JP2010503620A5 - - Google Patents
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- Publication number
- JP2010503620A5 JP2010503620A5 JP2009527455A JP2009527455A JP2010503620A5 JP 2010503620 A5 JP2010503620 A5 JP 2010503620A5 JP 2009527455 A JP2009527455 A JP 2009527455A JP 2009527455 A JP2009527455 A JP 2009527455A JP 2010503620 A5 JP2010503620 A5 JP 2010503620A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- lower alkyl
- hydrogen
- independently selected
- compound
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 62
- 229910052739 hydrogen Inorganic materials 0.000 claims 48
- 239000001257 hydrogen Substances 0.000 claims 48
- 150000002431 hydrogen Chemical class 0.000 claims 36
- 150000001875 compounds Chemical class 0.000 claims 27
- 239000003814 drug Substances 0.000 claims 16
- 229940124597 therapeutic agent Drugs 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 206010012735 Diarrhoea Diseases 0.000 claims 11
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 9
- 125000002252 acyl group Chemical group 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 239000003112 inhibitor Substances 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 7
- 230000003287 optical effect Effects 0.000 claims 7
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- 125000006239 protecting group Chemical group 0.000 claims 5
- 206010006895 Cachexia Diseases 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 4
- 125000005026 carboxyaryl group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 239000003085 diluting agent Substances 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 208000030507 AIDS Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010047700 Vomiting Diseases 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 230000002496 gastric effect Effects 0.000 claims 2
- 230000005176 gastrointestinal motility Effects 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 230000031891 intestinal absorption Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 241000193163 Clostridioides difficile Species 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000004232 Enteritis Diseases 0.000 claims 1
- 208000014540 Functional gastrointestinal disease Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 206010052402 Gastrointestinal hypermotility Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000031649 Postoperative Nausea and Vomiting Diseases 0.000 claims 1
- 206010049416 Short-bowel syndrome Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000019902 chronic diarrheal disease Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 201000006549 dyspepsia Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 230000035873 hypermotility Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 150000002678 macrocyclic compounds Chemical class 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- XQQBUAPQHNYYRS-UHFFFAOYSA-N Cc1ccc[s]1 Chemical compound Cc1ccc[s]1 XQQBUAPQHNYYRS-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US82523706P | 2006-09-11 | 2006-09-11 | |
| US60/825,237 | 2006-09-11 | ||
| PCT/US2007/019705 WO2008033328A2 (en) | 2006-09-11 | 2007-09-11 | Macrocyclic antagonists of the motilin receptor for treatment of gastrointestinal dysmotility disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010503620A JP2010503620A (ja) | 2010-02-04 |
| JP2010503620A5 true JP2010503620A5 (https=) | 2010-11-04 |
