JP2013507351A5 - - Google Patents
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- JP2013507351A5 JP2013507351A5 JP2012532676A JP2012532676A JP2013507351A5 JP 2013507351 A5 JP2013507351 A5 JP 2013507351A5 JP 2012532676 A JP2012532676 A JP 2012532676A JP 2012532676 A JP2012532676 A JP 2012532676A JP 2013507351 A5 JP2013507351 A5 JP 2013507351A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- pyrazol
- phenyl
- trifluoromethyl
- 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.)
- Granted
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- 102000020167 Calcium release-activated calcium channel Human genes 0.000 claims description 10
- 239000003112 inhibitor Substances 0.000 claims description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 10
- 108091022898 Calcium release-activated calcium channel Proteins 0.000 claims description 9
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 8
- 229910052791 calcium Inorganic materials 0.000 claims description 8
- 239000011575 calcium Substances 0.000 claims description 8
- 229940002612 prodrug Drugs 0.000 claims description 8
- 239000000651 prodrug Substances 0.000 claims description 8
- 108091006146 Channels Proteins 0.000 claims description 7
- 101150060735 orai1 gene Proteins 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 101150105461 Stim1 gene Proteins 0.000 claims description 3
- 230000000694 effects Effects 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 2
- -1 nitro, hydroxy Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000000753 cycloalkyl group Chemical group 0.000 claims 17
- 229910052760 oxygen Inorganic materials 0.000 claims 13
- 125000003342 alkenyl group Chemical group 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 125000000304 alkynyl group Chemical group 0.000 claims 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- 238000000034 method Methods 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000005842 heteroatom Chemical group 0.000 claims 9
- 229920006395 saturated elastomer Polymers 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 150000001204 N-oxides Chemical class 0.000 claims 7
- 150000002148 esters Chemical class 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 101100043696 Drosophila melanogaster Stim gene Proteins 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 6
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 6
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 6
- 239000003795 chemical substances by application Substances 0.000 claims 5
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 4
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 102100039319 Calcium release-activated calcium channel protein 1 Human genes 0.000 claims 3
- 101000745520 Homo sapiens Calcium release-activated calcium channel protein 1 Proteins 0.000 claims 3
- 101150066814 Orai3 gene Proteins 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 150000003857 carboxamides Chemical class 0.000 claims 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 3
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 3
