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
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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) | EP2542081A4 (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 |
RU2514427C2 (ru) | 2008-06-16 | 2014-04-27 | Юниверсити Оф Теннесси Рисёч Фаундейшн | Соединения для лечения рака |
US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
AU2010347233B2 (en) | 2010-03-01 | 2015-06-18 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
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 |
ES2858351T3 (es) | 2010-04-22 | 2021-09-30 | Vertex Pharma | Compuesto intermedio para proceso de producción de compuestos de cicloalquilcaraboxamido-indol |
JP5997156B2 (ja) | 2010-08-24 | 2016-09-28 | ジーティーエックス・インコーポレイテッド | 癌の治療のための化合物 |
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 |
EP2642998B1 (en) | 2010-11-24 | 2020-09-16 | 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 |
US9290500B2 (en) | 2012-02-17 | 2016-03-22 | Millennium Pharmaceuticals, Inc. | Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
TW201341367A (zh) | 2012-03-16 | 2013-10-16 | Axikin Pharmaceuticals Inc | 3,5-二胺基吡唑激酶抑制劑 |
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 |
AU2013259624B2 (en) | 2012-05-08 | 2017-10-19 | Lycera Corporation | Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of RORy and the treatment of disease |
KR20150007300A (ko) | 2012-05-08 | 2015-01-20 | 머크 샤프 앤드 돔 코포레이션 | Ror감마 활성의 억제를 위한 테트라히드로나프티리딘 및 관련 비시클릭 화합물 및 질환의 치료 |
UA117913C2 (uk) | 2012-05-31 | 2018-10-25 | Фінекс Фармас'Ютікалс Аг | КАРБОКСАМІД- АБО СУЛЬФОНАМІДЗАМІЩЕНІ ТІАЗОЛИ ТА СПОРІДНЕНІ ПОХІДНІ ЯК МОДУЛЯТОРИ ОРФАНОВОГО ЯДЕРНОГО РЕЦЕПТОРА RORγ |
JP2015525223A (ja) | 2012-06-14 | 2015-09-03 | ビーエーエスエフ ソシエタス・ヨーロピアBasf Se | 動物有害生物を駆除するための置換3−ピリジルチアゾール化合物および誘導体を使用する有害生物防除方法 |
GB201216018D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Pharmacologically active compounds |
GB201216017D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Inhibitor compounds |
US9139583B2 (en) | 2013-02-01 | 2015-09-22 | Acetylon Pharmaceuticals, Inc. | Selective HDAC3 inhibitors |
US9096549B2 (en) | 2013-02-01 | 2015-08-04 | Acetylon Pharmaceuticals, Inc. | Selective HDAC3 inhibitors |
RU2708247C2 (ru) | 2013-03-05 | 2019-12-05 | Юниверсити Оф Теннесси Рисерч Фаундейшн | Соединение для лечения рака |
WO2014151959A1 (en) | 2013-03-14 | 2014-09-25 | The Trustees Of Columbia University In The City Of New York | N-alkyl-2-phenoxyethanamines, their preparation and use |
ES2705247T3 (es) | 2013-03-14 | 2019-03-22 | Univ Columbia | 4-fenilpiperidinas, su preparación y uso |
ES2700541T3 (es) | 2013-03-14 | 2019-02-18 | Univ Columbia | Octahidrociclopentapirroles, su preparación y uso |
US9944644B2 (en) | 2013-03-14 | 2018-04-17 | The Trustees Of Columbia University In The City Of New York | Octahydropyrrolopyrroles their preparation and use |
EA032577B1 (ru) | 2013-07-02 | 2019-06-28 | Милленниум Фармасьютикалз, Инк. | Гетероарильные соединения, пригодные в качестве ингибиторов sumo-активирующего фермента |
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 |
CN106414432B (zh) | 2013-10-14 | 2019-06-14 | 卫材R&D管理有限公司 | 选择性取代的喹啉化合物 |
RU2671496C2 (ru) | 2013-10-14 | 2018-11-01 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Производные 5-пиперидин-8-цианохинолина |
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 |
US9809561B2 (en) | 2013-12-20 | 2017-11-07 | Merck Sharp & Dohme Corp. | Tetrahydronaphthyridine, benzoxazine, aza-benzoxazine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease |
WO2015095792A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Carbamate benzoxaxine propionic acids and acid derivatives for modulation 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 |
