JP2007537231A5 - - Google Patents
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- Publication number
- JP2007537231A5 JP2007537231A5 JP2007512552A JP2007512552A JP2007537231A5 JP 2007537231 A5 JP2007537231 A5 JP 2007537231A5 JP 2007512552 A JP2007512552 A JP 2007512552A JP 2007512552 A JP2007512552 A JP 2007512552A JP 2007537231 A5 JP2007537231 A5 JP 2007537231A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrrolidin
- methanone
- compound
- salt
- pharmaceutically acceptable
- 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
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- 150000003839 salts Chemical class 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 19
- -1 —NR a R b Chemical group 0.000 claims 12
- 239000012453 solvate Substances 0.000 claims 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 2
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000004943 pyrimidin-6-yl group Chemical group N1=CN=CC=C1* 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- JDQBLAQWJBHGNH-ZFWWWQNUSA-N (3,3-difluoropyrrolidin-1-yl)-[(2s,4s)-4-(2-ethoxy-7,8-dihydro-5h-pyrido[4,3-d]pyrimidin-6-yl)pyrrolidin-2-yl]methanone Chemical compound O=C([C@H]1NC[C@H](C1)N1CC2=CN=C(N=C2CC1)OCC)N1CCC(F)(F)C1 JDQBLAQWJBHGNH-ZFWWWQNUSA-N 0.000 claims 1
- JOEYRUNHVDLBCM-GJZGRUSLSA-N (3,3-difluoropyrrolidin-1-yl)-[(2s,4s)-4-[4-(4-methylpyrimidin-2-yl)piperazin-1-yl]pyrrolidin-2-yl]methanone Chemical compound CC1=CC=NC(N2CCN(CC2)[C@H]2C[C@H](NC2)C(=O)N2CC(F)(F)CC2)=N1 JOEYRUNHVDLBCM-GJZGRUSLSA-N 0.000 claims 1
- YQVZUCGTBYZKJR-KBPBESRZSA-N (3,3-difluoropyrrolidin-1-yl)-[(2s,4s)-4-[4-([1,3]oxazolo[4,5-c]pyridin-2-yl)piperazin-1-yl]pyrrolidin-2-yl]methanone Chemical compound C1C(F)(F)CCN1C(=O)[C@H]1NC[C@@H](N2CCN(CC2)C=2OC3=CC=NC=C3N=2)C1 YQVZUCGTBYZKJR-KBPBESRZSA-N 0.000 claims 1
- UJYFJSDMPVLXQF-AAEUAGOBSA-N (3-fluoroazetidin-1-yl)-[(2s,4s)-4-[2-(trifluoromethyl)-7,8-dihydro-5h-pyrido[4,3-d]pyrimidin-6-yl]pyrrolidin-2-yl]methanone Chemical compound C1C(F)CN1C(=O)[C@H]1NC[C@@H](N2CC3=CN=C(N=C3CC2)C(F)(F)F)C1 UJYFJSDMPVLXQF-AAEUAGOBSA-N 0.000 claims 1
- SVMVVQFUWVFMQG-YJBOKZPZSA-N (3-fluoroazetidin-1-yl)-[(2s,4s)-4-[4-[2-(trifluoromethyl)quinolin-4-yl]piperazin-1-yl]pyrrolidin-2-yl]methanone Chemical compound C1C(F)CN1C(=O)[C@H]1NC[C@@H](N2CCN(CC2)C=2C3=CC=CC=C3N=C(C=2)C(F)(F)F)C1 SVMVVQFUWVFMQG-YJBOKZPZSA-N 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- FEWIVIWLJAYUNJ-HOTGVXAUSA-N 2-[4-[(3s,5s)-5-(3-fluoroazetidine-1-carbonyl)pyrrolidin-3-yl]piperazin-1-yl]pyridine-3-carbonitrile Chemical compound C1C(F)CN1C(=O)[C@H]1NC[C@@H](N2CCN(CC2)C=2C(=CC=CN=2)C#N)C1 FEWIVIWLJAYUNJ-HOTGVXAUSA-N 0.000 claims 1
- JORHXWUOXGUKMM-ULQDDVLXSA-N 2-[4-[(3s,5s)-5-[(3s)-3-fluoropyrrolidine-1-carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyridine-3-carbonitrile Chemical compound C1[C@@H](F)CCN1C(=O)[C@H]1NC[C@@H](N2CCN(CC2)C=2C(=CC=CN=2)C#N)C1 JORHXWUOXGUKMM-ULQDDVLXSA-N 0.000 claims 1
- 208000010444 Acidosis Diseases 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 208000007848 Alcoholism Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000010392 Bone Fractures Diseases 0.000 claims 1
- 206010065687 Bone loss Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 208000032781 Diabetic cardiomyopathy Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010061818 Disease progression Diseases 0.000 claims 1
