JP2009506043A5 - - Google Patents
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- Publication number
- JP2009506043A5 JP2009506043A5 JP2008528076A JP2008528076A JP2009506043A5 JP 2009506043 A5 JP2009506043 A5 JP 2009506043A5 JP 2008528076 A JP2008528076 A JP 2008528076A JP 2008528076 A JP2008528076 A JP 2008528076A JP 2009506043 A5 JP2009506043 A5 JP 2009506043A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- diabetes
- obesity
- disease
- 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.)
- Granted
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 208000008589 Obesity Diseases 0.000 claims 7
- 235000020824 obesity Nutrition 0.000 claims 7
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000002249 Diabetes Complications Diseases 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 206010012601 Diabetes mellitus Diseases 0.000 claims 3
- 238000009472 formulation Methods 0.000 claims 3
- 208000001636 Diabetic Neuropathy Diseases 0.000 claims 2
- 206010012655 Diabetic complications Diseases 0.000 claims 2
- 206010012680 Diabetic neuropathy Diseases 0.000 claims 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 2
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 2
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 2
- 208000009576 Hypercholesterolemia Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000001083 Kidney Disease Diseases 0.000 claims 2
- 102100009453 LYN Human genes 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000001280 Prediabetic State Diseases 0.000 claims 2
- 201000010390 abdominal obesity-metabolic syndrome 1 Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 239000002775 capsule Substances 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical group 0.000 claims 2
- 201000001881 impotence Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 201000009104 prediabetes syndrome Diseases 0.000 claims 2
- 201000010874 syndrome Diseases 0.000 claims 2
- 210000000577 Adipose Tissue Anatomy 0.000 claims 1
- 210000004369 Blood Anatomy 0.000 claims 1
- 208000004981 Coronary Disease Diseases 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 201000008739 coronary artery disease Diseases 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 230000000051 modifying Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000004584 weight gain Effects 0.000 claims 1
- 235000019786 weight gain Nutrition 0.000 claims 1
Claims (16)
- LYNキナーゼの活性または発現を調節する化合物の有効量を含有する、哺乳動物の血糖値、体重増加もしくは脂肪組織値を低下させ、またはII型糖尿病、肥満もしくはメタボリック症候群を治療するための医薬組成物。
- 化合物が式
- アルキル基はメチルであり、そしてｎは１である請求項２記載の医薬組成物。
- ハロゲンは塩素であり、そしてｍは１である請求項２記載の医薬組成物。
- ＹはＯである請求項２記載の医薬組成物。
- Ｚは０である請求項２記載の医薬組成物。
- R1はメチルであり、ＹはＯであり、ＺはＯであり、ｎは１であり、そしてｍは０である請求項２記載の医薬組成物。
- R1はメタ位に存在する請求項７記載の医薬組成物。
- Ｘは塩素であり、ＹはＯであり、ＺはＯであり、ｎは０であり、そしてｍは１である請求項２記載の医薬組成物。
- Ｘはメタ位に存在する請求項９記載の医薬組成物。
- 哺乳動物はヒトである請求項１記載の医薬組成物。
- 有効量は0.1mg〜100mg／kgである請求項１記載の医薬組成物。
- 経口投与用である請求項１記載の医薬組成物。
- メタボリック症候群もしくはＸ症候群の治療もしくは予防、またはこれらの症候群と関連する疾患の治療に使用するための請求項１記載の医薬組成物であって、該疾患は肥満、前糖尿病およびII型糖尿病、ならびに肥満および糖尿病の合併症を含み；ここで、肥満および糖尿病の合併症は高コレステロール血症、高血圧症、冠状動脈性心疾患、糖尿病性神経障害、糖尿病性網膜症、勃起障害および腎疾患を含む上記組成物。
