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公开(公告)号:US20190202801A1
公开(公告)日:2019-07-04
申请号:US16334335
申请日:2017-09-18
IPC分类号: C07D401/10 , C07D403/10 , C07D413/10 , C07D403/14 , C07D405/10 , C07D471/06 , C07D241/04 , A61P23/00 , A61P29/00 , A61P1/00 , A61P25/28
CPC分类号: C07D401/10 , A61K45/06 , A61P1/00 , A61P23/00 , A61P25/28 , A61P29/00 , C07D205/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/58 , C07D211/60 , C07D211/62 , C07D231/12 , C07D241/04 , C07D265/30 , C07D295/205 , C07D309/08 , C07D333/38 , C07D333/40 , C07D401/04 , C07D403/10 , C07D403/14 , C07D405/10 , C07D413/10 , C07D471/06 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10
摘要: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
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公开(公告)号:US20190040024A1
公开(公告)日:2019-02-07
申请号:US16073854
申请日:2017-02-22
IPC分类号: C07D265/30 , C09K5/04
CPC分类号: C07D265/30 , C07C217/26 , C07D207/10 , C07D211/38 , C07D223/04 , C07D241/04 , C09K5/04 , C11D3/245 , C11D7/28 , C11D9/28
摘要: An acyclic fluorinated compound of formula (I) is amine-containing acyclic hydrofluoroethers. The acyclic fluorinated compound is useful as heat transfer, solvent cleaning, fire extinguishing agents and electrolyte solvents and additives.
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公开(公告)号:US20180327368A1
公开(公告)日:2018-11-15
申请号:US15543389
申请日:2016-01-13
申请人: Marianne Dorothy SADAR , Nasrin R. MAWJI , Carmen Adriana BANUELOS , Raymond John ANDERSEN , Javier Garcia FERNANDEZ , Kunzhong JIAN , The University of British Columbia University- Industry Liaison Office , British Columbia Cancer Agency Branch
发明人: Raymond John ANDERSEN , Javier Garcia FERNANDEZ , Kunzhong JIAN , Marianne Dorothy SADAR , Nasrin R. MAWJI , Carmen Adriana BANUELOS
IPC分类号: C07D249/04 , A61K31/4192 , C07D295/084 , A61K31/5375 , C07D233/60 , A61K31/4164 , A61K45/06
CPC分类号: C07D249/04 , A61K31/4164 , A61K31/4192 , A61K31/5375 , A61K45/06 , A61K51/0453 , A61K51/0459 , A61K51/0463 , A61K51/0465 , A61P35/00 , C07B59/002 , C07D233/60 , C07D265/30 , C07D295/084 , C07D295/088
摘要: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R11a, R11b, R11c, R11d, X, n1, n2, and n3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.