| JP5684474B2 JP5684474B2 (ja) | 2015-03-11 |
Family
ID=39030996
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009527455A Expired - Fee Related JP5684474B2 (ja) | 2006-09-11 | 2007-09-11 | 胃腸の運動障害疾患の治療のためのモチリン受容体の大環状アンタゴニスト |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9133235B2 (https=) |
| EP (2) | EP2054429B1 (https=) |
| JP (1) | JP5684474B2 (https=) |
| CN (1) | CN101528765B (https=) |
| CA (1) | CA2662897C (https=) |
| WO (1) | WO2008033328A2 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7521420B2 (en) | 2003-06-18 | 2009-04-21 | Tranzyme Pharma, Inc. | Macrocyclic antagonists of the motilin receptor |
| US7491695B2 (en) | 2003-06-18 | 2009-02-17 | Tranzyme Pharma Inc. | Methods of using macrocyclic modulators of the ghrelin receptor |
| US20080287371A1 (en) * | 2007-05-17 | 2008-11-20 | Tranzyme Pharma Inc. | Macrocyclic antagonists of the motilin receptor for modulation of the migrating motor complex |
| US8748650B2 (en) | 2008-08-29 | 2014-06-10 | Jsr Corporation | Method for production of N-carboxy amino acid anhydride and amino acid carbamate compound |
| JP2010078398A (ja) * | 2008-09-25 | 2010-04-08 | Saitama Univ | 消化管運動機能物質のスクリーニング方法 |
| JP2013508410A (ja) * | 2009-10-23 | 2013-03-07 | トランザイム・ファーマ，インコーポレイテッド | セリンプロテアーゼ酵素の大環状阻害剤を使用する方法 |
| EP2493910A1 (en) | 2009-10-30 | 2012-09-05 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same |
| JP2014505059A (ja) * | 2011-01-18 | 2014-02-27 | ジェネラル アトミクス | ヒドロラーゼ酵素基質およびその使用 |
| EP2684863B1 (en) * | 2011-03-10 | 2017-05-24 | National University Corporation Nagoya University | Iodoarene derivative, method for producing optically active spirolactone compound using same, and method for producing optically active cyclization adduct |
| CN102557989B (zh) * | 2011-12-19 | 2013-12-25 | 深圳翰宇药业股份有限公司 | 优利莫瑞林中间体以及优利莫瑞林制备方法 |
| US20180264061A1 (en) * | 2015-01-09 | 2018-09-20 | Jaguar Animal Health | Methods of Treating Diarrhea in Companion Animals |
| CN111747979B (zh) * | 2020-07-07 | 2021-10-08 | 新乡海滨药业有限公司 | 一种美罗培南关键中间体n-三甲基硅咪唑的制备方法 |
Family Cites Families (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6187625A (ja) | 1984-10-05 | 1986-05-06 | Satoshi Omura | 消化管収縮運動促進剤 |
| US5008249A (en) | 1985-08-31 | 1991-04-16 | Kitasato Kenkyusho | Therapeutic method of stimulating digestive tract contractile motion in mammals |
| US5175150A (en) | 1985-08-31 | 1992-12-29 | Kitasato, Kenkyusho | Erythromycin derivative |
| US5695952A (en) | 1986-09-12 | 1997-12-09 | Kyowa Hakko Kogyo Co., Ltd. | Method for producing Leu13 !motilin |
| US5420113A (en) | 1986-09-12 | 1995-05-30 | Kyowa Hakko Kogyo Co., Ltd. | [Leu13]motilin, DNAs coding for same and methods for producing same |
| US4920102A (en) | 1988-04-18 | 1990-04-24 | Eli Lilly And Company | Method for treating gastrointestinal disorders |
| US5459049A (en) | 1989-01-06 | 1995-10-17 | Sanwa Kagaku Kenkyushko Co., Ltd. | Motilin-like polypeptide and use thereof |
| EP0378078A1 (en) | 1989-01-06 | 1990-07-18 | Sanwa Kagaku Kenkyusho Co., Ltd. | Motilin-like polypeptide and use thereof |
| CA2103913A1 (en) | 1991-04-09 | 1992-10-10 | Leslie A. Freiberg | Macrocyclic lactam prokinetic agents |
| US5523401A (en) | 1991-04-09 | 1996-06-04 | Abbott Laboratories | Macrocyclic lactam prokinetic agents |