- VTHOULHKCFBBGL-UHFFFAOYSA-N n-[4-[5-cyclopropyl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]-1-methyl-3-(trifluoromethyl)thieno[2,3-c]pyrazole-5-carboxamide Chemical compound S1C=2N(C)N=C(C(F)(F)F)C=2C=C1C(=O)NC(C=C1)=CC=C1N1N=C(C(F)(F)F)C=C1C1CC1 VTHOULHKCFBBGL-UHFFFAOYSA-N 0.000 claims 3
- 238000006467 substitution reaction Methods 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- METKIMKYRPQLGS-UHFFFAOYSA-N atenolol Chemical compound CC(C)NCC(O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-UHFFFAOYSA-N 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- DLFVBJFMPXGRIB-UHFFFAOYSA-N thioacetamide Natural products CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 2
- DKFYJQLJWMQVNV-UHFFFAOYSA-N 2-(benzimidazol-1-yl)-n-[4-[5-cyclopropyl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]acetamide Chemical compound C=1C=C(NC(=O)CN2C3=CC=CC=C3N=C2)C=CC=1N1N=C(C(F)(F)F)C=C1C1CC1 DKFYJQLJWMQVNV-UHFFFAOYSA-N 0.000 claims 1
- UNHGMHPBBDOIDD-UHFFFAOYSA-N C1(CC1)C1=NN(C(=C1)C1CC1)C1=CC=C(C=N1)NC(=O)C=1C=C2N=CC=NC2=CC1.C1(CC1)C1=NN(C(=C1)C1CC1)C1=CC=C(C=N1)NC(=O)C=1C=C2C=CC=NC2=CC1 Chemical compound C1(CC1)C1=NN(C(=C1)C1CC1)C1=CC=C(C=N1)NC(=O)C=1C=C2N=CC=NC2=CC1.C1(CC1)C1=NN(C(=C1)C1CC1)C1=CC=C(C=N1)NC(=O)C=1C=C2C=CC=NC2=CC1 UNHGMHPBBDOIDD-UHFFFAOYSA-N 0.000 claims 1
- 229940126062 Compound A Drugs 0.000 claims 1
- 102100025027 E3 ubiquitin-protein ligase TRIM69 Human genes 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 101000830203 Homo sapiens E3 ubiquitin-protein ligase TRIM69 Proteins 0.000 claims 1
- WCQJVTYUCIYDSU-UHFFFAOYSA-N N1=CC=NC2=CC(=CC=C12)C(=O)NC1=CC=C(C=C1)N1N=C(C=C1C1CC1)C1CC1.N1=CC=CC2=CC(=CC=C12)C(=O)N Chemical compound N1=CC=NC2=CC(=CC=C12)C(=O)NC1=CC=C(C=C1)N1N=C(C=C1C1CC1)C1CC1.N1=CC=CC2=CC(=CC=C12)C(=O)N WCQJVTYUCIYDSU-UHFFFAOYSA-N 0.000 claims 1
- 102000004094 Stromal Interaction Molecule 1 Human genes 0.000 claims 1
- 108090000532 Stromal Interaction Molecule 1 Proteins 0.000 claims 1
- 108010030731 Stromal Interaction Molecule 2 Proteins 0.000 claims 1
- 102100035562 Stromal interaction molecule 2 Human genes 0.000 claims 1
- 125000000848 adenin-9-yl group Chemical group [H]N([H])C1=C2N=C([H])N(*)C2=NC([H])=N1 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 229940000406 drug candidate Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- RVVCOHUMRKGYOQ-UHFFFAOYSA-N n-[4-(3,5-dicyclopropylpyrazol-1-yl)phenyl]-2-imidazo[1,2-a]pyridin-2-ylacetamide;hydrochloride Chemical compound Cl.C=1N2C=CC=CC2=NC=1CC(=O)NC(C=C1)=CC=C1N1N=C(C2CC2)C=C1C1CC1 RVVCOHUMRKGYOQ-UHFFFAOYSA-N 0.000 claims 1
- JHUUUHBVXPRICU-UHFFFAOYSA-N n-[4-[5-cyclopropyl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]quinoxaline-6-carboxamide Chemical compound C=1C=C(NC(=O)C=2C=C3N=CC=NC3=CC=2)C=CC=1N1N=C(C(F)(F)F)C=C1C1CC1 JHUUUHBVXPRICU-UHFFFAOYSA-N 0.000 claims 1
- JVIJYZBGJKPMAQ-UHFFFAOYSA-N n-[6-[5-cyclopropyl-3-(trifluoromethyl)pyrazol-1-yl]pyridin-3-yl]-2h-benzotriazole-5-carboxamide Chemical compound C=1C=C(NC(=O)C=2C=C3N=NNC3=CC=2)C=NC=1N1N=C(C(F)(F)F)C=C1C1CC1 JVIJYZBGJKPMAQ-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 description 3
- 230000003389 potentiating effect Effects 0.000 description 3
- 238000003786 synthesis reaction Methods 0.000 description 3
