JP2013545791A5 - - Google Patents
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- Publication number
- JP2013545791A5 JP2013545791A5 JP2013543816A JP2013543816A JP2013545791A5 JP 2013545791 A5 JP2013545791 A5 JP 2013545791A5 JP 2013543816 A JP2013543816 A JP 2013543816A JP 2013543816 A JP2013543816 A JP 2013543816A JP 2013545791 A5 JP2013545791 A5 JP 2013545791A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- substituted
- ring
- cycloalkyl
- 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
- 125000001424 substituent group Chemical group 0.000 claims description 32
- 229910052799 carbon Inorganic materials 0.000 claims description 31
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
- -1 1,2,3,6-tetrahydro-pyridin-4-yl ring Chemical group 0.000 claims description 28
- 125000003118 aryl group Chemical group 0.000 claims description 23
- 229910052717 sulfur Inorganic materials 0.000 claims description 21
- 229910052760 oxygen Inorganic materials 0.000 claims description 19
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 125000002837 carbocyclic group Chemical group 0.000 claims description 17
- 150000001875 compounds Chemical class 0.000 claims description 17
- 125000000217 alkyl group Chemical group 0.000 claims description 16
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 15
- 125000000623 heterocyclic group Chemical group 0.000 claims description 15
- 125000005842 heteroatom Chemical group 0.000 claims description 13
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 8
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 6
- 125000001153 fluoro group Chemical group F* 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 4
- 239000000969 carrier Substances 0.000 claims description 3
- 239000003085 diluting agent Substances 0.000 claims description 3
- 201000010099 disease Diseases 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 125000006432 1-methyl cyclopropyl group Chemical group [H]C([H])([H])C1(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims description 2
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 claims description 2
- 230000004913 activation Effects 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 229920001577 copolymer Chemical class 0.000 claims 1
- YAEXNBGOCUGYHW-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1C(C1)Oc(nc2)c1cc2-c(cc1)ccc1S(C)(O)=O)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1C(C1)Oc(nc2)c1cc2-c(cc1)ccc1S(C)(O)=O)=O YAEXNBGOCUGYHW-UHFFFAOYSA-N 0.000 description 1
- PZCMKJKGSWYCBG-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1C(C1)Oc2c1cc(-c(cc1)ccc1S(C)(O)=O)nn2)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1C(C1)Oc2c1cc(-c(cc1)ccc1S(C)(O)=O)nn2)=O PZCMKJKGSWYCBG-UHFFFAOYSA-N 0.000 description 1
- 0 CC(C)(CC(CC1)C2(*)OC(**=*C([Al])=I)=C(*)C2)CN1C(O*)=O Chemical compound CC(C)(CC(CC1)C2(*)OC(**=*C([Al])=I)=C(*)C2)CN1C(O*)=O 0.000 description 1
- GBDYAPQZIGXIOC-UHFFFAOYSA-N CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(c(C)c1)ncc1S(C)(=O)=O)=O Chemical compound CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(c(C)c1)ncc1S(C)(=O)=O)=O GBDYAPQZIGXIOC-UHFFFAOYSA-N 0.000 description 1
- YTPCWZXAOUDNBY-UHFFFAOYSA-N CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(c(C)c1)ncc1S(C)=O)=O Chemical compound CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(c(C)c1)ncc1S(C)=O)=O YTPCWZXAOUDNBY-UHFFFAOYSA-N 0.000 description 1
- HLFPHPBEPQBUTB-UHFFFAOYSA-N CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(cc1)ccc1C(NC)=O)=O Chemical compound CC(C)OC(N(CC1)CCC1C(C1)Oc(cc2)c1cc2-c(cc1)ccc1C(NC)=O)=O HLFPHPBEPQBUTB-UHFFFAOYSA-N 0.000 description 1
