JP6611799B2 - 新規化合物 - Google Patents
新規化合物 Download PDFInfo
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- JP6611799B2 JP6611799B2 JP2017516387A JP2017516387A JP6611799B2 JP 6611799 B2 JP6611799 B2 JP 6611799B2 JP 2017516387 A JP2017516387 A JP 2017516387A JP 2017516387 A JP2017516387 A JP 2017516387A JP 6611799 B2 JP6611799 B2 JP 6611799B2
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- formula
- acid
- fluoro
- tetrahydro
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- 150000001875 compounds Chemical class 0.000 title claims description 220
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 39
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- MKIJZIVRJUMEAD-WXVAWEFUSA-N (3R)-4-[(3R)-3-fluoro-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]-3-[3-(2-methoxyethoxy)phenyl]butanoic acid Chemical compound F[C@]1(CN(CC1)C[C@H](CC(=O)O)C1=CC(=CC=C1)OCCOC)CCC1=NC=2NCCCC=2C=C1 MKIJZIVRJUMEAD-WXVAWEFUSA-N 0.000 claims description 5
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- MKIJZIVRJUMEAD-AJTFRIOCSA-N (3S)-4-[(3R)-3-fluoro-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]-3-[3-(2-methoxyethoxy)phenyl]butanoic acid Chemical compound F[C@]1(CN(CC1)C[C@@H](CC(=O)O)C1=CC(=CC=C1)OCCOC)CCC1=NC=2NCCCC=2C=C1 MKIJZIVRJUMEAD-AJTFRIOCSA-N 0.000 claims description 3
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- CPMDPSXJELVGJG-UHFFFAOYSA-N methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate Chemical group OC=1NC2=CC(=CC=C2C=1C(=NC1=CC=C(C=C1)N(C(CN1CCN(CC1)C)=O)C)C1=CC=CC=C1)C(=O)OC CPMDPSXJELVGJG-UHFFFAOYSA-N 0.000 claims description 2
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- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 description 14
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 13
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- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 9
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- 239000011701 zinc Substances 0.000 description 1
- 229930195724 β-lactose Natural products 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| GBGB1417002.1A GB201417002D0 (en) | 2014-09-26 | 2014-09-26 | Novel compound |
| GB1417002.1 | 2014-09-26 | ||
| PCT/EP2015/071776 WO2016046225A1 (en) | 2014-09-26 | 2015-09-22 | Novel compounds |
Publications (3)
| Publication Number | Publication Date |
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| JP2017528507A JP2017528507A (ja) | 2017-09-28 |
| JP2017528507A5 JP2017528507A5 (OSRAM) | 2018-01-25 |
| JP6611799B2 true JP6611799B2 (ja) | 2019-11-27 |
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| JP2017516387A Expired - Fee Related JP6611799B2 (ja) | 2014-09-26 | 2015-09-22 | 新規化合物 |
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| GB201305668D0 (en) | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| GB201417011D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417002D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201417018D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417094D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201604589D0 (en) * | 2016-03-18 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical compound |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| GB201604681D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| BR112019009245A2 (pt) | 2016-11-08 | 2019-07-16 | Bristol-Myers Squibb Company | azol amidas e aminas como inibidores de alfav integrina |
| EP3538526B1 (en) | 2016-11-08 | 2024-04-10 | Bristol-Myers Squibb Company | Cyclobutane- and azetidine-containing mono and spirocyclic compounds as alpha v integrin inhibitors |
| ES2925173T3 (es) | 2016-11-08 | 2022-10-14 | Bristol Myers Squibb Co | Acidos propiónicos sustituidos en la posición 3 como inhibidores de la integrina alfa V |
| WO2018089360A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Pyrrole amides as alpha v integrin inhibitors |
| CA3042714A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Indazole derivatives as a .alpha.v integrin antagonists |
| US10696672B2 (en) | 2016-12-23 | 2020-06-30 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| EP4147698A1 (en) | 2017-02-28 | 2023-03-15 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| BR112019017929A2 (pt) | 2017-02-28 | 2020-05-19 | Morphic Therapeutic Inc | inibidores de integrina (alfa-v)(beta-6) |
| WO2018167295A1 (en) * | 2017-03-17 | 2018-09-20 | Technische Universität München | LIGANDS FOR INTEGRIN αvβ8, SYNTHESIS AND USES THEREOF |
| MX2020004455A (es) | 2017-11-07 | 2020-07-24 | Bristol Myers Squibb Co | Derivados de pirrolopirazina como inhibidores de integrina alfa v. |
| CN108208177A (zh) * | 2017-11-28 | 2018-06-29 | 上海交通大学医学院附属新华医院 | 含丁酸类化合物的组合物及其应用 |
