JP2013521281A5 - - Google Patents
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- JP2013521281A5 JP2013521281A5 JP2012556056A JP2012556056A JP2013521281A5 JP 2013521281 A5 JP2013521281 A5 JP 2013521281A5 JP 2012556056 A JP2012556056 A JP 2012556056A JP 2012556056 A JP2012556056 A JP 2012556056A JP 2013521281 A5 JP2013521281 A5 JP 2013521281A5
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- cancer
- alkyl
- compound
- haloalkyl
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- 150000001875 compounds Chemical class 0.000 claims 19
- 201000011510 cancer Diseases 0.000 claims 14
- 125000001188 haloalkyl group Chemical group 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 4
- 206010025650 Malignant melanoma Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 2
- HRYJJMQDEVGSAQ-UHFFFAOYSA-N [2-(4-bromophenyl)-1H-imidazol-5-yl]-(3,4,5-trimethoxyphenyl)methanone Chemical compound COC1=C(OC)C(OC)=CC(C(=O)C=2N=C(NC=2)C=2C=CC(Br)=CC=2)=C1 HRYJJMQDEVGSAQ-UHFFFAOYSA-N 0.000 claims 2
- XDODKXXXAHTIRD-UHFFFAOYSA-N [2-(4-chlorophenyl)-1H-imidazol-5-yl]-(3,4,5-trimethoxyphenyl)methanone Chemical compound COC1=C(OC)C(OC)=CC(C(=O)C=2N=C(NC=2)C=2C=CC(Cl)=CC=2)=C1 XDODKXXXAHTIRD-UHFFFAOYSA-N 0.000 claims 2
- NQHVDNDKHQBFKP-UHFFFAOYSA-N [2-(4-methylphenyl)-1H-imidazol-5-yl]-(3,4,5-trimethoxyphenyl)methanone Chemical compound COC1=C(OC)C(OC)=CC(C(=O)C=2N=C(NC=2)C=2C=CC(C)=CC=2)=C1 NQHVDNDKHQBFKP-UHFFFAOYSA-N 0.000 claims 2
- 125000004432 carbon atoms Chemical group C* 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940079593 drugs Drugs 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010024324 Leukaemias Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- -1 O-alkyl Inorganic materials 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- AAXZBPGIFMJMRG-UHFFFAOYSA-N [1-methyl-2-(4-methylphenyl)imidazol-4-yl]-(3,4,5-trimethoxyphenyl)methanone Chemical compound COC1=C(OC)C(OC)=CC(C(=O)C=2N=C(N(C)C=2)C=2C=CC(C)=CC=2)=C1 AAXZBPGIFMJMRG-UHFFFAOYSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 201000001514 prostate carcinoma Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 0 CS1*CCC1 Chemical compound CS1*CCC1 0.000 description 1
Claims (17)
- 下記の構造式(II)で表される化合物。
R1、R2、R3、R4、R5、およびR6は、互いに独立して、水素、O−アルキル、O−ハロアルキル、F、Cl、Br、I、ハロアルキル、CF3、CN、−CH2CN、NH2、ヒドロキシル、−(CH2)iNHCH3、−(CH2)iNH2、−(CH2)iN(CH3)2、−OC(O)CF3、炭素数1〜5の直鎖もしくは分岐鎖のアルキル、ハロアルキル、アルキルアミノ、アミノアルキル、−OCH2Ph、−NHCO−アルキル、COOH、−C(O)Ph、C(O)O−アルキル、C(O)H、−C(O)NH2、またはNO2であり;
R10およびR11は、互いに独立して、水素、O−アルキル、O−ハロアルキル、F、Cl、Br、I、ハロアルキル、CF3、CN、−CH2CN、NH2、ヒドロキシル、−(CH2)iNHCH3、−(CH2)iNH2、−(CH2)iN(CH3)2、−OC(O)CF3、炭素数1〜5の直鎖もしくは分岐鎖のアルキル、ハロアルキル、アルキルアミノ、アミノアルキル、−OCH2Ph、−NHCO−アルキル、COOH、−C(O)Ph、C(O)O−アルキル、C(O)H、−C(O)NH2、またはNO2であり;
Xは、単結合、炭素数1〜5の炭化水素、SまたはOであり;
Yは、単結合、−C=O、−C=S、−C=N−NH2、−C=N−OH、−CH−OH、−C=CH−CN、−C=N−CN、−CH=CH−、−C=C(CH3)2、−C=N−OMe、−(C=O)−NH、−NH−(C=O)、-(C=O)−O、−O−(C=O)、−(CH2)1−5−(C=O)、(C=O)−(CH2)1−5、−(SO2)−NH−、−NH−(SO2)−、SO2、SO、またはSであり;
iは、0〜5の整数であり;
lは、1〜2の整数であり;
nは、1〜3の整数であり;
mは、1〜3の整数である。 - 請求項1に記載の化合物であって、
下記の構造式Vで表される化合物であることを特徴とする化合物。
R4、R5、およびR6は、互いに独立して、水素、O−アルキル、O−ハロアルキル、F、Cl、Br、I、ハロアルキル、CF3、CN、−CH2CN、NH2、ヒドロキシル、−(CH2)iNHCH3、−(CH2)iNH2、−(CH2)iN(CH3)2、−OC(O)CF3、炭素数1〜5の直鎖もしくは分岐鎖のアルキル、ハロアルキル、アルキルアミノ、アミノアルキル、−OCH2Ph、−NHCO−アルキル、COOH、−C(O)Ph、C(O)O−アルキル、C(O)H、−C(O)NH2、またはNO2であり;
