JP2015520151A5 - - Google Patents
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- JP2015520151A5 JP2015520151A5 JP2015511669A JP2015511669A JP2015520151A5 JP 2015520151 A5 JP2015520151 A5 JP 2015520151A5 JP 2015511669 A JP2015511669 A JP 2015511669A JP 2015511669 A JP2015511669 A JP 2015511669A JP 2015520151 A5 JP2015520151 A5 JP 2015520151A5
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- 150000001875 compounds Chemical class 0.000 claims 30
- 206010048962 Brain oedema Diseases 0.000 claims 15
- 201000010099 disease Diseases 0.000 claims 12
- 206010021143 Hypoxia Diseases 0.000 claims 8
- 230000001146 hypoxic Effects 0.000 claims 8
- 206010030113 Oedema Diseases 0.000 claims 7
- 208000006752 Brain Edema Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 102000010637 Aquaporins Human genes 0.000 claims 4
- 108010063290 Aquaporins Proteins 0.000 claims 4
- 208000006011 Stroke Diseases 0.000 claims 4
- 230000001404 mediated Effects 0.000 claims 4
- 150000003839 salts Chemical group 0.000 claims 4
- 208000009447 Cardiac Edema Diseases 0.000 claims 3
- 206010021036 Hyponatraemia Diseases 0.000 claims 3
- 208000003067 Myocardial Ischemia Diseases 0.000 claims 3
- 208000008513 Spinal Cord Injury Diseases 0.000 claims 3
- 230000001629 suppression Effects 0.000 claims 3
- 101710006658 AAEL003512 Proteins 0.000 claims 2
- 206010007554 Cardiac failure Diseases 0.000 claims 2
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 2
- 208000008208 Craniocerebral Trauma Diseases 0.000 claims 2
- 206010015037 Epilepsy Diseases 0.000 claims 2
- 206010019280 Heart failure Diseases 0.000 claims 2
- 206010027599 Migraine Diseases 0.000 claims 2
- 208000008085 Migraine Disorders Diseases 0.000 claims 2
- 208000003435 Optic Neuritis Diseases 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 201000006233 congestive heart failure Diseases 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 230000005486 microgravity Effects 0.000 claims 2
- 230000002107 myocardial Effects 0.000 claims 2
- 125000001476 phosphono group Chemical group [H]OP(*)(=O)O[H] 0.000 claims 2
- 201000001365 retinal ischemia Diseases 0.000 claims 2
- 102100017238 AVP Human genes 0.000 claims 1
- 101700084127 AVP Proteins 0.000 claims 1
- 206010000269 Abscess Diseases 0.000 claims 1
- 210000004369 Blood Anatomy 0.000 claims 1
- 210000004556 Brain Anatomy 0.000 claims 1
- 210000003169 Central Nervous System Anatomy 0.000 claims 1
- 206010070976 Craniocerebral injury Diseases 0.000 claims 1
- 208000001380 Diabetic Ketoacidosis Diseases 0.000 claims 1
- 208000002296 Eclampsia Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 208000007386 Hepatic Encephalopathy Diseases 0.000 claims 1
- 206010019663 Hepatic failure Diseases 0.000 claims 1
