JP2001521934A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2001521934A5 JP2001521934A5 JP2000518962A JP2000518962A JP2001521934A5 JP 2001521934 A5 JP2001521934 A5 JP 2001521934A5 JP 2000518962 A JP2000518962 A JP 2000518962A JP 2000518962 A JP2000518962 A JP 2000518962A JP 2001521934 A5 JP2001521934 A5 JP 2001521934A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heteroaryl
- optionally
- group
- phenyl
- 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
- 125000000217 alkyl group Chemical group 0.000 description 137
- -1 cyclopentanyl Chemical group 0.000 description 120
- 125000001072 heteroaryl group Chemical group 0.000 description 116
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 73
- 125000001624 naphthyl group Chemical group 0.000 description 58
- 125000003342 alkenyl group Chemical group 0.000 description 46
- 125000004076 pyridyl group Chemical group 0.000 description 32
- 229910052736 halogen Inorganic materials 0.000 description 30
- 150000002367 halogens Chemical class 0.000 description 30
- 125000004093 cyano group Chemical group *C#N 0.000 description 29
- 125000003545 alkoxy group Chemical group 0.000 description 28
- 125000003282 alkyl amino group Chemical group 0.000 description 24
- 125000001544 thienyl group Chemical group 0.000 description 24
- 125000000753 cycloalkyl group Chemical group 0.000 description 23
- 125000003118 aryl group Chemical group 0.000 description 16
- 125000000392 cycloalkenyl group Chemical group 0.000 description 16
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 16
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 16
- 229910052799 carbon Inorganic materials 0.000 description 14
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 12
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 12
- 229910052717 sulfur Inorganic materials 0.000 description 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 10
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical group NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 description 9
- 150000001721 carbon Chemical group 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 9
- 125000005553 heteroaryloxy group Chemical group 0.000 description 9
- 125000003373 pyrazinyl group Chemical group 0.000 description 9
- 125000003226 pyrazolyl group Chemical group 0.000 description 9
- 125000002098 pyridazinyl group Chemical group 0.000 description 9
- 125000000714 pyrimidinyl group Chemical group 0.000 description 9
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 description 8
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 8
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 8
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 description 8
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 description 8
- 125000005046 dihydronaphthyl group Chemical group 0.000 description 8
- 125000002541 furyl group Chemical group 0.000 description 8
- 229910052739 hydrogen Inorganic materials 0.000 description 8
- 239000001257 hydrogen Substances 0.000 description 8
- 125000002883 imidazolyl group Chemical group 0.000 description 8
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 description 8
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 description 8
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 description 8
- 125000001786 isothiazolyl group Chemical group 0.000 description 8
- 125000000842 isoxazolyl group Chemical group 0.000 description 8
- 229910052760 oxygen Inorganic materials 0.000 description 8
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 description 8
- 125000000168 pyrrolyl group Chemical group 0.000 description 8
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 8
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 7
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 7
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 description 6