- 150000001669 calcium Chemical class 0.000 description 2
- JGUMDUSKGJDSFG-UHFFFAOYSA-N 5-[2-methyl-5-(trifluoromethyl)pyrazol-3-yl]thiophene-2-carboxamide Chemical class CN1N=C(C(F)(F)F)C=C1C1=CC=C(C(N)=O)S1 JGUMDUSKGJDSFG-UHFFFAOYSA-N 0.000 description 1
- 208000037765 diseases and disorders Diseases 0.000 description 1
- 238000007876 drug discovery Methods 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000000115 thoracic cavity Anatomy 0.000 description 1
Applications Claiming Priority (15)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2439CH2009 | 2009-10-08 | ||
| IN2439/CHE/2009 | 2009-10-08 | ||
| IN2636CH2009 | 2009-10-30 | ||
| IN2636/CHE/2009 | 2009-10-30 | ||
| US26554009P | 2009-12-01 | 2009-12-01 | |
| US61/265,540 | 2009-12-01 | ||
| IN158/CHE/2010 | 2010-01-25 | ||
| IN158CH2010 | 2010-01-25 | ||
| IN1514CH2010 | 2010-06-02 | ||
| IN1513/CHE/2010 | 2010-06-02 | ||
| IN1513CH2010 | 2010-06-02 | ||
| IN1514/CHE/2010 | 2010-06-02 | ||
| IN2385/CHE/2010 | 2010-08-19 | ||
| IN2385CH2010 | 2010-08-19 | ||
| PCT/IB2010/002539 WO2011042798A1 (en) | 2009-10-08 | 2010-10-07 | Pyrazoles derivatives modulators of calcium release -activated calcium channel and methods for treatment of non- small cell lung cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015160031A Division JP6266568B2 (ja) | 2009-10-08 | 2015-08-14 | カルシウム放出依存性カルシウムチャネルのピラゾール誘導体モジュレータおよび非小細胞肺癌の治療方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013507351A JP2013507351A (ja) | 2013-03-04 |
| JP2013507351A5 true JP2013507351A5 (https=) | 2013-11-14 |
| JP5909312B2 JP5909312B2 (ja) | 2016-04-26 |
Family
ID=43447834
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012532676A Expired - Fee Related JP5909312B2 (ja) | 2009-10-08 | 2010-10-07 | カルシウム放出依存性カルシウムチャネルのピラゾール誘導体モジュレータおよび非小細胞肺癌の治療方法 |
| JP2015160031A Expired - Fee Related JP6266568B2 (ja) | 2009-10-08 | 2015-08-14 | カルシウム放出依存性カルシウムチャネルのピラゾール誘導体モジュレータおよび非小細胞肺癌の治療方法 |
| JP2017243778A Pending JP2018080176A (ja) | 2009-10-08 | 2017-12-20 | カルシウム放出依存性カルシウムチャネルのピラゾール誘導体モジュレータおよび非小細胞肺癌の治療方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015160031A Expired - Fee Related JP6266568B2 (ja) | 2009-10-08 | 2015-08-14 | カルシウム放出依存性カルシウムチャネルのピラゾール誘導体モジュレータおよび非小細胞肺癌の治療方法 |
| JP2017243778A Pending JP2018080176A (ja) | 2009-10-08 | 2017-12-20 | カルシウム放出依存性カルシウムチャネルのピラゾール誘導体モジュレータおよび非小細胞肺癌の治療方法 |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US8993612B2 (https=) |
| EP (1) | EP2509974B1 (https=) |
| JP (3) | JP5909312B2 (https=) |
| CN (3) | CN104788430B (https=) |
| CA (1) | CA2784277C (https=) |
| DK (1) | DK2509974T3 (https=) |
| EA (1) | EA025302B8 (https=) |
| ES (1) | ES2676317T3 (https=) |
| HR (1) | HRP20181014T1 (https=) |
| HU (1) | HUE039261T2 (https=) |
| LT (1) | LT2509974T (https=) |
| PL (1) | PL2509974T3 (https=) |
| RS (1) | RS57441B1 (https=) |
| SI (1) | SI2509974T1 (https=) |
| SM (1) | SMT201800361T1 (https=) |
| TR (1) | TR201809711T4 (https=) |
| WO (1) | WO2011042798A1 (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8377970B2 (en) * | 2009-10-08 | 2013-02-19 | Rhizen Pharmaceuticals Sa | Modulators of calcium release-activated calcium channel |