- LZCLRPYCYCEKBS-UHFFFAOYSA-N CC1(CN(C)CC1)O Chemical compound CC1(CN(C)CC1)O LZCLRPYCYCEKBS-UHFFFAOYSA-N 0.000 description 1
- KPGFWZMUGOLTFK-UHFFFAOYSA-N CN(C1)CC1(F)[F]C Chemical compound CN(C1)CC1(F)[F]C KPGFWZMUGOLTFK-UHFFFAOYSA-N 0.000 description 1
- NVBHAFAVARZYFO-UHFFFAOYSA-N CN(C1)CC1OC Chemical compound CN(C1)CC1OC NVBHAFAVARZYFO-UHFFFAOYSA-N 0.000 description 1
- FLVFPAIGVBQGET-UHFFFAOYSA-N CN(CC1)CC1O Chemical compound CN(CC1)CC1O FLVFPAIGVBQGET-UHFFFAOYSA-N 0.000 description 1
- VJUDVVHGQMPPEI-UHFFFAOYSA-N CNCC1OCCC1 Chemical compound CNCC1OCCC1 VJUDVVHGQMPPEI-UHFFFAOYSA-N 0.000 description 1
- VCVSKQNPBCXRAM-UHFFFAOYSA-N CNCc1c[o]cn1 Chemical compound CNCc1c[o]cn1 VCVSKQNPBCXRAM-UHFFFAOYSA-N 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10195814.8 | 2010-12-17 | ||
| EP10195814 | 2010-12-17 | ||
| PCT/EP2011/073067 WO2012080476A1 (en) | 2010-12-17 | 2011-12-16 | Fused dihydropyrans as gpr119 modulators for the treatment of diabetes, obesity and related diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013545791A JP2013545791A (ja) | 2013-12-26 |
| JP2013545791A5 true JP2013545791A5 (https=) | 2015-02-05 |
| JP6011543B2 JP6011543B2 (ja) | 2016-10-19 |
Family
ID=45470522
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013543816A Active JP6011543B2 (ja) | 2010-12-17 | 2011-12-16 | 糖尿病、肥満および関連疾患の治療のためのｇｐｒ１１９モジュレーターとしての縮合ジヒドロフラン |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8669271B2 (https=) |
| EP (1) | EP2651931B1 (https=) |
| JP (1) | JP6011543B2 (https=) |
| AR (1) | AR084349A1 (https=) |
| UY (1) | UY33805A (https=) |
| WO (1) | WO2012080476A1 (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8481731B2 (en) | 2009-06-24 | 2013-07-09 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| UY33805A (es) | 2010-12-17 | 2012-07-31 | Boehringer Ingelheim Int | ?Derivados de dihidrobenzofuranil-piperidinilo, aza-dihidrobenzofuranilpiperidinilo y diaza-dihidrobenzofuranil-piperidinilo, composiciones farmacéuticas que los contienen y usos de los mismos?. |
| US8778926B2 (en) * | 2011-01-21 | 2014-07-15 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| US8822471B2 (en) | 2011-03-14 | 2014-09-02 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| KR101913619B1 (ko) * | 2011-06-09 | 2018-12-28 | 리젠 파마슈티컬스 소시에떼 아노님 | Gpr-119의 조절제로서의 신규한 화합물 |
| US8921398B2 (en) | 2011-06-09 | 2014-12-30 | Boehringer Ingelheim International Gmbh | N-cyclopropyl-N-piperidinyl-amide derivatives, pharmaceutical compositions and uses thereof |
| US8853239B2 (en) | 2011-12-09 | 2014-10-07 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| US9012456B2 (en) * | 2012-02-28 | 2015-04-21 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| US8809361B2 (en) * | 2012-05-07 | 2014-08-19 | Boehringer Ingelheim International Gmbh | 2,3-dihydrofuro[2,3-c]pyridines, their use as modulators of the G-protein-coupled receptor GPR119 and pharmaceutical compositions thereof |
| JP6119088B2 (ja) * | 2012-06-12 | 2017-04-26 | 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 | ２，３−ジヒドロ−フロ［２，３−ｃ］ピリジン−２−イル−ピペリジン誘導体、それらを含む医薬組成物及びその使用 |
| CA2878625A1 (en) | 2012-07-11 | 2014-01-16 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| EP2984080B1 (en) | 2013-04-12 | 2017-08-30 | Bayer CropScience Aktiengesellschaft | Novel triazolinthione derivatives |
| JP6397482B2 (ja) | 2013-04-12 | 2018-09-26 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 新規トリアゾール誘導体 |
| BR112015025679A8 (pt) | 2013-04-12 | 2020-02-11 | Bayer Cropscience Ag | novos derivados de triazol |
| EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| MX373103B (es) | 2014-02-13 | 2020-04-17 | Incyte Holdings Corp | Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1). |