- 化合物がLYNキナーゼの活性または発現を上向き調節する請求項１記載の医薬組成物。
- 式
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70979805P | 2005-08-22 | 2005-08-22 | |
| US60/709,798 | 2005-08-22 | ||
| US80853306P | 2006-05-26 | 2006-05-26 | |
| US60/808,533 | 2006-05-26 | ||
| PCT/US2006/032788 WO2007024863A2 (en) | 2005-08-22 | 2006-08-22 | Methods and formulations for modulating lyn kinase activity and treating related disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009506043A JP2009506043A (ja) | 2009-02-12 |
| JP2009506043A5 true JP2009506043A5 (ja) | 2009-09-24 |
| JP5113752B2 JP5113752B2 (ja) | 2013-01-09 |
Family
ID=37635750
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008528076A Active JP5113752B2 (ja) | 2005-08-22 | 2006-08-22 | Ｌｙｎキナーゼの活性を調節し、関連する疾患を治療するための方法および製剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (8) | US7776870B2 (ja) |
| EP (1) | EP1924262B1 (ja) |
| JP (1) | JP5113752B2 (ja) |
| KR (2) | KR101577554B1 (ja) |
| AT (1) | ATE533488T1 (ja) |
| AU (1) | AU2006283211B2 (ja) |
| BR (1) | BRPI0615046C1 (ja) |
| CA (1) | CA2620065C (ja) |
| HK (1) | HK1120738A1 (ja) |
| IL (1) | IL189603A0 (ja) |
| NZ (1) | NZ565955A (ja) |
| WO (1) | WO2007024863A2 (ja) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006283211B2 (en) | 2005-08-22 | 2012-06-21 | Melior Pharmaceuticals I, Inc. | Methods and formulations for modulating Lyn kinase activity and treating related disorders |
| US20100152215A1 (en) * | 2007-02-20 | 2010-06-17 | Melior Pharmaceuticals I, Inc. | Methods of identifying activators of lyn kinase |
| US20100160339A1 (en) * | 2007-05-21 | 2010-06-24 | Mayo Foundation For Medical Education And Research | Treating pancreatitis |
| JP2010534668A (ja) * | 2007-07-23 | 2010-11-11 | メリオール・ディスカヴァリー・インコーポレイテッド | Ｉｒｓ−１及びａｋｔを活性化する方法 |
| US8552184B2 (en) * | 2008-07-03 | 2013-10-08 | Melior Pharmaceuticals I, Inc. | Compounds and methods for treating disorders related to glucose metabolism |
| US20130158055A1 (en) * | 2010-05-28 | 2013-06-20 | Andrew G. Reaume | Prevention Of Pancreatic Beta Cell Degeneration |
| WO2013090319A2 (en) * | 2011-12-12 | 2013-06-20 | Melior Pharmaceuticals I, Inc. | Treatment of type i and type ii diabetes |
| US9687486B2 (en) * | 2012-12-20 | 2017-06-27 | The Trustees Of Columbia University In The City Of New York | Methods of treating atherosclerosis or myeloproliferative neoplasms by administering a lyn kinase activator |
| JOP20200093A1 (ar) | 2015-01-09 | 2017-06-16 | Kyowa Kirin Co Ltd | طريقة لإنتاج مشتق ثيازول |
| JP7182605B2 (ja) | 2017-04-10 | 2022-12-02 | メリオール・ファーマスーティカルズ・ワン・インコーポレイテッド | ｌｙｎキナーゼ活性化因子及びＴＲＰＭ８アゴニストを含む組成物及び医薬の製造におけるそれらの使用 |
| WO2019164799A1 (en) | 2018-02-21 | 2019-08-29 | Melior Pharmaceuticals I, Inc. | Treatment of liver diseases |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3174901A (en) * | 1963-01-31 | 1965-03-23 | Jan Marcel Didier Aron Samuel | Process for the oral treatment of diabetes |
| US3922345A (en) * | 1971-10-29 | 1975-11-25 | Pfizer | Pyrimidinones and hydroxy pyrimidines |
