JP2009513703A5 - - Google Patents
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- JP2009513703A5 JP2009513703A5 JP2008538935A JP2008538935A JP2009513703A5 JP 2009513703 A5 JP2009513703 A5 JP 2009513703A5 JP 2008538935 A JP2008538935 A JP 2008538935A JP 2008538935 A JP2008538935 A JP 2008538935A JP 2009513703 A5 JP2009513703 A5 JP 2009513703A5
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- 125000000217 alkyl group Chemical group 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 25
- 201000010099 disease Diseases 0.000 claims 24
- 239000008194 pharmaceutical composition Substances 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 16
- 239000011780 sodium chloride Substances 0.000 claims 16
- 150000001204 N-oxides Chemical class 0.000 claims 13
- -1 hydrate Substances 0.000 claims 13
- 239000012453 solvate Substances 0.000 claims 13
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 claims 12
- 229910052799 carbon Inorganic materials 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 206010028576 Myeloproliferative disease Diseases 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 206010024324 Leukaemias Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004103 aminoalkyl group Chemical group 0.000 claims 5
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 5
- 210000001185 Bone Marrow Anatomy 0.000 claims 4
- 108091000081 Phosphotransferases Proteins 0.000 claims 4
- 102000001253 Protein Kinases Human genes 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 230000002496 gastric Effects 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 102100019516 JAK2 Human genes 0.000 claims 3
- 101700016050 JAK2 Proteins 0.000 claims 3
- 208000008456 Leukemia, Myelogenous, Chronic, BCR-ABL Positive Diseases 0.000 claims 3
- 201000006934 chronic myeloid leukemia Diseases 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010005949 Bone cancer Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000002047 Essential Thrombocythemia Diseases 0.000 claims 2
- 208000009745 Eye Disease Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 102000036507 JAK family Human genes 0.000 claims 2
- 108091020259 JAK family Proteins 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010025310 Other lymphomas Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 208000008696 Polycythemia Vera Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 206010047461 Viral infection Diseases 0.000 claims 2
