JP2020523367A5 - - Google Patents
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- JP2020523367A5 JP2020523367A5 JP2019568760A JP2019568760A JP2020523367A5 JP 2020523367 A5 JP2020523367 A5 JP 2020523367A5 JP 2019568760 A JP2019568760 A JP 2019568760A JP 2019568760 A JP2019568760 A JP 2019568760A JP 2020523367 A5 JP2020523367 A5 JP 2020523367A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- carboxamide
- substituted
- naphthylidine
- fluoro
- 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.)
- Ceased
Links
- 125000000217 alkyl group Chemical group 0.000 claims 108
- 125000001153 fluoro group Chemical group F* 0.000 claims 57
- -1 chloro, bromo, iodo Chemical group 0.000 claims 43
- 125000001424 substituent group Chemical group 0.000 claims 34
- 208000029549 Muscle injury Diseases 0.000 claims 27
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 23
- 125000004043 oxo group Chemical group O=* 0.000 claims 22
- 125000004093 cyano group Chemical group *C#N 0.000 claims 18
- 125000003545 alkoxy group Chemical group 0.000 claims 17
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 14
- 125000002393 azetidinyl group Chemical group 0.000 claims 13
- 125000001309 chloro group Chemical group Cl* 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- SBUKLPSBNFWJCU-UHFFFAOYSA-N ClIBr Chemical compound ClIBr SBUKLPSBNFWJCU-UHFFFAOYSA-N 0.000 claims 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 210000003205 muscle Anatomy 0.000 claims 6
- 201000006938 muscular dystrophy Diseases 0.000 claims 6
- 125000002971 oxazolyl group Chemical group 0.000 claims 6
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 5
- 210000003979 eosinophil Anatomy 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 208000014674 injury Diseases 0.000 claims 5
- 150000003857 carboxamides Chemical class 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 206010013801 Duchenne Muscular Dystrophy Diseases 0.000 claims 3
- 208000006673 asthma Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 210000002435 tendon Anatomy 0.000 claims 3
- 230000001256 tonic effect Effects 0.000 claims 3
- 230000008736 traumatic injury Effects 0.000 claims 3
- 206010010356 Congenital anomaly Diseases 0.000 claims 2
- 208000034656 Contusions Diseases 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 102100029100 Hematopoietic prostaglandin D synthase Human genes 0.000 claims 2
- 101710082112 Hematopoietic prostaglandin D synthase Proteins 0.000 claims 2
- 208000027418 Wounds and injury Diseases 0.000 claims 2
- 210000001264 anterior cruciate ligament Anatomy 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 206010006451 bronchitis Diseases 0.000 claims 2
- 230000009519 contusion Effects 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 230000006378 damage Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- KLDGHPMEPAPPFX-UHFFFAOYSA-N pyrido[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=CN=CC2=CC(C(=O)N)=CN=C21 KLDGHPMEPAPPFX-UHFFFAOYSA-N 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 230000003252 repetitive effect Effects 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000033309 Analgesic asthma syndrome Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003694 Atrophy Diseases 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 1
- 206010011224 Cough Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 208000006313 Delayed Hypersensitivity Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 208000004262 Food Hypersensitivity Diseases 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 206010018691 Granuloma Diseases 0.000 claims 1
