RU2012131341A - Индол-пиперидинилбензиламины как ингибиторы бета-триптазы - Google Patents
Индол-пиперидинилбензиламины как ингибиторы бета-триптазы Download PDFInfo
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- RU2012131341A RU2012131341A RU2012131341/04A RU2012131341A RU2012131341A RU 2012131341 A RU2012131341 A RU 2012131341A RU 2012131341/04 A RU2012131341/04 A RU 2012131341/04A RU 2012131341 A RU2012131341 A RU 2012131341A RU 2012131341 A RU2012131341 A RU 2012131341A
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- alkyl
- alkoxy
- optionally substituted
- arthritis
- haloalkoxy
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- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims abstract 12
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 11
- 125000004438 haloalkoxy group Chemical group 0.000 claims abstract 8
- 206010003246 arthritis Diseases 0.000 claims abstract 6
- 229910052794 bromium Inorganic materials 0.000 claims abstract 6
- 229910052801 chlorine Inorganic materials 0.000 claims abstract 6
- 229910052731 fluorine Inorganic materials 0.000 claims abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 6
- 125000003118 aryl group Chemical group 0.000 claims abstract 5
- 150000001875 compounds Chemical class 0.000 claims abstract 5
- 201000010099 disease Diseases 0.000 claims abstract 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims abstract 4
- 208000027866 inflammatory disease Diseases 0.000 claims abstract 3
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims abstract 2
- 201000005569 Gout Diseases 0.000 claims abstract 2
- 206010018634 Gouty Arthritis Diseases 0.000 claims abstract 2
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims abstract 2
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims abstract 2
- 229940100389 Sulfonylurea Drugs 0.000 claims abstract 2
- 206010048873 Traumatic arthritis Diseases 0.000 claims abstract 2
- 125000003368 amide group Chemical group 0.000 claims abstract 2
- 150000001408 amides Chemical class 0.000 claims abstract 2
- 230000002917 arthritic effect Effects 0.000 claims abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims abstract 2
- 239000003085 diluting agent Substances 0.000 claims abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 claims abstract 2
- 229910052736 halogen Inorganic materials 0.000 claims abstract 2
- 150000002367 halogens Chemical class 0.000 claims abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 2
- 229910052740 iodine Inorganic materials 0.000 claims abstract 2
- 208000018937 joint inflammation Diseases 0.000 claims abstract 2
- 201000008482 osteoarthritis Diseases 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims abstract 2
- 201000005404 rubella Diseases 0.000 claims abstract 2
- 125000001424 substituent group Chemical group 0.000 claims abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 claims abstract 2
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical group OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000004001 thioalkyl group Chemical group 0.000 claims abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 206010010741 Conjunctivitis Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000006663 (C1-C6) perfluoroalkyl group Chemical group 0.000 claims 1
- 206010002198 Anaphylactic reaction Diseases 0.000 claims 1
- 208000037260 Atherosclerotic Plaque Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 208000032544 Cicatrix Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- 206010028594 Myocardial fibrosis Diseases 0.000 claims 1
- 201000004404 Neurofibroma Diseases 0.000 claims 1
- 208000008469 Peptic Ulcer Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 230000036783 anaphylactic response Effects 0.000 claims 1
- 208000003455 anaphylaxis Diseases 0.000 claims 1
- 210000001188 articular cartilage Anatomy 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 230000001969 hypertrophic effect Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000028169 periodontal disease Diseases 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 231100000241 scar Toxicity 0.000 claims 1
- 230000037387 scars Effects 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 125000005010 perfluoroalkyl group Chemical group 0.000 abstract 1
- 239000010802 sludge Substances 0.000 abstract 1