- 206010053198 Inappropriate antidiuretic hormone secretion Diseases 0.000 claims 1
- 206010061216 Infarction Diseases 0.000 claims 1
- 206010022114 Injury Diseases 0.000 claims 1
- 206010061256 Ischaemic stroke Diseases 0.000 claims 1
- 208000007903 Liver Failure Diseases 0.000 claims 1
- 206010025130 Lupus encephalitis Diseases 0.000 claims 1
- 208000008466 Metabolic Disease Diseases 0.000 claims 1
- 206010028013 Mountain sickness acute Diseases 0.000 claims 1
- 208000010125 Myocardial Infarction Diseases 0.000 claims 1
- 210000004165 Myocardium Anatomy 0.000 claims 1
- 206010033712 Papilloedema Diseases 0.000 claims 1
- 206010036790 Productive cough Diseases 0.000 claims 1
- 206010038886 Retinal oedema Diseases 0.000 claims 1
- 206010041549 Spinal cord compression Diseases 0.000 claims 1
- 206010063036 Spinal cord oedema Diseases 0.000 claims 1
- 210000003802 Sputum Anatomy 0.000 claims 1
- 208000005765 Traumatic Brain Injury Diseases 0.000 claims 1
- 208000005735 Water Intoxication Diseases 0.000 claims 1
- KBZOIRJILGZLEJ-LGYYRGKSSA-N argipressin Chemical compound C([C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@@H](C(N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N1)=O)N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C1=CC=CC=C1 KBZOIRJILGZLEJ-LGYYRGKSSA-N 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 230000017531 blood circulation Effects 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 230000001472 cytotoxic Effects 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 201000009910 diseases by infectious agent Diseases 0.000 claims 1
- 201000008284 inappropriate ADH syndrome Diseases 0.000 claims 1
- 201000004044 liver cirrhosis Diseases 0.000 claims 1
- 231100000835 liver failure Toxicity 0.000 claims 1
- 201000009906 meningitis Diseases 0.000 claims 1
- 201000011195 retinal edema Diseases 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 201000010874 syndrome Diseases 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 229960003726 vasopressin Drugs 0.000 claims 1
- 0 CC(C)(C(C1)=CC(*C(C=C(CCC(*)=*)OI(*)(*)=O)=O)=CC1C(F)(F)F)F Chemical compound CC(C)(C(C1)=CC(*C(C=C(CCC(*)=*)OI(*)(*)=O)=O)=CC1C(F)(F)F)F 0.000 description 2
- UQRLOIYSRFRJKL-UHFFFAOYSA-N OC(c(cc(cc1)Cl)c1OCC(C1O)(C1O)O)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 Chemical compound OC(c(cc(cc1)Cl)c1OCC(C1O)(C1O)O)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 UQRLOIYSRFRJKL-UHFFFAOYSA-N 0.000 description 1
Claims (28)
- R1が、クロロおよびブロモから選択され;R3およびR5が、両方トリフルオロメチルであり;R2、R4およびR6が全てHである、請求項1または2に記載の化合物。
- R6が、置換されたホスホノ基であるか、または置換されていないホスホノ基である、請求項1または2に記載の化合物。
- 疾患または症状が、浮腫である、請求項1または3〜8のいずれかに記載の化合物。
- 浮腫が、脳浮腫である、請求項9に記載の化合物。
