JP2005500312A5 - - Google Patents
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- Publication number
- JP2005500312A5 JP2005500312A5 JP2003506912A JP2003506912A JP2005500312A5 JP 2005500312 A5 JP2005500312 A5 JP 2005500312A5 JP 2003506912 A JP2003506912 A JP 2003506912A JP 2003506912 A JP2003506912 A JP 2003506912A JP 2005500312 A5 JP2005500312 A5 JP 2005500312A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- formula
- independently
- compound
- halo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 40
- 150000001875 compounds Chemical class 0.000 claims 28
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000001475 halogen functional group Chemical group 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 239000000651 prodrug Substances 0.000 claims 10
- 229940002612 prodrug Drugs 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 239000012453 solvate Substances 0.000 claims 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000001624 naphthyl group Chemical group 0.000 claims 6
- -1 —CH 3 —a F a Chemical group 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 238000006243 chemical reaction Methods 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- XDWUCRMGZVGWNS-UHFFFAOYSA-N 1,3a-dihydropentalene Chemical compound C1=CC=C2CC=CC21 XDWUCRMGZVGWNS-UHFFFAOYSA-N 0.000 claims 2
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 2
- XBLVHTDFJBKJLG-UHFFFAOYSA-N Ethyl nicotinate Chemical compound CCOC(=O)C1=CC=CN=C1 XBLVHTDFJBKJLG-UHFFFAOYSA-N 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- PIEXCQIOSMOEOU-UHFFFAOYSA-N 1-bromo-3-chloro-5,5-dimethylimidazolidine-2,4-dione Chemical compound CC1(C)N(Br)C(=O)N(Cl)C1=O PIEXCQIOSMOEOU-UHFFFAOYSA-N 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 208000013016 Hypoglycemia Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 239000004305 biphenyl Substances 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 229940064982 ethylnicotinate Drugs 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008203 oral pharmaceutical composition Substances 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 230000003647 oxidation Effects 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0102300A SE0102300D0 (sv) | 2001-06-26 | 2001-06-26 | Compounds |
| PCT/GB2002/002873 WO2003000267A1 (en) | 2001-06-26 | 2002-06-24 | Amino nicotinate derivatives as glucokinase (glk) modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005500312A JP2005500312A (ja) | 2005-01-06 |
| JP2005500312A5 true JP2005500312A5 (enExample) | 2005-12-22 |
Family
ID=20284652
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003506912A Withdrawn JP2005500312A (ja) | 2001-06-26 | 2002-06-24 | グルコキナーゼ（ｇｌｋ）モジュレーターとしてのアミノニコチネート誘導体 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20040214868A1 (enExample) |
| EP (1) | EP1404335A1 (enExample) |
| JP (1) | JP2005500312A (enExample) |
| KR (1) | KR20040029324A (enExample) |
| CN (1) | CN1520296A (enExample) |
| AR (1) | AR037996A1 (enExample) |
| AU (1) | AU2002314330B2 (enExample) |
| BR (1) | BR0210711A (enExample) |
| CA (1) | CA2451249A1 (enExample) |
| IL (1) | IL159403A0 (enExample) |
| MX (1) | MXPA03012004A (enExample) |
| NO (1) | NO20035766L (enExample) |
| NZ (1) | NZ530203A (enExample) |
| SE (1) | SE0102300D0 (enExample) |
| WO (1) | WO2003000267A1 (enExample) |
| ZA (1) | ZA200309979B (enExample) |
Families Citing this family (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE287360T1 (de) | 1999-12-22 | 2005-02-15 | Soremartec Sa | Verfahren zum umhüllen eines nahrungsmittels, und erzeugtes produkt |
| SE0102299D0 (sv) | 2001-06-26 | 2001-06-26 | Astrazeneca Ab | Compounds |
| SE0102764D0 (sv) | 2001-08-17 | 2001-08-17 | Astrazeneca Ab | Compounds |
| AU2003258491A1 (en) * | 2002-09-05 | 2004-03-29 | Neurosearch A/S | Amide derivatives and their use as chloride channel blockers |
| GB0226931D0 (en) | 2002-11-19 | 2002-12-24 | Astrazeneca Ab | Chemical compounds |
| GB0226930D0 (en) * | 2002-11-19 | 2002-12-24 | Astrazeneca Ab | Chemical compounds |