JP2017507950A (ja) | 2014-02-27 | 2017-03-23 | リセラ・コーポレイションLycera Corporation | レチノイン酸受容体関連オーファン受容体ガンマのアゴニストを使用する養子細胞療法及び関連治療方法 |
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 |
RU2744460C2 (ru) | 2014-04-15 | 2021-03-09 | Вертекс Фармасьютикалз Инкорпорейтед | Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости |
EP4036094A1 (en) | 2014-04-30 | 2022-08-03 | The Trustees of Columbia University in the City of New York | Substituted 4-phenylpiperidines, their preparation and use |
WO2015171558A2 (en) | 2014-05-05 | 2015-11-12 | Lycera Corporation | BENZENESULFONAMIDO AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORγ AND THE TREATEMENT OF DISEASE |
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 |
WO2015171628A1 (en) | 2014-05-06 | 2015-11-12 | Gtx, 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 |
UA122963C2 (uk) | 2014-07-01 | 2021-01-27 | Мілленніум Фармасьютікалз, Інк. | Гетероарильні сполуки, придатні як інгібітори sumo-активуючого ферменту |
MY191736A (en) | 2014-12-23 | 2022-07-13 | Axikin Pharmaceuticals Inc | 3,5-diaminopyrazole kinase inhibitors |
JP2018510135A (ja) | 2015-02-11 | 2018-04-12 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | RORγT阻害剤としての置換ピラゾール化合物及びその使用 |
CN107846898B (zh) * | 2015-05-01 | 2023-07-14 | 佐治亚州立大学研究基金会 | 用于管理低氧诱导因子相关病症的二苯基甲醇衍生物 |
EP3292119A4 (en) | 2015-05-05 | 2018-10-03 | Lycera Corporation | DIHYDRO-2H-BENZO[b][1,4]OXAZINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORy 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 |
CA3002850A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as rorgammat inhibitors and uses thereof |
AU2016344111A1 (en) | 2015-10-27 | 2018-05-10 | Merck Sharp & Dohme Corp. | Substituted bicyclic pyrazole compounds as RORgammaT inhibitors and uses thereof |
JP2018531958A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | RORγT阻害薬としてのヘテロアリール置換安息香酸及びその使用 |
EP3402780A1 (en) | 2016-01-14 | 2018-11-21 | Beth Israel Deaconess Medical Center, Inc. | Mast-cell modulators and uses thereof |
US10774064B2 (en) | 2016-06-02 | 2020-09-15 | Cadent Therapeutics, Inc. | Potassium channel modulators |
EP3730487B1 (en) | 2016-06-13 | 2022-04-27 | Gilead Sciences, Inc. | Azetidine derivatives as fxr (nr1h4) modulators |
CA2968836A1 (en) | 2016-06-13 | 2017-12-13 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
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 |
CN110099898B (zh) | 2016-10-24 | 2023-07-25 | 优曼尼蒂治疗公司 | 化合物及其用途 |
ES2906078T3 (es) | 2017-01-23 | 2022-04-13 | Cadent Therapeutics Inc | Moduladores del canal de potasio |
PT3600309T (pt) | 2017-03-28 | 2022-10-03 | Gilead Sciences Inc | Combinações terapêuticas para o tratamento de doenças hepáticas |
GB201709840D0 (en) | 2017-06-20 | 2017-08-02 | Inst Of Cancer Research: Royal Cancer Hospital | Methods and medical uses |
EP3645531A1 (en) | 2017-06-29 | 2020-05-06 | Bayer Aktiengesellschaft | Thiazole compounds useful as prmt5 inhibitors |
MA49566A (fr) | 2017-07-11 | 2020-05-20 | Vertex Pharma | Carboxamides utilisés en tant qu'inhibiteurs des canaux sodiques |
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 |
US11292791B2 (en) | 2017-09-15 | 2022-04-05 | Forma Therapeutics, Inc. | Tetrahydro-imidazo quinoline compositions as CBP/P300 inhibitors |
EP3700934A4 (en) | 2017-10-24 | 2021-10-27 | Yumanity Therapeutics, Inc. | COMPOUNDS AND USES OF THESE COMPOUNDS |
CA3078769A1 (en) | 2017-10-27 | 2019-05-02 | Boehringer Ingelheim International Gmbh | Pyridine carbonyl derivatives and therapeutic uses thereof as trpc6 inhibitors |
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 |
CN112437664A (zh) * | 2018-05-15 | 2021-03-02 | 田纳西大学研究基金会 | 用于治疗胰腺癌的化合物 |
