JP2007529527A5 - - Google Patents
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- JP2007529527A5 JP2007529527A5 JP2007503986A JP2007503986A JP2007529527A5 JP 2007529527 A5 JP2007529527 A5 JP 2007529527A5 JP 2007503986 A JP2007503986 A JP 2007503986A JP 2007503986 A JP2007503986 A JP 2007503986A JP 2007529527 A5 JP2007529527 A5 JP 2007529527A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- group
- carboxy
- phenyl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 117
- 125000003118 aryl group Chemical group 0.000 claims 53
- 150000001875 compounds Chemical class 0.000 claims 42
- 125000001424 substituent group Chemical group 0.000 claims 41
- -1 hydroxy, cyano, amino Chemical group 0.000 claims 39
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 39
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 38
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 33
- 229910052739 hydrogen Inorganic materials 0.000 claims 32
- 239000001257 hydrogen Substances 0.000 claims 32
- 125000001072 heteroaryl group Chemical group 0.000 claims 31
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 30
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 29
- 125000003545 alkoxy group Chemical group 0.000 claims 23
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 19
- 229910052736 halogen Inorganic materials 0.000 claims 15
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 15
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 14
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 13
- 125000005100 aryl amino carbonyl group Chemical group 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 125000002541 furyl group Chemical group 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 125000004076 pyridyl group Chemical group 0.000 claims 11
- 208000002193 Pain Diseases 0.000 claims 10
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 10
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 9
- 125000006563 (C1-3) alkylaminocarbonyl group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000001309 chloro group Chemical group Cl* 0.000 claims 8
- 125000004104 aryloxy group Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 125000005167 cycloalkylaminocarbonyl group Chemical group 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 6
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 6
- 125000001769 aryl amino group Chemical group 0.000 claims 5
- 125000001246 bromo group Chemical group Br* 0.000 claims 5
- 125000005241 heteroarylamino group Chemical group 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 125000003831 tetrazolyl group Chemical group 0.000 claims 5
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 238000009472 formulation Methods 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 230000005856 abnormality Effects 0.000 claims 3
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 3
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 2
- 125000006602 (C1-C3) alkylsulfonylamino group Chemical group 0.000 claims 2
- 208000000094 Chronic Pain Diseases 0.000 claims 2
- 206010012735 Diarrhoea Diseases 0.000 claims 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 101100244562 Pseudomonas aeruginosa (strain ATCC 15692 / DSM 22644 / CIP 104116 / JCM 14847 / LMG 12228 / 1C / PRS 101 / PAO1) oprD gene Proteins 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 108700023159 delta Opioid Receptors Proteins 0.000 claims 2
- 102000048124 delta Opioid Receptors Human genes 0.000 claims 2
- 208000010643 digestive system disease Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 102000051367 mu Opioid Receptors Human genes 0.000 claims 2
- 208000004296 neuralgia Diseases 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 125000006513 pyridinyl methyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 108020001612 μ-opioid receptors Proteins 0.000 claims 2
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 claims 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 241001024304 Mino Species 0.000 claims 1
- 206010068620 Post procedural constipation Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 206010054048 Postoperative ileus Diseases 0.000 claims 1
- 208000026137 Soft tissue injury Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 1
- 125000005189 alkyl hydroxy group Chemical group 0.000 claims 1
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000005176 gastrointestinal motility Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 208000027753 pain disease Diseases 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 208000037821 progressive disease Diseases 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US55334204P | 2004-03-15 | 2004-03-15 | |
| US60/553,342 | 2004-03-15 | ||
| PCT/US2005/008339 WO2005090315A1 (en) | 2004-03-15 | 2005-03-14 | Novel compounds as opioid receptor modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007529527A JP2007529527A (ja) | 2007-10-25 |
| JP2007529527A5 true JP2007529527A5 (enExample) | 2009-01-08 |
| JP4778954B2 JP4778954B2 (ja) | 2011-09-21 |
Family
ID=34962827
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007503986A Expired - Fee Related JP4778954B2 (ja) | 2004-03-15 | 2005-03-14 | オピオイド受容体調節薬としての新規な化合物 |
Country Status (35)
Families Citing this family (62)