- 208000001756 Virus Disease Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 201000005216 brain cancer Diseases 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 201000002077 muscle cancer Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- 201000004681 psoriasis Diseases 0.000 claims 2
- 201000007196 sexual disease Diseases 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 230000017613 viral reproduction Effects 0.000 claims 2
- 206010000880 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000007046 Leukemia, Myeloid, Acute Diseases 0.000 claims 1
- 208000003476 Primary Myelofibrosis Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 230000003110 anti-inflammatory Effects 0.000 claims 1
- 102000004965 antibodies Human genes 0.000 claims 1
- 108090001123 antibodies Proteins 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940045988 antineoplastic drugs Protein kinase inhibitors Drugs 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
- 230000004927 fusion Effects 0.000 claims 1
- 125000005842 heteroatoms Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 230000002584 immunomodulator Effects 0.000 claims 1
- 229940121354 immunomodulators Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 201000002674 obstructive nephropathy Diseases 0.000 claims 1
- 125000005254 oxyacyl group Chemical group 0.000 claims 1
- 229920000728 polyester Polymers 0.000 claims 1
- 201000007914 proliferative diabetic retinopathy Diseases 0.000 claims 1
- 239000003909 protein kinase inhibitor Substances 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229960001663 sulfanilamide Drugs 0.000 claims 1
- 125000000565 sulfonamide group Chemical group 0.000 claims 1
- 230000001225 therapeutic Effects 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
Claims (47)
- 構造(A)を有する化合物、または、化合物(A)の薬学的に許容できる塩、水和物、溶媒和物、結晶形、N−酸化物、もしくは個々のジアステレオマー:
式中、
Xは、結合、O、およびCH2からなる群より選択され;Yは、結合およびNR9からなる群より選択されるか;または、XおよびYは一緒に結合であり;
R1およびR2の各々は独立して、H、C1−C6非置換のアルキル、置換もしくは非置換のC 3 −C 8 シクロアルキル、置換もしくは非置換のC 3 −C 14 ヘテロ環、置換もしくは非置換のC 5 −C 14 アリール、および置換もしくは非置換のヘテロアリールからなる群より選択されるか;または、R1およびR2は一緒に結合であるか;または、R1およびR2は一緒に、(CH2)m、(CH2)r−S−(CH2)m、(CH2)r−SO−(CH2)m、(CH2)r−SO2−(CH2)m、(CH2)r−NR9−(CH2)m、および(CH2)r−O−(CH2)mからなる群より選択される部分を形成し;
p、q、r、n、mの各々は独立して、0〜6の間の値を有する整数であり;
R9は、H、C1−C6アルキル、C 3 −C6シクロアルキル、C 3 −C6分枝アルキル、C1−C6置換アルキル、C1−C6アミノアルキル、およびC1−C6ヒドロキシアルキルからなる群より選択され;
G0は、N、O、H、およびCHからなる群より選択され、
但し、G 0 がNである場合には;