| US8993612B2 (en) * | 2009-10-08 | 2015-03-31 | Rhizen Pharmaceuticals Sa | Modulators of calcium release-activated calcium channel and methods for treatment of non-small cell lung cancer |
| JP6112486B2 (ja) | 2010-04-27 | 2017-04-12 | カルシメディカ，インク． | 細胞内カルシウムを調節する化合物 |
| US10703722B2 (en) | 2010-04-27 | 2020-07-07 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| EP2563759B1 (en) | 2010-04-27 | 2022-04-06 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| EP2609095A4 (en) | 2010-08-27 | 2014-06-18 | Calcimedica Inc | COMPOUNDS MODULATING INTRACELLULAR CALCIUM |
| US20120316182A1 (en) | 2011-06-10 | 2012-12-13 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| WO2013059677A1 (en) | 2011-10-19 | 2013-04-25 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| JP2014532656A (ja) * | 2011-10-28 | 2014-12-08 | シンタ ファーマシューティカルズ コーポレーション | 炎症および免疫関連用途のための化合物 |
| CN104878098A (zh) * | 2011-12-19 | 2015-09-02 | 上海吉凯基因化学技术有限公司 | 人stim1基因的用途及其相关药物 |
| US9512116B2 (en) | 2012-10-12 | 2016-12-06 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
| CN105102448B (zh) | 2013-02-28 | 2018-03-06 | 百时美施贵宝公司 | 作为rock1和rock2抑制剂的苯基吡唑衍生物 |
| EP2970138B1 (en) * | 2013-03-13 | 2019-01-16 | Canadian Blood Services | Pyrazole derivatives and their uses thereof |
| GB201309333D0 (en) | 2013-05-23 | 2013-07-10 | Agency Science Tech & Res | Purine diones as WNT pathway modulators |
| EP2865758A1 (en) | 2013-10-22 | 2015-04-29 | Sylentis, S.A.U. | siRNA and their use in methods and compositions for inhibiting the expression of the ORAI1 gene |
| CN106414429B (zh) * | 2014-06-03 | 2020-01-03 | 爱杜西亚药品有限公司 | 吡唑化合物及其作为t型钙通道阻断剂的用途 |
| PL2982982T3 (pl) * | 2014-08-06 | 2018-03-30 | Centre Hospitalier Regional Et Univ De Brest | Sposób badania przesiewowego związków przy użyciu błonowego STIM1 |
| KR102525131B1 (ko) | 2014-10-08 | 2023-04-24 | 레드엑스 파마 피엘씨 | Wnt 신호 경로의 억제제로서의 N-피리디닐 아세트아미드 유도체 |
| PT3204381T (pt) * | 2014-10-08 | 2022-07-18 | Redx Pharma Plc | Derivados de n-piridinil acetamida como inibidores da via de sinalização wnt |
| CN107207431B (zh) * | 2015-01-13 | 2021-02-09 | 维夫雷昂生物科学有限责任公司 | Ca2+释放激活的Ca2+(CRAC)通道的调节剂及其药物用途 |
| EP3778595B1 (en) | 2015-02-27 | 2021-08-25 | Calcimedica, Inc. | Pancreatitis treatment |
| KR102229608B1 (ko) * | 2015-08-03 | 2021-03-19 | 아이크노스 사이언스 에스. 아. | Ror 감마 조절제로서의 신규한 화합물 |
| CA2995094A1 (en) | 2015-08-07 | 2017-02-16 | Calcimedica, Inc. | Use of crac channel inhibitors for the treatment of stroke and traumatic brain injury |
| ITUA20164199A1 (it) | 2016-06-08 | 2017-12-08 | Univ Degli Studi Del Piemonte Orientale Amedeo Avogadro | Modulatori di soce compisizioni e relativi usi |
| CA3050348A1 (en) | 2017-02-06 | 2018-08-09 | Idorsia Pharmaceuticals Ltd | A novel process for the synthesis of 1-aryl-1-trifluoromethylcyclopropanes |
| CN107475299A (zh) * | 2017-09-13 | 2017-12-15 | 信雅生物科技（苏州）有限公司 | 研究stim1基因在非小细胞肺癌中发挥作用的方法及其应用 |
| AU2018353533A1 (en) * | 2017-10-17 | 2020-05-28 | Rhizen Pharmaceuticals Sa | CRAC channel modulators for treating esophageal cancer |
| WO2019082124A1 (en) | 2017-10-26 | 2019-05-02 | Rhizen Pharmaceuticals Sa | COMPOSITION AND METHOD FOR THE TREATMENT OF LARGE B-CELL DIFFUSED LYMPHOMA |
