JP2011524355A5 - - Google Patents
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- JP2011524355A5 JP2011524355A5 JP2011513603A JP2011513603A JP2011524355A5 JP 2011524355 A5 JP2011524355 A5 JP 2011524355A5 JP 2011513603 A JP2011513603 A JP 2011513603A JP 2011513603 A JP2011513603 A JP 2011513603A JP 2011524355 A5 JP2011524355 A5 JP 2011524355A5
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- JP
- Japan
- Prior art keywords
- chr
- substituted
- cancer
- alkyl
- 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.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 40
- 229910052739 hydrogen Inorganic materials 0.000 claims 27
- 229910052801 chlorine Inorganic materials 0.000 claims 23
- 125000002837 carbocyclic group Chemical group 0.000 claims 21
- 229910052731 fluorine Inorganic materials 0.000 claims 21
- 206010028980 Neoplasm Diseases 0.000 claims 19
- 229910052794 bromium Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 17
- 150000002431 hydrogen Chemical class 0.000 claims 16
- 201000011510 cancer Diseases 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 11
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 10
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 7
- 239000003112 inhibitor Substances 0.000 claims 7
- -1 substituted —O Chemical class 0.000 claims 7
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000006545 (C1-C9) alkyl group Chemical group 0.000 claims 4
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 4
- 206010033128 Ovarian cancer Diseases 0.000 claims 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 4
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 4
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 4
- 201000010881 cervical cancer Diseases 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 230000001684 chronic effect Effects 0.000 claims 4
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- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 3
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- 108010000817 Leuprolide Proteins 0.000 claims 2
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- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
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- 201000005746 Pituitary adenoma Diseases 0.000 claims 2
- 206010061538 Pituitary tumour benign Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
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- 208000000277 Splenic Neoplasms Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 210000001744 T-lymphocyte Anatomy 0.000 claims 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 2
- 206010057644 Testis cancer Diseases 0.000 claims 2
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 208000023915 Ureteral Neoplasms Diseases 0.000 claims 2
- 206010046392 Ureteric cancer Diseases 0.000 claims 2
- 206010046431 Urethral cancer Diseases 0.000 claims 2
- 206010046458 Urethral neoplasms Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 2
- 201000005969 Uveal melanoma Diseases 0.000 claims 2
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 2
- 201000005188 adrenal gland cancer Diseases 0.000 claims 2
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 2
- 210000003719 b-lymphocyte Anatomy 0.000 claims 2
- 210000000013 bile duct Anatomy 0.000 claims 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 201000007455 central nervous system cancer Diseases 0.000 claims 2
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- 208000029742 colonic neoplasm Diseases 0.000 claims 2
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- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 239000002254 cytotoxic agent Substances 0.000 claims 2
- 210000001198 duodenum Anatomy 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 201000003444 follicular lymphoma Diseases 0.000 claims 2
- 201000010175 gallbladder cancer Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 230000002496 gastric effect Effects 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 210000002751 lymph Anatomy 0.000 claims 2
- 208000003747 lymphoid leukemia Diseases 0.000 claims 2
- 230000036210 malignancy Effects 0.000 claims 2
- 208000029559 malignant endocrine neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 208000026045 malignant tumor of parathyroid gland Diseases 0.000 claims 2
- KKZJGLLVHKMTCM-UHFFFAOYSA-N mitoxantrone Chemical compound O=C1C2=C(O)C=CC(O)=C2C(=O)C2=C1C(NCCNCCO)=CC=C2NCCNCCO KKZJGLLVHKMTCM-UHFFFAOYSA-N 0.000 claims 2
- 229960001156 mitoxantrone Drugs 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 201000002575 ocular melanoma Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 208000021310 pituitary gland adenoma Diseases 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 208000016800 primary central nervous system lymphoma Diseases 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 206010038038 rectal cancer Diseases 0.000 claims 2
- 201000001275 rectum cancer Diseases 0.000 claims 2