nは、1〜3の整数である。 - 請求項3に記載の化合物であって、
前記R3が、FまたはClであることを特徴とする化合物。 - 請求項3に記載の化合物であって、
前記R4が、ClまたはOCH 3 であることを特徴とする化合物。 - 請求項3に記載の化合物であって、
前記R5が水素であることを特徴とする化合物。 - 請求項1〜7のいずれかに記載の化合物、またはその異性体、薬学的に許容される塩、医薬品、互変異性体、水和物、N−酸化物あるいはそれらの組み合わせ。
- 請求項8に記載の化合物および薬学的に許容される担体を含む医薬組成物。
- 請求項8に記載の化合物を、癌の処置に有効な条件の下で癌を患う被検体に投与することを含む、癌の処置、抑制、重症度軽減、リスク軽減、または阻害の方法。
- 請求項10に記載の方法であって、
前記癌が、前立腺癌、乳癌、卵巣癌、皮膚癌、メラノーマ、肺癌、大腸癌、白血病、腎臓癌、CNS癌、およびそれらの組み合わせからなる群から選択されることを特徴とする方法。 - 請求項11に記載の方法であって、
前記癌が、メラノーマ癌、転移性メラノーマ癌、前立腺癌または卵巣癌であることを特徴とする方法。 - 請求項10に記載の方法であって、
前記投与が別の癌治療との併用で行われることを特徴とする方法。 - 請求項8に記載の化合物を、薬剤耐性腫瘍の処置に有効な条件の下で癌を患う被検体に投与することを含む、薬剤耐性腫瘍を処置する方法。
- 請求項14に記載の方法であって、
前記腫瘍が、メラノーマ癌腫瘍、転移性メラノーマ腫瘍、前立腺癌腫または卵巣癌腫瘍であることを特徴とする方法。 - 請求項14に記載の方法であって、
前記投与が別の癌治療との併用で行われることを特徴とする方法。 - 請求項8に記載の化合物を提供すること、および癌細胞の死滅に有効な条件の下で癌細胞を化合物に接触させることを含む、癌性細胞を破壊する方法。
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US30936010P | 2010-03-01 | 2010-03-01 | |
US61/309,360 | 2010-03-01 | ||
US31579010P | 2010-03-19 | 2010-03-19 | |
US61/315,790 | 2010-03-19 | ||
US37667510P | 2010-08-24 | 2010-08-24 | |
US61/376,675 | 2010-08-24 | ||
PCT/US2010/062418 WO2011109059A1 (en) | 2010-03-01 | 2010-12-29 | Compounds for treatment of cancer |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2013521281A JP2013521281A (ja) | 2013-06-10 |
JP2013521281A5 true JP2013521281A5 (ja) | 2014-02-20 |
JP5879273B2 JP5879273B2 (ja) | 2016-03-08 |
Family
ID=44542481
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2012556056A Expired - Fee Related JP5879273B2 (ja) | 2010-03-01 | 2010-12-29 | 癌を処置するための化合物 |
Country Status (11)
Country | Link |
---|---|
US (1) | US9334242B2 (ja) |
EP (2) | EP3064204A1 (ja) |
JP (1) | JP5879273B2 (ja) |
KR (2) | KR20120130777A (ja) |
CN (2) | CN102883607B (ja) |
AU (1) | AU2010347233B2 (ja) |
CA (1) | CA2791738C (ja) |
IL (3) | IL221710A (ja) |
MX (1) | MX2012010115A (ja) |
RU (1) | RU2581367C2 (ja) |
WO (1) | WO2011109059A1 (ja) |
Families Citing this family (99)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
PT2959900T (pt) | 2008-06-16 | 2017-06-22 | Univ Tennessee Res Found | Composto para tratamento do cancro |
US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
CN102883607B (zh) | 2010-03-01 | 2015-07-22 | Gtx公司 | 用于治疗癌的化合物 |
US11084811B2 (en) | 2010-03-01 | 2021-08-10 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
MX2012012204A (es) | 2010-04-22 | 2012-12-05 | Vertex Pharma | Proceso para producir compuestos de cicloalquilcarboxamido-indol. |
AU2011293353B2 (en) * | 2010-08-24 | 2015-02-26 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
EP2638014B1 (en) | 2010-11-08 | 2017-01-04 | Lycera Corporation | N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of ror-gamma activity and the treatment of diseases |
WO2012071369A2 (en) | 2010-11-24 | 2012-05-31 | The Trustees Of Columbia University In The City Of New York | A non-retinoid rbp4 antagonist for treatment of age-related macular degeneration and stargardt disease |
GB201104267D0 (en) | 2011-03-14 | 2011-04-27 | Cancer Rec Tech Ltd | Pyrrolopyridineamino derivatives |
EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
KR20140123104A (ko) | 2012-02-17 | 2014-10-21 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 유비퀴틴 활성화 효소의 피라졸로피리미디닐 억제제 |