| BE790125A (fr) * | 1971-10-29 | 1973-04-16 | Pfizer | Nouvelles pyrimidinones et nouvelles hydroxypyrimidines |
| US4080454A (en) | 1976-07-16 | 1978-03-21 | Pfizer Inc. | 5-M-Tolyloxyuracil, anti-ulcer agent |
| US4612376A (en) | 1983-03-25 | 1986-09-16 | Fujisawa Pharmaceutical Co., Ltd. | Substituted-3,4-dihydro-4-(2,4,6-trimethoxyphenylimino)-2(1H)-pyrimidones useful as cardiotonic, antihypertensive, cerebrovascular vasodilator and anti-platelet agent |
| US5698155A (en) | 1991-05-31 | 1997-12-16 | Gs Technologies, Inc. | Method for the manufacture of pharmaceutical cellulose capsules |
| GB9214720D0 (en) | 1992-07-10 | 1992-08-19 | Wellcome Found | Enzyme inhibitors |
| SE9203753D0 (sv) | 1992-12-11 | 1992-12-11 | Kabi Pharmacia Ab | Expression system for producing apolipoprotein ai-m |
| US5476855A (en) | 1993-11-02 | 1995-12-19 | Mahmoud H. el Kouni | Enzyme inhibitors, their synthesis and methods for use |
| US6900304B2 (en) | 1996-01-31 | 2005-05-31 | The Regents Of The University Of California | Emission ratiometric indicators of phosphorylation |
| US20020019346A1 (en) | 1997-05-21 | 2002-02-14 | Children's Medical Center Corporation | Treatment of prostate cancer by inhibiting lyn tyrosine kinase |
| US6037323A (en) | 1997-09-29 | 2000-03-14 | Jean-Louis Dasseux | Apolipoprotein A-I agonists and their use to treat dyslipidemic disorders |
| US6004925A (en) | 1997-09-29 | 1999-12-21 | J. L. Dasseux | Apolipoprotein A-I agonists and their use to treat dyslipidemic disorders |
| US6410255B1 (en) | 1999-05-05 | 2002-06-25 | Aurora Biosciences Corporation | Optical probes and assays |
| US20010036479A1 (en) | 2000-01-14 | 2001-11-01 | Gillian Cave | Glyburide composition |
| GB0104422D0 (en) | 2001-02-22 | 2001-04-11 | Glaxo Group Ltd | Quinoline derivative |
| US20030198666A1 (en) | 2002-01-07 | 2003-10-23 | Richat Abbas | Oral insulin therapy |
| US7985422B2 (en) | 2002-08-05 | 2011-07-26 | Torrent Pharmaceuticals Limited | Dosage form |
| US7232828B2 (en) | 2002-08-10 | 2007-06-19 | Bethesda Pharmaceuticals, Inc. | PPAR Ligands that do not cause fluid retention, edema or congestive heart failure |
| ATE372324T1 (de) | 2003-04-30 | 2007-09-15 | Inst For Pharm Discovery Inc | Substituierte heteroarylverbindungen als inhibitoren von proteintyrosinphosphatasen |
| US20050208054A1 (en) | 2003-12-09 | 2005-09-22 | University Of Massachusetts | Methods of identifying insulin response modulators and uses therefor |
| EP1541694A1 (en) | 2003-12-12 | 2005-06-15 | Sirenade Pharmaceuticals AG | Methods of identifying, selecting and/or characterizing compounds which modulate the activity of a Src family kinase |
| US20060035302A1 (en) * | 2004-06-21 | 2006-02-16 | Applera Corporation | Kinase substrates with multiple phosphorylation sites |
| EP1827434B1 (en) | 2004-11-30 | 2014-01-15 | Amgen Inc. | Quinolines and quinazoline analogs and their use as medicaments for treating cancer |
| WO2007016975A1 (en) | 2005-07-29 | 2007-02-15 | F. Hoffmann-La Roche Ag | Kinase and phosphatase assays based on fret |