R 3 およびR 4 の各々は独立して、H、C 1 −C 6 アルキル、C 1 −C 6 置換もしくは非置換のヒドロキシアルキルもしくはアミノアルキル、C 3 −C 6 置換もしくは非置換の分枝アルキル、置換もしくは非置換のC 5 −C 14 アリール、および置換もしくは非置換のC 5 −C 14 ヘテロアリールからなる群より選択されるか;または、R 3 およびR 4 は一緒に、(CH 2 ) m 、(CH 2 ) r −S−(CH 2 ) m 、(CH 2 ) r −SO−(CH 2 ) m 、(CH 2 ) r −SO 2 −(CH 2 ) m 、(CH 2 ) r −NR 9 −(CH 2 ) m 、および(CH 2 ) r −O−(CH 2 ) m からなる群より選択される部分を形成するか;または、R 3 およびR 4 はG 0 と一緒になって、芳香環、ヘテロ芳香環、環式もしくはヘテロ環式環システムを形成し;
さらに、G 0 がOである場合には;
R 3 は、H、C 1 −C 6 アルキル、C 1 −C 6 置換もしくは非置換のヒドロキシアルキルもしくはアミノアルキル、置換もしくは非置換の分枝C 3 −C 6 アルキル、置換もしくは非置換のC 3 −C 8 シクロアルキル、炭素もしくは窒素を介して結合した置換C 3 −C 14 ヘテロ環、置換もしくは非置換のC 5 −C 14 アリール、および炭素もしくは窒素を介して結合した置換もしくは非置換のC 5 −C 14 ヘテロアリールからなる群より選択され、基R 4 は存在せず;または、R 1 およびR 3 は一緒に、(CH 2 ) m 、(CH 2 ) r −S−(CH 2 ) m 、(CH 2 ) r −SO−(CH 2 ) m 、(CH 2 ) r −SO 2 −(CH 2 ) m 、(CH 2 ) r −NR 9 −(CH 2 ) m 、および(CH 2 ) r −O−(CH 2 ) m からなる群より選択される部分を形成し;
さらに、G 0 =CHである場合には;
R 3 およびR 4 の各々は独立して、H、C 1 −C 6 アルキル、C 1 −C 6 置換もしくは非置換のヒドロキシアルキルもしくはアミノアルキル、置換もしくは非置換のC 3 −C 6 分枝アルキル、置換もしくは非置換のC 5 −C 14 アリール、炭素もしくは窒素を介して結合した置換もしくは非置換のC 3 −C 14 ヘテロ環、および炭素もしくは窒素を介して結合した置換もしくは非置換のC 5 −C 14 ヘテロアリールからなる群より選択されるか;または、R 3 およびR 4 は一緒に、(CHR 9 ) r −(CHR 9 ) m −(CHR 9 ) p 、(CHR 9 ) r −S−(CHR 9 ) m 、(CHR 9 ) r −SO−(CHR 9 ) m 、(CHR 9 ) r −SO 2 −(CHR 9 ) m 、(CHR 9 ) r −NR 9 −(CHR 9 ) m 、および(CHR 9 ) r −O−(CHR 9 ) m からなる群より選択される部分を形成し;
2個を超えない基GがNであることができるという条件で、各Gは独立して、NもしくはCR 6 であるか、またはXに結合する場合にCであり、かつ各R 6 は互いに他の基R 6 から独立しており;
R5は、メチルであり;
であり、R6 、R7 、R 8 の各々は独立して、H、C 2 −C6置換もしくは非置換のアルケニル、C 2 −C6置換もしくは非置換のアルキニル、C1−C6 置換もしくは非置換のヒドロキシアルキルもしくはアミノアルキル、C 3 −C6置換もしくは非置換のシクロアルキル、置換もしくは非置換のC 5 −C 14 アリール、炭素もしくはヘテロ原子を介して結合した置換もしくは非置換のC 5 −C 14 ヘテロアリール、ハロゲン、CF3、−OCF3、SO2H、SO2(C1−C6アルキル)、SO2−ヘテロ環、SO2−シクロアルキル、SO2N(C1−C6アルキル)H、SO2N(C1−C6アルキル)(C1−C6アルキル)、SO2NH(C 3 −C6シクロアルキル)、SO2NH−ヘテロ環、SO2N(C 3 −C6分枝アルキル)H、NH2、NH(C 1 −C 6 アルキル)、N(C 1 −C 6 アルキル)(C 1 −C 6 アルキル)、NO2、CN、CONH2、CONH(C 1 −C 6 アルキル)、CON(C 1 −C 6 アルキル)(C 1 −C 6 アルキル)、CO−(C1−C6アルキル)、CO−ヘテロ環、COOH、COO−(C1−C6アルキル)、NHCO−(C1−C6アルキル)、およびNHCONH−アリールからなる群より選択されるか;または、R 6 およびR 7 は一緒に、もしくはR 7 およびR 8 は一緒に、もしくはR 6 およびR 8 は一緒に、−HN−CH=CH−、−HN−N=CH−、−HN−N=N−、−O(CH 2 ) n O−、−S(CH 2 ) n S−、−N=CH−S−、−CH=N−O−、−CH=N−S−、−N=CH−O−、−C=N−O−、−CH=CH−CH=CH−、−N=CH−CH=CH−、−CH=N−CH=CH−、−O−CH=CH、および−S−CH=CH−からなる群より独立して選択される部分を形成し;
Aは、O、NH、N−(C1−C6アルキル)、CH2、S、SO、およびSO2からなる群より選択され;
G1は、CH、およびNからなる群より選択され;
G2は、CR7、およびNからなる群より選択され、各基R7は、他のどの基R7からも独立し;
置換されたアルキル、アルケニル、アルキニル、シクロアルキル、アリール、ヘテロアリール、またはヘテロ環は、存在する場合各存在について、ヒドロキシ、アルコキシ、メルカプト、シクロアルキル、ヘテロ環、アリール、ハロゲン、シアノ、ニトロ、アミノ、アミド、アルデヒド、アシル、オキシアシル、カルボキシル、スルホニル、スルホンアミド、またはスルフリルからなる群より選択される1個または複数の置換基を有する。 - 請求項1〜3のいずれか1項記載の化合物の少なくとも1つ、またはそのN−酸化物、またはその薬学的に許容できる塩、水和物、溶媒和物、結晶形、もしくは個々のジアステレオマー、およびそのための薬学的に許容できる担体を含有する、医薬組成物。