RU2014141674A (ru) | 2012-03-16 | 2016-05-10 | Аксикин Фармасьютикалз, Инк. | 3,5-диаминопиразоловые ингибиторы киназы |
US9333202B2 (en) | 2012-05-01 | 2016-05-10 | The Trustees Of Columbia University In The City Of New York | Non-retinoid antagonists for treatment of age-related macular degeneration and stargardt disease |
JP6242868B2 (ja) | 2012-05-08 | 2017-12-06 | リセラ・コーポレイションLycera Corporation | RORγのアゴニストとしての使用のためおよび疾患の処置のためのテトラヒドロ[1,8]ナフチリジンスルホンアミドおよび関連化合物 |
RU2014149136A (ru) | 2012-05-08 | 2016-07-10 | Мерк Шарп И Доум Корп. | ТЕТРАГИДРОНАФТИРИДИНОВЫЕ И РОДСТВЕННЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ RORγ АКТИВНОСТИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ |
KR101742954B1 (ko) | 2012-05-31 | 2017-06-02 | 페넥스 파마슈티컬스 아게 | 고아 핵 수용체 ror[감마]의 조절제로서의 카복사미드 또는 설폰아미드가 치환된 티아졸 및 관련된 유도체 |
CN104640442A (zh) | 2012-06-14 | 2015-05-20 | 巴斯夫欧洲公司 | 使用取代3-吡啶基噻唑化合物和衍生物防除动物有害物的灭害方法 |
GB201216017D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Inhibitor compounds |
GB201216018D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Pharmacologically active compounds |
WO2014121062A1 (en) | 2013-02-01 | 2014-08-07 | Acetylon Pharmaceuticals, Inc. | Selective hdac3 inhibitors |
US9139583B2 (en) | 2013-02-01 | 2015-09-22 | Acetylon Pharmaceuticals, Inc. | Selective HDAC3 inhibitors |
MX2015011713A (es) * | 2013-03-05 | 2016-05-09 | Univ Tennessee Res Foundation | Compuestos para el tratamiento de cancer. |
US9944644B2 (en) | 2013-03-14 | 2018-04-17 | The Trustees Of Columbia University In The City Of New York | Octahydropyrrolopyrroles their preparation and use |
DK2968304T3 (en) | 2013-03-14 | 2019-01-28 | Univ Columbia | 4-PHENYLPIPERIDINES, THEIR PREPARATION AND USE. |
US9637450B2 (en) | 2013-03-14 | 2017-05-02 | The Trustees Of Columbia University In The City Of New York | Octahydrocyclopentapyrroles, their preparation and use |
US9938291B2 (en) | 2013-03-14 | 2018-04-10 | The Trustess Of Columbia University In The City Of New York | N-alkyl-2-phenoxyethanamines, their preparation and use |
CA2916468C (en) | 2013-07-02 | 2019-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryl compounds useful as inhibitors of sumo activating enzyme |
JO3425B1 (ar) | 2013-07-15 | 2019-10-20 | Novartis Ag | مشتقات البابيريدينيل-اندول واستخدامها كعامل متمم لمثبطات b |
NZ631142A (en) | 2013-09-18 | 2016-03-31 | Axikin Pharmaceuticals Inc | Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors |
KR102103256B1 (ko) | 2013-10-14 | 2020-04-23 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 선택적으로 치환된 퀴놀린 화합물 |
KR102365952B1 (ko) | 2013-10-14 | 2022-02-22 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 선택적으로 치환된 퀴놀린 화합물 |
US9783511B2 (en) | 2013-12-20 | 2017-10-10 | Lycera Corporation | Carbamate benzoxazine propionic acids and acid derivatives for modulation of RORgamma activity and the treatment of disease |
WO2015095795A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
WO2015095788A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
CN103755664B (zh) * | 2014-01-22 | 2016-08-17 | 沈阳药科大学 | 4-芳基噻(硒)唑类化合物及其用途 |
EP3110429A4 (en) | 2014-02-27 | 2018-02-21 | Lycera Corporation | Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma & related therapeutic methods |