| US20070025953A1 (en) | 2005-07-27 | 2007-02-01 | Jones Michael R | Co-therapy for diabetic conditions |
| AU2006283211B2 (en) | 2005-08-22 | 2012-06-21 | Melior Pharmaceuticals I, Inc. | Methods and formulations for modulating Lyn kinase activity and treating related disorders |
| AU2006286601B2 (en) | 2005-09-01 | 2012-07-05 | F. Hoffmann-La Roche Ag | Diaminopyrimidines as P2X3 and P2X2/3 modulators |
| KR100881728B1 (ko) | 2007-05-04 | 2009-02-06 | 주식회사 하이닉스반도체 | 루테늄전극을 구비한 반도체소자 및 그 제조 방법 |
| JP2010534668A (ja) | 2007-07-23 | 2010-11-11 | メリオール・ディスカヴァリー・インコーポレイテッド | Ｉｒｓ−１及びａｋｔを活性化する方法 |
| US8552184B2 (en) * | 2008-07-03 | 2013-10-08 | Melior Pharmaceuticals I, Inc. | Compounds and methods for treating disorders related to glucose metabolism |
| WO2010078300A1 (en) | 2008-12-29 | 2010-07-08 | The Board Of Trustees Of The University Of Alabama | Dual functioning ionic liquids and salts thereof |
| US20130158055A1 (en) | 2010-05-28 | 2013-06-20 | Andrew G. Reaume | Prevention Of Pancreatic Beta Cell Degeneration |
| WO2015127474A1 (en) | 2014-02-24 | 2015-08-27 | Energesis Pharmaceuticals, Inc. | Methods and compositions for inducing differentiation of human brown adipocyte progenitors |
| JP7182605B2 (ja) * | 2017-04-10 | 2022-12-02 | メリオール・ファーマスーティカルズ・ワン・インコーポレイテッド | ｌｙｎキナーゼ活性化因子及びＴＲＰＭ８アゴニストを含む組成物及び医薬の製造におけるそれらの使用 |
-
2006
- 2006-08-22 AU AU2006283211A patent/AU2006283211B2/en active Active
- 2006-08-22 CA CA2620065A patent/CA2620065C/en active Active
- 2006-08-22 WO PCT/US2006/032788 patent/WO2007024863A2/en active Application Filing
- 2006-08-22 BR BRPI0615046A patent/BRPI0615046C1/pt active IP Right Grant
- 2006-08-22 KR KR1020147016962A patent/KR101577554B1/ko active IP Right Grant
- 2006-08-22 EP EP06813647A patent/EP1924262B1/en active Active
- 2006-08-22 NZ NZ565955A patent/NZ565955A/en unknown
- 2006-08-22 US US11/507,652 patent/US7776870B2/en active Active
- 2006-08-22 KR KR1020087006891A patent/KR101452518B1/ko active IP Right Grant
- 2006-08-22 AT AT06813647T patent/ATE533488T1/de active
- 2006-08-22 JP JP2008528076A patent/JP5113752B2/ja active Active
-
2008
- 2008-02-19 IL IL189603A patent/IL189603A0/en active IP Right Grant
- 2008-11-19 HK HK08112628.7A patent/HK1120738A1/xx unknown
-
2010
- 2010-07-15 US US12/837,067 patent/US8343985B2/en active Active
-
2012
- 2012-11-30 US US13/690,548 patent/US8835448B2/en active Active
-
2014
- 2014-02-18 US US14/182,380 patent/US9216959B2/en active Active
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2015
- 2015-11-13 US US14/941,473 patent/US9763945B2/en active Active
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2017
- 2017-08-23 US US15/684,130 patent/US10251883B2/en active Active
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2019
- 2019-02-27 US US16/286,976 patent/US11033548B2/en active Active
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2021
- 2021-05-07 US US17/314,543 patent/US20210361652A1/en active Pending
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