JP2003500403A5 - - Google Patents
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- Publication number
- JP2003500403A5 JP2003500403A5 JP2000619792A JP2000619792A JP2003500403A5 JP 2003500403 A5 JP2003500403 A5 JP 2003500403A5 JP 2000619792 A JP2000619792 A JP 2000619792A JP 2000619792 A JP2000619792 A JP 2000619792A JP 2003500403 A5 JP2003500403 A5 JP 2003500403A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- aryl
- independently
- alkenyl
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 description 47
- 125000003118 aryl group Chemical group 0.000 description 35
- 125000000217 alkyl group Chemical group 0.000 description 30
- 125000001424 substituent group Chemical group 0.000 description 27
- 230000002452 interceptive effect Effects 0.000 description 21
- 125000003342 alkenyl group Chemical group 0.000 description 19
- 125000005843 halogen group Chemical group 0.000 description 12
- 125000004404 heteroalkyl group Chemical group 0.000 description 12
- 239000000203 mixture Substances 0.000 description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 10
- 229910052739 hydrogen Inorganic materials 0.000 description 10
- 239000001257 hydrogen Substances 0.000 description 10
- 125000003710 aryl alkyl group Chemical group 0.000 description 9
- 125000001072 heteroaryl group Chemical group 0.000 description 9
- 125000002252 acyl group Chemical group 0.000 description 8
- 125000000304 alkynyl group Chemical group 0.000 description 8
- 125000005842 heteroatom Chemical group 0.000 description 7
- 125000003435 aroyl group Chemical group 0.000 description 6
- 125000004429 atom Chemical group 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 5
- 125000002947 alkylene group Chemical group 0.000 description 4
- 229920006395 saturated elastomer Polymers 0.000 description 4
- 206010040070 Septic Shock Diseases 0.000 description 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 3
- 125000005647 linker group Chemical group 0.000 description 3
- -1 oxime ester Chemical class 0.000 description 3
- 150000003839 salts Chemical class 0.000 description 3
- 125000006850 spacer group Chemical group 0.000 description 3
- 206010040047 Sepsis Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 2
- SQDFHQJTAWCFIB-UHFFFAOYSA-N n-methylidenehydroxylamine Chemical compound ON=C SQDFHQJTAWCFIB-UHFFFAOYSA-N 0.000 description 2
- 150000002923 oximes Chemical class 0.000 description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 2
- 230000007112 pro inflammatory response Effects 0.000 description 2
- 230000002685 pulmonary effect Effects 0.000 description 2
- 125000000547 substituted alkyl group Chemical group 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical group C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 description 1
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical group C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 description 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 description 1
- 0 CIN(C*1)**C*1I* Chemical compound CIN(C*1)**C*1I* 0.000 description 1
- 206010063094 Cerebral malaria Diseases 0.000 description 1
- 206010009900 Colitis ulcerative Diseases 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 208000011231 Crohn disease Diseases 0.000 description 1
- 201000005569 Gout Diseases 0.000 description 1
- 206010018634 Gouty Arthritis Diseases 0.000 description 1
- 208000009329 Graft vs Host Disease Diseases 0.000 description 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 1
- 208000007542 Paresis Diseases 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 206010063837 Reperfusion injury Diseases 0.000 description 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 description 1
- 201000010001 Silicosis Diseases 0.000 description 1
- 206010044248 Toxic shock syndrome Diseases 0.000 description 1
- 231100000650 Toxic shock syndrome Toxicity 0.000 description 1
