JP2017528486A5 - - Google Patents
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- JP2017528486A5 JP2017528486A5 JP2017514899A JP2017514899A JP2017528486A5 JP 2017528486 A5 JP2017528486 A5 JP 2017528486A5 JP 2017514899 A JP2017514899 A JP 2017514899A JP 2017514899 A JP2017514899 A JP 2017514899A JP 2017528486 A5 JP2017528486 A5 JP 2017528486A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- medicament
- compound
- aryl
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 31
- 239000003814 drug Substances 0.000 claims 27
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 26
- 125000003118 aryl group Chemical group 0.000 claims 17
- -1 3- (hydroxymethyl) phenyl Chemical group 0.000 claims 15
- 208000035475 disorder Diseases 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 12
- 125000004404 heteroalkyl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 208000007536 Thrombosis Diseases 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 102000001399 Kallikrein Human genes 0.000 claims 4
- 108060005987 Kallikrein Proteins 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 4
- 208000005189 Embolism Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 208000001435 Thromboembolism Diseases 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000004474 heteroalkylene group Chemical group 0.000 claims 3
- 230000004968 inflammatory condition Effects 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 208000032382 Ischaemic stroke Diseases 0.000 claims 2
- 208000003788 Neoplasm Micrometastasis Diseases 0.000 claims 2
- 108090000190 Thrombin Proteins 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000030533 eye disease Diseases 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 229960004072 thrombin Drugs 0.000 claims 2
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 1
- 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 206010014522 Embolism venous Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010019860 Hereditary angioedema Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 102100038297 Kallikrein-1 Human genes 0.000 claims 1
- 101710176219 Kallikrein-1 Proteins 0.000 claims 1
- 206010067125 Liver injury Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000011219 Netherton syndrome Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 1
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 206010051379 Systemic Inflammatory Response Syndrome Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 230000001548 androgenic effect Effects 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 230000023555 blood coagulation Effects 0.000 claims 1
- 230000001269 cardiogenic effect Effects 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 231100000012 chronic liver injury Toxicity 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 201000011190 diabetic macular edema Diseases 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 239000003889 eye drop Substances 0.000 claims 1
- 229940012356 eye drops Drugs 0.000 claims 1
- 239000003527 fibrinolytic agent Substances 0.000 claims 1
- 230000003480 fibrinolytic effect Effects 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 208000029824 high grade glioma Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 208000012947 ischemia reperfusion injury Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 150000003217 pyrazoles Chemical group 0.000 claims 1
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical group OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 claims 1
- 230000002207 retinal effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 230000008728 vascular permeability Effects 0.000 claims 1
- 208000004043 venous thromboembolism Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462051511P | 2014-09-17 | 2014-09-17 | |