- 125000001162 cycloheptenyl group Chemical group C1(=CCCCCC1)* 0.000 description 6
- 125000005241 heteroarylamino group Chemical group 0.000 description 6
- 150000002431 hydrogen Chemical class 0.000 description 6
- 125000005184 naphthylamino group Chemical group C1(=CC=CC2=CC=CC=C12)N* 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 6
- QYCGBAJADAGLLK-UHFFFAOYSA-N 1-(cyclohepten-1-yl)cycloheptene Chemical group C1CCCCC=C1C1=CCCCCC1 QYCGBAJADAGLLK-UHFFFAOYSA-N 0.000 description 5
- VSIYJQNFMOOGCU-UHFFFAOYSA-N 1-(cyclohexen-1-yl)cyclohexene Chemical group C1CCCC(C=2CCCCC=2)=C1 VSIYJQNFMOOGCU-UHFFFAOYSA-N 0.000 description 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 5
- 125000001041 indolyl group Chemical group 0.000 description 5
- 229910052757 nitrogen Inorganic materials 0.000 description 5
- 150000003839 salts Chemical class 0.000 description 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 description 4
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 4
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 description 4
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 description 4
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 4
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 4
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 description 4
- 125000003678 cyclohexadienyl group Chemical group C1(=CC=CCC1)* 0.000 description 4
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 description 3
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 3
- 125000004122 cyclic group Chemical group 0.000 description 3
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 description 3
- 125000000623 heterocyclic group Chemical group 0.000 description 3
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 description 3
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 description 3
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 3
- 125000004742 propyloxycarbonyl group Chemical group 0.000 description 3
- 125000000081 (C5-C8) cycloalkenyl group Chemical group 0.000 description 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 description 2
- 206010040070 Septic Shock Diseases 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 description 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 description 2
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 description 2
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 2
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 description 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 2
- UPRSNNXRXUQSAZ-UHFFFAOYSA-N 1-(5-tert-butyl-2-pyridin-3-ylpyrazol-3-yl)-3-(4-cyanonaphthalen-1-yl)urea Chemical compound N1=C(C(C)(C)C)C=C(NC(=O)NC=2C3=CC=CC=C3C(C#N)=CC=2)N1C1=CC=CN=C1 UPRSNNXRXUQSAZ-UHFFFAOYSA-N 0.000 description 1
- BJHGYSMDHBBCDP-UHFFFAOYSA-N 1-[5-tert-butyl-2-(3,4-dimethylphenyl)pyrazol-3-yl]-3-(4-fluorophenyl)urea Chemical compound C1=C(C)C(C)=CC=C1N1C(NC(=O)NC=2C=CC(F)=CC=2)=CC(C(C)(C)C)=N1 BJHGYSMDHBBCDP-UHFFFAOYSA-N 0.000 description 1
- IVBPBKLZQGEAEA-UHFFFAOYSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-(2-fluorophenyl)urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)NC=2C(=CC=CC=2)F)=CC(C(C)(C)C)=N1 IVBPBKLZQGEAEA-UHFFFAOYSA-N 0.000 description 1
- IANFRRHFTBSTBQ-UHFFFAOYSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-(4-methoxynaphthalen-1-yl)urea Chemical compound C12=CC=CC=C2C(OC)=CC=C1NC(=O)NC1=CC(C(C)(C)C)=NN1C1=CC=C(C)C=C1 IANFRRHFTBSTBQ-UHFFFAOYSA-N 0.000 description 1
- UDSIRMFEVOSPBU-UHFFFAOYSA-N 1-[5-tert-butyl-2-(6-methylpyridin-3-yl)pyrazol-3-yl]-3-(4-chlorophenyl)urea Chemical compound C1=NC(C)=CC=C1N1C(NC(=O)NC=2C=CC(Cl)=CC=2)=CC(C(C)(C)C)=N1 UDSIRMFEVOSPBU-UHFFFAOYSA-N 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 description 1
- 206010006895 Cachexia Diseases 0.000 description 1
- 206010007559 Cardiac failure congestive Diseases 0.000 description 1