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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Abstract
1. Соединение формулыгдеR1 представляет собой F, Cl, Br, OCHCOCH, OCHCONW1W2, CHOH или необязательно замещенный алкил, галогеналкил, алкокси или галогеналкокси;где W1 и W2 представляют собой независимо Н или алкил;R2 представляет собой Н, F, Cl, Br, ОН, СНОН, алкил или алкокси;R4 представляет собой алкил, необязательно замещенный одной или несколькими группами, выбранными из гидрокси, алкокси, галогеналкокси, циклоалкила, гетероциклоалкила, арила, необязательно замещенного арила и гетероарила или необязательно замещенного гетероарила; иR5 представляет собой Н, галоген, алкокси, галогеналкокси, алкил, амидо, карбоксил, уреил, сульфониламидо, сульфонилмочевину, алкил, необязательно замещенный одной или несколькими группами, выбранными из гидрокси, алкокси, галогеналкокси, циклоалкила, гетероциклоалкила, арила или гетероарила, илиего соль, или его энантиомер, или диастереомер,где необязательные заместители, выбраны из группы, включающей (С-С)алкил, (С-С)алкенил, (С-С)перфторалкил, фенил, гидрокси, -СОН, эфир, амид, (С-С)алкокси, (С-С)тиоалкил, (С-С)пертфоралкокси, -NH, Cl, Br, I, F, -NH(С-С)алкил и -N((С-С)алкил).2. Фармацевтическая композиция, содержащая соединение по п.1 в комбинации с по меньшей мере одним фармацевтически приемлемым наполнителем, разбавителем или носителем.3. Способ лечения заболевания у пациента, причем указанное заболевание выбрано из группы, состоящей из воспалительного заболевания, например, воспаления сустава, включая артрит, ревматоидный артрит и другое артритическое состояние, такое как ревматоидный спондилит, подагрический артрит, травматический артрит, краснушный артрит, псориатический артрит, остеоартрит или другое хроническ�
Claims (3)
1. Соединение формулы
где
R1 представляет собой F, Cl, Br, OCH2CO2CH3, OCH2CONW1W2, CH2OH или необязательно замещенный алкил, галогеналкил, алкокси или галогеналкокси;
где W1 и W2 представляют собой независимо Н или алкил;
R2 представляет собой Н, F, Cl, Br, ОН, СН2ОН, алкил или алкокси;
R4 представляет собой алкил, необязательно замещенный одной или несколькими группами, выбранными из гидрокси, алкокси, галогеналкокси, циклоалкила, гетероциклоалкила, арила, необязательно замещенного арила и гетероарила или необязательно замещенного гетероарила; и
R5 представляет собой Н, галоген, алкокси, галогеналкокси, алкил, амидо, карбоксил, уреил, сульфониламидо, сульфонилмочевину, алкил, необязательно замещенный одной или несколькими группами, выбранными из гидрокси, алкокси, галогеналкокси, циклоалкила, гетероциклоалкила, арила или гетероарила, или
его соль, или его энантиомер, или диастереомер,
где необязательные заместители, выбраны из группы, включающей (С1-С6)алкил, (С2-С6)алкенил, (С1-С6)перфторалкил, фенил, гидрокси, -СО2Н, эфир, амид, (С1-С6)алкокси, (С1-С6)тиоалкил, (С1-С6)пертфоралкокси, -NH2, Cl, Br, I, F, -NH(С1-С6)алкил и -N((С1-С6)алкил)2.
2. Фармацевтическая композиция, содержащая соединение по п.1 в комбинации с по меньшей мере одним фармацевтически приемлемым наполнителем, разбавителем или носителем.
3. Способ лечения заболевания у пациента, причем указанное заболевание выбрано из группы, состоящей из воспалительного заболевания, например, воспаления сустава, включая артрит, ревматоидный артрит и другое артритическое состояние, такое как ревматоидный спондилит, подагрический артрит, травматический артрит, краснушный артрит, псориатический артрит, остеоартрит или другое хроническое воспалительное заболевание сустава или заболевания разрушения суставного хряща, глазного конъюнктивита, весеннего конъюнктивита, воспалительного заболевания кишечника, астмы, аллергического ринита, интерстициального заболевания легких, фиброза, склеродермии, легочного фиброза, цирроза печени, миокардиального фиброза, нейрофибром, гипертрофических рубцов, различных дерматологических состояний, например, атопического дерматита и псориаза, инфаркта миокарда, инсульта, стенокардии или других последствий разрыва атеросклеротической бляшки, а также периодонтального заболевания, диабетической ретинопатии, дегенерации желтого пятна, острой дегенерации желтого пятна, влажной дегенерации желтого пятна, опухолевого роста, анафилаксии, рассеянного склероза, пептических язв или синцитиальной вирусной инфекции; включающий введение указанному пациенту терапевтически эффективного количества соединения по п.1.