| US201462051585P | 2014-09-17 | 2014-09-17 | |
| US62/051,511 | 2014-09-17 | ||
| US62/051,585 | 2014-09-17 | ||
| PCT/US2015/050809 WO2016044662A1 (en) | 2014-09-17 | 2015-09-17 | Pyrazolyl-substituted pyridone compounds as serine protease inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020087253A Division JP2020143112A (ja) | 2014-09-17 | 2020-05-19 | セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017528486A JP2017528486A (ja) | 2017-09-28 |
| JP2017528486A5 true JP2017528486A5 (enExample) | 2018-11-01 |
Family
ID=55533876
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017514899A Pending JP2017528486A (ja) | 2014-09-17 | 2015-09-17 | セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 |
| JP2020087253A Pending JP2020143112A (ja) | 2014-09-17 | 2020-05-19 | セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020087253A Pending JP2020143112A (ja) | 2014-09-17 | 2020-05-19 | セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US10189810B2 (enExample) |
| EP (1) | EP3194369A4 (enExample) |
| JP (2) | JP2017528486A (enExample) |
| KR (1) | KR20170048410A (enExample) |
| CN (1) | CN106687445A (enExample) |
| AU (2) | AU2015317522A1 (enExample) |
| BR (1) | BR112017004704A2 (enExample) |
| CA (1) | CA2960790A1 (enExample) |
| IL (1) | IL250965A0 (enExample) |
| MX (1) | MX2017003624A (enExample) |
| RU (1) | RU2017112739A (enExample) |
| SG (1) | SG11201701940UA (enExample) |
| WO (1) | WO2016044662A1 (enExample) |
| ZA (1) | ZA201701799B (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3421036B8 (en) * | 2013-03-15 | 2020-12-30 | Verseon International Corporation | Multisubstituted aromatic compounds as serine protease inhibitors |
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| RU2017112739A (ru) * | 2014-09-17 | 2018-10-17 | Версеон Корпорейшн | Пиразолил-замещенные пиридоновые соединения как ингибиторы сериновых протеаз |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| RS60900B1 (sr) | 2016-02-19 | 2020-11-30 | Sprint Bioscience Ab | Jedinjenja 6-heterociklil-4-morfolin-4-ilpiridin-2-ona korisna za lečenje kancera i dijabetesa |
| RU2754664C2 (ru) * | 2016-02-19 | 2021-09-06 | Спринт Биосайенс Аб | 6-арил-4-морфолин-1-илпиридоны, пригодные для лечения рака или диабета |
| CN106008362B (zh) * | 2016-05-24 | 2018-08-10 | 杰达维（上海）医药科技发展有限公司 | 一种嘧啶衍生物的制备方法 |
| SG10201913616UA (en) | 2016-05-31 | 2020-03-30 | Kalvista Pharmaceuticals Ltd | Pyrazole derivatives as plasma kallikrein inhibitors |
| GB201609603D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| TWI760428B (zh) * | 2017-01-26 | 2022-04-11 | 日商三井化學Agro股份有限公司 | 吡啶酮化合物及以吡啶酮化合物作為有效成分的農園藝用殺菌劑 |
| TWI788343B (zh) * | 2017-04-18 | 2023-01-01 | 美商塞爾基因定量細胞研究公司 | 治療用化合物 |
| MX2020005168A (es) | 2017-11-29 | 2020-08-20 | Kalvista Pharmaceuticals Ltd | Formas de dosificacion que contienen un inhibidor calicreina de plasma. |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| CN110386932A (zh) | 2018-04-20 | 2019-10-29 | 艾科思莱德制药公司 | 用于抗肿瘤疗法中的双重atm和dna-pk抑制剂 |
| CN113164765A (zh) * | 2018-07-13 | 2021-07-23 | 维颂国际公司 | 凝血酶抑制剂、制剂及其用途 |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| CN110467601B (zh) * | 2019-08-29 | 2021-07-02 | 杭州市西溪医院 | 一种吡唑联吡啶酮类化合物、中间体及其制备方法及应用 |
| DE102020103516B4 (de) | 2020-02-11 | 2023-12-07 | Universität Zu Lübeck | Antivirale Wirkstoffe mit breiter Aktivität |
| BR102020009679A2 (pt) | 2020-05-14 | 2021-11-23 | Fundação Universidade Federal Do Abc - Ufabc | Anticorpos recombinantes humanos para inibição da calicreína tecidual humana 7 (klk7) e uso em doenças relacionadas ao processo de descamação da pele |
| CA3199999A1 (en) | 2020-11-25 | 2022-06-02 | Deciphera Pharmaceuticals, Llc | Morpholino derivatives as vsp34 inhibitors for use in the treatment of a viral infection |