| PL378117A1 (pl) | 2003-02-11 | 2006-03-06 | Prosidion Limited | Tricyklopodstawione związki amidowe |
| BRPI0407283A (pt) | 2003-02-13 | 2006-01-31 | Banyu Pharma Co Ltd | Composto, composição farmacêutica, e, agente ativador de glucoquinase, agentes terapêuticos e/ou agentes preventivos para diabetes melito e obesidade |
| WO2004076420A1 (ja) | 2003-02-26 | 2004-09-10 | Banyu Pharmaceutical Co., Ltd. | ヘテロアリールカルバモイルベンゼン誘導体 |
| GB0325402D0 (en) * | 2003-10-31 | 2003-12-03 | Astrazeneca Ab | Compounds |
| GB0327760D0 (en) * | 2003-11-29 | 2003-12-31 | Astrazeneca Ab | Compounds |
| GB0327761D0 (en) * | 2003-11-29 | 2003-12-31 | Astrazeneca Ab | Compounds |
| GB0328178D0 (en) * | 2003-12-05 | 2004-01-07 | Astrazeneca Ab | Compounds |
| EP2048137A1 (en) * | 2004-02-18 | 2009-04-15 | AstraZeneca AB | Benzamide derivatives and their use as glucokinase activating agents. |
| TW200600086A (en) * | 2004-06-05 | 2006-01-01 | Astrazeneca Ab | Chemical compound |
| GB0423043D0 (en) * | 2004-10-16 | 2004-11-17 | Astrazeneca Ab | Compounds |
| TW200714597A (en) * | 2005-05-27 | 2007-04-16 | Astrazeneca Ab | Chemical compounds |
| KR20110084339A (ko) | 2005-07-09 | 2011-07-21 | 아스트라제네카 아베 | 당뇨병 치료에 있어 ｇｌｋ 활성화제로서 사용하기 위한 헤테로아릴 벤즈아미드 유도체 |
| 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 |
| ES2426345T3 (es) | 2005-07-20 | 2013-10-22 | Eli Lilly And Company | Compuesto unidos en posición 1-amino |
| JP2007063225A (ja) | 2005-09-01 | 2007-03-15 | Takeda Chem Ind Ltd | イミダゾピリジン化合物 |
| NZ566877A (en) | 2005-09-29 | 2010-05-28 | Sanofi Aventis | Phenyl-1,2,4-oxadiazolone derivatives, processes for their preparation and their use as pharmaceuticals |
| CN101312940B (zh) | 2005-11-17 | 2012-11-14 | 伊莱利利公司 | 胰高血糖素受体拮抗剂、制备和治疗用途 |
| EP2001875A2 (en) | 2006-03-08 | 2008-12-17 | Takeda San Diego, Inc. | Glucokinase activators |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| EP2049518B1 (en) | 2006-05-31 | 2011-08-31 | Takeda San Diego, Inc. | Indazole and isoindole derivatives as glucokinase activating agents. |
| AU2007287070C1 (en) | 2006-08-24 | 2013-02-14 | University Of Tennessee Research Foundation | Substituted acylanilides and methods of use thereof |
| AR063028A1 (es) | 2006-10-06 | 2008-12-23 | Banyu Pharma Co Ltd | Derivados heterociclicos de piridin-2-carboxamida activadores de glucoquinasas, utiles para el tratamiento de diabetes y obesidad y composiciones farmaceuticas que los contienen. |
| TW200825060A (en) * | 2006-10-26 | 2008-06-16 | Astrazeneca Ab | Chemical compounds |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| JP5069752B2 (ja) * | 2006-12-15 | 2012-11-07 | グラクソ グループ リミテッド | Ｅｐ４受容体アゴニストとしてのベンズアミド誘導体 |
| JP5419706B2 (ja) | 2006-12-20 | 2014-02-19 | タケダ カリフォルニア インコーポレイテッド | グルコキナーゼアクチベーター |
| WO2008116107A2 (en) | 2007-03-21 | 2008-09-25 | Takeda San Diego, Inc. | Piperazine derivatives as glucokinase activators |
| JP2010138073A (ja) * | 2007-03-30 | 2010-06-24 | Taisho Pharmaceutical Co Ltd | ピコリン酸アミド化合物 |
| JP2010533729A (ja) | 2007-07-17 | 2010-10-28 | プレキシコン，インコーポレーテッド | キナーゼ調節のための化合物と方法、及びそのための適応 |
| MX2011001333A (es) | 2008-08-04 | 2011-03-15 | Astrazeneca Ab | Derivados de pirazolo [3, 4] pirimidin-4-ilo y sus usos para tratar la diabetes y obesidad. |
| GEP20135793B (en) | 2008-09-11 | 2013-03-25 | Pfizer | Heteroaryls amide derivatives and their use as glucokinase activators |
| 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 |
| WO2010103437A1 (en) | 2009-03-11 | 2010-09-16 | Pfizer Inc. | Benzofuranyl derivatives used as glucokinase inhibitors |
| CA2738573C (en) | 2009-04-03 | 2013-02-19 | F. Hoffmann-La Roche Ag | Compositions of propane-1 sulfonic acid {3-[5-(4-chloro-phenyl)-1h-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide and uses thereof |
| WO2010116176A1 (en) | 2009-04-09 | 2010-10-14 | Astrazeneca Ab | Pyrazolo [4, 5-e] pyrimidine derivative and its use to treat diabetes and obesity |
| AR076220A1 (es) | 2009-04-09 | 2011-05-26 | Astrazeneca Ab | Derivados de pirazol [4,5 - e] pirimidina |
| AU2010276215A1 (en) * | 2009-07-21 | 2012-02-16 | Auckland Uniservices Limited | Heteroaryl benzamides, compositions and methods of use |