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| US20080050367A1 (en) | 1998-04-07 | 2008-02-28 | Guriq Basi | Humanized antibodies that recognize beta amyloid peptide |
| TWI239847B (en) | 1997-12-02 | 2005-09-21 | Elan Pharm Inc | N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease |
| LT2653465T (lt) * | 2004-03-15 | 2016-09-12 | Janssen Pharmaceutica Nv | Opioidinio receptoriaus moduliatoriai |
| KR101204751B1 (ko) | 2004-05-14 | 2012-11-27 | 얀센 파마슈티카 엔.브이. | 카복사미도 아편유사약물 화합물 |
| WO2006066089A1 (en) | 2004-12-15 | 2006-06-22 | Neuralab Limited | Humanized amyloid beta antibodies for use in improving cognition |
| BRPI0607792A2 (pt) * | 2005-03-14 | 2009-06-13 | Janssen Pharmaceutica Nv | processo para a preparação de moduladores de opióides |
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| JP5473334B2 (ja) * | 2005-12-23 | 2014-04-16 | ジーランド ファーマ アクティーゼルスカブ | 修飾リジン模倣化合物 |
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| HRP20202008T1 (hr) | 2013-03-14 | 2021-02-19 | Epizyme, Inc. | Inhibitori arginin-metiltransferaze i njihove uporabe |
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| CN105777584B (zh) * | 2016-03-28 | 2018-01-02 | 成都伊诺达博医药科技有限公司 | 丙氨酸衍生物的制备方法 |
| CN105693554B (zh) * | 2016-04-06 | 2017-08-08 | 成都伊诺达博医药科技有限公司 | 丙氨酸衍生物的制备方法 |
| WO2017191650A1 (en) * | 2016-05-03 | 2017-11-09 | Msn Laboratories Private Limited | Process for the preparation of 5-[[[(2s)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1s)-1-(4-phenyl-1h-imidazol-2-yl)ethyl]amino]methyl-2-methoxybenzoic acid and its polymorphs thereof |
| EP3463333A4 (en) * | 2016-05-30 | 2019-11-20 | Sun Pharmaceutical Industries Limited | PROCESS FOR THE PREPARATION OF ELUXADOLINE |
| WO2017221213A1 (en) * | 2016-06-23 | 2017-12-28 | Sun Pharmaceutical Industries Limited | Processes for the preparation of eluxadoline |
| WO2018020450A2 (en) | 2016-07-28 | 2018-02-01 | Lupin Limited | Process for the preparation of eluxadoline |
| CZ2016548A3 (cs) | 2016-09-07 | 2018-03-14 | Zentiva, K.S. | Pevné formy eluxadolinu |
| WO2018047131A1 (en) * | 2016-09-09 | 2018-03-15 | Sun Pharmaceutical Industries Limited | Amorphous eluxadoline |
| EP3515434A4 (en) * | 2016-09-20 | 2020-02-26 | Sun Pharmaceutical Industries Limited | PROCESSES FOR THE PREPARATION OF ELUXADOLINE |
| WO2018138272A1 (en) | 2017-01-27 | 2018-08-02 | Quimica Sintetica, S. A. | Eluxadoline crystalline form and process for the preparation thereof |
| WO2018138274A1 (en) | 2017-01-27 | 2018-08-02 | Quimica Sintetica, S. A. | Eluxadoline crystalline forms and processes for their preparation |
| WO2018202865A1 (en) | 2017-05-05 | 2018-11-08 | Zealand Pharma A/S | Gap junction intercellular communication modulators and their use for the treatment of diabetic eye disease |
| WO2019008604A1 (en) | 2017-07-07 | 2019-01-10 | Cipla Limited | NEW FORMS OF MU-OPIOID RECEPTOR AGONIST |
| WO2019144805A1 (zh) * | 2018-01-25 | 2019-08-01 | 四川科伦博泰生物医药股份有限公司 | 取代的苯乙胺化合物及其制备方法和用途 |
| WO2019197274A1 (en) | 2018-04-09 | 2019-10-17 | Quimica Sintetica, S. A. | Process for the preparation of opioid modulators |
| US20210251964A1 (en) | 2018-08-20 | 2021-08-19 | Allergan Holdings Unlimited Company | Polymorphs of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid |
| CN120058958A (zh) | 2018-09-24 | 2025-05-30 | 视点制药公司 | 靶向HPTP-β（VE-PTP）和VEGF的多特异性抗体 |
| EP3659433B1 (de) * | 2018-11-30 | 2021-01-20 | Phytobiotics Futterzusatzstoffe GmbH | System zur analyse von tierausscheidungsbildern |
| CN111377832A (zh) * | 2018-12-27 | 2020-07-07 | 江苏联昇化学有限公司 | 一种伊卢多啉中间体制备的新方法 |
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| US20230118152A1 (en) | 2020-03-30 | 2023-04-20 | Allergan Holdings Unlimited Company | Forms of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid |
| CN116348465A (zh) * | 2020-07-28 | 2023-06-27 | 爵士制药爱尔兰有限公司 | 稠合双环raf抑制剂的手性合成 |
| US11850319B2 (en) | 2020-09-29 | 2023-12-26 | Abl Ip Holding Llc | Techniques for directing ultraviolet energy towards a moving surface |
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| CN114163348A (zh) * | 2020-11-27 | 2022-03-11 | 成都泰蓉生物科技有限公司 | 一种氨酰基取代的l-苯丙氨酸的合成方法 |
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| US20020072017A1 (en) * | 2000-10-19 | 2002-06-13 | Hudnall Phillip Montgomery | Stabilized p-phenylenediamine-type photographic color developers in free base form |
| CN100400040C (zh) | 2000-10-30 | 2008-07-09 | 詹森药业有限公司 | 三肽酶抑制剂 |
| ATE347549T1 (de) * | 2001-10-15 | 2006-12-15 | Janssen Pharmaceutica Nv | Neue substituierte 4-phenyl-4-(1h-imidazo-2-yl)- piperidin-derivate und ihre anwendung als selective delta-opioid-agonisten |
| US7041681B2 (en) * | 2002-04-29 | 2006-05-09 | Janssen Pharmaceutica N.V. | Compounds as opioid receptor modulators |
| LT2653465T (lt) | 2004-03-15 | 2016-09-12 | Janssen Pharmaceutica Nv | Opioidinio receptoriaus moduliatoriai |
| EP1753749B1 (en) * | 2004-05-03 | 2014-07-30 | Janssen Pharmaceutica NV | Novel indole derivatives as selective androgen receptor modulators (sarms) |
| BRPI0607792A2 (pt) * | 2005-03-14 | 2009-06-13 | Janssen Pharmaceutica Nv | processo para a preparação de moduladores de opióides |
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2006
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2012
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