Family Cites Families (118)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE627393A (enExample) | 1962-01-23 | |||
| BE793955A (fr) | 1972-01-15 | 1973-07-12 | Merck Patent Gmbh | Arylpiperazines et leur procede de preparation |
| DE2409753A1 (de) | 1974-03-01 | 1975-09-11 | Basf Ag | Substituierte pyrazole |
| US4256108A (en) | 1977-04-07 | 1981-03-17 | Alza Corporation | Microporous-semipermeable laminated osmotic system |
| US4160452A (en) | 1977-04-07 | 1979-07-10 | Alza Corporation | Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina |
| US4265874A (en) | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| PH23506A (en) | 1986-05-23 | 1989-08-16 | Smithkline Beckman Corp | 1-aralkyl-substituted-1,2,4,-triazole-5-thiols as dopamine- -hydroxylase inhibitors |
| JPH089541B2 (ja) | 1988-03-07 | 1996-01-31 | 三井東圧化学株式会社 | ピラゾール類を主成分とする脳浮腫抑制剤 |
| JP2784925B2 (ja) | 1988-09-07 | 1998-08-13 | 日本農薬株式会社 | ３又は５−フェニルピラゾール類又はその塩及び除草剤 |
| DE69212850T2 (de) | 1991-01-15 | 1997-03-06 | Alcon Lab Inc | Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| JP3810097B2 (ja) | 1993-01-15 | 2006-08-16 | 明治製菓株式会社 | ピロリジン−２−イルカルボニル複素環式化合物誘導体 |
| US5466823A (en) | 1993-11-30 | 1995-11-14 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides |
| RU2139281C1 (ru) | 1993-11-30 | 1999-10-10 | Джи Ди Сирл энд Компани | Пиразолилзамещенный бензолсульфонамид или его фармацевтически приемлемая соль, фармацевтическая композиция, способ лечения от воспаления или связанного с воспалением заболевания |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| JPH10509708A (ja) | 1994-11-10 | 1998-09-22 | コア セラピューティクス，インコーポレイティド | プロテイン・キナーゼのインヒビターとして有用な医薬ピラゾール組成物 |
| US5733955A (en) | 1995-02-10 | 1998-03-31 | The Goodyear Tire & Rubber Company | Asphalt cement modification |
| JP3663522B2 (ja) | 1995-08-12 | 2005-06-22 | 日本農薬株式会社 | 植物生育調節用組成物及びその使用方法 |
| US5756529A (en) | 1995-09-29 | 1998-05-26 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies |
| WO1997013756A1 (en) | 1995-10-13 | 1997-04-17 | Otsuka Kagaku Kabushiki Kaisha | Pyrazole derivatives and insecticidal compositions containing the same as active ingredient |
| US5792761A (en) | 1996-08-12 | 1998-08-11 | Merck & Co., Inc. | Thrombin inhibitors |
| DE19632773A1 (de) | 1996-08-14 | 1998-02-19 | Basf Ag | Neue Thrombininhibitoren |
| GB9622370D0 (en) | 1996-10-28 | 1997-01-08 | Merck Sharp & Dohme | Therapeutic agents |
| US5869500A (en) | 1996-12-13 | 1999-02-09 | Hoffmann-La Roche Inc. | Pyridone compounds useful in treating Alzheimer's disease |
| CN1246847A (zh) | 1996-12-23 | 2000-03-08 | 杜邦药品公司 | 作为Xa因子抑制剂的含氮杂芳族化合物 |
| BR9808398A (pt) * | 1997-03-21 | 2000-05-16 | Novartis Ag | Derivados pirazol com atividade herbicida |
| WO2000009500A2 (en) | 1998-08-11 | 2000-02-24 | Nihon Bayer Agrochem K.K. | Nematicidal pyrazoles |
| KR20000047461A (ko) | 1998-12-29 | 2000-07-25 | 성재갑 | 트롬빈 억제제 |
| SE9900070D0 (sv) | 1999-01-13 | 1999-01-13 | Astra Ab | New use |
| AR023510A1 (es) | 1999-04-21 | 2002-09-04 | Astrazeneca Ab | Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina. |
| AU5020400A (en) | 1999-05-20 | 2000-12-12 | E.I. Du Pont De Nemours And Company | Heteroaryloxypyrimidine insecticides and acaricides |
| BR0013143A (pt) | 1999-08-12 | 2002-06-11 | Pharmacia Italia Spa | Derivados de 3 (5) amino pirazol, processo para sua preparação e uso dos mesmos como agentes antitumorais |
| US6632815B2 (en) | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| JP2003509412A (ja) | 1999-09-17 | 2003-03-11 | シーオーアール セラピューティクス インコーポレイテッド | Ｘａ因子阻害剤 |
| WO2001040223A2 (en) | 1999-12-02 | 2001-06-07 | Novartis Ag | Aminoheterocyclylamides as pesticides and antiparasitic agents |