| DE4200145A1 (de) | 1992-01-07 | 1993-07-08 | Kali Chemie Pharma Gmbh | 7,10-epoxy-oxacyclododecan-derivate, verfahren und zwischenprodukte zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| HK1010054A1 (en) | 1992-01-21 | 1999-06-11 | Abbott Laboratories | 4"-deoxyerythromycin derivatives |
| CA2092045C (en) | 1992-03-19 | 2004-08-10 | Setsuo Harada | Erythromycin derivatives, preparation and use thereof |
| MY113693A (en) | 1992-05-26 | 2002-05-31 | Chugai Pharmaceutical Co Ltd | Erythromycin derivatives having an enterokinesis stimulating action |
| US5422341A (en) | 1993-08-06 | 1995-06-06 | Ohmeda Pharmaceutical Products Division Inc. | Motilin-like polypeptides with gastrointestinal motor stimulating activity |
| US5470830A (en) | 1993-08-06 | 1995-11-28 | Ohmeda Pharmaceutical Products Division Inc. | Motilin-like polypeptides that inhibit gastrointestinal motor activity |
| JP3449766B2 (ja) | 1993-11-19 | 2003-09-22 | 中外製薬株式会社 | モチリンアンタゴニスト |
| US6077943A (en) | 1996-03-01 | 2000-06-20 | Takeda Chemical Industries, Ltd. | Method of producing erythromycin derivative |
| JP3901239B2 (ja) | 1996-03-13 | 2007-04-04 | 大正製薬株式会社 | アリールアルカン誘導体 |
| US5734012A (en) | 1996-05-16 | 1998-03-31 | Ohmeda Pharmaceutical Products Division Inc. | Cyclic motilin-like polypeptides with gastrointestinal motor stimulating activity |
| US5712253A (en) | 1996-06-18 | 1998-01-27 | Abbott Laboratories | Macrocyclic 13-membered ring derivatives of erythromycins A and B |
| DE19644195A1 (de) | 1996-10-24 | 1998-04-30 | Solvay Pharm Gmbh | 10,13,15-Trioxatricyclo[9.2.1.1.·9·.·6·]-pentadecanon-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| US5922849A (en) | 1996-11-22 | 1999-07-13 | Abbott Laboratories | Process for preparation of N-demethyl-4"-deoxy-erthromycins A and B |
| WO1998023629A1 (fr) | 1996-11-26 | 1998-06-04 | Chugai Seiyaku Kabushiki Kaisha | Composes de macrolides comportant une chaine a 13 elements, medicament les contenant et leur procede de preparation |
| CA2284733C (en) | 1997-03-24 | 2010-10-26 | Zymogenetics, Inc. | Motilin homologs |
| US6291653B1 (en) | 1997-03-24 | 2001-09-18 | Zymogenetics, Inc. | Antibodies to motilin homologs |
| US6380158B1 (en) | 1997-03-24 | 2002-04-30 | Zymogenetics, Inc. | Motilin homologs |
| TW460478B (en) | 1997-08-15 | 2001-10-21 | Chugai Pharmaceutical Co Ltd | Phenethylamine derivatives |
| US5972939A (en) | 1997-10-28 | 1999-10-26 | Ortho-Mcneil Pharmaceutical, Inc. | Cyclopentene derivatives useful as antagonists of the motilin receptor |
| US6165985A (en) | 1998-02-13 | 2000-12-26 | Solvay Pharmaceuticals Gmbh | 11-acetyl-12,13-dioxabicyclo[8.2.1]-tridecenone derivatives, processes for their preparation and pharmaceutical compositions comprising them |
| US6084079A (en) | 1998-05-15 | 2000-07-04 | Keyes; Robert F. | Process for preparing N-demethyl-N-alkyl erythromycin derivatives |
| CA2330251A1 (en) | 1998-06-12 | 1999-12-16 | Merck & Co., Inc. | Cloning and identification of the motilin receptor |
| TW509699B (en) | 1998-09-24 | 2002-11-11 | Chugau Pharmaceutical Co Ltd | Ethylamine derivatives |
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| AU2001250820A1 (en) | 2000-03-13 | 2001-09-24 | Ortho-Mcneil Pharmaceutical, Inc. | Novel cyclohexene derivatives useful as antagonists of the motilin receptor |
| US6511980B2 (en) | 2000-05-05 | 2003-01-28 | Ortho Mcneil Pharmaceutical, Inc. | Substituted diamine derivatives useful as motilin antagonists |