AU2019270089B2 (en) * | 2018-05-15 | 2022-11-10 | University Of Tennessee Research Foundation | Compounds for treatment of triple negative breast cancer and ovarian cancer |
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 |
US10870648B2 (en) | 2018-06-29 | 2020-12-22 | Forma Therapeutics, Inc. | Inhibiting CREB binding protein (CBP) |
CA3113234A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Tri-substituted heteroaryl 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 |
US11993586B2 (en) | 2018-10-22 | 2024-05-28 | Novartis Ag | 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 |
SI3911647T1 (sl) | 2019-01-15 | 2024-04-30 | Gilead Sciences, Inc. | Izoksazolna spojina kot agonist FXR in farmacevtski sestavki, ki jo obsegajo |
CA3127791A1 (en) | 2019-01-24 | 2020-07-30 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
JP2022519906A (ja) | 2019-02-19 | 2022-03-25 | ギリアード サイエンシーズ, インコーポレイテッド | Fxrアゴニストの固体形態 |
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 |
AR120680A1 (es) | 2019-12-06 | 2022-03-09 | Vertex Pharma | Tetrahidrofuranos sustituidos como moduladores de canales de sodio |
KR102346187B1 (ko) * | 2019-12-26 | 2021-12-31 | 울산과학기술원 | 디히드로퓨란 유도체 및 이의 합성 방법 |
WO2021203100A1 (en) * | 2020-04-03 | 2021-10-07 | Veru Inc. | Methods of treating coronavirus |
US11801243B2 (en) | 2020-09-23 | 2023-10-31 | Forma Therapeutics, Inc. | Bromodomain inhibitors for androgen receptor-driven cancers |
US11795168B2 (en) | 2020-09-23 | 2023-10-24 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP) |
AR126073A1 (es) | 2021-06-04 | 2023-09-06 | Vertex Pharma | N-(hidroxialquil(hetero)aril)tetrahidrofuran 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 |
CN1092649C (zh) | 1994-12-15 | 2002-10-16 | 三共株式会社 | 噻唑烷酮化合物或以其作为有效成分的心绞痛治疗剂或预防剂 |
CA2214386C (en) | 1995-03-02 | 2001-12-04 | Sadao Ishihara | Optically active thiazolidinone derivatives |
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 |
EP1244617B1 (en) | 1999-12-27 | 2005-02-16 | Ortho-McNeil Pharmaceutical, Inc. | Substituted aminoalkylamide derivatives as antagonists of follicle stimulating hormone |
ES2288948T3 (es) | 2000-05-11 | 2008-02-01 | Consejo Superior De Investigaciones Cientificas | Inhibidores heterociclicos del glicogeno sintasa quinasa gsk-3. |
AU2002231139B2 (en) | 2000-12-21 | 2007-03-22 | Bristol-Myers Squibb Company | Thiazolyl inhibitors of tec family tyrosine kinases |
CA2443600A1 (en) | 2001-04-19 | 2002-10-31 | Vertex Pharmaceuticals Incorporated | Heterocyclyldicarbamides as caspase inhibitors |
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 |
WO2003027100A1 (en) | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | Substituted 3-pyridyl pyrimidines as c17,20 lyase inhibitors |
MXPA04002931A (es) | 2001-10-12 | 2005-04-11 | Bayer Pharmaceuticals Corp | Heterociclos que contienen nitrogeno de 5 miembros sustituidos con fenilo para el tratamiento de la obesidad. |
JP2005513026A (ja) | 2001-11-15 | 2005-05-12 | インサイト サン ディエゴ インコーポレイテッド | 高コレステロール血症、異脂肪血症および他の代謝障害;癌、および他の疾患を治療するn−置換複素環 |
CN1633420A (zh) | 2002-04-08 | 2005-06-29 | 托伦脱药品有限公司 | 噻唑烷-4-腈和类似物以及它们作为二肽基-肽酶抑制剂的用途 |
WO2003090680A2 (en) | 2002-04-23 | 2003-11-06 | 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 |
MXPA05008309A (es) | 2003-02-10 | 2005-09-20 | Amgen Inc | Ligandos de receptor vaniloide y su uso en tratamientos. |
EP1594847A2 (en) | 2003-02-12 | 2005-11-16 | Transtech Pharma, Inc. | Substituted azole derivatives as therapeutic agents |
PL378919A1 (pl) | 2003-04-10 | 2006-06-12 | Avanir Pharmaceuticals | Pochodne imidazolu do leczenia zaburzeń alergicznych i nadmiernego rozrostu |
WO2004103959A2 (en) | 2003-05-16 | 2004-12-02 | Ambit Biosciences Corporation | Heterocyclic compounds and uses thereof |