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公开(公告)号:US10059655B2
公开(公告)日:2018-08-28
申请号:US15104736
申请日:2014-12-17
申请人: Luis Brito , Delai Chen , Gabriel Grant Gamber , Andrew Geall , Kevin Love , Thomas Zabawa , Frederic Zecri
发明人: Luis Brito , Delai Chen , Gabriel Grant Gamber , Andrew Geall , Kevin Love , Thomas Zabawa , Frederic Zecri
IPC分类号: C07C229/12 , C07C229/38 , C07D205/04 , C07D265/30 , C07D207/12 , C07D207/16 , C07D211/22 , C07D295/088 , C07D211/46 , C07D211/60 , C07D211/62 , C07D295/15 , C07C271/20 , C07C219/04 , A61K47/18 , A61K9/127 , A61K9/51 , A61K31/7105 , A61K31/713 , A61K39/39 , C07C271/22 , C07D211/06 , C07D211/34 , C07D211/44
CPC分类号: C07C229/12 , A61K9/1272 , A61K9/5123 , A61K31/7105 , A61K31/713 , A61K39/12 , A61K39/39 , A61K47/18 , A61K2039/53 , A61K2039/55555 , C07C219/04 , C07C229/38 , C07C271/20 , C07C271/22 , C07D205/04 , C07D207/12 , C07D207/16 , C07D211/06 , C07D211/22 , C07D211/34 , C07D211/44 , C07D211/46 , C07D211/60 , C07D211/62 , C07D265/30 , C07D295/088 , C07D295/15 , C12N2760/18534
摘要: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, n and p are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
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公开(公告)号:US20180179158A1
公开(公告)日:2018-06-28
申请号:US15580008
申请日:2016-06-13
发明人: Jürg DREIER , Berangere GAUCHER , Eric DESARBRE
IPC分类号: C07D211/26 , A61P31/04 , A61K31/5377 , A61K31/65 , A61K31/4465 , C07D205/04 , A61K31/397 , C07D207/09 , A61K31/40 , C07D265/30 , A61K31/5375 , C07D207/14 , C07D211/58 , A61K31/4468 , C07D207/16 , A61K31/4025 , C07D403/12 , A61K31/4178 , A61K31/4439 , C07D401/12 , C07D409/12 , A61K31/427 , C07D417/12 , C07D413/12 , A61K31/4155 , A61K31/4245 , C07D417/14 , C07D401/14 , A61K31/444 , C07D413/14
CPC分类号: C07D211/26 , A61K31/397 , A61K31/40 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/444 , A61K31/4465 , A61K31/4468 , A61K31/5375 , A61K31/5377 , A61K31/65 , A61P31/04 , C07D205/04 , C07D207/09 , C07D207/14 , C07D207/16 , C07D211/58 , C07D265/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要: The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein ASC is —N(R8)(R9)ASC-1 ASC-1 is Ring A represents a 4- to 6-membered saturated ring containing carbon atoms as ring members in addition to the nitrogen atom and wherein one CH2 moiety in ring A is optionally replaced by CH(R21) and wherein one carbon atom in ring A that is not adjacent to the nitrogen atom is optionally replaced by O, and wherein ring A is connected to X via a carbon atom; X represents a bond, —CH2- or —C(═O)—; AR1, AR2 represent independently phenyl or a 5- to 6-membered heteroaryl ring containing one to three heteroatoms selected from O, S and N, wherein AR1 is connected to L1 via a carbon atom, and wherein AR2 is connected to L1 and L2 via a carbon atom; R1, R2, R3 represent independently hydrogen, halogen, cyano, hydroxyl, C1-C6alkyl, C1-C6haloalkyl, C3-C8cycloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, —C1-C6alkylene-N(R12)R13, —N(R12)R13, —C(O)OR111, —C(O)N(R12)R13, —S(O)OR11 or phenyl; R4 represents hydroxyl, hydrogen, halogen, nitro, cyano, amino, C1-C6alkyl optionally substituted by 1 to 5 R14, C2-C6alkenyl optionally substituted by 1 to 5 R14, C2-C6alkynyl optionally substituted by 1 to 5 R14, C1-C6alkoxy optionally substituted by 1 to 5 R14, C2-C6alkenyloxy optionally substituted by 1 to 5 R14, C2-C6alkynyloxy optionally substituted by 1 to 5 R14, —C(O)OR15, —CHO, —C(O)N(R16)R17, —C1-C6alkylene-N(R9)(R16)R17, —O-Cycle-P