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| FR1057580 | 2010-09-21 | ||
| PCT/US2010/061461 WO2011079102A1 (en) | 2009-12-23 | 2010-12-21 | Indolyl-piperidinyl benzylamines as beta-tryptase inhibitors |
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| PL2986594T3 (pl) | 2013-04-15 | 2017-10-31 | Fmc Corp | Amidy grzybobójcze |
| US20170157135A1 (en) * | 2013-11-25 | 2017-06-08 | Novogen Limited | Functionalised and substituted indoles as anti-cancer agents |
| WO2015157005A1 (en) | 2014-04-10 | 2015-10-15 | E I Du Pont De Nemours And Company | Substituted tolyl fungicide mixtures |
| EP3519816A4 (en) | 2016-09-29 | 2020-05-06 | The Regents of the University of California | Compounds for increasing neural plasticity |
| AU2018238138A1 (en) * | 2017-03-21 | 2019-10-17 | Arbutus Biopharma Corporation | Substituted dihydroindene-4-carboxamides and analogs thereof, and methods using same |
| CA3072746A1 (en) | 2017-08-14 | 2019-02-21 | Epizyme, Inc. | Methods of treating cancer by inhibiting setd2 |
| MX2021001690A (es) * | 2018-08-14 | 2021-07-21 | Epizyme Inc | Indoles sustituidos y metodos de uso de los mismos. |
| TWI846654B (zh) | 2018-11-06 | 2024-06-21 | 美商富曼西公司 | 經取代之甲苯基殺真菌劑 |
| CN109438214B (zh) * | 2018-11-13 | 2021-06-11 | 大连奇凯医药科技有限公司 | 高纯度5-溴-2,4-二氟苯甲酸的制备方法 |
| KR20210134928A (ko) | 2019-02-27 | 2021-11-11 | 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 | 뇌 장애를 치료하기 위한 n-치환된 인돌 및 다른 헤테로사이클 |
| JP2022521789A (ja) | 2019-02-27 | 2022-04-12 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 脳障害を治療するためのアゼピノ－インドール及び他の複素環化合物 |
| UY39189A (es) | 2020-05-06 | 2021-12-31 | Fmc Corp | Fungicidas de tolilo sustituido y sus mezclas |
| CN113372223B (zh) * | 2021-05-20 | 2022-10-28 | 宁波职业技术学院 | 一种2-氟-3-溴-苄胺的制备方法 |
| AU2022337841B2 (en) * | 2021-09-03 | 2024-12-05 | Shenzhen 01 Life Science And Technology Co., Ltd. | Indole compound, and preparation method therefor and use thereof |
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| IL152830A0 (en) * | 2000-05-22 | 2003-06-24 | Aventis Pharma Inc | Arylmethylamine derivatives for use as tryptase inhibitors |
| GB0012362D0 (en) * | 2000-05-22 | 2000-07-12 | Aventis Pharma Ltd | Chemical compounds |
| EP1678146A1 (en) | 2003-10-23 | 2006-07-12 | Pharmacia Corporation | Pyrimidine compounds for the treatment of inflammation |
| DOP2005000039A (es) * | 2004-03-26 | 2005-10-31 | Aventis Pharma Inc | Hidrocloruro de [4-(5-aminometil-2-fluoro-fenil)- piperidin-1-il]-(4-bomo-3-metil-5-propoxi-tiofen-2-il)-metanona como un inhibidor de la triptasa de mastocitos |
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| FR2955324A1 (fr) * | 2010-01-15 | 2011-07-22 | Sanofi Aventis | [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees |
| SG181501A1 (en) * | 2009-12-23 | 2012-07-30 | Sanofi Sa | Prodrugs of [4[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(1h-pyrrolo-pyridin-yl)-methanones and synthesis thereof |
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| SG181504A1 (en) | 2012-07-30 |
| TW201132633A (en) | 2011-10-01 |
| KR20120097410A (ko) | 2012-09-03 |
| EP2516419A1 (en) | 2012-10-31 |
| AR079662A1 (es) | 2012-02-08 |
| JP2013515733A (ja) | 2013-05-09 |
| CN102770425A (zh) | 2012-11-07 |
| WO2011079102A1 (en) | 2011-06-30 |
| MX2012006805A (es) | 2012-07-10 |
| AU2010333779A1 (en) | 2012-07-12 |
| CA2784894A1 (en) | 2011-06-30 |
| UY33155A (es) | 2011-07-29 |
| US20120245161A1 (en) | 2012-09-27 |
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