ZA200510137B (en) | 2003-07-24 | 2007-04-25 | Leo Pharma As | Novel aminobenzophenone compounds |
US7501538B2 (en) | 2003-08-08 | 2009-03-10 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions and methods of use |
US20060014740A1 (en) | 2003-11-18 | 2006-01-19 | Miller Duane D | Analogs exhibiting inhibition of cell proliferation, methods of making, and uses thereof |
JP2007513090A (ja) | 2003-11-18 | 2007-05-24 | 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 | チアゾリジノンアミド、チアゾリジンカルボン酸アミド、その製造方法、およびその使用方法 |
BRPI0417543A (pt) | 2003-12-12 | 2007-03-27 | Wyeth Corp | quinolinas úteis no tratamento de doença cardiovascular |
US7326732B2 (en) | 2004-02-12 | 2008-02-05 | Pharmagene Laboratories Limited | EP2 receptor agonists |
AU2005221138A1 (en) | 2004-03-08 | 2005-09-22 | Wyeth | Ion channel modulators |
CA2565965A1 (en) | 2004-05-06 | 2006-07-27 | Plexxikon, Inc. | Pde4b inhibitors and uses therefor |
CA2584493A1 (en) | 2004-06-18 | 2006-01-05 | Gpc Biotech, Inc. | Kinase inhibitors for treating cancers |
PL1781649T3 (pl) | 2004-08-17 | 2009-01-30 | Hoffmann La Roche | Podstawione hydantoiny |
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 |
PT1828148E (pt) | 2004-12-13 | 2010-05-04 | Leo Pharma As | Compostos de amino benzofenona substituídos por triazol |
WO2006076575A2 (en) | 2005-01-13 | 2006-07-20 | Bristol-Myers Squibb Company | Substituted biaryl compounds as factor xia inhibitors |
JP2008527007A (ja) | 2005-01-14 | 2008-07-24 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | Raf−キナーゼ阻害活性を有するシンナミドおよびヒドロシンナミド誘導体 |
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 |
NZ565470A (en) | 2005-07-29 | 2010-11-26 | 4Sc Ag | Novel heterocyclic NF-kB inhibitors |
US8030339B2 (en) | 2005-10-14 | 2011-10-04 | Neurosearch A/S | Imidazole derivatives for the treatment of anxiety and related diseases |
JP5305914B2 (ja) | 2005-11-15 | 2013-10-02 | 大塚製薬株式会社 | オキサゾール化合物及び医薬組成物 |
CA2636826C (en) | 2006-01-18 | 2011-11-29 | F.Hoffmann-La Roche Ag | Thiazoles as 11 beta-hsd1 inhibitors |
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 |
AR061893A1 (es) | 2006-07-13 | 2008-10-01 | Bayer Cropscience Sa | Derivados de hidroximoil-tetrazoil fungicidas |
PE20080948A1 (es) | 2006-07-25 | 2008-09-10 | Irm Llc | Derivados de imidazol como moduladores de la senda de hedgehog |
AU2007281747B2 (en) | 2006-08-07 | 2013-11-07 | Ironwood Pharmaceuticals, Inc. | Indole compounds |
JP4450857B2 (ja) | 2006-08-08 | 2010-04-14 | 中外製薬株式会社 | Pi3k阻害剤としてのピリミジン誘導体およびその用途 |
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 |
JP2010513519A (ja) | 2006-12-22 | 2010-04-30 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | キナーゼインヒビター活性を有するある種のピラゾリン誘導体 |
US20080255213A1 (en) | 2007-04-14 | 2008-10-16 | 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 |
WO2009076454A2 (en) | 2007-12-12 | 2009-06-18 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
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 |
RU2514427C2 (ru) * | 2008-06-16 | 2014-04-27 | Юниверсити Оф Теннесси Рисёч Фаундейшн | Соединения для лечения рака |
KR101134194B1 (ko) | 2009-12-03 | 2012-04-09 | 서울대학교산학협력단 | 헤테로바이아릴피리딘 유도체 화합물의 제조방법 및 이러한 방법에 의해 제조된 헤테로바이아릴피리딘 유도체 화합물 |
AU2010347233B2 (en) | 2010-03-01 | 2015-06-18 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
WO2012027716A1 (en) | 2010-08-27 | 2012-03-01 | Collabrx, Inc. | Method to treat melanoma in braf inhibitor-resistant subjects |
EP2694510B1 (en) | 2011-04-07 | 2015-10-14 | Bayer Intellectual Property GmbH | Imidazopyridazines as akt kinase inhibitors |
-
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- 2010-12-29 AU AU2010347233A patent/AU2010347233B2/en not_active Ceased
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