- 241000282412 Homo Species 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000034693 Laceration Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 206010028331 Muscle rupture Diseases 0.000 claims 1
- 208000021642 Muscular disease Diseases 0.000 claims 1
- 208000023178 Musculoskeletal disease Diseases 0.000 claims 1
- 208000000112 Myalgia Diseases 0.000 claims 1
- 201000009623 Myopathy Diseases 0.000 claims 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 1
- HEWVQMIXEMUPRL-HDJSIYSDSA-N OC(C)(C)[C@@H]1CC[C@H](CC1)NC(=O)C1=CC2=C(N=C(N=C2)OC)N=C1 Chemical compound OC(C)(C)[C@@H]1CC[C@H](CC1)NC(=O)C1=CC2=C(N=C(N=C2)OC)N=C1 HEWVQMIXEMUPRL-HDJSIYSDSA-N 0.000 claims 1
- 206010030216 Oesophagitis Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 206010049422 Precancerous skin lesion Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010039203 Road traffic accident Diseases 0.000 claims 1
- 206010052568 Urticaria chronic Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 230000037444 atrophy Effects 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000024376 chronic urticaria Diseases 0.000 claims 1
- 206010010121 compartment syndrome Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 230000008602 contraction Effects 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 125000006317 cyclopropyl amino group Chemical group 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000006881 esophagitis Diseases 0.000 claims 1
- 210000003414 extremity Anatomy 0.000 claims 1
- 230000001815 facial effect Effects 0.000 claims 1
- 235000020932 food allergy Nutrition 0.000 claims 1
- 210000004394 hip joint Anatomy 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000013150 knee replacement Methods 0.000 claims 1
- 201000010901 lateral sclerosis Diseases 0.000 claims 1
- 230000007774 longterm Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000005264 motor neuron disease Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000013465 muscle pain Diseases 0.000 claims 1
- 230000003387 muscular Effects 0.000 claims 1
- ONLRKTIYOMZEJM-UHFFFAOYSA-N n-methylmethanamine oxide Chemical compound C[NH+](C)[O-] ONLRKTIYOMZEJM-UHFFFAOYSA-N 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 230000000399 orthopedic effect Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 230000036544 posture Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 238000011084 recovery Methods 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 230000001932 seasonal effect Effects 0.000 claims 1
- 210000002027 skeletal muscle Anatomy 0.000 claims 1
- 210000000278 spinal cord Anatomy 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 230000001360 synchronised effect Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000000472 traumatic effect Effects 0.000 claims 1
- 208000001319 vasomotor rhinitis Diseases 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762518779P | 2017-06-13 | 2017-06-13 | |
| US62/518,779 | 2017-06-13 | ||
| US201762522869P | 2017-06-21 | 2017-06-21 | |
| US62/522,869 | 2017-06-21 | ||
| PCT/IB2018/054206 WO2018229629A1 (en) | 2017-06-13 | 2018-06-11 | Chemical compounds as h-pgds inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020523367A JP2020523367A (ja) | 2020-08-06 |
| JP2020523367A5 true JP2020523367A5 (https=) | 2021-06-10 |
Family