- 201000006704 Ulcerative Colitis Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 description 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 description 1
- 125000004450 alkenylene group Chemical group 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 208000019664 bone resorption disease Diseases 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 230000032823 cell division Effects 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 208000024908 graft versus host disease Diseases 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 208000002551 irritable bowel syndrome Diseases 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 230000036303 septic shock Effects 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/316,761 | 1999-05-21 | ||
| US09/316,761 US6589954B1 (en) | 1998-05-22 | 1999-05-21 | Compounds and methods to treat cardiac failure and other disorders |
| US15459499P | 1999-09-17 | 1999-09-17 | |
| US60/154,594 | 1999-09-17 | ||
| US20260800P | 2000-05-09 | 2000-05-09 | |
| US60/202,608 | 2000-05-09 | ||
| PCT/US2000/014003 WO2000071535A1 (en) | 1999-05-21 | 2000-05-19 | INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003500403A JP2003500403A (ja) | 2003-01-07 |
| JP2003500403A5 true JP2003500403A5 (enExample) | 2007-07-05 |
Family
ID=27387611
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000619792A Pending JP2003500403A (ja) | 1999-05-21 | 2000-05-19 | ｐ３８キナーゼのインヒビターとしてのインドール型誘導体 |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP1178983B1 (enExample) |
| JP (1) | JP2003500403A (enExample) |
| KR (1) | KR100743377B1 (enExample) |
| CN (1) | CN1310906C (enExample) |
| AT (1) | ATE376547T1 (enExample) |
| AU (2) | AU772295B2 (enExample) |
| BG (1) | BG106091A (enExample) |
| BR (1) | BR0011274A (enExample) |
| CA (1) | CA2372567A1 (enExample) |
| CZ (1) | CZ20014126A3 (enExample) |
| DE (1) | DE60036868D1 (enExample) |
| HR (1) | HRP20010854A2 (enExample) |
| HU (1) | HUP0201261A3 (enExample) |
| IL (1) | IL146309A0 (enExample) |
| MX (1) | MXPA01011976A (enExample) |
| NO (1) | NO20015655L (enExample) |
| NZ (1) | NZ515285A (enExample) |
| PL (1) | PL352032A1 (enExample) |
| SK (1) | SK16482001A3 (enExample) |
| WO (1) | WO2000071535A1 (enExample) |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6541477B2 (en) | 1999-08-27 | 2003-04-01 | Scios, Inc. | Inhibitors of p38-a kinase |
| AU2001241927A1 (en) * | 2000-02-28 | 2001-09-12 | Scios Inc. | Inhibitors of p38-alpha kinase |
| US6573262B2 (en) | 2000-07-10 | 2003-06-03 | Bristol-Myers Sqibb Company | Composition and antiviral activity of substituted indoleoxoacetic piperazine derivatives |
| DE10037310A1 (de) * | 2000-07-28 | 2002-02-07 | Asta Medica Ag | Neue Indolderivate und deren Verwendung als Arzneimittel |
| ES2279837T3 (es) | 2000-11-20 | 2007-09-01 | Scios Inc. | Inhibidores de tipo piperidina/piperazina de la quinasa p38. |
| EP1339708A2 (en) | 2000-11-20 | 2003-09-03 | Scios Inc. | Indole-type inhibitors of p38 kinase |
| WO2002062423A1 (en) * | 2001-02-02 | 2002-08-15 | Bristol-Myers Squibb Company | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| US20030207910A1 (en) | 2001-02-02 | 2003-11-06 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| US20040110785A1 (en) | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| EP1427416A2 (en) | 2001-09-13 | 2004-06-16 | Synta Pharmaceuticals Corporation | 3-glyoxlylamideindoles for treating cancer |
| WO2003022274A2 (en) * | 2001-09-13 | 2003-03-20 | Synta Pharmaceuticals Corp. | 2-aroylimidazole compounds for treating cancer |
| GB0124933D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| GB0124938D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| CA2466665A1 (en) * | 2001-11-09 | 2003-05-22 | Scios Inc. | Method to treat cystic fibrosis |