GB201403536D0 (en) | 2014-02-28 | 2014-04-16 | Cancer Rec Tech Ltd | Inhibitor compounds |
CN103864785B (zh) * | 2014-03-11 | 2015-12-09 | 中国农业大学 | 一类氮杂吲哚骨架的噻唑啉衍生物及其制备方法与应用 |
ES2957761T3 (es) | 2014-04-15 | 2024-01-25 | Vertex Pharma | Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de la conductancia transmembrana de fibrosis quística |
DK3137168T3 (da) | 2014-04-30 | 2022-03-21 | Univ Columbia | Substituerede 4-phenylpiperidiner, deres fremstilling og anvendelse |
JP6728061B2 (ja) | 2014-05-05 | 2020-07-22 | リセラ・コーポレイションLycera Corporation | RORγアゴニストとして用いるテトラヒドロキノリンスルホンアミド及び関連化合物ならびに疾患の治療 |
US10189777B2 (en) | 2014-05-05 | 2019-01-29 | Lycera Corporation | Benzenesulfonamido and related compounds for use as agonists of RORγ and the treatment of disease |
EP3708164A1 (en) * | 2014-05-06 | 2020-09-16 | Oncternal Therapeutics, Inc | Compounds for treatment of cancer |
CN103980248B (zh) * | 2014-05-10 | 2015-11-18 | 浙江大学 | 3,5-二取代-4-氨基噻吩-2-甲醛化合物及其制备方法 |
HUE045748T2 (hu) | 2014-07-01 | 2020-01-28 | Millennium Pharm Inc | Heteroaril vegyületek mint SUMO aktiváló enzimek inhibitorai |
KR102034202B1 (ko) | 2014-12-23 | 2019-10-18 | 에스엠에이 세라퓨틱스 아이엔씨. | 3,5-디아미노피라졸 키나제 억제제 |
CA2975997A1 (en) | 2015-02-11 | 2016-08-18 | Merck Sharp & Dohme Corp. | Substituted pyrazole compounds as rorgammat inhibitors and uses thereof |
US10772858B2 (en) | 2015-05-01 | 2020-09-15 | Georgia State University Research Foundation, Inc. | Benzhydrol derivatives for the management of conditions related to hypoxia inducible factors |
CA2982847A1 (en) | 2015-05-05 | 2016-11-10 | Lycera Corporation | Dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of ror.gamma. and the treatment of disease |
US10611740B2 (en) | 2015-06-11 | 2020-04-07 | Lycera Corporation | Aryl dihydro-2H-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease |
EP3368535B1 (en) | 2015-10-27 | 2020-12-02 | Merck Sharp & Dohme Corp. | Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof |
AU2016344115A1 (en) | 2015-10-27 | 2018-05-10 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as rorgammat inhibitors and uses thereof |
CA3002846A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | Substituted bicyclic pyrazole compounds as rorgammat inhibitors and uses thereof |
CN108602775B (zh) | 2016-01-14 | 2022-04-29 | 贝思以色列女会吏医学中心公司 | 肥大细胞调节剂及其用途 |
AU2017275657B2 (en) | 2016-06-02 | 2021-08-19 | Novartis Ag | Potassium channel modulators |
CA2968836A1 (en) | 2016-06-13 | 2017-12-13 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
PT3730487T (pt) | 2016-06-13 | 2022-07-22 | Gilead Sciences Inc | Derivados de azetidina como moduladores de fxr (nr1h4) |
CN106279027A (zh) * | 2016-07-26 | 2017-01-04 | 沈阳药科大学 | (1‑芳基‑1h‑吡唑‑4‑基)(3,4,5‑三甲氧基苯基)甲酮、甲酮肟类化合物及其用途 |
CN106187923A (zh) * | 2016-08-01 | 2016-12-07 | 沈阳药科大学 | 2‑芳基‑4‑芳酰基‑三氮唑类化合物及其用途 |
CN107840842A (zh) | 2016-09-19 | 2018-03-27 | 北京天诚医药科技有限公司 | 炔代杂环化合物、其制备方法及其在医药学上的应用 |
WO2018081167A1 (en) | 2016-10-24 | 2018-05-03 | Yumanity Therapeutics | Compounds and uses thereof |
RS62899B1 (sr) | 2017-01-23 | 2022-03-31 | Cadent Therapeutics Inc | Modulatori kalijumovih kanala |
US20180280394A1 (en) | 2017-03-28 | 2018-10-04 | Gilead Sciences, Inc. | Methods of treating liver disease |