| ES3019404T3 (en) | 2018-08-29 | 2025-05-20 | Morphic Therapeutic Inc | Integrin inhibitors |
| ES3027421T3 (en) * | 2018-08-29 | 2025-06-13 | Morphic Therapeutic Inc | Inhibitors of (alpha-v)(beta-6) integrin |
| SI3844162T1 (sl) * | 2018-08-29 | 2025-06-30 | Morphic Therapeutic, Inc. | Zaviralci integrina alfa v beta6 |
| WO2020047208A1 (en) * | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| JP2022512648A (ja) * | 2018-10-09 | 2022-02-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 心筋線維化の処置のためのαＶ－インテグリン（ＣＤ５１）阻害剤の使用 |
| CA3119807A1 (en) * | 2018-12-04 | 2020-06-11 | Sumitomo Dainippon Pharma Oncology, Inc. | Cdk9 inhibitors and polymorphs thereof for use as agents for treatment of cancer |
| GB202010626D0 (en) | 2020-07-10 | 2020-08-26 | Univ Nottingham | Compound |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| IL136495A0 (en) | 1997-12-17 | 2001-06-14 | Merck & Co Inc | Integrin receptor antagonists |
| JP2002508323A (ja) | 1997-12-17 | 2002-03-19 | メルク エンド カムパニー インコーポレーテッド | インテグリン受容体拮抗薬 |
| EE200100642A (et) | 1999-06-02 | 2003-02-17 | Merck & Co., Inc. | Alfa-v integriinretseptori antagonistid ja farmatseutiline kompositsioon |
| AU748949B2 (en) | 1999-06-23 | 2002-06-13 | Merck & Co., Inc. | Integrin receptor antagonists |
| WO2001024797A1 (en) * | 1999-10-04 | 2001-04-12 | Merck & Co., Inc. | Integrin receptor antagonists |
| YU32502A (sh) | 1999-11-08 | 2004-12-31 | Merck & Co.Inc. | Postupak i intermedijeri za proizvodnju imidazolidinonskih antagonista alfa v integrina |
| US6921767B2 (en) | 2000-06-15 | 2005-07-26 | Pharmacia Corporation | Cycloalkyl alkanoic acids as integrin receptor antagonists derivatives |
| JP2004511434A (ja) * | 2000-06-15 | 2004-04-15 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸 |
| CA2416751A1 (en) | 2000-07-26 | 2002-01-31 | Merck & Co., Inc. | Alpha v integrin receptor antagonists |
| AU2001290772A1 (en) | 2000-09-14 | 2002-03-26 | Merck And Co., Inc. | Alpha v integrin receptor antagonists |
| EP1349548A4 (en) | 2001-01-03 | 2004-06-02 | Merck & Co Inc | METHOD AND COMPOSITIONS FOR TREATING PERIODONTOSIS |
| DE10112771A1 (de) | 2001-03-16 | 2002-09-26 | Merck Patent Gmbh | Inhibitoren des Integrins alpha¶v¶beta¶6¶ |
| MY130622A (en) | 2001-11-05 | 2007-07-31 | Novartis Ag | Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (pde4) inhibitors |
| MY147019A (en) | 2002-03-13 | 2012-10-15 | Biogen Idec Inc | Anti-alpha v beta 6 antibodies |
| US20040224986A1 (en) | 2002-08-16 | 2004-11-11 | Bart De Corte | Piperidinyl targeting compounds that selectively bind integrins |
| EP1592421A1 (en) | 2002-12-20 | 2005-11-09 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| US6932865B2 (en) | 2003-04-11 | 2005-08-23 | Lockheed Martin Corporation | System and method of making single-crystal structures through free-form fabrication techniques |
| HRP20140147T1 (hr) | 2007-03-23 | 2014-03-28 | Amgen Inc. | 3-supstituirani derivati hinolina ili hinoksalina i njihova uporaba kao inhibitora fosfatidilinozitol 3-kinaze (pi3k) |
| US8563566B2 (en) | 2007-08-01 | 2013-10-22 | Valeant Pharmaceuticals International | Naphthyridine derivatives as potassium channel modulators |
| JP2011500823A (ja) | 2007-10-22 | 2011-01-06 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体 |
| WO2011111880A1 (ko) | 2010-03-08 | 2011-09-15 | 주식회사 메디젠텍 | 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물 |
| GB201305668D0 (en) * | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| WO2015048819A1 (en) | 2013-09-30 | 2015-04-02 | The Regents Of The University Of California | Anti-alphavbeta1 integrin compounds and methods |
| GB201417002D0 (en) * | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201417011D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417094D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417018D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| EP3925959A1 (en) | 2015-02-19 | 2021-12-22 | OcuTerra Therapeutics, Inc. | Fluorinated derivatives of 3-(2-oxo-3-(3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl)imidazolidin-1-yl)propanoic acid and uses thereof |
| WO2016145258A1 (en) | 2015-03-10 | 2016-09-15 | The Regents Of The University Of California | Anti-alphavbeta1 integrin inhibitors and methods of use |
| GB201604589D0 (en) | 2016-03-18 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical compound |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
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2014
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- 2015-09-22 EP EP18191644.6A patent/EP3428167A1/en not_active Withdrawn
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- 2015-09-22 DK DK15767475.5T patent/DK3197892T3/en active
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