- 脳浮腫が、細胞毒性の脳浮腫である、請求項10に記載の化合物。
- 脳浮腫が、外傷、脳卒中、神経膠腫、髄膜炎、急性高山病、癲癇性発作、感染、代謝障害、低酸素症、水中毒、肝不全、肝性脳症または糖尿病性ケトアシドーシスの結果生じる脳浮腫である、請求項10または11に記載の化合物。
- 脳浮腫が、微小重力暴露、放射線暴露、侵襲性の中枢神経系処置、膿瘍、子癇、クロイツフェルト−ヤコブ病、またはループス脳炎の結果生じる脳浮腫である、請求項10または11に記載の化合物。
- 脳浮腫が、脳卒中の結果生じる脳浮腫である、請求項10〜12のいずれかに記載の化合物。
- 脳浮腫が、虚血性脳卒中の結果生じる脳浮腫である、請求項14に記載の化合物。
- 脳浮腫が、頭部外傷の結果生じる脳浮腫である、請求項10または11に記載の化合物。
- 脳浮腫が、外傷性脳損傷の結果生じる脳浮腫である、請求項10または11に記載の化合物。
- 低酸素症が、心不全またはその他の脳への血液潅流の遮断により引き起こされる低酸素症である、請求項12に記載の化合物。
- 低酸素症が、脳卒中により引き起こされる低酸素症である、請求項12に記載の化合物。
- 疾患または症状が、脊髄浮腫、網膜浮腫、微小重力暴露もしくは放射線暴露の結果生じる視神経浮腫、低酸素症の結果生じる浮腫、または心臓浮腫である、請求項9に記載の化合物。
- 脊髄浮腫が、脊髄外傷の結果生じる脊髄浮腫である、請求項20に記載の化合物。
- 脊髄外傷が、脊髄圧迫である、請求項21に記載の化合物。
- 患者が脳卒中、頭部損傷または脊髄損傷を患ってから3時間以内に処置が開始される、請求項9〜12のいずれか、または14〜17のいずれかに記載の化合物。
- 心臓浮腫が、心臓虚血またはその他の心臓への血流の遮断の結果生じる心臓浮腫である、請求項20に記載の化合物。
- 低ナトリウム血症および過剰な水分貯留が、心不全、肝硬変、ネフローゼ障害または抗利尿ホルモン分泌異常症候群(SIADH)の結果生じるものである、請求項1に記載の化合物。
- アクアポリンにより仲介される疾患または症状を処置または抑制するための、請求項1または3〜8のいずれかに記載の式1aの化合物を含む医薬組成物あって、前記疾患または症状は、浮腫、癲癇、視神経脊髄炎、片頭痛、低ナトリウム血症、網膜虚血、および過剰な水分貯留から選択される、医薬組成物。
- 請求項9〜25のいずれかに記載される用途に使用される、請求項26に記載の医薬組成物。
- アクアポリンにより仲介される疾患または症状を処置または抑制するための、請求項2〜8のいずれかに記載の式1aの化合物を含む医薬組成物あって、前記疾患または症状は、心筋虚血、心筋梗塞、心筋低酸素症、およびうっ血性心不全から選択され、前記式1aの化合物をアクアポリン阻害に有効な量で含む、医薬組成物。
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261644268P | 2012-05-08 | 2012-05-08 | |
US61/644,268 | 2012-05-08 | ||
US201261651778P | 2012-05-25 | 2012-05-25 | |
US61/651,778 | 2012-05-25 | ||
US201361799606P | 2013-03-15 | 2013-03-15 | |
US61/799,606 | 2013-03-15 | ||
PCT/US2013/040194 WO2013169939A2 (en) | 2012-05-08 | 2013-05-08 | New methods |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2017210529A Division JP6570597B2 (ja) | 2012-05-08 | 2017-10-31 | 新規方法 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2015520151A JP2015520151A (ja) | 2015-07-16 |
JP2015520151A5 true JP2015520151A5 (ja) | 2016-06-23 |
JP6238969B2 JP6238969B2 (ja) | 2017-11-29 |
Family
ID=49551452
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015511669A Active JP6238969B2 (ja) | 2012-05-08 | 2013-05-08 | 新規方法 |
JP2017210529A Active JP6570597B2 (ja) | 2012-05-08 | 2017-10-31 | 新規方法 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2017210529A Active JP6570597B2 (ja) | 2012-05-08 | 2017-10-31 | 新規方法 |
Country Status (14)
Country | Link |
---|---|
US (4) | US9994514B2 (ja) |
EP (1) | EP2846787B1 (ja) |
JP (2) | JP6238969B2 (ja) |
KR (1) | KR102200176B1 (ja) |
CN (2) | CN109512805B (ja) |
AU (2) | AU2013259526B2 (ja) |
BR (1) | BR112014027983B1 (ja) |
CA (1) | CA2872012C (ja) |
ES (1) | ES2699646T3 (ja) |
HK (1) | HK1208363A1 (ja) |
IL (1) | IL235512B (ja) |
MX (1) | MX363473B (ja) |
RU (1) | RU2671495C2 (ja) |
WO (1) | WO2013169939A2 (ja) |
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