| JP2021501160A (ja) | 2017-10-30 | 2021-01-14 | ルヒゼン ファーマスティカルズ エスエー | 血液がんおよび固形がんの処置のためのカルシウム放出活性化カルシウムチャネルモジュレーター |
| WO2020053834A1 (en) | 2018-09-14 | 2020-03-19 | Rhizen Pharmaceuticals Sa | Compositions comprising a crac inhibitor and a corticosteroid and methods of use thereof |
| US11155560B2 (en) | 2018-10-30 | 2021-10-26 | Kronos Bio, Inc. | Substituted pyrazolo[1,5-a]pyrimidines for modulating CDK9 activity |
| JP2023528537A (ja) | 2020-03-20 | 2023-07-04 | カルシメディカ，インク． | 急性肺傷害及び急性呼吸窮迫症候群を処置するための方法及び組成物 |
| CA3198798A1 (en) | 2020-11-13 | 2022-05-19 | Kenneth Stauderman | Improved synthesis of crac channel inhibitors |
| CN116789613A (zh) * | 2023-06-13 | 2023-09-22 | 安庆朗坤药业有限公司 | 一种5-羧基苯并三氮唑的制备方法 |
Family Cites Families (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4385414B2 (ja) * | 1997-10-13 | 2009-12-16 | アステラス製薬株式会社 | アミド若しくはアミン誘導体 |
| AU751139B2 (en) * | 1997-10-13 | 2002-08-08 | Astellas Pharma Inc. | Amide derivative |
| WO1999062885A1 (en) | 1998-06-05 | 1999-12-09 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted 1-(4-aminophenyl)pyrazoles and their use as anti-inflammatory agents |
| JP2000256358A (ja) * | 1999-03-10 | 2000-09-19 | Yamanouchi Pharmaceut Co Ltd | ピラゾール誘導体 |
| TW502019B (en) * | 1999-03-26 | 2002-09-11 | Cocensys Inc | Aryl substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles, and the use thereof |
| US20010044445A1 (en) | 1999-04-08 | 2001-11-22 | Bamaung Nwe Y. | Azole inhibitors of cytokine production |
| EP1143013A1 (en) | 2000-04-03 | 2001-10-10 | Warner-Lambert Company | Methods and compositions for screening Icrac modulators |
| WO2002089793A1 (en) | 2001-05-07 | 2002-11-14 | Smithkline Beecham Corporation | Sulfonamides |
| AU2002333524A1 (en) | 2001-09-11 | 2003-03-24 | Glaxosmithkline K.K. | Furo-and thienopyrimidine derivatives as angiogenesis 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 |
| US7452675B2 (en) | 2002-01-25 | 2008-11-18 | The Queen's Medical Center | Methods of screening for TRPM4b modulators |
| US7645588B2 (en) | 2003-03-04 | 2010-01-12 | Calcimedica, Inc. | Composition comprising a cell comprising a STIM1 protein and an agent that modulates intracellular calcium and methods of use |
| TWI376370B (en) | 2003-07-23 | 2012-11-11 | Synta Pharmaceuticals Corp | Compounds for inflammation and immune-related uses |
| JP2006076990A (ja) | 2004-03-12 | 2006-03-23 | Bayer Cropscience Ag | 殺虫性ベンゼンジカルボキサミド類 |
| CN1930129A (zh) * | 2004-03-12 | 2007-03-14 | 拜尔农作物科学股份公司 | N1－((吡唑－1－基甲基)－2－甲基苯基)－邻苯二酰胺衍生物及相关的复合杀虫剂 |
| KR20070057965A (ko) | 2004-09-21 | 2007-06-07 | 신타 파마슈티칼스 코프. | 염증 및 면역 관련 용도를 위한 화합물 |
| EP1805218A2 (en) | 2004-10-29 | 2007-07-11 | Chemicon International, Inc. | Compositions and methods for the assay of g-protein coupled receptors and their ligands |
| KR20140018997A (ko) | 2005-01-07 | 2014-02-13 | 신타 파마슈티칼스 코프. | 염증 및 면역 관련 용도를 위한 화합물 |
| EP1846388A4 (en) | 2005-01-25 | 2011-12-07 | Synta Pharmaceuticals Corp | THIOPHEN COMPOUNDS FOR IGNITIONS AND THE IMMUNE SYSTEM APPLICATIONS |
| PL1848435T3 (pl) | 2005-01-25 | 2016-08-31 | Synta Pharmaceuticals Corp | Związki przeciwko zapaleniom i zastosowania związane z odpornością |