| AU2001273040A1 (en) | 2000-06-27 | 2002-01-08 | Du Pont Pharmaceuticals Company | Factor xa inhibitors |
| US6884804B2 (en) | 2001-05-16 | 2005-04-26 | Vertex Pharmaceuticals Incorporated | Inhibitors of Src and other protein kinases |
| US6589997B2 (en) | 2001-06-29 | 2003-07-08 | North Shore-Long Island Jewish Health System | Small-molecule modulators of hepatocyte growth factor/scatter factor activities |
| SI21097A (sl) | 2001-12-04 | 2003-06-30 | Univerza V Ljubljani | Inhibitorji trombina |
| WO2003062206A2 (en) | 2002-01-23 | 2003-07-31 | Arena Pharmaceuticals, Inc. | Small molecule modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto |
| SE0200198D0 (sv) | 2002-01-23 | 2002-01-23 | Astrazeneca Ab | New use |
| JP2003313103A (ja) | 2002-02-20 | 2003-11-06 | Sankyo Agro Kk | ４−アシルアミノピラゾール誘導体を有効成分として含有する農薬 |
| GB0214139D0 (en) | 2002-06-19 | 2002-07-31 | Glaxo Group Ltd | Chemical compounds |
| DE10229070A1 (de) | 2002-06-28 | 2004-01-15 | Merck Patent Gmbh | Phenylderivate 5 |
| TW200424183A (en) * | 2002-08-09 | 2004-11-16 | Nps Pharma Inc | New compounds |
| WO2004035564A1 (en) | 2002-10-17 | 2004-04-29 | Syngenta Participations Ag | Pyridine derivatives useful as herbicides |
| US7192976B2 (en) | 2002-12-21 | 2007-03-20 | Angion Biomedica Corporation | Small molecule modulators of hepatocyte growth factor (scatter factor) activity |
| MXPA05006200A (es) | 2002-12-23 | 2005-08-19 | Aventis Pharma Gmbh | Derivados de pirazol como inhibidores del factor xa. |
| US20060229335A1 (en) | 2002-12-24 | 2006-10-12 | Bradley Teegarden | Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a |
| US20040147561A1 (en) | 2002-12-27 | 2004-07-29 | Wenge Zhong | Pyrid-2-one derivatives and methods of use |
| JP2004231528A (ja) | 2003-01-28 | 2004-08-19 | Sankyo Agro Kk | アミド誘導体 |
| GB0308318D0 (en) | 2003-04-10 | 2003-05-14 | Merck Sharp & Dohme | Therapeutic agents |
| ATE522525T1 (de) | 2003-05-01 | 2011-09-15 | Bristol Myers Squibb Co | Arylsubstituierte pyrazolamidverbindungen, die als kinase-inhibitoren von nutzen sind |
| PE20050525A1 (es) | 2003-05-02 | 2005-09-08 | Elan Pharm Inc | Derivados de pirazol sustituido y compuestos relacionados como antagonistas del receptor de bradiquinina b1 |
| EP1479679A1 (en) | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Triazole-derivatives as factor Xa inhibitors |
| US7223780B2 (en) | 2003-05-19 | 2007-05-29 | Sanofi-Aventis Deutschland Gmbh | Triazole-derivatives as blood clotting enzyme factor Xa inhibitors |
| WO2005030751A2 (en) | 2003-09-08 | 2005-04-07 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| CN102060806A (zh) | 2003-09-11 | 2011-05-18 | iTherX药品公司 | 细胞因子抑制剂 |
| WO2005030128A2 (en) | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Pyrazole modulators of metabotropic glutamate receptors |
| TW200526588A (en) | 2003-11-17 | 2005-08-16 | Smithkline Beecham Corp | Chemical compounds |
| US20080188527A1 (en) | 2003-12-23 | 2008-08-07 | Cashman John R | Synthetic Compounds and Derivatives as Modulators of Smoking or Nicotine Ingestion and Lung Cancer |
| KR101258504B1 (ko) | 2004-03-26 | 2013-04-26 | 메틸진 인코포레이티드 | 히스톤 데아세틸라제의 억제제 |
| US7429604B2 (en) * | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| US7235530B2 (en) | 2004-09-27 | 2007-06-26 | Dyax Corporation | Kallikrein inhibitors and anti-thrombolytic agents and uses thereof |
| JP2008526887A (ja) | 2005-01-10 | 2008-07-24 | ユニバーシティ オブ コネチカット | カンナビノイド受容体に作用する新規なヘテロピロール類似体 |
| JPWO2006109846A1 (ja) | 2005-04-06 | 2008-11-20 | 武田薬品工業株式会社 | トリアゾール誘導体およびその用途 |
| GB0507577D0 (en) | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| CN100427481C (zh) | 2005-05-26 | 2008-10-22 | 沈阳化工研究院 | 一种芳基醚类化合物及其制备与应用 |