ID=62948277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019568760A Ceased JP2020523367A (ja) | 2017-06-13 | 2018-06-11 | Ｈ−ｐｇｄｓ阻害剤としての化学化合物 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US11149035B2 (https=) |
| EP (1) | EP3638672A1 (https=) |
| JP (1) | JP2020523367A (https=) |
| CN (1) | CN110753692A (https=) |
| BR (1) | BR112019026452A2 (https=) |
| CA (1) | CA3066979A1 (https=) |
| TW (1) | TW201908311A (https=) |
| UY (1) | UY37764A (https=) |
| WO (1) | WO2018229629A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3085293A1 (en) * | 2017-12-13 | 2019-06-20 | Glaxosmithkline Intellectual Property Development Limited | Fused pyridines which act as inhibitors of h-pgds |
| JP2022506850A (ja) * | 2018-11-08 | 2022-01-17 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド | 化学化合物 |
| CN109651241B (zh) * | 2018-12-27 | 2021-02-09 | 上海毕得医药科技股份有限公司 | 一种4-溴-6-氯烟醛的合成方法 |
| WO2021256569A1 (ja) | 2020-06-19 | 2021-12-23 | 佐藤製薬株式会社 | Ｈ－ｐｇｄｓを阻害する縮環化合物 |
| CN112430632B (zh) * | 2020-11-18 | 2022-09-13 | 上海合全药物研发有限公司 | 2-((反式)-4-氨基环己烷基)异丙醇的制备方法 |
| MX2023005747A (es) | 2020-11-18 | 2023-07-28 | Deciphera Pharmaceuticals Llc | Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismos. |
| CA3240926A1 (en) | 2021-12-17 | 2023-06-22 | Sato Pharmaceutical Co., Ltd. | Azaindole derivative inhibiting h-pgds |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1361768A (zh) | 1999-06-02 | 2002-07-31 | Nps药物有限公司 | 代谢移变的谷氨酸盐受体拮抗剂和它们治疗中枢神经系统疾病的用途 |
| US6576265B1 (en) | 1999-12-22 | 2003-06-10 | Acell, Inc. | Tissue regenerative composition, method of making, and method of use thereof |
| EP1389209B1 (en) | 2001-04-24 | 2009-04-08 | Purdue Research Foundation | Folate mimetics and folate-receptor binding conjugates thereof |
| US7868204B2 (en) | 2001-09-14 | 2011-01-11 | Methylgene Inc. | Inhibitors of histone deacetylase |
| US8163769B2 (en) | 2002-03-12 | 2012-04-24 | Abbott Laboratories | Antibacterial compounds |
| WO2004014377A1 (en) | 2002-08-13 | 2004-02-19 | Warner-Lambert Company Llc | 4-hydroxyquinoline derivatives as matrix metalloproteinase inhibitors |
| WO2004056744A1 (en) | 2002-12-23 | 2004-07-08 | Janssen Pharmaceutica N.V. | Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors |
| WO2005035526A1 (en) | 2003-10-09 | 2005-04-21 | Argenta Discovery Ltd. | Bicyclic compounds and their therapeutic use |
| WO2005094805A1 (ja) | 2004-04-01 | 2005-10-13 | Institute Of Medicinal Molecular Design. Inc. | イミン誘導体及びアミド誘導体 |
| TW200720255A (en) | 2005-07-13 | 2007-06-01 | Taiho Pharmaceutical Co Ltd | Benzoimidazole compound capable of inhibiting prostaglandin d synthetase |
| JP2007051121A (ja) | 2005-07-22 | 2007-03-01 | Taiho Yakuhin Kogyo Kk | プロスタグランジンｄ合成酵素を阻害するピリミジン化合物 |
| PE20110118A1 (es) | 2005-10-04 | 2011-03-08 | Aventis Pharma Inc | Compuestos de pirimidina amida como inhibidores de pgds |
| EP2129660A2 (en) | 2006-12-19 | 2009-12-09 | Pfizer Products Inc. | Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases |
| DK2142516T3 (da) | 2007-03-30 | 2013-04-15 | Sanofi Sa | Pyrimidinhydrazidforbindelser i ders egenskab af pgds-inhibitorer |
| GB0706793D0 (en) | 2007-04-05 | 2007-05-16 | Evotec Ag | Compounds |
| US9603848B2 (en) | 2007-06-08 | 2017-03-28 | Senomyx, Inc. | Modulation of chemosensory receptors and ligands associated therewith |
| TW201010997A (en) * | 2008-06-18 | 2010-03-16 | Pfizer Ltd | Nicotinamide derivatives |
| CA2725481A1 (en) * | 2008-06-18 | 2009-12-23 | Pfizer Limited | Nicotinamide derivatives |