| US20120178765A1 (en) * | 2009-09-22 | 2012-07-12 | Yuhan Corporation | Novel glucokinase activators and processes for the preparation thereof |
| JP2013510166A (ja) | 2009-11-06 | 2013-03-21 | プレキシコン インコーポレーテッド | キナーゼ調節のための化合物、方法およびその適用 |
| PE20141360A1 (es) | 2011-02-07 | 2014-10-13 | Plexxikon Inc | Compuestos y metodos para la modulacion de quinasas e indicaciones para los mismos. |
| TWI558702B (zh) | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
| CN102786468A (zh) * | 2011-05-18 | 2012-11-21 | 中国医学科学院药物研究所 | Gk和ppar双重激动活性的烟酸类衍生物 |
| US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| US9744149B2 (en) | 2012-07-13 | 2017-08-29 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| US10258596B2 (en) | 2012-07-13 | 2019-04-16 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| US9969683B2 (en) | 2012-07-13 | 2018-05-15 | Gtx, Inc. | Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS) |
| US10987334B2 (en) | 2012-07-13 | 2021-04-27 | University Of Tennessee Research Foundation | Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs) |
| US12685719B2 (en) | 2012-07-13 | 2026-07-21 | University Of Tennessee Research Foundation | Treatment of breast cancer with selective androgen receptor modulators and cyclin-dependent kinase 4/6 inhibitors |
| US9622992B2 (en) | 2012-07-13 | 2017-04-18 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| EP3733170A1 (en) | 2012-07-13 | 2020-11-04 | Oncternal Therapeutics, Inc. | A method of treating androgen receptor (ar) -positive breast cancers with selective androgen receptor modulator (sarms) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| KR20140092696A (ko) * | 2013-01-16 | 2014-07-24 | 주식회사유한양행 | 신규의 페닐에티닐 벤즈아마이드 글루코키나제 활성화제 및 그의 제조방법 |
| GB201714777D0 (en) | 2017-09-14 | 2017-11-01 | Univ London Queen Mary | Agent |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1400540A (en) * | 1972-12-06 | 1975-07-16 | Smith Kline French Lab | Salicylamides and compositions thereof |
| GB1561350A (en) * | 1976-11-05 | 1980-02-20 | May & Baker Ltd | Benzamide derivatives |
| US5849735A (en) * | 1995-01-17 | 1998-12-15 | American Cyanamid Company | Tricyclic benzazepine vasopressin antagonists |
| JPH08301760A (ja) * | 1995-05-10 | 1996-11-19 | Shiseido Co Ltd | 皮膚外用剤 |
| HK1046139B (zh) * | 1999-03-29 | 2004-12-10 | 霍夫曼-拉罗奇有限公司 | 葡糖激酶活化剂 |
| US6353111B1 (en) * | 1999-12-15 | 2002-03-05 | Hoffmann-La Roche Inc. | Trans olefinic glucokinase activators |
| EP1282612B1 (en) * | 2000-05-03 | 2004-12-29 | F. Hoffmann-La Roche Ag | Alkynyl phenyl heteroaromatic glucokinase activators |
| SE0102764D0 (sv) * | 2001-08-17 | 2001-08-17 | Astrazeneca Ab | Compounds |
| GB0325402D0 (en) * | 2003-10-31 | 2003-12-03 | Astrazeneca Ab | Compounds |
-
2001
- 2001-06-26 SE SE0102300A patent/SE0102300D0/xx unknown
-
2002
- 2002-06-24 US US10/482,572 patent/US20040214868A1/en active Granted
- 2002-06-24 CN CNA028129458A patent/CN1520296A/zh active Pending
- 2002-06-24 MX MXPA03012004A patent/MXPA03012004A/es active IP Right Grant
- 2002-06-24 NZ NZ530203A patent/NZ530203A/en unknown
- 2002-06-24 JP JP2003506912A patent/JP2005500312A/ja not_active Withdrawn
- 2002-06-24 IL IL15940302A patent/IL159403A0/xx unknown
- 2002-06-24 BR BR0210711-2A patent/BR0210711A/pt not_active IP Right Cessation
- 2002-06-24 EP EP02740900A patent/EP1404335A1/en not_active Ceased
- 2002-06-24 AU AU2002314330A patent/AU2002314330B2/en not_active Ceased
- 2002-06-24 WO PCT/GB2002/002873 patent/WO2003000267A1/en not_active Ceased
- 2002-06-24 KR KR10-2003-7016791A patent/KR20040029324A/ko not_active Ceased
- 2002-06-24 CA CA002451249A patent/CA2451249A1/en not_active Abandoned
- 2002-06-26 AR ARP020102403A patent/AR037996A1/es not_active Application Discontinuation
-
2003
- 2003-12-22 NO NO20035766A patent/NO20035766L/no not_active Application Discontinuation
- 2003-12-23 ZA ZA200309979A patent/ZA200309979B/en unknown
-
2006
- 2006-12-07 US US11/634,966 patent/US20070112040A1/en not_active Abandoned
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