| CA2630233A1 (en) | 2005-12-05 | 2007-06-14 | Boehringer Ingelheim International Gmbh | Substituted pyrazole compounds useful as soluble epoxide hydrolase inhibitors |
| US20090118336A1 (en) | 2006-05-03 | 2009-05-07 | Laurent David | Pyrazole derivatives and their use as pi3k inhibitors |
| WO2007146712A2 (en) | 2006-06-09 | 2007-12-21 | Kemia, Inc. | Therapy using cytokine inhibitors |
| DE102006032824A1 (de) | 2006-07-14 | 2008-01-17 | Bayer Healthcare Ag | Substituierte Indazole |
| AU2007276205A1 (en) | 2006-07-17 | 2008-01-24 | Boehringer Ingelheim International Gmbh | New indications for direct thrombin inhibitors in the cardiovascular field |
| EP2051707B1 (en) | 2006-07-31 | 2013-07-17 | Activesite Pharmaceuticals, Inc. | Inhibitors of plasma kallikrein |
| WO2008023235A1 (en) | 2006-08-25 | 2008-02-28 | Pfizer Products Inc. | Pyrazole derivatives as anti-platelet and anti-thrombotic agents |
| WO2008062739A1 (en) | 2006-11-20 | 2008-05-29 | Japan Tobacco Inc. | Pyrazoles and use thereof as drugs |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| WO2008061796A2 (en) | 2006-11-24 | 2008-05-29 | Ac Immune Sa | Compounds for the treatment of diseases associated with amyloid or amyloid-like proteins |
| JP2010513519A (ja) | 2006-12-22 | 2010-04-30 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | キナーゼインヒビター活性を有するある種のピラゾリン誘導体 |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| WO2008105383A1 (ja) | 2007-02-26 | 2008-09-04 | Toray Industries, Inc. | ピラゾール誘導体およびその医薬用途 |
| GB0714129D0 (en) | 2007-07-19 | 2007-08-29 | Smithkline Beecham Corp | compounds |
| US20110071289A1 (en) | 2007-08-06 | 2011-03-24 | Dainippon Sumitomo Pharma Co., Ltd. | Aminopyrazole amide derivative |
| KR101559597B1 (ko) | 2007-09-28 | 2015-10-12 | 다케다 야쿠힌 고교 가부시키가이샤 | ５―원 헤테로시클릭 화합물 |
| AU2008345225A1 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| EP2259679A4 (en) | 2008-01-31 | 2011-09-14 | Joslin Diabetes Ct | METHODS OF TREATING KALLIKREIN RELATED DISORDERS |
| AU2009212135B2 (en) | 2008-02-07 | 2014-08-21 | Massachusetts Eye & Ear Infirmary | Compounds that enhance Atoh-1 expression |
| WO2009140621A2 (en) | 2008-05-15 | 2009-11-19 | Duke University | Compositions and methods relating to heat shock transcription factor activating compounds and targets thereof |
| CL2009001214A1 (es) | 2008-05-19 | 2010-12-31 | Schering Corp | Compuestos derivados de heterociclo, moduladores de serina proteasas composicion fa<rmacaeutica que los comprende; y su uso en el tratamiento de trastornos tromboembolicos |
| EP2313093A4 (en) | 2008-07-10 | 2012-03-28 | Angion Biomedica Corp | METHOD AND COMPOSITIONS FOR LOW-MOLECULAR MODULATORS OF THE HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY |
| US8273900B2 (en) | 2008-08-07 | 2012-09-25 | Novartis Ag | Organic compounds |
| WO2010017902A1 (de) | 2008-08-14 | 2010-02-18 | Bayer Cropscience Aktiengesellschaft | Insektizide 4-phenyl-1h-pyrazole |
| US20110306640A1 (en) | 2008-08-19 | 2011-12-15 | Boehringer Ingelheim International Gmbh | Dabigatran in tumour therapy |
| BRPI0917507A2 (pt) | 2008-08-19 | 2015-11-17 | Boehring Ingelheim Internat Gmbh | dabigatrana para a caterização cardíaca percutânea intervencionista |
| CA2734804A1 (en) | 2008-08-19 | 2010-02-25 | Boehringer Ingelheim International Gmbh | Use of dabigatranetexilate for treating patients with pulmonary hypertension |
| BRPI1011192A2 (pt) | 2009-05-07 | 2016-03-15 | Gruenenthal Gmbh | derivados de carboxamida e ureia aromáticas substituídas como ligantes de receptor de vaniloide, composição farmacêutica, uso e processo para preparação dos referidos derivados |
| CA2829790C (en) * | 2010-03-30 | 2018-06-05 | Verseon Corporation | Multisubstituted aromatic compounds as inhibitors of thrombin |