| US20050085509A1 (en) * | 2001-11-22 | 2005-04-21 | Kanji Takahashi | Piperidin-2-one derivative compounds and drugs containing these compounds as the active ingredient |
| AU2003224025A1 (en) * | 2002-04-05 | 2003-10-20 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | p38 kinase inhibitors for treating mucus hypersecretion |
| GB0209818D0 (en) | 2002-04-30 | 2002-06-05 | Koninkl Philips Electronics Nv | Antenna arrangement |
| JP2005538066A (ja) | 2002-07-09 | 2005-12-15 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | 新規な抗コリン作用薬及びｐ３８キナーゼ阻害剤を用いた新規な医薬組成物 |
| US7268139B2 (en) | 2002-08-29 | 2007-09-11 | Scios, Inc. | Methods of promoting osteogenesis |
| CA2497408A1 (en) * | 2002-09-03 | 2004-03-18 | Sarvajit Chakravarty | Indole-type derivatives as inhibitors of p38 kinase |
| CN1713910A (zh) | 2002-10-09 | 2005-12-28 | 西奥斯股份有限公司 | 作为p38激酶抑制剂的氮杂吲哚衍生物 |
| EP1583535A4 (en) * | 2002-12-06 | 2008-03-19 | Scios Inc | METHOD FOR TREATING DIABETES |
| CA2517517C (en) | 2003-03-03 | 2012-12-18 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| ATE534649T1 (de) | 2003-05-15 | 2011-12-15 | Arqule Inc | Imidazothiazole und imidazoxazolderivative als inhibitoren von p38 |
| US20070010529A1 (en) * | 2003-05-19 | 2007-01-11 | Kanji Takahashi | Nitrogenous heterocyclic compounds and medical use thereof |
| GB0318814D0 (en) | 2003-08-11 | 2003-09-10 | Smithkline Beecham Corp | Novel compounds |
| US7244441B2 (en) | 2003-09-25 | 2007-07-17 | Scios, Inc. | Stents and intra-luminal prostheses containing map kinase inhibitors |
| GB0402138D0 (en) | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
| GB0402140D0 (en) | 2004-01-30 | 2004-03-03 | Smithkline Beecham Corp | Novel compounds |
| US7829560B2 (en) | 2004-07-08 | 2010-11-09 | Arqule, Inc. | 1,4-disubstituted naphthalenes as inhibitors of P38 MAP kinase |
| US20060035893A1 (en) | 2004-08-07 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
| EP2258704A1 (en) | 2004-10-19 | 2010-12-08 | ArQule, Inc. | Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 map kinase |
| US20060100432A1 (en) | 2004-11-09 | 2006-05-11 | Matiskella John D | Crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione |
| PE20060777A1 (es) | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas |
| EP1676574A3 (en) | 2004-12-30 | 2006-07-26 | Johnson & Johnson Vision Care, Inc. | Methods for promoting survival of transplanted tissues and cells |
| US8399666B2 (en) | 2005-11-04 | 2013-03-19 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| US7977359B2 (en) | 2005-11-04 | 2011-07-12 | Amira Pharmaceuticals, Inc. | 5-lipdxygenase-activating protein (FLAP) inhibitors |
| GB2431927B (en) * | 2005-11-04 | 2010-03-17 | Amira Pharmaceuticals Inc | 5-Lipoxygenase-activating protein (FLAP) inhibitors |
| US7851476B2 (en) | 2005-12-14 | 2010-12-14 | Bristol-Myers Squibb Company | Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-C]pyridin-3-YL]-1,2-dioxoethyl]-piperazine |
| RU2442777C2 (ru) | 2006-01-31 | 2012-02-20 | Эррэй Биофарма Инк. | Ингибиторы киназ и способы их применения |
| US7807671B2 (en) | 2006-04-25 | 2010-10-05 | Bristol-Myers Squibb Company | Diketo-piperazine and piperidine derivatives as antiviral agents |
| WO2008024391A1 (en) * | 2006-08-22 | 2008-02-28 | Scios Inc. | Pharmaceutical formulations of an indole-type derivative and related methods of use |
| EP1992344A1 (en) | 2007-05-18 | 2008-11-19 | Institut Curie | P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation |
| AR072008A1 (es) * | 2008-06-13 | 2010-07-28 | Merck & Co Inc | Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38 |
| US8546431B2 (en) | 2008-10-01 | 2013-10-01 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| WO2010065743A2 (en) * | 2008-12-03 | 2010-06-10 | Nanotherapeutics, Inc. | Bicyclic compounds and methods of making and using same |
| US9359300B2 (en) | 2010-12-06 | 2016-06-07 | Confluence Life Sciences, Inc. | Methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds |
| WO2012078674A1 (en) * | 2010-12-06 | 2012-06-14 | Confluence Life Sciences, Inc. | Substituted indole/indazole-pyrimidinyl compounds |
| DK2648516T3 (da) | 2010-12-06 | 2019-01-02 | Aclaris Therapeutics Inc | Substituerede pyridinon-pyridinylforbindelser |
| US8563558B2 (en) | 2010-12-06 | 2013-10-22 | Confluence Life Sciences, Inc. | Substituted pyridine urea compounds |
| WO2013086208A1 (en) | 2011-12-06 | 2013-06-13 | Confluence Life Sciences, Inc. | Substituted pyrimidinone-phenyl-pyrimidinyl compounds |
| SI3003039T1 (sl) | 2013-06-07 | 2021-08-31 | Aclaris Therapeutics, Inc. | Metil/fluoro-piridinil-metoksi substituirane spojine piridinon-piridinila in fluoro-pirimidinil-metoksi substituirane spojine piridinon-piridinila |
| WO2017151409A1 (en) | 2016-02-29 | 2017-09-08 | University Of Florida Research Foundation, Incorporated | Chemotherapeutic methods |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| EP3692144A1 (en) | 2017-10-05 | 2020-08-12 | Fulcrum Therapeutics, Inc. | Use of p38 inhibitors to reduce expression of dux4 |
| EP4125891A4 (en) | 2020-03-27 | 2024-08-21 | Aclaris Therapeutics, Inc. | PROCESS, COMPOSITIONS AND CRYSTALLINE FORMS OF SUBSTITUTED PYRIDINONE-PYRIDINYL COMPOUNDS |
| JP7763510B2 (ja) * | 2021-09-03 | 2025-11-04 | 深▲セン▼零一生命科技有限責任公司 | インドール化合物、その製造方法、及び使用 |
| CN118546081A (zh) * | 2023-02-27 | 2024-08-27 | 上海交通大学 | 一类肉桂酰胺衍生物及其应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2028530A1 (en) * | 1989-11-21 | 1991-05-22 | Christian Hubschwerlen | Substituted pyrimidobenzimidazole derivatives |
| US5283248A (en) * | 1989-11-21 | 1994-02-01 | Hoffmann-La Roche Inc. | Amino substituted pyrimido[1,6-2]benzimidazoles |
| WO1998006715A1 (en) * | 1996-08-09 | 1998-02-19 | Smithkline Beecham Corporation | Novel piperazine containing compounds |
| US6093742A (en) * | 1997-06-27 | 2000-07-25 | Vertex Pharmaceuticals, Inc. | Inhibitors of p38 |
| JP2002515891A (ja) * | 1997-12-19 | 2002-05-28 | スミスクライン・ビーチャム・コーポレイション | 新規なピペリジン含有化合物 |
| NZ508790A (en) * | 1998-05-22 | 2003-10-31 | Scios Inc | Heterocyclic compounds and methods to treat cardiac failure and other disorders |
| WO2000012074A2 (en) * | 1998-08-28 | 2000-03-09 | Scios Inc. | Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase |
-
2000
- 2000-05-19 WO PCT/US2000/014003 patent/WO2000071535A1/en not_active Ceased
- 2000-05-19 JP JP2000619792A patent/JP2003500403A/ja active Pending
- 2000-05-19 AT AT00939322T patent/ATE376547T1/de not_active IP Right Cessation
- 2000-05-19 HR HR20010854A patent/HRP20010854A2/hr not_active Application Discontinuation
- 2000-05-19 CZ CZ20014126A patent/CZ20014126A3/cs unknown
- 2000-05-19 KR KR1020017014870A patent/KR100743377B1/ko not_active Expired - Fee Related
- 2000-05-19 SK SK1648-2001A patent/SK16482001A3/sk unknown
- 2000-05-19 DE DE60036868T patent/DE60036868D1/de not_active Expired - Lifetime
- 2000-05-19 EP EP00939322A patent/EP1178983B1/en not_active Expired - Lifetime
- 2000-05-19 PL PL00352032A patent/PL352032A1/xx unknown
- 2000-05-19 CA CA002372567A patent/CA2372567A1/en not_active Abandoned
- 2000-05-19 HU HU0201261A patent/HUP0201261A3/hu unknown
- 2000-05-19 IL IL14630900A patent/IL146309A0/xx active IP Right Grant
- 2000-05-19 MX MXPA01011976A patent/MXPA01011976A/es not_active Application Discontinuation
- 2000-05-19 BR BR0011274-7A patent/BR0011274A/pt not_active Application Discontinuation
- 2000-05-19 NZ NZ515285A patent/NZ515285A/xx not_active IP Right Cessation
- 2000-05-19 AU AU54424/00A patent/AU772295B2/en not_active Ceased
- 2000-05-19 CN CNB00807724XA patent/CN1310906C/zh not_active Expired - Fee Related
-
2001
- 2001-11-08 BG BG106091A patent/BG106091A/xx unknown
- 2001-11-20 NO NO20015655A patent/NO20015655L/no unknown
-
2004
- 2004-07-22 AU AU2004203356A patent/AU2004203356A1/en not_active Abandoned
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