JP2013540714A5 - - Google Patents
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- Publication number
- JP2013540714A5 JP2013540714A5 JP2013526503A JP2013526503A JP2013540714A5 JP 2013540714 A5 JP2013540714 A5 JP 2013540714A5 JP 2013526503 A JP2013526503 A JP 2013526503A JP 2013526503 A JP2013526503 A JP 2013526503A JP 2013540714 A5 JP2013540714 A5 JP 2013540714A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- heterocyclyl
- carbocyclyl
- substituted
- 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
- 125000000623 heterocyclic group Chemical group 0.000 claims description 53
- 125000001424 substituent group Chemical group 0.000 claims description 48
- 125000001072 heteroaryl group Chemical group 0.000 claims description 34
- 125000000217 alkyl group Chemical group 0.000 claims description 33
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 30
- 125000003118 aryl group Chemical group 0.000 claims description 25
- 150000001875 compounds Chemical class 0.000 claims description 20
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 17
- 229910052717 sulfur Inorganic materials 0.000 claims description 15
- 229910052760 oxygen Inorganic materials 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 8
- 229910052757 nitrogen Inorganic materials 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 6
- 125000001153 fluoro group Chemical group F* 0.000 claims description 6
- -1 aryl-C 1-3 -alkyl Chemical group 0.000 claims description 5
- 125000002541 furyl group Chemical group 0.000 claims description 5
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 5
- 125000002971 oxazolyl group Chemical group 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 5
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 5
- 125000004076 pyridyl group Chemical group 0.000 claims description 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 5
- 125000000335 thiazolyl group Chemical group 0.000 claims description 5
- 125000001425 triazolyl group Chemical group 0.000 claims description 5
- 125000002393 azetidinyl group Chemical group 0.000 claims description 4
- 125000003566 oxetanyl group Chemical group 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 125000002883 imidazolyl group Chemical group 0.000 claims description 3
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims description 3
- 125000001544 thienyl group Chemical group 0.000 claims description 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 2
- 102000000452 Acetyl-CoA carboxylase Human genes 0.000 claims description 2
- 108010016219 Acetyl-CoA carboxylase Proteins 0.000 claims description 2
- 108010018763 Biotin carboxylase Proteins 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 2
- 125000001070 dihydroindolyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 125000004611 dihydroisoindolyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims description 2
- 125000005044 dihydroquinolinyl group Chemical group N1(CC=CC2=CC=CC=C12)* 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 description 4
- 125000005842 heteroatom Chemical group 0.000 description 3
- 0 *c1ccc(*)cc1 Chemical compound *c1ccc(*)cc1 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 125000005046 dihydronaphthyl group Chemical group 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 238000011282 treatment Methods 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10175456.2 | 2010-09-06 | ||
| EP10175456 | 2010-09-06 | ||
| PCT/EP2011/065332 WO2012032014A1 (en) | 2010-09-06 | 2011-09-05 | Ethyne derivatives, pharmaceutical compositions and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013540714A JP2013540714A (ja) | 2013-11-07 |
| JP2013540714A5 true JP2013540714A5 (OSRAM) | 2014-10-23 |
| JP5928737B2 JP5928737B2 (ja) | 2016-06-01 |
Family
ID=44584179
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013526503A Active JP5928737B2 (ja) | 2010-09-06 | 2011-09-05 | エチン誘導体、医薬組成物及びその使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US8877754B2 (OSRAM) |
| EP (1) | EP2614054B1 (OSRAM) |
| JP (1) | JP5928737B2 (OSRAM) |
| WO (1) | WO2012032014A1 (OSRAM) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6378752B2 (ja) * | 2013-05-17 | 2018-08-22 | 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 | ピロリジン誘導体、その医薬組成物及び使用 |
| WO2015036892A1 (en) | 2013-09-12 | 2015-03-19 | Pfizer Inc. | Use of acetyl-coa carboxylase inhibitors for treating acne vulgaris |
| EP2924027A1 (en) * | 2014-03-28 | 2015-09-30 | Basf Se | Substituted [1,2,4]triazole and imidazole fungicidal compounds |
| SI3233843T1 (sl) | 2014-12-16 | 2019-12-31 | Novartis Ag | Spojine izoksazol hidroksamične kisline kot LPXC inhibitorji |
| WO2017117708A1 (en) * | 2016-01-05 | 2017-07-13 | Hua Medicine (Shanghai) Ltd. | Pyrazole derivatives |
| SG11201810656WA (en) | 2016-06-14 | 2018-12-28 | Novartis Ag | Crystalline form of (r)-4-(5-(cyclopropylethynyl)isoxazol-3-yl)-n-hydroxy-2-methyl-2-(methylsulfonyl)butanamide as an antibacterial agent |
| MA53430A (fr) * | 2018-08-24 | 2021-06-30 | Xeniopro GmbH | Nouveaux composés |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4042584A (en) * | 1974-08-19 | 1977-08-16 | Merck & Co., Inc. | Ethynylaryl phenyl cyclopropyl thiazines and morpholines |
| HUT73813A (en) * | 1993-06-30 | 1996-09-30 | Wellcome Found | Anti-athero-sclerotic diaryl compounds, process to prepare them and pharmaceutical compositions contg. them |
| CA2407416C (en) | 2000-05-03 | 2006-07-18 | Paige Erin Mahaney | Alkynyl phenyl heteroaromatic glucokinase activators |
| WO2002024656A1 (en) * | 2000-09-22 | 2002-03-28 | Nihon Nohyaku Co., Ltd. | N-(4-pyrazolyl)amide derivatives, chemicals for agricultural and horticultural use, and usage of the same |
| DE10219294A1 (de) * | 2002-04-25 | 2003-11-13 | Schering Ag | Substituierte N-(1,4,5,6-Tetrahydro-cyclopentapyrazol-3-yl)-Derivate, deren Herstellung und Verwendung als Arzneimittel |
| US7524862B2 (en) | 2004-04-14 | 2009-04-28 | Boehringer Ingelheim International Gmbh | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
| WO2008002671A2 (en) | 2006-06-29 | 2008-01-03 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors |
| EA020885B1 (ru) | 2008-01-22 | 2015-02-27 | Мерк Патент Гмбх | Ингибиторы протеинкиназы и их применение |
| US8501804B2 (en) * | 2008-10-27 | 2013-08-06 | Takeda Pharmaceutical Company Limited | Bicyclic compound |
-
2011
- 2011-08-17 US US13/211,475 patent/US8877754B2/en active Active
- 2011-09-05 JP JP2013526503A patent/JP5928737B2/ja active Active
- 2011-09-05 EP EP11754650.7A patent/EP2614054B1/en active Active
- 2011-09-05 WO PCT/EP2011/065332 patent/WO2012032014A1/en not_active Ceased
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