- 206010013883 Dwarfism Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 206010017076 Fracture Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 206010056438 Growth hormone deficiency Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000031773 Insulin resistance syndrome Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010027417 Metabolic acidosis Diseases 0.000 claims 1
- 208000029725 Metabolic bone disease Diseases 0.000 claims 1
- 206010049088 Osteopenia Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 201000007930 alcohol dependence Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 206010016256 fatigue Diseases 0.000 claims 1
- QWEWGXUTRTXFRF-KBPBESRZSA-N gosogliptin Chemical compound C1C(F)(F)CCN1C(=O)[C@H]1NC[C@@H](N2CCN(CC2)C=2N=CC=CN=2)C1 QWEWGXUTRTXFRF-KBPBESRZSA-N 0.000 claims 1
- 230000010243 gut motility Effects 0.000 claims 1
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 208000000509 infertility Diseases 0.000 claims 1
- 230000036512 infertility Effects 0.000 claims 1
- 231100000535 infertility Toxicity 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 206010022437 insomnia Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 231100000397 ulcer Toxicity 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 230000003313 weakening effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57030004P | 2004-05-12 | 2004-05-12 | |
| US66430505P | 2005-03-21 | 2005-03-21 | |
| PCT/IB2005/001194 WO2005116014A1 (en) | 2004-05-12 | 2005-04-29 | Proline derivatives and their use as dipeptidyl peptidase iv inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007537231A JP2007537231A (ja) | 2007-12-20 |
| JP2007537231A5 true JP2007537231A5 (https=) | 2008-04-10 |
| JP4227660B2 JP4227660B2 (ja) | 2009-02-18 |
Family
ID=34966115
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007512552A Expired - Fee Related JP4227660B2 (ja) | 2004-05-12 | 2005-04-29 | ジペプチジルペプチダーゼｉｖインヒビターとしてのプロリン誘導体およびそれらの使用 |
Country Status (36)
Families Citing this family (130)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1368349B1 (de) * | 2001-02-24 | 2007-02-14 | Boehringer Ingelheim Pharma GmbH & Co.KG | Xanthinderivate, deren herstellung und deren verwendung als arzneimittel |
| 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 |
| PL1753748T3 (pl) | 2004-05-12 | 2010-01-29 | Pfizer Prod Inc | Pochodne proliny i ich zastosowanie jako inhibitorów peptydazy dipeptylowej IV |
| 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 |
| WO2006071875A1 (en) | 2004-12-29 | 2006-07-06 | Millennium Pharmaceuticals, Inc. | Compounds useful as chemokine receptor antagonists |
| WO2006071958A1 (en) | 2004-12-29 | 2006-07-06 | Millennium Pharmaceuticals, Inc. | Compounds useful as chemokine receptor antagonists |
| WO2006073167A1 (ja) * | 2005-01-07 | 2006-07-13 | Ono Pharmaceutical Co., Ltd. | ピロリジン誘導体 |
| 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 |
| PE20071221A1 (es) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas |
| AU2007235876A1 (en) | 2006-04-12 | 2007-10-18 | Probiodrug Ag | Enzyme inhibitors |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| EP2540725A1 (de) | 2006-05-04 | 2013-01-02 | Boehringer Ingelheim International GmbH | Polymorphe von 1-((4-Methyl-chinazolin-2-yl)methyl)-3-methyl-7-(2-butin-1-yl)-8-(3-(R)-amino-piperidin-1-yl)xanthin |
