 JP JP2011521643A patent/JP2011529955A/ja not_active Withdrawn
- 2009-08-03 CA CA2732165A patent/CA2732165A1/en not_active Abandoned
- 2009-08-03 CN CN2009801395833A patent/CN102171213A/zh active Pending
- 2009-08-03 BR BRPI0917589A patent/BRPI0917589A2/pt not_active IP Right Cessation
- 2009-08-03 KR KR1020117004895A patent/KR20110052676A/ko not_active Application Discontinuation
- 2009-08-03 WO PCT/GB2009/050970 patent/WO2010015849A2/en active Application Filing
- 2009-08-03 AU AU2009278929A patent/AU2009278929B2/en not_active Expired - Fee Related
- 2009-08-03 PE PE2011000125A patent/PE20110568A1/es not_active Application Discontinuation
- 2009-08-03 MX MX2011001333A patent/MX2011001333A/es not_active Application Discontinuation
- 2009-08-03 AR ARP090102973A patent/AR072900A1/es unknown
- 2009-08-04 TW TW098126200A patent/TW201011026A/zh unknown
- 2009-08-04 US US12/535,293 patent/US8143263B2/en not_active Expired - Fee Related
- 2009-08-04 UY UY0001032032A patent/UY32032A/es not_active Application Discontinuation
-
2011
- 2011-01-20 IL IL210778A patent/IL210778A0/en unknown
- 2011-02-01 CO CO11011423A patent/CO6351730A2/es not_active Application Discontinuation
- 2011-02-04 SV SV2011003829A patent/SV2011003829A/es not_active Application Discontinuation
- 2011-02-04 CL CL2011000249A patent/CL2011000249A1/es unknown
- 2011-02-04 EC EC2011010809A patent/ECSP11010809A/es unknown
- 2011-02-04 CR CR20110065A patent/CR20110065A/es unknown
- 2011-02-04 DO DO2011000047A patent/DOP2011000047A/es unknown
- 2011-03-03 ZA ZA2011/01663A patent/ZA201101663B/en unknown
Also Published As
Publication number | Publication date |
---|---|
KR20110052676A (ko) | 2011-05-18 |
SV2011003829A (es) | 2011-07-01 |
EA201100097A1 (ru) | 2011-10-31 |
AU2009278929A8 (en) | 2011-03-10 |
BRPI0917589A2 (pt) | 2015-11-17 |
MX2011001333A (es) | 2011-03-15 |
ZA201101663B (en) | 2011-11-30 |
US20100093757A1 (en) | 2010-04-15 |
US8143263B2 (en) | 2012-03-27 |
DOP2011000047A (es) | 2011-02-28 |
WO2010015849A2 (en) | 2010-02-11 |
CO6351730A2 (es) | 2011-12-20 |
AU2009278929A1 (en) | 2010-02-11 |
JP2011529955A (ja) | 2011-12-15 |
EP2324028A2 (en) | 2011-05-25 |
PE20110568A1 (es) | 2011-09-07 |
AU2009278929B2 (en) | 2012-07-05 |
IL210778A0 (en) | 2011-03-31 |
WO2010015849A3 (en) | 2010-04-01 |
CR20110065A (es) | 2011-05-10 |
UY32032A (es) | 2010-03-26 |
CL2011000249A1 (es) | 2011-07-15 |
CA2732165A1 (en) | 2010-02-11 |
TW201011026A (en) | 2010-03-16 |
ECSP11010809A (es) | 2011-03-31 |
CN102171213A (zh) | 2011-08-31 |
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