| DE10040630A1 (de) | 2000-08-16 | 2002-03-07 | Thomas Hupp | Stent zur Implantation in die Halsschlagader |
| EP1312612A4 (en) | 2000-08-24 | 2004-09-22 | Chugai Pharmaceutical Co Ltd | CYCLIC PEPTIDE DERIVATIVE |
| AU2002225724A1 (en) | 2000-12-01 | 2002-07-08 | Kosan Biosciences, Inc. | Motilide compounds |
| US20020094962A1 (en) | 2000-12-01 | 2002-07-18 | Gary Ashley | Motilide compounds |
| WO2002059141A1 (fr) | 2001-01-25 | 2002-08-01 | Chugai Seiyaku Kabushiki Kaisha | Derives peptidiques |
| KR20020066476A (ko) | 2001-02-12 | 2002-08-19 | 쥬가이 세이야쿠 가부시키가이샤 | 펩타이드 유도체의 제조방법 |
| JP2004530108A (ja) | 2001-02-15 | 2004-09-30 | コーサン バイオサイエンシーズ， インコーポレイテッド | 治療効力を評価するための方法 |
| DE50204789D1 (de) | 2001-05-10 | 2005-12-08 | Solvay Pharm Gmbh | Neue 1-amidomethylcarbonyl-piperidinderivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| ES2316805T3 (es) | 2002-08-29 | 2009-04-16 | Pfizer Inc. | Compuestos motilidos. |
| US7521420B2 (en) | 2003-06-18 | 2009-04-21 | Tranzyme Pharma, Inc. | Macrocyclic antagonists of the motilin receptor |
| US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
| US7491695B2 (en) | 2003-06-18 | 2009-02-17 | Tranzyme Pharma Inc. | Methods of using macrocyclic modulators of the ghrelin receptor |
| US7550431B2 (en) | 2003-07-31 | 2009-06-23 | Tranzyme Pharma Inc. | Spatially-defined macrocycles incorporating peptide bond surrogates |
| ATE490264T1 (de) | 2003-07-31 | 2010-12-15 | Tranzyme Pharma Inc | Räumlich definierte makrocyclische verbindungen, die sich für die entdeckung von arzneimittel eignen |
| US7407941B2 (en) | 2003-08-26 | 2008-08-05 | Pfizer, Inc. | N-desmethyl-N-substituted-11-deoxyerythromycin compounds |
| US7338954B2 (en) | 2003-09-17 | 2008-03-04 | Bristol-Myers Squibb Company | Compounds useful as motilin agonists and method |
| US7262195B2 (en) | 2003-09-17 | 2007-08-28 | Bristol-Myers Squibb Company | Compounds useful as motilin agonists and method |
| US7211568B2 (en) | 2003-12-18 | 2007-05-01 | Kosan Biosciences Incorporated | 9-Desoxoerythromycin compounds as prokinetic agents |
| WO2006046977A1 (en) | 2004-10-26 | 2006-05-04 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor antagonists and methods of using the same |
| TW200633714A (en) | 2004-12-28 | 2006-10-01 | Chugai Pharmaceutical Co Ltd | Drugs for the treatment and/or prophylaxis of gastroparesis symptom |
| US7582611B2 (en) | 2005-05-24 | 2009-09-01 | Pfizer Inc. | Motilide compounds |
| EP1891090A2 (en) | 2005-06-13 | 2008-02-27 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same |
| US20060293243A1 (en) | 2005-06-17 | 2006-12-28 | Navneet Puri | Stable, buffered, pharmaceutical compositions including motilin-like peptides |
| US20060287243A1 (en) | 2005-06-17 | 2006-12-21 | Navneet Puri | Stable pharmaceutical compositions including motilin-like peptides |
-
2007
- 2007-09-11 EP EP20070838009 patent/EP2054429B1/en not_active Ceased
- 2007-09-11 EP EP20110075225 patent/EP2431380A3/en not_active Withdrawn
- 2007-09-11 US US12/440,802 patent/US9133235B2/en active Active
- 2007-09-11 CA CA2662897A patent/CA2662897C/en not_active Expired - Fee Related
- 2007-09-11 JP JP2009527455A patent/JP5684474B2/ja not_active Expired - Fee Related
- 2007-09-11 CN CN200780033494.1A patent/CN101528765B/zh not_active Expired - Fee Related
- 2007-09-11 WO PCT/US2007/019705 patent/WO2008033328A2/en not_active Ceased
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