| SI3105218T1 (sl) | 2014-02-13 | 2019-11-29 | Incyte Corp | Ciklopropilamini kot inhibitorji LSD1 |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| US20180339976A1 (en) | 2015-04-02 | 2018-11-29 | Bayer Cropscience Aktiengesellschaft | Novel triazole derivatives |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| LT3334709T (lt) | 2015-08-12 | 2025-03-10 | Incyte Holdings Corporation | Lsd1 inhibitoriaus druskos |
| US10208030B2 (en) | 2016-04-08 | 2019-02-19 | Mankind Pharma Ltd. | GPR119 agonist compounds |
| US10526345B2 (en) * | 2016-04-08 | 2020-01-07 | Mankind Pharma Ltd. | Compounds as GPR119 agonists |
| US10954229B2 (en) | 2016-04-08 | 2021-03-23 | Mankind Pharma Ltd. | GPR119 agonist compounds |
| JP6999574B2 (ja) | 2016-04-22 | 2022-01-18 | インサイト・コーポレイション | Ｌｓｄ１阻害剤の製剤 |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| IL295825A (en) | 2020-02-28 | 2022-10-01 | Kallyope Inc | gpr40 agonists |
| WO2021236617A1 (en) | 2020-05-19 | 2021-11-25 | Kallyope, Inc. | Ampk activators |
| CA3183575A1 (en) | 2020-06-26 | 2021-12-30 | Iyassu Sebhat | Ampk activators |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007003961A2 (en) | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| US20080103123A1 (en) * | 2006-08-30 | 2008-05-01 | Biovitrum | New compounds |
| ATE528300T1 (de) * | 2006-12-06 | 2011-10-15 | Glaxosmithkline Llc | Bizyklische verbindungen und ihre verwendung als antidiabetika |
| CN101668756A (zh) * | 2007-05-04 | 2010-03-10 | 百时美施贵宝公司 | [6,6]和[6,7]-双环gpr119 g蛋白偶合受体激动剂 |
| WO2008137436A1 (en) * | 2007-05-04 | 2008-11-13 | Bristol-Myers Squibb Company | [6,5]-bicyclic gpr119 g protein-coupled receptor agonists |
| RU2443699C2 (ru) * | 2007-09-20 | 2012-02-27 | Айрм Ллк | Соединения и композиции в качестве модуляторов активности gpr119 |
| WO2009106565A1 (en) * | 2008-02-27 | 2009-09-03 | Biovitrum Ab (Publ) | Agonists of gpr119 |
| WO2009150144A1 (en) * | 2008-06-10 | 2009-12-17 | Inovacia Ab | New gpr119modulators |
| US20120016119A1 (en) * | 2009-01-22 | 2012-01-19 | Yasunori Tsuboi | NOVEL PYRROLO(2,3-d)PYRIMIDINE COMPOUND |
| JP5657518B2 (ja) * | 2009-02-18 | 2015-01-21 | 武田薬品工業株式会社 | 縮合複素環化合物 |
| EA201200046A1 (ru) | 2009-06-24 | 2012-08-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Новые соединения, фармацевтическая композиция и связанные с ними способы |
| US8481731B2 (en) | 2009-06-24 | 2013-07-09 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| WO2011140161A1 (en) | 2010-05-06 | 2011-11-10 | Bristol-Myers Squibb Company | Benzofuranyl analogues as gpr119 modulators |
| EP2566864B1 (en) | 2010-05-07 | 2014-09-03 | Boehringer Ingelheim International GmbH | Pyridazinones as gpr119 agonists |
| UY33805A (es) | 2010-12-17 | 2012-07-31 | Boehringer Ingelheim Int | ?Derivados de dihidrobenzofuranil-piperidinilo, aza-dihidrobenzofuranilpiperidinilo y diaza-dihidrobenzofuranil-piperidinilo, composiciones farmacéuticas que los contienen y usos de los mismos?. |
| US8778926B2 (en) | 2011-01-21 | 2014-07-15 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| US8822471B2 (en) | 2011-03-14 | 2014-09-02 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
-
2011
- 2011-12-15 UY UY0001033805A patent/UY33805A/es not_active Application Discontinuation
- 2011-12-16 AR ARP110104756A patent/AR084349A1/es unknown
- 2011-12-16 EP EP11807666.0A patent/EP2651931B1/en active Active
- 2011-12-16 JP JP2013543816A patent/JP6011543B2/ja active Active
- 2011-12-16 WO PCT/EP2011/073067 patent/WO2012080476A1/en not_active Ceased
- 2011-12-16 US US13/327,823 patent/US8669271B2/en active Active
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