- 206010063094 Cerebral malaria Diseases 0.000 description 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 1
- 206010009900 Colitis ulcerative Diseases 0.000 description 1
- 208000011231 Crohn disease Diseases 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 241000701022 Cytomegalovirus Species 0.000 description 1
- 206010012442 Dermatitis contact Diseases 0.000 description 1
- 201000005569 Gout Diseases 0.000 description 1
- 206010018634 Gouty Arthritis Diseases 0.000 description 1
- 102000004457 Granulocyte-Macrophage Colony-Stimulating Factor Human genes 0.000 description 1
- 108010017213 Granulocyte-Macrophage Colony-Stimulating Factor Proteins 0.000 description 1
- 208000031886 HIV Infections Diseases 0.000 description 1
- 206010020164 HIV infection CDC Group III Diseases 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- 208000007514 Herpes zoster Diseases 0.000 description 1
- 241000713772 Human immunodeficiency virus 1 Species 0.000 description 1
- 241000713340 Human immunodeficiency virus 2 Species 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 1
- 108090001005 Interleukin-6 Proteins 0.000 description 1
- 108090001007 Interleukin-8 Proteins 0.000 description 1
- 208000034578 Multiple myelomas Diseases 0.000 description 1
- 206010028289 Muscle atrophy Diseases 0.000 description 1
- 208000000112 Myalgia Diseases 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 208000010191 Osteitis Deformans Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 208000027868 Paget disease Diseases 0.000 description 1
- 206010035226 Plasma cell myeloma Diseases 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 206010037660 Pyrexia Diseases 0.000 description 1
- 208000033464 Reiter syndrome Diseases 0.000 description 1
- 206010063837 Reperfusion injury Diseases 0.000 description 1
- 206010039085 Rhinitis allergic Diseases 0.000 description 1
- 206010040047 Sepsis Diseases 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 206010044248 Toxic shock syndrome Diseases 0.000 description 1
- 231100000650 Toxic shock syndrome Toxicity 0.000 description 1
- 208000030886 Traumatic Brain injury Diseases 0.000 description 1
- 108060008682 Tumor Necrosis Factor Proteins 0.000 description 1
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 description 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 1
- 201000006704 Ulcerative Colitis Diseases 0.000 description 1
- 206010046851 Uveitis Diseases 0.000 description 1
- 201000010105 allergic rhinitis Diseases 0.000 description 1
- 230000036783 anaphylactic response Effects 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 125000004599 benzpyrazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 description 1
- 208000019664 bone resorption disease Diseases 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000037976 chronic inflammation Diseases 0.000 description 1
- 208000037893 chronic inflammatory disorder Diseases 0.000 description 1
- 208000010247 contact dermatitis Diseases 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 208000024908 graft versus host disease Diseases 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000000302 ischemic effect Effects 0.000 description 1
- 208000027202 mammary Paget disease Diseases 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 208000013465 muscle pain Diseases 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 125000001844 prenyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 208000002574 reactive arthritis Diseases 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 230000036303 septic shock Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- 241000701161 unidentified adenovirus Species 0.000 description 1
- 241001529453 unidentified herpesvirus Species 0.000 description 1
- 241000712461 unidentified influenza virus Species 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6410297P | 1997-11-03 | 1997-11-03 | |
| US60/064,102 | 1997-11-03 | ||