GB201709840D0 (en) | 2017-06-20 | 2017-08-02 | Inst Of Cancer Research: Royal Cancer Hospital | Methods and medical uses |
US20200123147A1 (en) | 2017-06-29 | 2020-04-23 | Bayer Aktiengesellschaft | Thiazole compounds useful as prmt5 inhibitors |
JOP20200001A1 (ar) | 2017-07-11 | 2022-10-30 | Vertex Pharma | كاربوكسأميدات بوصفها معدلات لقنوات الصوديوم |
CN109180649B (zh) * | 2017-08-18 | 2021-03-12 | 四川百利药业有限责任公司 | 一种含吲哚环的ido抑制剂及其制备方法 |
MA50250A (fr) | 2017-09-15 | 2020-07-22 | Forma Therapeutics Inc | Compositions de tétrahydroimidazo quinoléine utilisées en tant qu'inhibiteurs de cbp/p300 |
CA3083000A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
PL3700902T3 (pl) | 2017-10-27 | 2023-09-04 | Boehringer Ingelheim International Gmbh | Inhibitory trpc6 |
CN108358864B (zh) * | 2017-12-15 | 2020-07-17 | 五邑大学 | 一种2-酰基-5-苯基噁唑类微管蛋白抑制剂的制备方法及应用 |
JP2021523915A (ja) * | 2018-05-15 | 2021-09-09 | ユニバーシティ オブ テネシー リサーチ ファウンデーション | 膵臓癌の治療のための化合物 |
MX2020012291A (es) * | 2018-05-15 | 2021-03-25 | Univ Tennessee Res Found | Compuestos para el tratamiento de cancer de mama triple negativo y cancer de ovario. |
CN109020904B (zh) * | 2018-06-15 | 2021-05-25 | 沈阳药科大学 | 2-芳基-4-芳酰基-5-脂环胺基-2h-三氮唑类化合物及其用途 |
SG11202012767UA (en) | 2018-06-29 | 2021-01-28 | Forma Therapeutics Inc | Inhibiting creb binding protein (cbp) |
EP3853234A1 (en) | 2018-09-18 | 2021-07-28 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
CN110950848B (zh) * | 2018-09-27 | 2024-03-26 | 徐诺药业 | 新型氨基吡唑类衍生物的合成与应用 |
CA3116339A1 (en) | 2018-10-22 | 2020-04-30 | Cadent Therapeutics, Inc. | Crystalline forms of potassium channel modulators |
CN109503509B (zh) * | 2018-12-17 | 2021-10-19 | 湘潭大学 | 4-苯乙烯基噻唑及衍生物及其合成方法 |
CA3124702A1 (en) | 2019-01-15 | 2020-07-23 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
CA3127791A1 (en) | 2019-01-24 | 2020-07-30 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
CA3129949C (en) | 2019-02-19 | 2024-04-30 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
CN112142711B (zh) * | 2019-06-28 | 2022-03-29 | 中国科学院上海药物研究所 | 取代噻吩类化合物、其制备方法及其用途 |
TW202128675A (zh) | 2019-12-06 | 2021-08-01 | 美商維泰克斯製藥公司 | 作為鈉通道調節劑之經取代四氫呋喃 |
KR102346187B1 (ko) * | 2019-12-26 | 2021-12-31 | 울산과학기술원 | 디히드로퓨란 유도체 및 이의 합성 방법 |
JOP20220138A1 (ar) * | 2020-04-03 | 2023-01-30 | Veru Inc | طرق مُعالجة فيروس كورونا |
US11795168B2 (en) | 2020-09-23 | 2023-10-24 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP) |
US11801243B2 (en) | 2020-09-23 | 2023-10-31 | Forma Therapeutics, Inc. | Bromodomain inhibitors for androgen receptor-driven cancers |
PE20241335A1 (es) | 2021-06-04 | 2024-07-03 | Vertex Pharma | N-(hidroxialquil (hetero)aril) tetrahidrofurano carboxamidas como moduladores de canales de sodio |
CN113620930B (zh) * | 2021-07-12 | 2022-08-16 | 南京烁慧医药科技有限公司 | 一种含磺酰胺结构的化合物及其制备方法和应用、一种药物组合物及应用 |
CN113929591A (zh) * | 2021-10-09 | 2022-01-14 | 中国科学技术大学 | 具有抗增殖活性的抑制剂 |
CN115504964A (zh) * | 2022-04-12 | 2022-12-23 | 海创药业股份有限公司 | 氘代杂环酮类化合物及其用途 |
CN114751891B (zh) * | 2022-04-27 | 2023-04-07 | 广东晨康生物科技有限公司 | 一种(2-(1h-吲哚-3-基)-1h-咪唑-4-基)苯基甲酮类化合物及其应用 |
CN114805307B (zh) * | 2022-04-29 | 2024-08-09 | 南京雷正医药科技有限公司 | 一种用于制备冠状病毒治疗药物的吲哚类化合物 |
WO2024180474A1 (en) * | 2023-02-27 | 2024-09-06 | Assia Chemical Industries Ltd. | Solid state forms of sabizabulin and process for preparation thereof |