| EP1875925A1 (en) | 2005-04-22 | 2008-01-09 | Astellas Pharma Inc. | Preventive or remedy for bowel disease |
| WO2007004038A1 (en) | 2005-07-05 | 2007-01-11 | Pfizer Products Inc. | Aminothiazole derivatives as agonists of the thrombopoietin receptor |
| TW200806641A (en) | 2006-01-25 | 2008-02-01 | Synta Pharmaceuticals Corp | Substituted aromatic compounds for inflammation and immune-related uses |
| US7816535B2 (en) | 2006-01-25 | 2010-10-19 | Synta Pharmaceuticals Corp. | Vinyl-phenyl derivatives for inflammation and immune-related uses |
| WO2007087429A2 (en) | 2006-01-25 | 2007-08-02 | Synta Pharmaceuticals Corp. | Phenyl and pyridyl compounds for inflammation and immune-related uses |
| TW200806290A (en) | 2006-01-25 | 2008-02-01 | Synta Pharmaceuticals Corp | Substituted biaryl compounds for inflammation and immune-related uses |
| US8455658B2 (en) | 2006-01-25 | 2013-06-04 | Synta Pharmaceuticals Corp. | Thiazole and thiadiazole compounds for inflammation and immune-related uses |
| US20070254926A1 (en) | 2006-01-31 | 2007-11-01 | Jun Jiang | Pyridylphenyl compounds for inflammation and immune-related uses |
| AU2007227210A1 (en) | 2006-03-20 | 2007-09-27 | Synta Pharmaceuticals Corp. | Benzoimidazolyl-parazine compounds for inflammation and immune-related uses |
| AU2007230911A1 (en) | 2006-03-23 | 2007-10-04 | Synta Pharmaceuticals Corp. | Benzimidazolyl-pyridine compounds for inflammation and immune-related uses |
| AU2007238225A1 (en) | 2006-04-10 | 2007-10-25 | Beth Israel Deaconess Medical Center | CRAC modulators and use of same for drug discovery |
| US20080039392A1 (en) | 2006-05-26 | 2008-02-14 | The Regents Of The University Of California | CRAC channel and modulator screening methods |
| WO2008016643A2 (en) | 2006-08-01 | 2008-02-07 | Cytokinetics, Incorporated | Certain chemical entities, compositions, and methods |
| US8779154B2 (en) | 2006-09-26 | 2014-07-15 | Qinglin Che | Fused ring compounds for inflammation and immune-related uses |
| US20080207641A1 (en) | 2006-11-13 | 2008-08-28 | Synta Pharmaceuticals Corp. | Cyclohexenyl-aryl compounds for inflammation and immune-related uses |
| JP2010519206A (ja) | 2007-02-16 | 2010-06-03 | シンタ ファーマシューティカルズ コーポレーション | 炎症及び免疫関連使用のための置換縮合環化合物 |
| NZ580195A (en) | 2007-03-05 | 2012-03-30 | Univ Queensland | Targeting crac for breast cancer therapy and/or diagnosis |
| KR101217754B1 (ko) | 2007-03-23 | 2013-01-02 | 더 퀸스 메디컬 센터 | Ｓｔｉｍ2 활성을 측정하기 위한 분석 및 방법 |
| CA2688417C (en) | 2007-05-24 | 2017-04-25 | Calcimedica, Inc. | Calcium channel proteins and uses thereof |
| WO2009017831A1 (en) | 2007-08-01 | 2009-02-05 | Synta Pharmaceuticals Corp. | Vinyl-aryl derivatives for inflammation and immune-related uses |
| CA2695143A1 (en) | 2007-08-01 | 2009-02-05 | Synta Pharmaceuticals Corp. | Heterocycle-aryl compounds for inflammation and immune-related uses |
| CA2695148A1 (en) | 2007-08-01 | 2009-02-05 | Synta Pharmaceuticals Corp. | Pyridine compounds for inflammation and immune-related uses |