| PCT/US1998/022907 WO1999023091A1 (en) | 1997-11-03 | 1998-10-29 | Aromatic heterocyclic compounds as anti-inflammatory agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2001521934A JP2001521934A (ja) | 2001-11-13 |
| JP2001521934A5 true JP2001521934A5 (https=) | 2006-01-05 |
Family
ID=22053575
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000518962A Pending JP2001521934A (ja) | 1997-11-03 | 1998-10-29 | 抗炎症薬としての芳香族ヘテロ環式化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US6080763A (https=) |
| EP (1) | EP1028953A1 (https=) |
| JP (1) | JP2001521934A (https=) |
| AU (1) | AU1367599A (https=) |
| CA (1) | CA2308428A1 (https=) |
| WO (1) | WO1999023091A1 (https=) |
Families Citing this family (117)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE529109T1 (de) * | 1997-12-22 | 2011-11-15 | Bayer Healthcare Llc | Hemmung der p38 kinase aktivität durch substituierte heterocyclische harnstoffe |
| PT1056725E (pt) * | 1997-12-22 | 2006-09-29 | Bayer Pharmaceuticals Corp | Inibicao da raf-quinase usando ureias heterociclicas substituidas com arilo e heteroarilo |
| IL136768A0 (en) * | 1997-12-22 | 2001-06-14 | Bayer Ag | INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS |
| US7329670B1 (en) * | 1997-12-22 | 2008-02-12 | Bayer Pharmaceuticals Corporation | Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas |
| US7517880B2 (en) | 1997-12-22 | 2009-04-14 | Bayer Pharmaceuticals Corporation | Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas |
| US20080300281A1 (en) * | 1997-12-22 | 2008-12-04 | Jacques Dumas | Inhibition of p38 Kinase Activity Using Aryl and Heteroaryl Substituted Heterocyclic Ureas |
| US20070244120A1 (en) * | 2000-08-18 | 2007-10-18 | Jacques Dumas | Inhibition of raf kinase using substituted heterocyclic ureas |
| WO1999051580A1 (en) * | 1998-04-08 | 1999-10-14 | Abbott Laboratories | Pyrazole inhibitors of cytokine production |
| US20080269265A1 (en) * | 1998-12-22 | 2008-10-30 | Scott Miller | Inhibition Of Raf Kinase Using Symmetrical And Unsymmetrical Substituted Diphenyl Ureas |
| ME00275B (me) | 1999-01-13 | 2011-02-10 | Bayer Corp | ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE |
| US7928239B2 (en) | 1999-01-13 | 2011-04-19 | Bayer Healthcare Llc | Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas |
| US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| EP1158985B1 (en) | 1999-01-13 | 2011-12-28 | Bayer HealthCare LLC | OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS |
| EP1140840B1 (en) | 1999-01-13 | 2006-03-22 | Bayer Pharmaceuticals Corp. | -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| UA73492C2 (en) * | 1999-01-19 | 2005-08-15 | Aromatic heterocyclic compounds as antiinflammatory agents | |
| EP1690854A1 (en) * | 1999-03-12 | 2006-08-16 | Boehringer Ingelheim Pharmaceuticals, Inc. | Heterocyclic urea and related compounds useful as anti-inflammatory agents |
| ATE278674T1 (de) * | 1999-03-12 | 2004-10-15 | Boehringer Ingelheim Pharma | Heterocyklischer harnstoff und verwandte verbindungen als entzündungshemmende mittel |
| AU2004200240B2 (en) * | 1999-03-12 | 2007-04-26 | Boehringer Ingelheim Pharmaceuticals Inc. | Compounds useful as anti-inflammatory agents |
| EP1466906A1 (en) * | 1999-03-12 | 2004-10-13 | Boehringer Ingelheim Pharmaceuticals Inc. | Heterocyclic urea and related compounds useful as anti-inflammatory agents |
| MXPA02004004A (es) * | 1999-10-29 | 2002-10-23 | Boehringer Ingelheim Pharma | Proceso para la preparacion de pirazoles substituidos. |
| EP1232150B1 (en) * | 1999-11-16 | 2007-10-10 | Boehringer Ingelheim Pharmaceuticals Inc. | Urea derivatives as anti-inflammatory agents |
| GB0016787D0 (en) | 2000-07-07 | 2000-08-30 | Pfizer Ltd | Compounds useful in therapy |
| US6645990B2 (en) | 2000-08-15 | 2003-11-11 | Amgen Inc. | Thiazolyl urea compounds and methods of uses |