| US8536185B2 (en) | 2008-09-22 | 2013-09-17 | Cayman Chemical Company, Incorporated | Multiheteroaryl compounds as inhibitors of H-PGDS and their use for treating prostaglandin D2 mediated diseases |
| RU2496778C2 (ru) | 2009-03-09 | 2013-10-27 | Тайхо Фармасьютикал Ко., Лтд. | Пиперазиновое соединение, ингибирующее простагландин-d-синтазу |
| JP2011042643A (ja) | 2009-07-24 | 2011-03-03 | Bayer Cropscience Ag | 殺虫性カルボキサミド類 |
| JPWO2011043359A1 (ja) | 2009-10-06 | 2013-03-04 | 協和発酵キリン株式会社 | 芳香族複素環化合物を含有する医薬 |
| CN107875155A (zh) | 2009-10-08 | 2018-04-06 | 赛诺菲 | 苯基噁二唑衍生物在制备治疗变应性或炎性疾病的药物中的用途 |
| EP2527340B1 (en) * | 2010-01-22 | 2016-08-17 | Taiho Pharmaceutical Co., Ltd. | Piperazine compound having a pgds inhibitory effect |
| GB201007347D0 (en) | 2010-04-30 | 2010-06-16 | Karus Therapeutics Ltd | Compounds |
| US9290453B2 (en) * | 2010-12-23 | 2016-03-22 | Merck Sharp & Dohme Corp. | Quinolines and aza-quinolines as CRTH2 receptor modulators |
| US20130072473A1 (en) | 2011-05-09 | 2013-03-21 | Proteostasis Therapeutics, Inc. | Compounds for treating protein folding disorders |
| HK1203412A1 (en) | 2011-12-28 | 2015-10-30 | Global Blood Therapeutics, Inc. | Substituted heteroaryl aldehyde compounds and methods for their use in increasing tissue oxygenation |
| US9187474B2 (en) | 2012-03-07 | 2015-11-17 | Deciphera Pharmaceuticals, Llc | Raf inhibitor compounds |
| MX363388B (es) | 2012-07-27 | 2019-03-20 | Biogen Ma Inc | Agentes moduladores de autotaxina. |
| EA027809B1 (ru) | 2012-07-27 | 2017-09-29 | Биоген Айдек Ма Инк. | Соединения, которые являются s1p-модулирующими агентами и/или atx-модулирующими агентами |
| US10005720B2 (en) | 2013-04-05 | 2018-06-26 | North Carolina Central University | Compounds useful for the treatment of metabolic disorders and synthesis of the same |
| RU2685234C1 (ru) | 2013-12-09 | 2019-04-17 | Юсб Байофарма Спрл | Конденсированные бициклические гетероароматические производные в качестве модуляторов активности tnf |
| WO2016009076A1 (en) | 2014-07-17 | 2016-01-21 | Merck Patent Gmbh | Novel naphthryidines and isoquinolines and their use as cdk8/19 inhibitors |
| CA2974784A1 (en) | 2015-01-23 | 2016-07-28 | Gvk Biosciences Private Limited | Inhibitors of trka kinase |
| CN108430992A (zh) * | 2015-12-17 | 2018-08-21 | 阿斯特克斯医疗公司 | 作为h-pgds抑制剂的喹啉-3-甲酰胺 |
| US10898469B2 (en) * | 2016-02-26 | 2021-01-26 | Sumitomo Dainippon Pharma Co., Ltd. | Imidazolylamide derivative |
| JOP20190072A1 (ar) * | 2016-10-13 | 2019-04-07 | Glaxosmithkline Ip Dev Ltd | مشتقات 1، 3 سيكلوبوتان ثنائي الاستبدال أو آزيتيدين كمثبطات للإنزيم المخلق للبروستاجلاندين d المكون للدم |
| CA3085293A1 (en) * | 2017-12-13 | 2019-06-20 | Glaxosmithkline Intellectual Property Development Limited | Fused pyridines which act as inhibitors of h-pgds |
-
2018
- 2018-06-11 EP EP18742598.8A patent/EP3638672A1/en not_active Withdrawn
- 2018-06-11 CN CN201880039565.7A patent/CN110753692A/zh active Pending
- 2018-06-11 BR BR112019026452-3A patent/BR112019026452A2/pt not_active Application Discontinuation
- 2018-06-11 UY UY0001037764A patent/UY37764A/es unknown
- 2018-06-11 US US16/621,927 patent/US11149035B2/en not_active Expired - Fee Related
- 2018-06-11 CA CA3066979A patent/CA3066979A1/en not_active Abandoned
- 2018-06-11 JP JP2019568760A patent/JP2020523367A/ja not_active Ceased
- 2018-06-11 WO PCT/IB2018/054206 patent/WO2018229629A1/en not_active Ceased
- 2018-06-11 TW TW107119972A patent/TW201908311A/zh unknown
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