| CN101851207B (zh) | 2010-06-11 | 2012-01-25 | 扬州康伊尔医药科技有限公司 | 抗病毒化合物中间体1-酰基-吡唑-3-羧酸及其制备方法 |
| JP5878171B2 (ja) | 2010-06-24 | 2016-03-08 | ギリアード サイエンシーズ， インコーポレイテッド | 抗ウイルス剤としてのピラゾロ［１，５−ａ］ピリミジン |
| JPWO2012020820A1 (ja) | 2010-08-11 | 2013-10-28 | 大正製薬株式会社 | ヘテロアリール−ピラゾール誘導体 |
| MX355782B (es) | 2010-11-03 | 2018-04-30 | Dow Agrosciences Llc | Composiciones pesticidas y procesos relacionados a las mismas. |
| WO2012065019A2 (en) | 2010-11-12 | 2012-05-18 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of p13k alpha |
| EP2688872A4 (en) | 2011-03-22 | 2014-08-27 | Merck Sharp & Dohme | AMIDOPYRAZOLHEMMER OF INTERLEUKIN RECEPTOR-MEDIATED KINASES |
| WO2012142308A1 (en) | 2011-04-13 | 2012-10-18 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
| WO2012154880A1 (en) | 2011-05-09 | 2012-11-15 | Proteostasis Therapeutics, Inc. | Proteostasis regulators for treating cystic fibrosis and other protein misfolding diseases |
| RU2631487C2 (ru) | 2011-05-17 | 2017-09-22 | Плексксикон Инк. | Модуляция киназ и показания к её применению |
| WO2013039985A2 (en) | 2011-09-12 | 2013-03-21 | The Johns Hopkins University | Serine protease inhibitors |
| WO2013049591A2 (en) | 2011-09-29 | 2013-04-04 | Verseon Corporation | Dual inhibitor compounds and methods of use thereof |
| US9139564B2 (en) * | 2011-12-27 | 2015-09-22 | Ironwood Pharmaceuticals, Inc. | 2-benzyl, 3-(pyrimidin-2-yl) substituted pyrazoles useful as sGC stimulators |
| EP2807157A1 (en) | 2012-01-27 | 2014-12-03 | Novartis AG | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| KR20150021036A (ko) | 2012-06-14 | 2015-02-27 | 다이이찌 산쿄 가부시키가이샤 | 피페리디닐피라졸로피리딘 유도체 |
| TWI498325B (zh) | 2013-01-18 | 2015-09-01 | Hoffmann La Roche | ３－取代吡唑及其用途 |
| EP3421036B8 (en) * | 2013-03-15 | 2020-12-30 | Verseon International Corporation | Multisubstituted aromatic compounds as serine protease inhibitors |
| WO2015087995A1 (ja) | 2013-12-13 | 2015-06-18 | 第一三共株式会社 | シクロアルキル又はヘテロシクリルピラゾロピリジン誘導体 |
| HRP20241145T1 (hr) | 2014-02-06 | 2024-11-22 | Nxera Pharma Uk Limited | Biciklički aza spojevi kao agonisti muskarinskih receptora |
| RU2017112739A (ru) * | 2014-09-17 | 2018-10-17 | Версеон Корпорейшн | Пиразолил-замещенные пиридоновые соединения как ингибиторы сериновых протеаз |
-
2015
- 2015-09-17 RU RU2017112739A patent/RU2017112739A/ru not_active Application Discontinuation
- 2015-09-17 AU AU2015317522A patent/AU2015317522A1/en not_active Abandoned
- 2015-09-17 US US15/512,037 patent/US10189810B2/en active Active
- 2015-09-17 BR BR112017004704A patent/BR112017004704A2/pt not_active Application Discontinuation
- 2015-09-17 CN CN201580050088.0A patent/CN106687445A/zh active Pending
- 2015-09-17 CA CA2960790A patent/CA2960790A1/en not_active Abandoned
- 2015-09-17 SG SG11201701940UA patent/SG11201701940UA/en unknown
- 2015-09-17 EP EP15841577.8A patent/EP3194369A4/en not_active Withdrawn
- 2015-09-17 MX MX2017003624A patent/MX2017003624A/es unknown
- 2015-09-17 KR KR1020177007352A patent/KR20170048410A/ko not_active Withdrawn
- 2015-09-17 JP JP2017514899A patent/JP2017528486A/ja active Pending
- 2015-09-17 WO PCT/US2015/050809 patent/WO2016044662A1/en not_active Ceased
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2017
- 2017-03-06 IL IL250965A patent/IL250965A0/en unknown
- 2017-03-13 ZA ZA2017/01799A patent/ZA201701799B/en unknown
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2018
- 2018-12-07 US US16/213,272 patent/US20190359586A1/en not_active Abandoned
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2020
- 2020-03-26 AU AU2020202167A patent/AU2020202167A1/en not_active Abandoned
- 2020-05-19 JP JP2020087253A patent/JP2020143112A/ja active Pending
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