| US7235576B1 (en) | 2001-01-12 | 2007-06-26 | Bayer Pharmaceuticals Corporation | Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| EP1362037A1 (en) * | 2001-02-15 | 2003-11-19 | Boehringer Ingelheim Pharmaceuticals Inc. | Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents |
| US7371763B2 (en) * | 2001-04-20 | 2008-05-13 | Bayer Pharmaceuticals Corporation | Inhibition of raf kinase using quinolyl, isoquinolyl or pyridyl ureas |
| WO2003005999A2 (en) * | 2001-07-11 | 2003-01-23 | Boehringer Ingelheim Pharmaceuticals, Inc. | Methods of treating cytokine mediated diseases |
| US6603000B2 (en) | 2001-07-11 | 2003-08-05 | Boehringer Ingelheim Pharmaceuticals, Inc. | Synthesis for heteroarylamine compounds |
| EP1709965A3 (en) | 2001-07-11 | 2006-12-27 | Boehringer Ingelheim Pharmaceuticals, Inc. | Methods of treating cytokine mediate diseases |
| WO2003022273A1 (en) * | 2001-09-13 | 2003-03-20 | Boehringer Ingelheim Pharmaceuticals, Inc. | Methods of treating cytokine mediated diseases |
| WO2003026649A1 (en) * | 2001-09-27 | 2003-04-03 | Applied Research Systems Ars Holding N.V. | Methods of increasing endogenous testosterone levels |
| US7132438B2 (en) | 2001-10-09 | 2006-11-07 | Amgen Inc. | Benzimidazole derivatives |
| EP1438048A1 (en) * | 2001-10-18 | 2004-07-21 | Boehringer Ingelheim Pharmaceuticals Inc. | 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors |
| US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| WO2003047579A1 (en) * | 2001-12-03 | 2003-06-12 | Bayer Pharmaceuticals Corporation | Aryl urea compounds in combination with other cytostatic or cytotoxic agents for treating human cancers |
| DE10159329A1 (de) * | 2001-12-03 | 2003-06-18 | Haarmann & Reimer Gmbh | Verfahren zur Herstellung von beta-Ketonitrilen |
| WO2003068229A1 (en) | 2002-02-11 | 2003-08-21 | Bayer Pharmaceuticals Corporation | Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors |
| SI1478358T1 (sl) | 2002-02-11 | 2013-09-30 | Bayer Healthcare Llc | Sorafenib tozilat za zdravljenje bolezni, značilnih po abnormalni angiogenezi |
| US20040023961A1 (en) * | 2002-02-11 | 2004-02-05 | Bayer Corporation | Aryl ureas with raf kinase and angiogenisis inhibiting activity |
| ATE529406T1 (de) * | 2002-02-11 | 2011-11-15 | Bayer Healthcare Llc | Aryl-harnstoffe als kinase inhibitoren |
| EP1480973B1 (en) | 2002-02-25 | 2008-02-13 | Boehringer Ingelheim Pharmaceuticals Inc. | 1,4-disubstituted benzofused cycloalkyl urea compounds useful in treating cytokine mediated diseases |
| EP1549621A1 (en) * | 2002-08-08 | 2005-07-06 | Boehringer Ingelheim Pharmaceuticals Inc. | Fluorinated phenyl-naphthalenyl-urea compounds as inhibitors of cytokines involved in inflammatory processes |
| DE10257358A1 (de) * | 2002-12-09 | 2004-07-08 | Bayer Healthcare Ag | Substituierte Pyrrole |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| US7202257B2 (en) * | 2003-12-24 | 2007-04-10 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| WO2004063192A1 (en) * | 2003-01-10 | 2004-07-29 | Pharmacopeia Drug Discovery, Inc. | Imidazolyl pyrimidine derivatives useful as il-8 receptor modulators |
| US7557129B2 (en) | 2003-02-28 | 2009-07-07 | Bayer Healthcare Llc | Cyanopyridine derivatives useful in the treatment of cancer and other disorders |
| US7521447B2 (en) * | 2003-03-03 | 2009-04-21 | 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 |
| US20050090426A1 (en) * | 2003-03-24 | 2005-04-28 | Blumberg Richard S. | Methods of inhibiting inflammation |
| US20050234073A1 (en) * | 2003-03-24 | 2005-10-20 | Blumberg Richard S | Methods of inhibiting inflammation |
| EP1636585B2 (en) | 2003-05-20 | 2012-06-13 | Bayer HealthCare LLC | Diaryl ureas with kinase inhibiting activity |
| EP1663978B1 (en) | 2003-07-23 | 2007-11-28 | Bayer Pharmaceuticals Corporation | Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions |
| EP1650195A4 (en) * | 2003-07-30 | 2008-09-17 | Kowa Co | METHOD FOR INHIBITING OSTEOPONTIN PRODUCTION |