- XがOである、請求項1記載の化合物。
- G0がNである、請求項1記載の化合物。
- G0がNである、請求項5記載の化合物。
- Yが結合であり、R1およびR2がそれぞれHである、請求項7記載の化合物。
- R3およびR4がG 0 と一緒にヘテロ環式環を形成する、請求項7または8記載の化合物。
- R 3 およびR 4 の各々がHである、請求項7または8記載の化合物。
- Xが結合であり、Yが結合であり、p、q、およびnの各々が0であり、かつR 3 およびR 4 がG 0 と一緒にヘテロ環式環を形成する、請求項6記載の化合物。
- G 1 およびG 2 の各々がCHであり、かつR 7 がSO 2 NH−(C 3 −C 6 分枝アルキル)である、請求項9記載の化合物。
- G 1 およびG 2 の各々がCHであり、かつR 7 がSO 2 NH−(C 3 −C 6 分枝アルキル)である、請求項11記載の化合物。
- 請求項14記載の化合物、またはその薬学的に許容できる塩、水和物、溶媒和物、結晶形、N−酸化物、もしくは個々のジアステレオマー、および薬学的に許容できる担体を含む、医薬組成物。
- 請求項15記載の化合物、またはその薬学的に許容できる塩、水和物、溶媒和物、結晶形、N−酸化物、もしくは個々のジアステレオマー、および薬学的に許容できる担体を含む、医薬組成物。
- 請求項1〜3、5〜15、および18のいずれか一項記載の化合物の少なくとも1つ、またはそのN−酸化物、またはその薬学的に許容できる塩、水和物、溶媒和物、結晶形の塩、もしくは個々のジアステレオマー、および薬学的に許容できる担体の組合せを組み合わせることを含む、医薬組成物を製造する方法。
- 治療的有効量の請求項1〜3、5〜15、および18のいずれか一項記載の化合物、またはその薬学的に許容できる塩、水和物、溶媒和物、結晶形、N−酸化物、もしくは個々のジアステレオマーを含む、JAK2ファミリーキナーゼに関連している障害を治療するための医薬組成物。
- 障害が、血管新生関連障害である、請求項20記載の医薬組成物。
- 障害が、骨髄増殖性障害、癌、眼疾患、炎症、乾癬、またはウイルス感染症である、請求項20記載の医薬組成物。
- 障害が、増殖性糖尿病性網膜症である、請求項20記載の医薬組成物。
- 障害が、任意の骨髄関連障害である、請求項20記載の医薬組成物。
- 障害が、骨髄増殖性障害である、請求項20記載の医薬組成物。
- 骨髄増殖性障害が、キナーゼの変異に起因して生じる、請求項25記載の医薬組成物。
- 骨髄増殖性障害が、JAKファミリーキナーゼ経路の機能獲得に起因して生じる、請求項25記載の医薬組成物。
- 骨髄増殖性障害が、JAKファミリーキナーゼ経路の機能獲得に起因した遺伝子またはタンパク質の融合の結果として生じる、請求項25記載の医薬組成物。
- 障害が、真性赤血球増加症である、請求項20記載の医薬組成物。
- 障害が、本態性血小板血症である、請求項20記載の医薬組成物。
- 障害が、骨髄様化生を伴う骨髄線維症である、請求項20記載の医薬組成物。
- 障害が、消化管/胃腸管の癌、結腸癌、肝癌、皮膚癌、乳癌、卵巣癌、前立腺癌、リンパ腫、白血病、腎癌、肺癌、筋肉の癌、骨癌、膀胱癌、および脳の癌からなる群より選択される癌である、請求項20記載の医薬組成物。
- 障害が白血病である、請求項20記載の医薬組成物。
- 白血病が急性骨髄性白血病である、請求項33記載の医薬組成物。
- 白血病が慢性骨髄性白血病(CML)である、請求項33記載の医薬組成物。
- 慢性骨髄性白血病が、現在の治療に対し耐性を示す、請求項35記載の医薬組成物。
- 治療的有効量の請求項14記載の化合物、またはその薬学的に許容できる塩、水和物、溶媒和物、結晶形、N−酸化物、もしくは個々のジアステレオマーを含む、患者において骨髄増殖性障害を治療するための医薬組成物。
- 治療的有効量の請求項15記載の化合物、またはその薬学的に許容できる塩、水和物、溶媒和物、結晶形、N−酸化物、もしくは個々のジアステレオマーを含む、患者において骨髄増殖性障害を治療するための医薬組成物。
- 治療的有効量の請求項1〜3、5〜15および18のいずれか一項記載の化合物の少なくとも1つ、またはそのN−酸化物、またはそれらの薬学的に許容できる塩、水和物、溶媒和物、結晶形、もしくは個々のジアステレオマーを、抗炎症薬、化学療法薬、免疫調節薬、治療的抗体、またはプロテインキナーゼ阻害剤と組み合わせて含む、治療が必要な患者においてJAK2ファミリーキナーゼに関連している障害を治療するための医薬組成物。
- JAK2ファミリーキナーゼに関連している障害を治療するための医薬の製造における、治療的有効量の請求項1〜3、5〜15および18のいずれか一項記載の化合物の少なくとも1つ、またはその薬学的に許容できる塩、水和物、溶媒和物、結晶形、N−酸化物もしくは個々のジアステレオマーの使用。
- 障害が、骨髄増殖性障害、癌、眼疾患、炎症、乾癬、またはウイルス感染症である、請求項40記載の使用。
- 障害が、任意の骨髄関連障害である、請求項40記載の使用。
- 障害が、骨髄増殖性障害である、請求項40記載の使用。
- 障害が、真性赤血球増加症である、請求項40記載の使用。
- 障害が、本態性血小板血症である、請求項40記載の使用。
- 障害が、消化管/胃腸管の癌、結腸癌、肝癌、皮膚癌、乳癌、卵巣癌、前立腺癌、リンパ腫、白血病、腎癌、肺癌、筋肉の癌、骨癌、膀胱癌、および脳の癌からなる群より選択される癌である、請求項40記載の使用。
- 障害が白血病である、請求項40記載の使用。
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