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 (enExample) | 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 (enExample) |
| EP (1) | EP2651931B1 (enExample) |
| JP (1) | JP6011543B2 (enExample) |
| AR (1) | AR084349A1 (enExample) |
| UY (1) | UY33805A (enExample) |
| WO (1) | WO2012080476A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012530758A (ja) | 2009-06-24 | 2012-12-06 | 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 | 新規化合物、医薬組成物及びそれに関する方法 |
| 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?. |
| CN103443097A (zh) * | 2011-01-21 | 2013-12-11 | 勃林格殷格翰国际有限公司 | 作为gpr119调节剂用于治疗糖尿病、肥胖症以及相关病症的稠合的二氢呋喃化合物 |
| JP5935154B2 (ja) | 2011-03-14 | 2016-06-15 | 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 | Ｇｐｒ１１９モジュレーターとしてのｎ−シクロプロピル−ｎ−ピペリジニルベンズアミド |
| US8921398B2 (en) | 2011-06-09 | 2014-12-30 | Boehringer Ingelheim International Gmbh | N-cyclopropyl-N-piperidinyl-amide derivatives, pharmaceutical compositions and uses thereof |
| CN103958495B (zh) * | 2011-06-09 | 2018-06-22 | 理森制药股份公司 | 作为gpr-119的调节剂的化合物 |
| 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 |
| EP2858996B1 (en) | 2012-06-12 | 2016-12-07 | Boehringer Ingelheim International GmbH | 4-(2,3-Dihydro-furo[2,3-c]pyridin-2-yl)-piperidine-1-carboxylic acid ester derivatives as G-protein-coupled receptor 119 (GPR119) agonists for the treatment of metabolic disorders, such as diabetes, dyslipidemia and obesity |
| EP2872127A1 (en) | 2012-07-11 | 2015-05-20 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| US9668481B2 (en) | 2013-04-12 | 2017-06-06 | Bayer Cropscience Aktiengesellschaft | Triazole derivatives |
| US9822099B2 (en) | 2013-04-12 | 2017-11-21 | Bayer Cropscience Aktiengesellschaft | Triazole derivatives |
| JP2016522800A (ja) | 2013-04-12 | 2016-08-04 | 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 | 新規トリアゾリンチオン誘導体 |
| DK3105218T3 (da) | 2014-02-13 | 2019-11-04 | Incyte Corp | Cyclopropylaminer som lsd1-inhibitorer |
| TWI720451B (zh) | 2014-02-13 | 2021-03-01 | 美商英塞特控股公司 | 作為lsd1抑制劑之環丙胺 |
| TW201613860A (en) | 2014-02-13 | 2016-04-16 | Incyte Corp | Cyclopropylamines as LSD1 inhibitors |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| US9695168B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016156294A1 (en) | 2015-04-02 | 2016-10-06 | Bayer Cropscience Aktiengesellschaft | Triazol derivatives as fungicides |
| PE20180455A1 (es) | 2015-04-03 | 2018-03-05 | Incyte Corp | Compuestos heterociclicos como inhibidores de lsd1 |
| UA126277C2 (uk) | 2015-08-12 | 2022-09-14 | Інсайт Корпорейшн | Солі інгібітору lsd1 |
| 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 |
| MA44725A (fr) | 2016-04-22 | 2019-02-27 | Incyte Corp | Formulations d'un inhibiteur de lsd1 |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| JP7745559B2 (ja) | 2020-02-28 | 2025-09-29 | キャリーオペ，インク． | Ｇｐｒ４０アゴニスト |
| CA3178994A1 (en) | 2020-05-19 | 2021-11-25 | Iyassu Sebhat | Ampk activators |
| CN116390925A (zh) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008545008A (ja) * | 2005-06-30 | 2008-12-11 | プロシディオン・リミテッド | Ｇｐｃｒアゴニスト |
| AU2007291252A1 (en) * | 2006-08-30 | 2008-03-06 | Inovacia Ab | Pyridine compounds for treating GPR119 related disorders |
| BRPI0719941A2 (pt) * | 2006-12-06 | 2014-04-22 | Smithkline Beecham Corp | Composto, uso de um composto, método para o tratamento de distúrbios ou condições metabólicos, composição farmacêutica, e, processo para a preparação de uma composição farmacêutica |
| JP2010526145A (ja) * | 2007-05-04 | 2010-07-29 | ブリストル−マイヤーズ スクイブ カンパニー | ［６，６］および［６，７］−二環式ｇｐｒ１１９ｇタンパク質結合受容体アゴニスト |
| US8093257B2 (en) * | 2007-05-04 | 2012-01-10 | Bristol-Myers Squibb Company | [6,5]-bicyclic GPR119 G protein-coupled receptor agonists |
| EP2197873B1 (en) * | 2007-09-20 | 2014-07-16 | Irm Llc | Compounds and compositions as modulators of gpr119 activity |
| 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 |
| EP2390254A1 (en) * | 2009-01-22 | 2011-11-30 | Mitsubishi Tanabe Pharma Corporation | NOVEL PYRROLOÝ2,3-d¨PYRIMIDINE COMPOUND |
| US8410089B2 (en) * | 2009-02-18 | 2013-04-02 | Takeda Pharmaceutical Company Limited | Fused heterocyclic ring compound |
| JP2012530758A (ja) | 2009-06-24 | 2012-12-06 | 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 | 新規化合物、医薬組成物及びそれに関する方法 |
| US8293729B2 (en) | 2009-06-24 | 2012-10-23 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| US8729084B2 (en) | 2010-05-06 | 2014-05-20 | Bristol-Myers Squibb Company | Benzofuranyl analogues as GPR119 modulators |
| US8772323B2 (en) | 2010-05-07 | 2014-07-08 | Boehringer Ingelheim International Gmbh | Benzoxazole- and tetrahydrobenzoxazole-substituted 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?. |
| CN103443097A (zh) | 2011-01-21 | 2013-12-11 | 勃林格殷格翰国际有限公司 | 作为gpr119调节剂用于治疗糖尿病、肥胖症以及相关病症的稠合的二氢呋喃化合物 |
| JP5935154B2 (ja) | 2011-03-14 | 2016-06-15 | 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 | Ｇｐｒ１１９モジュレーターとしてのｎ−シクロプロピル−ｎ−ピペリジニルベンズアミド |
-
2011
- 2011-12-15 UY UY0001033805A patent/UY33805A/es not_active Application Discontinuation
- 2011-12-16 WO PCT/EP2011/073067 patent/WO2012080476A1/en not_active Ceased
- 2011-12-16 AR ARP110104756A patent/AR084349A1/es unknown
- 2011-12-16 JP JP2013543816A patent/JP6011543B2/ja active Active
- 2011-12-16 US US13/327,823 patent/US8669271B2/en active Active
- 2011-12-16 EP EP11807666.0A patent/EP2651931B1/en active Active
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