| WO2005023761A2 (en) | 2003-09-11 | 2005-03-17 | Kemia, Inc. | Cytokine inhibitors |
| US7377277B2 (en) * | 2003-10-27 | 2008-05-27 | Oriel Therapeutics, Inc. | Blister packages with frames and associated methods of fabricating dry powder drug containment systems |
| DE102004015007A1 (de) * | 2004-03-26 | 2005-10-13 | Bayer Healthcare Ag | Substituierte Imidazole |
| SMAP200600037A (it) * | 2004-04-22 | 2006-11-22 | Procter & Gamble | Uree trisostituite come inibitori di citochina |
| EP2295426A1 (en) | 2004-04-30 | 2011-03-16 | Bayer HealthCare, LLC | Substituted pyrazolyl urea derivatives useful in the treatment of cancer |
| US7485657B2 (en) * | 2004-05-12 | 2009-02-03 | Boehringer Ingelheim Pharmaceuticals, Inc. | Anti-cytokine heterocyclic compounds |
| AU2005276117C1 (en) | 2004-08-23 | 2013-04-18 | Yeda Research And Development Co. Ltd. At The Weizmann Institute Of Science | Peptide inhibitors for mediating stress responses |
| US7741479B2 (en) * | 2004-12-07 | 2010-06-22 | Locus Pharmaceuticals, Inc. | Urea inhibitors of MAP kinases |
| US7612200B2 (en) * | 2004-12-07 | 2009-11-03 | Locus Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| WO2006068591A1 (en) * | 2004-12-20 | 2006-06-29 | Astrazeneca Ab | Novel pyrazole derivatives and their use as modulators of nicotinic acetylcholine receptors |
| CA2592118C (en) | 2004-12-23 | 2015-11-17 | Deciphera Pharmaceuticals, Llc | Urea derivatives as enzyme modulators |
| DE102005008183A1 (de) | 2005-02-23 | 2006-08-31 | Bayer Healthcare Ag | Heterocyclylamid-substituierte Imidazole |
| EP1881955A1 (en) * | 2005-05-12 | 2008-01-30 | Boehringer Ingelheim International GmbH | Bis-amination of aryl halides |
| DE102005033103A1 (de) | 2005-07-15 | 2007-01-25 | Bayer Healthcare Ag | Heterocyclylamid-substituierte Thiazole, Pyrrole und Thiophene |
| DE102005037499A1 (de) | 2005-08-09 | 2007-02-15 | Merck Patent Gmbh | Pyrazolderivate |
| US7714127B2 (en) * | 2005-10-06 | 2010-05-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Process for making heteroaryl amine intermediate compounds |
| US20070185098A1 (en) * | 2006-01-04 | 2007-08-09 | Locus Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| RS52298B (sr) * | 2006-01-31 | 2012-12-31 | Array Biopharma Inc. | Inhibitori kinaze i postupak njihove upotrebe |
| US8188113B2 (en) | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| US7790756B2 (en) | 2006-10-11 | 2010-09-07 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| JP2010514692A (ja) | 2006-12-20 | 2010-05-06 | バイエル ヘルスケア リミティド ライアビリティ カンパニー | 癌の治療に有用なヒドロキシメチルフェニルピラゾリル尿素化合物 |
| US20110189167A1 (en) * | 2007-04-20 | 2011-08-04 | Flynn Daniel L | Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases |
| WO2008131276A1 (en) * | 2007-04-20 | 2008-10-30 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| GB0818033D0 (en) | 2008-10-02 | 2008-11-05 | Respivert Ltd | Novel compound |
| JP2012504591A (ja) | 2008-10-02 | 2012-02-23 | レスピバート・リミテツド | ｐ３８ＭＡＰキナーゼ阻害剤 |
| JP5444365B2 (ja) * | 2008-10-29 | 2014-03-19 | デシフェラ ファーマシューティカルズ，エルエルシー | 抗癌活性および抗増殖活性を示すシクロプロパンアミドおよび類似物質 |
| MX2011006219A (es) | 2008-12-11 | 2011-06-28 | Respivert Ltd | Inhibidores de la proteina cinasa activada por el mitogeno p38. |
| GB0905955D0 (en) | 2009-04-06 | 2009-05-20 | Respivert Ltd | Novel compounds |
| CA2835835C (en) | 2011-05-13 | 2019-04-02 | Array Biopharma Inc. | Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors |
| CA2836503C (en) | 2011-05-23 | 2020-09-22 | Yeda Research And Development Co. Ltd. | Use of akt phosphorylation as a biomarker for prognosing neurodegenerative diseases and treating same |
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| EP2890460B1 (en) | 2012-08-29 | 2017-02-22 | Respivert Limited | Kinase inhibitors |
| US9783556B2 (en) | 2012-08-29 | 2017-10-10 | Respivert Limited | Kinase inhibitors |
| US20150225373A1 (en) | 2012-08-29 | 2015-08-13 | Respivert Limited | Kinase inhibitors |