| US8263641B2 (en) | 2007-09-10 | 2012-09-11 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| US8324219B2 (en) | 2007-09-20 | 2012-12-04 | Synta Pharmaceuticals Corp. | Substituted benzoimidazolyl-pyrazine compounds for inflammation and immune-related uses |
| US8389567B2 (en) | 2007-12-12 | 2013-03-05 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| US20110052643A1 (en) | 2008-01-07 | 2011-03-03 | Synta Pharmaceuticals Corp. | Compounds for inflammation and immune-related uses |
| TWI392673B (zh) | 2008-08-27 | 2013-04-11 | Calcimedica Inc | 調控細胞內鈣離子濃度之化合物 |
| US8524763B2 (en) | 2008-09-22 | 2013-09-03 | Calcimedica, Inc. | Inhibitors of store operated calcium release |
| US20110269743A1 (en) | 2008-09-22 | 2011-11-03 | CalciMedica, Inc | Phenylthiophenyldihydrobenzothiazepine inhibitors of store operated calcium release |
| US20110257177A1 (en) | 2008-09-22 | 2011-10-20 | Calcimedica, Inc. | Benzylthiotetrazole inhibitors of store operated calcium release |
| AU2009300316A1 (en) | 2008-10-01 | 2010-04-08 | Synta Pharmaceuticals Corp. | Compounds for inflammation and immune-related uses |
| AU2009300318A1 (en) | 2008-10-01 | 2010-04-08 | Synta Pharmaceuticals Corp. | Compounds for inflammation and immune-related uses |
| AU2009300317A1 (en) | 2008-10-01 | 2010-04-08 | Synta Pharmaceuticals Corp. | Compounds for inflammation and immune-related uses |
| US8143269B2 (en) | 2008-10-03 | 2012-03-27 | Calcimedica, Inc. | Inhibitors of store operated calcium release |
| WO2010048559A2 (en) | 2008-10-24 | 2010-04-29 | Calcimedica Inc. | Phenylpyrazole inhibitors of store operated calcium release |
| US8993612B2 (en) * | 2009-10-08 | 2015-03-31 | Rhizen Pharmaceuticals Sa | Modulators of calcium release-activated calcium channel and methods for treatment of non-small cell lung cancer |
-
2010
- 2010-10-06 US US12/899,410 patent/US8993612B2/en not_active Expired - Fee Related
- 2010-10-07 HR HRP20181014TT patent/HRP20181014T1/hr unknown
- 2010-10-07 TR TR2018/09711T patent/TR201809711T4/tr unknown
- 2010-10-07 EP EP10776149.6A patent/EP2509974B1/en active Active
- 2010-10-07 ES ES10776149.6T patent/ES2676317T3/es active Active
- 2010-10-07 SI SI201031711T patent/SI2509974T1/en unknown
- 2010-10-07 SM SM20180361T patent/SMT201800361T1/it unknown
- 2010-10-07 CN CN201510114126.6A patent/CN104788430B/zh not_active Expired - Fee Related
- 2010-10-07 RS RS20180791A patent/RS57441B1/sr unknown
- 2010-10-07 CN CN201910890829.6A patent/CN110627724A/zh active Pending
- 2010-10-07 DK DK10776149.6T patent/DK2509974T3/en active
- 2010-10-07 JP JP2012532676A patent/JP5909312B2/ja not_active Expired - Fee Related
- 2010-10-07 PL PL10776149T patent/PL2509974T3/pl unknown
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- 2010-10-07 HU HUE10776149A patent/HUE039261T2/hu unknown
- 2010-10-07 WO PCT/IB2010/002539 patent/WO2011042798A1/en not_active Ceased
- 2010-10-07 CN CN201080055388.5A patent/CN102958925B/zh not_active Expired - Fee Related
- 2010-10-07 LT LTEP10776149.6T patent/LT2509974T/lt unknown
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2015
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- 2015-08-14 JP JP2015160031A patent/JP6266568B2/ja not_active Expired - Fee Related
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