Family Cites Families (78)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CH528514A (de) * | 1969-05-22 | 1972-09-30 | Bayer Ag | Verfahren zur Herstellung von Acylimidazolen |
US4721712A (en) | 1984-06-12 | 1988-01-26 | Pfizer Inc. | 1,3-disubstituted 2-oxindoles as analgesic and anti-inflammatory agents |
US4609670A (en) * | 1984-11-13 | 1986-09-02 | Eli Lilly And Company | Imidazolium hypoglycemic agents |
CN1030415A (zh) | 1987-02-20 | 1989-01-18 | 山之内制药株式会社 | 饱和的杂环碳酰胺衍生物和它的制备方法 |
ES2245660T3 (es) | 1990-11-30 | 2006-01-16 | Otsuka Pharmaceutical Co., Ltd. | Derivados de azol y su utilizacion como inhibidores de los radicales superoxidos. |
US5120749A (en) | 1991-02-20 | 1992-06-09 | Abbott Laboratories | Platelet activating antagonists |
NO924963L (no) | 1991-12-27 | 1993-06-28 | Sankyo Co | Pyridyltiazolidinkarboksylsyreamid-derivater og fremgangsmaate til fremstilling derav |
JP3393891B2 (ja) * | 1992-08-18 | 2003-04-07 | 塩野義製薬株式会社 | イミダゾール類の製造方法 |
US5514690A (en) | 1992-11-17 | 1996-05-07 | E. R. Squibb & Sons, Inc. | Aminocarbonyl (thiocarbonyl) and cyanoguanidine derivatives of quinoline and indoline |
DK0798298T3 (da) | 1994-12-15 | 2001-10-22 | Sankyo Co | Thiazolidinon- eller oxazolidonderivater til behandling af angina pectoris eller sammensætninger indeholdende samme som aktiv bestanddel |
PT812835E (pt) | 1995-03-02 | 2001-08-30 | Sankyo Co | Derivados opticamente activos de tiazolidinona |
JP2004067510A (ja) | 1997-12-26 | 2004-03-04 | Mitsubishi Pharma Corp | 新規イミダゾール誘導体 |
US6828344B1 (en) | 1998-02-25 | 2004-12-07 | Genetics Institute, Llc | Inhibitors of phospholipase enzymes |
AU7354900A (en) | 1999-09-09 | 2001-04-10 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
JP2001240593A (ja) | 1999-10-12 | 2001-09-04 | Japan Tobacco Inc | 高トリグリセリド血症治療薬及び抗肥満薬 |
DE60018213T2 (de) | 1999-12-27 | 2005-12-29 | Ortho-Mcneil Pharmaceutical, Inc. | Substituierte aminoalkylamid-derivate als antagonisten des follikel-stimulierenden hormons |
HUP0302002A3 (en) | 2000-05-11 | 2007-02-28 | Consejo Superior Investigacion | Heterocyclic inhibitors of glycogen synthase kinase gsk-3, their use and pharmaceutical compositions containing them |
CA2433018A1 (en) | 2000-12-21 | 2002-06-27 | Joel C. Barrish | Thiazolyl inhibitors of tec family tyrosine kinases |
US20030096737A1 (en) | 2001-04-19 | 2003-05-22 | Anita Diu-Hercend | Caspase inhibitors and uses thereof |
WO2003016338A1 (en) | 2001-08-15 | 2003-02-27 | Parker Hughes Institute | Crystal structure of the btk kinase domain |
TWI231757B (en) | 2001-09-21 | 2005-05-01 | Solvay Pharm Bv | 1H-Imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity |
AR036608A1 (es) | 2001-09-24 | 2004-09-22 | Bayer Corp | Derivados de imidazol, composiciones farmaceuticas y el uso de dichos derivados para la fabricacion de un medicamento para el tratamiento de la obesidad |
US20040267017A1 (en) | 2001-09-26 | 2004-12-30 | Bierer Donald E | 3-pyridyl or 4-isoquinolinyl thiazoles as c17, 20 lyase inhibitors |
WO2003027096A1 (en) | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | Substituted 3-pyridyl imidazoles as c17,20 lyase inhibitors |
CA2463441A1 (en) | 2001-10-12 | 2003-05-08 | Bayer Pharmaceuticals Corporation | Phenyl substituted 5-membered nitrogen containing heterocycles for the treatment of obesity |