| WO2014078372A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078325A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| RS55593B1 (sr) | 2012-11-13 | 2017-06-30 | Array Biopharma Inc | Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola |
| WO2014078378A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078417A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| MX374242B (es) | 2012-11-13 | 2025-03-05 | Array Biopharma Inc | Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa. |
| WO2014078328A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9822118B2 (en) | 2012-11-13 | 2017-11-21 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2014078331A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9981959B2 (en) | 2012-11-13 | 2018-05-29 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| US9067894B1 (en) * | 2013-03-07 | 2015-06-30 | Vanderbilt University | Compound, composition, and method of activating GIRK potassium channel and use of same for treating conditions of interest |
| AU2014246866B2 (en) | 2013-04-02 | 2018-05-10 | Oxular Acquisitions Limited | Kinase inhibitor |
| EP2981534B1 (en) | 2013-04-02 | 2017-07-19 | Topivert Pharma Limited | Kinase inhibitors based upon n-alkyl pyrazoles |
| WO2015039333A1 (en) * | 2013-09-22 | 2015-03-26 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| CA2934199A1 (en) | 2013-12-20 | 2015-06-25 | Respivert Limited | Urea derivatives useful as kinase inhibitors |
| MA40434B1 (fr) | 2014-05-15 | 2019-09-30 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorophényl)-1-(2-méthoxyéthyl)pyrrolidin-3-yl)-3-(4-méthyl-3-(2-méthylpyrimidin-5-yl)-1-phényl-1h-pyrazol-5-yl)urée comme inhibiteur de la kinase trka |
| MA40774A (fr) | 2014-10-01 | 2017-08-08 | Respivert Ltd | Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38 |
| US9701175B2 (en) * | 2015-04-14 | 2017-07-11 | Ford Global Technologies, Llc | Hybrid vehicle split exhaust system with exhaust driven electric machine and A/C compressor |
| EA201892213A1 (ru) | 2016-04-06 | 2019-05-31 | Топайверт Фарма Лимитед | Ингибиторы киназ |
| CA3065284A1 (en) * | 2017-06-14 | 2018-12-20 | Universite Laval | Novel urea compounds and bioisosteres thereof and their use for treating inflammation and inflammation-related pathologies |
| IL276398B2 (en) | 2018-01-31 | 2026-03-01 | Deciphera Pharmaceuticals Llc | Combination therapy for mastocytosis |
| CN118416236A (zh) | 2018-01-31 | 2024-08-02 | 德西费拉制药有限责任公司 | 治疗胃肠道间质瘤的组合疗法 |
| WO2020185812A1 (en) | 2019-03-11 | 2020-09-17 | Teva Pharmaceuticals International Gmbh | Solid state forms of ripretinib |
| EP4013412B1 (en) | 2019-08-12 | 2026-01-28 | Deciphera Pharmaceuticals, LLC | Ripretinib for treating gastrointestinal stromal tumors |
| TWI878335B (zh) | 2019-08-12 | 2025-04-01 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| EP4084779B1 (en) | 2019-12-30 | 2024-10-09 | Deciphera Pharmaceuticals, LLC | Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea |
| MX2022008103A (es) | 2019-12-30 | 2022-09-19 | Deciphera Pharmaceuticals Llc | Formulaciones de inhibidores de la cinasa amorfa y metodos de estas. |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
| US11905279B1 (en) * | 2023-10-13 | 2024-02-20 | King Faisal University | Benzylidene derivatives of fenobam as anti-inflammatory agents |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4171364A (en) * | 1971-10-01 | 1979-10-16 | Eli Lilly And Company | N-heterocyclic ureas as immune regulants |
| US3990879A (en) * | 1974-12-26 | 1976-11-09 | Eli Lilly And Company | Method of controlling aquatic weeds |
| US4171367A (en) * | 1977-02-18 | 1979-10-16 | Abbott Laboratories | Pyrazolyl amino imidazolines |
| DE2963332D1 (en) * | 1978-05-26 | 1982-09-02 | Lepetit Spa | Pyrazolo (3,4-c) and thiazolo (5,4-c) isoquinolines, methods for preparing them, these compounds for use as antiinflammatory, cns-depressant and anti-anxiety agents and pharmaceutical compositions thereof |