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 201000003708 skin melanoma Diseases 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 201000002314 small intestine cancer Diseases 0.000 claims 2
- 201000002471 spleen cancer Diseases 0.000 claims 2
- 210000002784 stomach Anatomy 0.000 claims 2
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- 210000001215 vagina Anatomy 0.000 claims 2
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- YJGVMLPVUAXIQN-LGWHJFRWSA-N (5s,5ar,8ar,9r)-5-hydroxy-9-(3,4,5-trimethoxyphenyl)-5a,6,8a,9-tetrahydro-5h-[2]benzofuro[5,6-f][1,3]benzodioxol-8-one Chemical compound COC1=C(OC)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O)[C@@H]3[C@@H]2C(OC3)=O)=C1 YJGVMLPVUAXIQN-LGWHJFRWSA-N 0.000 claims 1
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims 1
- LKJPYSCBVHEWIU-KRWDZBQOSA-N (R)-bicalutamide Chemical compound C([C@@](O)(C)C(=O)NC=1C=C(C(C#N)=CC=1)C(F)(F)F)S(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-KRWDZBQOSA-N 0.000 claims 1
- 102100025573 1-alkyl-2-acetylglycerophosphocholine esterase Human genes 0.000 claims 1
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 claims 1
- GCKMFJBGXUYNAG-UHFFFAOYSA-N 17alpha-methyltestosterone Natural products C1CC2=CC(=O)CCC2(C)C2C1C1CCC(C)(O)C1(C)CC2 GCKMFJBGXUYNAG-UHFFFAOYSA-N 0.000 claims 1
- SXFWKZNLYYRHMK-UHFFFAOYSA-N 1h-indolo[7,6-f]quinoline Chemical class C1=CC=C2C3=C(NC=C4)C4=CC=C3C=CC2=N1 SXFWKZNLYYRHMK-UHFFFAOYSA-N 0.000 claims 1
- HXHAJRMTJXHJJZ-UHFFFAOYSA-N 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-(4-pyrrolidin-1-ylbutylcarbamoylamino)-1,2-thiazole-4-carboxamide Chemical compound S1N=C(OCC=2C(=CC(Br)=CC=2F)F)C(C(=O)N)=C1NC(=O)NCCCCN1CCCC1 HXHAJRMTJXHJJZ-UHFFFAOYSA-N 0.000 claims 1
- VVIAGPKUTFNRDU-UHFFFAOYSA-N 6S-folinic acid Natural products C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-UHFFFAOYSA-N 0.000 claims 1
- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims 1
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- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims 1
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- 102100031480 Dual specificity mitogen-activated protein kinase kinase 1 Human genes 0.000 claims 1
- 101710146526 Dual specificity mitogen-activated protein kinase kinase 1 Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
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- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical group OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims 1
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| US9127259B2 (en) | 2008-03-31 | 2015-09-08 | Pacific Biosciences Of California, Inc. | Enzymes resistant to photodamage |
| US10195213B2 (en) | 2015-03-13 | 2019-02-05 | Unity Biotechnology, Inc. | Chemical entities that kill senescent cells for use in treating age-related disease |
| SI3788042T1 (sl) | 2018-04-29 | 2025-06-30 | Beigene Switzerland Gmbh | Zaviralci BCL-2 |
| WO2021083135A1 (en) | 2019-10-28 | 2021-05-06 | Beigene, Ltd. | Bcl-2 INHIBITORS |
| JP7839962B2 (ja) | 2020-04-15 | 2026-04-03 | ビーワン メディシンズ ワン ゲーエムベーハー | Ｂｃｌ－２阻害剤 |
| WO2023102378A1 (en) | 2021-11-30 | 2023-06-08 | Kura Oncology, Inc. | Macrocyclic compounds having farnesyltransferase inhibitory activity |
| US20260007685A1 (en) * | 2022-07-15 | 2026-01-08 | Berrybio (Hong Kong) Limited | Anti-apoptotic bcl-2 family protein degraders, pharmaceutical compositions, and therapeutic applications |
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| DE2724073A1 (de) | 1976-06-03 | 1977-12-22 | Fujisawa Pharmaceutical Co | 3,7-disubstituierte 3-cephem-4- carbonsaeuren und sie enthaltende pharmazeutische zubereitungen |
| US6720338B2 (en) | 2000-09-20 | 2004-04-13 | Abbott Laboratories | N-acylsulfonamide apoptosis promoters |
| US6727264B1 (en) | 2001-07-05 | 2004-04-27 | Synaptic Pharmaceutical Corporation | Substituted anilinic piperidines as MCH selective antagonists |
| US7199135B2 (en) | 2001-07-05 | 2007-04-03 | H. Lundbeck A/S | Substituted alkyl amido piperidines |
| JPWO2004026292A1 (ja) | 2002-09-20 | 2006-01-12 | 株式会社ツムラ | 鎮咳薬 |
| US7319111B2 (en) | 2003-02-20 | 2008-01-15 | Encysive Pharmaceuticals, Inc. | Phenylenediamine Urotensin-II receptor antagonists and CCR-9 antagonists |
| WO2005049593A2 (en) | 2003-11-13 | 2005-06-02 | Abbott Laboratories | N-acylsulfonamide apoptosis promoters |
| EP1888550B1 (en) | 2005-05-12 | 2014-06-25 | AbbVie Bahamas Ltd. | Apoptosis promoters |
| US8101799B2 (en) * | 2005-07-21 | 2012-01-24 | Ardea Biosciences | Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK |
| WO2007076055A2 (en) * | 2005-12-22 | 2007-07-05 | Entremed, Inc. | Compositions and methods comprising proteinase activated receptor antagonists |
| KR100843351B1 (ko) | 2007-01-30 | 2008-07-03 | 한국과학기술연구원 | 중추신경계 질환 치료제로 유효한ｎ-벤질-ｎ-(2-디메틸아미노-에틸)-벤젠술폰아미드 화합물 |
| WO2008129288A2 (en) * | 2007-04-19 | 2008-10-30 | Boehringer Ingelheim International Gmbh | Disulfonamides useful in the treatment of inflammation |
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