EP1456187A4 (en) | 2001-11-15 | 2005-02-09 | Incyte San Diego Inc | N-SUBSTITUTED HETEROCYCLES FOR THE TREATMENT OF HYPERCHOLESTERINEMIA, DYSLIPIDEMIA AND OTHER METABOLIC DISORDER, CANCER AND OTHER DISEASES |
AU2003214534B2 (en) | 2002-04-08 | 2006-08-31 | Torrent Pharmaceuticals Ltd. | Thiazolidine-4-carbonitriles and analogues and their use as dipeptidyl-peptidas inhibitors |
AU2003223708A1 (en) | 2002-04-23 | 2003-11-10 | Axys Pharmaceuticals, Inc. | Novel phenyl derivatives as inducers of apoptosis |
TW200404796A (en) | 2002-08-19 | 2004-04-01 | Ono Pharmaceutical Co | Nitrogen-containing compound |
WO2004052280A2 (en) * | 2002-12-10 | 2004-06-24 | Imclone Systems Incorporated | Anti-angiogenic compounds and their use in cancer treatment |
CA2515215A1 (en) | 2003-02-10 | 2004-08-26 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
EP1594847A2 (en) | 2003-02-12 | 2005-11-16 | Transtech Pharma, Inc. | Substituted azole derivatives as therapeutic agents |
CN1826111A (zh) | 2003-04-10 | 2006-08-30 | 阿文尼尔药品公司 | 用于治疗变应性和过增生性疾病的咪唑衍生物 |
EP1626713A2 (en) | 2003-05-16 | 2006-02-22 | Ambit Biosciences Corporation | Heterocyclic compounds and uses thereof |
ATE469878T1 (de) | 2003-07-24 | 2010-06-15 | Leo Pharma As | Aminobenzophenonverbindungen |
US7501538B2 (en) | 2003-08-08 | 2009-03-10 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions and methods of use |
CN1902184A (zh) | 2003-11-18 | 2007-01-24 | 田纳西大学研究基金会 | 噻唑烷酮酰胺、噻唑烷羧酸酰胺、其制备方法及其用途 |
US20060014740A1 (en) | 2003-11-18 | 2006-01-19 | Miller Duane D | Analogs exhibiting inhibition of cell proliferation, methods of making, and uses thereof |
BRPI0417543A (pt) | 2003-12-12 | 2007-03-27 | Wyeth Corp | quinolinas úteis no tratamento de doença cardiovascular |
WO2005080367A1 (en) | 2004-02-12 | 2005-09-01 | Pharmagene Laboratories Limited | Ep2 receptor agonists |
BRPI0508594A (pt) | 2004-03-08 | 2007-08-21 | Wyeth Corp | moduladores de canal de ìon |
WO2006078287A2 (en) | 2004-05-06 | 2006-07-27 | Plexxikon, Inc. | Pde4b inhibitors and uses therefor |
WO2006002119A2 (en) | 2004-06-18 | 2006-01-05 | Gpc Biotech, Inc. | Kinase inhibitors for treating cancers |
MX2007001846A (es) | 2004-08-17 | 2007-03-28 | Hoffmann La Roche | Hidantoinas sustituidas. |
US20060211603A1 (en) | 2004-08-18 | 2006-09-21 | Vicuron Pharmaceuticals Inc. | Ramoplanin derivatives possessing antibacterial activity |
EP1627876A1 (en) | 2004-08-20 | 2006-02-22 | Ferring B.V. | Heterocyclic condensed compounds useful as antidiuretic agents |
EP1637529A1 (en) | 2004-09-20 | 2006-03-22 | 4Sc Ag | Novel piperidin-4-yl-thiazole-carboxamide analogues as inhibitors of T-cell proliferation and uses thereof |
RU2394818C2 (ru) | 2004-12-13 | 2010-07-20 | Лео Фарма А/С | Триазолзамещенные аминобензофеноновые соединения |
CN101137412B (zh) | 2005-01-13 | 2012-11-07 | 布里斯托尔-迈尔斯·斯奎布公司 | 用作凝血因子XIa抑制剂的取代的二芳基化合物 |
CA2594860A1 (en) | 2005-01-14 | 2006-07-20 | Millennium Pharmaceuticals, Inc. | Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity |
EP2354140A1 (en) | 2005-05-20 | 2011-08-10 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