| GB2054555A (en) * | 1979-07-27 | 1981-02-18 | Abbott Lab | Pyrazolyl amino imidazolines |
| US4265900A (en) * | 1979-10-29 | 1981-05-05 | Mcneilab, Inc. | N-Aryl-N'-imidazol-2-ylureas |
| HU185294B (en) * | 1980-12-29 | 1984-12-28 | Chinoin Gyogyszer Es Vegyeszet | Process for producing substituted urea derivatives |
| GB8908869D0 (en) * | 1989-04-19 | 1989-06-07 | Shell Int Research | A process for the preparation of aromatic ureas |
| WO1991004027A1 (en) * | 1989-09-15 | 1991-04-04 | Pfizer Inc. | New n-aryl and n-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme a: cholesterol acyl transferase (acat) |
| US5162360A (en) * | 1991-06-24 | 1992-11-10 | Warner-Lambert Company | 2-heteroatom containing urea and thiourea ACAT inhibitors |
| US5356897A (en) * | 1991-09-09 | 1994-10-18 | Fujisawa Pharmaceutical Co., Ltd. | 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines |
| AU4028393A (en) * | 1992-05-28 | 1993-12-30 | Pfizer Inc. | New (N)-aryl and (N)-heteroarylurea derivatives as inhibitors of acyl coenzyme a:cholesterol acyl transferase (ACAT) |
| GB9302275D0 (en) * | 1993-02-05 | 1993-03-24 | Smithkline Beecham Plc | Novel compounds |
| CZ219597A3 (cs) * | 1995-01-12 | 1998-03-18 | Smithkline Beecham Corporation | Nové sloučeniny |
| AU702887B2 (en) * | 1995-10-31 | 1999-03-11 | Merck & Co., Inc. | Substituted pyridyl pyrroles, compositions containing such compounds and methods of use |
| IL136768A0 (en) * | 1997-12-22 | 2001-06-14 | Bayer Ag | INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS |
-
1998
- 1998-10-29 EP EP98957405A patent/EP1028953A1/en not_active Withdrawn
- 1998-10-29 US US09/181,743 patent/US6080763A/en not_active Expired - Lifetime
- 1998-10-29 WO PCT/US1998/022907 patent/WO1999023091A1/en not_active Ceased
- 1998-10-29 JP JP2000518962A patent/JP2001521934A/ja active Pending
- 1998-10-29 CA CA002308428A patent/CA2308428A1/en not_active Abandoned
- 1998-10-29 AU AU13675/99A patent/AU1367599A/en not_active Abandoned
-
1999
- 1999-12-14 US US09/461,446 patent/US6228881B1/en not_active Expired - Lifetime
-
2001
- 2001-03-14 US US09/808,084 patent/US6432995B2/en not_active Expired - Lifetime
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2001521934A5 (https=) | ||
| RU2220142C2 (ru) | Ароматические гетероциклические соединения как противовоспалительные средства | |
| ES2251360T3 (es) | Compuestos heterociclicos aromaticos en calidad de agentes antiinflamatorios. | |
| JP2007502843A5 (https=) | ||
| US6080763A (en) | Aromatic heterocyclic compounds and their use as anti-inflammatory agents | |
| JP4162406B2 (ja) | ヘテロアリール置換ウレア化合物の新規合成方法 | |
| US7718693B2 (en) | Receptor antagonists and their methods of use | |
| KR100659007B1 (ko) | 아미드 화합물 및 그 의약으로서의 용도 | |
| US20110046137A1 (en) | Pyrazole Derivatives as P2X7 Modulators | |
| US20080262042A1 (en) | Pyrrole compounds | |
| RU2001126337A (ru) | Соединения, пригодные в качестве противовоспалительных агентов | |
| JP2004521087A5 (https=) | ||
| JP2004536845A5 (https=) | ||
| WO2000039116A1 (en) | Aminopyrazole derivatives | |
| RU96103386A (ru) | Три-замещенные имидазолы, обладающие многочисленными терапевтическими свойствами, способ получения, фармацевтическая композиция, способ лечения | |
| JP2005530722A5 (https=) | ||
| SK90297A3 (en) | 1,4,5-tri-substituted imidazole compounds, producing method thereof, pharmaceutical composition containing them and their use | |
| US20080139621A1 (en) | Thrombopoietin Mimetics | |
| CA2584666A1 (en) | Pyrimidine derivative condensed with a non-aromatic ring | |
| JP2007524707A5 (https=) | ||
| JP2007501831A5 (https=) | ||
| CA2628844A1 (en) | Pyrazole derivatives and their medical use | |
| RU2003115612A (ru) | Производные амидоалкилпиперидинов и амидоалкилпиперазинов, пригодные для лечения нарушений нервной системы | |
| JP2007522111A5 (https=) | ||
| JP2008509955A5 (https=) |