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| TW200815405A (en) * | 2006-06-09 | 2008-04-01 | Astrazeneca Ab | Novel compounds |
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| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| ATE554085T1 (de) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | Neue inhibitoren von glutaminylcyclase |
| EP2142514B1 (en) | 2007-04-18 | 2014-12-24 | Probiodrug AG | Thiourea derivatives as glutaminyl cyclase inhibitors |
| PE20090987A1 (es) * | 2007-08-16 | 2009-08-14 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de pirazol-o-glucosido |
| 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. |
| UA108596C2 (xx) | 2007-11-09 | 2015-05-25 | Інгібітори пептиддеформілази | |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| EP2108960A1 (en) | 2008-04-07 | 2009-10-14 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY |
| PE20100156A1 (es) * | 2008-06-03 | 2010-02-23 | Boehringer Ingelheim Int | Tratamiento de nafld |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| BRPI0916997A2 (pt) | 2008-08-06 | 2020-12-15 | Boehringer Ingelheim International Gmbh | Inibidor de dpp-4 e seu uso |
| NZ604091A (en) * | 2008-08-15 | 2014-08-29 | Boehringer Ingelheim Int | Purin derivatives for use in the treatment of fab-related diseases |
| CN102149407A (zh) | 2008-09-10 | 2011-08-10 | 贝林格尔.英格海姆国际有限公司 | 治疗糖尿病和相关病症的组合疗法 |
| 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 |
| WO2010071819A1 (en) * | 2008-12-19 | 2010-06-24 | Schering Corporation | Bicyclic heterocyclic derivatives and methods of use thereof |
| CN102256976A (zh) | 2008-12-23 | 2011-11-23 | 贝林格尔.英格海姆国际有限公司 | 有机化合物的盐形式 |
| 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 |
| AR075204A1 (es) | 2009-01-29 | 2011-03-16 | Boehringer Ingelheim Int | Inhibidores de dpp-4 y composiciones farmaceuticas que los comprenden, utiles para tratar enfermedades metabolicas en pacientes pediatricos, particularmente diabetes mellitus tipo 2 |
| AU2010212823B2 (en) | 2009-02-13 | 2016-01-28 | Boehringer Ingelheim International Gmbh | Antidiabetic medications comprising a DPP-4 inhibitor (linagliptin) optionally in combination with other antidiabetics |
| JP5685550B2 (ja) | 2009-02-13 | 2015-03-18 | 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 | Ｓｇｌｔ２阻害剤、ｄｐｐ−ｉｖ阻害剤、更に必要により抗糖尿病薬を含む医薬組成物及びその使用 |
| AR077642A1 (es) | 2009-07-09 | 2011-09-14 | Arena Pharm Inc | Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo |
| JP5934645B2 (ja) | 2009-09-11 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体 |
| KR20240090632A (ko) | 2009-11-27 | 2024-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| EP2338888A1 (en) | 2009-12-24 | 2011-06-29 | Almirall, S.A. | Imidazopyridine derivatives as JAK inhibitors |
| JP6026284B2 (ja) | 2010-03-03 | 2016-11-16 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤 |
| NZ602312A (en) | 2010-03-10 | 2014-02-28 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
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| DK2547679T3 (en) | 2010-03-19 | 2016-01-11 | Pfizer | 2,3 dihydro-1H-inden-1-yl-2,7-diazaspiro [3.6] nonane derivatives and their use as antagonists or inverse agonists of ghrelin receptor |
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| CN103917529B (zh) | 2011-11-11 | 2016-08-17 | 辉瑞大药厂 | 2-硫代嘧啶酮类 |
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