EP1926487A2 (en) | 2005-07-19 | 2008-06-04 | University of Tennessee Research Foundation | Thiazolidinone amides, thiazolidine carboxylic acid amides, and serine amides, including polyamine conjugates thereof, as selective anti-cancer agents |
KR20080031038A (ko) | 2005-07-29 | 2008-04-07 | 4에스체 악티엔게젤샤프트 | 신규의 헤테로환 NF-κB 억제제 |
CA2625974A1 (en) | 2005-10-14 | 2007-04-19 | Neurosearch A/S | Imidazole derivatives for the treatment of anxiety and related diseases |
PT1954684E (pt) | 2005-11-15 | 2014-07-17 | Otsuka Pharma Co Ltd | Composto e composição farmacêutica de oxazol |
BRPI0710479A2 (pt) | 2006-01-18 | 2012-08-14 | Hoffmann La Roche | composto, processo para sua preparaÇço, composiÇço farmacÊutica, uso de um composto e mÉtodo de tratamento de doenÇa ou desosrdem metabàlica. |
EP1832585A1 (en) | 2006-03-10 | 2007-09-12 | ORIDIS BIOMED Forschungs- und Entwicklungs GmbH | Thiazole-piperidine derivatives for treatment of hyperproliferative diseases |
EP1834954A1 (en) | 2006-03-15 | 2007-09-19 | 4Sc Ag | Thiazoles as NF-kB Inhibitors (proteasome inhibitors) |
WO2007115805A2 (en) | 2006-04-05 | 2007-10-18 | European Molecular Biology Laboratory (Embl) | Aurora kinase inhibitors |
WO2007146230A2 (en) | 2006-06-14 | 2007-12-21 | Merck & Co., Inc. | Non-nucleoside reverse transcriptase inhibitors |
JP5329402B2 (ja) | 2006-07-13 | 2013-10-30 | バイエル・クロップサイエンス・アーゲー | 殺菌剤ヒドロキシモイル−テトラゾール誘導体 |
PE20080948A1 (es) | 2006-07-25 | 2008-09-10 | Irm Llc | Derivados de imidazol como moduladores de la senda de hedgehog |
JP5406716B2 (ja) | 2006-08-07 | 2014-02-05 | アイアンウッド ファーマシューティカルズ インコーポレイテッド | インドール化合物 |
PL2050749T3 (pl) | 2006-08-08 | 2018-03-30 | Chugai Seiyaku Kabushiki Kaisha | Pochodna pirymidyny jako inhibitor pi3k i jej zastosowanie |
WO2008023720A1 (fr) | 2006-08-23 | 2008-02-28 | Astellas Pharma Inc. | COMPOSÉ D'URÉE OU SEL DUDIT COMPOSé |
WO2008030448A1 (en) | 2006-09-07 | 2008-03-13 | Millennium Pharmaceuticals, Inc. | Phenethylamide derivatives with kinase inhibitory activity |
KR100932093B1 (ko) | 2006-09-27 | 2009-12-16 | 주식회사종근당 | 미세소관 형성 저해제로서 유용한 벤조페논 유도체 |
WO2008079277A1 (en) | 2006-12-22 | 2008-07-03 | Millennium Pharmaceuticals, Inc. | Certain pyrazoline derivatives with kinase inhibitory activity |
WO2008128179A1 (en) | 2007-04-14 | 2008-10-23 | The University Of Tennessee Research Foundation | Thiazolidinone amides, thiazolidine carboxylic acid amides, and serine amides, including polyamine conjugates thereof, as selective anti-cancer agents |
US20090142832A1 (en) | 2007-11-29 | 2009-06-04 | James Dalton | Indoles, Derivatives, and Analogs Thereof and Uses Therefor |
US8389567B2 (en) | 2007-12-12 | 2013-03-05 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
PT2959900T (pt) * | 2008-06-16 | 2017-06-22 | Univ Tennessee Res Found | Composto para tratamento do cancro |
US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
KR101134194B1 (ko) | 2009-12-03 | 2012-04-09 | 서울대학교산학협력단 | 헤테로바이아릴피리딘 유도체 화합물의 제조방법 및 이러한 방법에 의해 제조된 헤테로바이아릴피리딘 유도체 화합물 |
CN102883607B (zh) | 2010-03-01 | 2015-07-22 | Gtx公司 | 用于治疗癌的化合物 |
WO2012027716A1 (en) | 2010-08-27 | 2012-03-01 | Collabrx, Inc. | Method to treat melanoma in braf inhibitor-resistant subjects |
CN103596957B (zh) | 2011-04-07 | 2016-12-07 | 拜耳知识产权有限责任公司 | 作为akt激酶抑制剂的咪唑并哒嗪 |
-
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