or —O-Cycle-Q; R5, R6, R7 represent independently hydrogen, halogen, cyano, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; R8 represents hydrogen, methyl or ASC-1; R9 is methyl or absent, and wherein when R9 is present the respective nitrogen atom carries a positive charge; R10 represents hydrogen or methyl; R11 represents independently at each occurrence hydrogen or C1-C6alkyl; R12, R13 represent independently at each occurrence hydrogen or C1-C6alkyl; R14 represents independently at each occurrence halogen, cyano, hydroxyl, C1-C6alkoxy, C1-C6haloalkoxy, C3-C8cycloalkyl, —C(O)OR11, —CHO, —C(O)N(R12)R13, —C1-C6alkylene-N(R12)R13, partially unsaturated C3-C8 carbocyclic ring optionally substituted by 1 to 3 R18, or a saturated or partially unsaturated C3-C8 heterocyclic ring optionally substituted by 1 to 3 R18 containing carbon atoms as ring members and one or two ring members independently selected from N(R9)(R12), N(R9) and O; Cycle-Q represents independently at each occurrence phenyl optionally substituted by 1 to 3 R19 or a 5- to 6-membered heteroaryl ring containing one to four heteroatoms selected from O, S and N, optionally substituted by 1 to 3 R19; R15 represents independently at each occurrence hydrogen or C1-C6alkyl optionally substituted by 1 to 5 R14; R16 and R17 represent independently at each occurrence hydrogen or C1-C6alkyl optionally substituted by 1 to 5 R14; R18 and R19 represent independently at each occurrence halogen, cyano, hydroxyl, oxo, amino, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or —CO(O)R11; R20 represents independently at each occurrence hydrogen or methyl; R21 represents N(R20)2 or CH2-N(R20)2; LI represents —CH═CH—, —CH2-O—, —O—CH2-, —CH2-O—CH2-, —CH2-S—, —S—CH2-, —CH2-S(O)—, —CH2-S(O2)-, —S(O)—CH2-; —S(O2)-CH2-, —C(CH3)(CH3)-, —C(═O)—NH—, —NH—C(═O)—, —CH2-CH2-, —CH═CH—CH2-, —CH2-NH—C(═O)—, —C(═O)—NH—CH2, —C═C—, —S(O2)-NH—CH2-, —S(O2)-NH, —O—CH2-CH2-O—, —O—, —NH— CH2-, —CH2-NH—, —CH2-CH2-O—, or —NH—C(═O)—CH2-O—, or a bond; L2 represents C1-C7alkylene, wherein one or more CH2 moieties in the alkylene are optionally replaced independently by —N(R9)(R20)-, —CH(N(R9)(R20)(R20))-, or —C(═O)—, wherein within L2 there are no adjacent C(═O) moieties or adjacent —N(R9)(R20)— moieties, and wherein the terminal moiety of L2 is not —N(R9) (R20)-, or L2 represents —O—C1-C6alkylene-, or L2 represents a bond, providing that X represents —CH2- when L2 is a bond; as well as methods of using the compounds of formula I for treating or preventing bacterial infections.
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公开(公告)号:US10005792B2
公开(公告)日:2018-06-26
申请号:US15508074
申请日:2015-09-03
申请人: CTXT PTY LTD
发明人: Ylva Elisabet Bergman , Romina Lessene , Danny Ganame , Richard Charles Foitzik , Benjamin Joseph Morrow , Michelle Ang Camerino , Scott Raymond Walker , H. Rachel Lagiakos , John Feutrill , Paul Anthony Stupple
IPC分类号: C07D207/12 , C07D209/44 , C07D211/22 , C07D211/46 , C07D211/58 , C07D211/76 , C07D213/81 , C07D213/82 , C07D217/06 , C07D217/12 , C07D231/14 , C07D231/20 , C07D231/56 , C07D235/08 , C07D271/08 , C07D271/10 , C07D261/18 , C07D277/56 , C07D277/68 , C07D265/30 , C07D265/34 , C07D401/04 , C07D401/12 , C07D413/04 , C07D451/02 , C07D451/14 , C07D491/08 , C07D491/107 , C07C233/78 , C07C235/42 , C07C235/60 , C07D295/192
CPC分类号: C07D491/107 , C07C233/78 , C07C235/42 , C07C235/50 , C07C235/60 , C07C311/08 , C07C2602/06 , C07C2602/08 , C07C2602/10 , C07D205/04 , C07D207/12 , C07D209/44 , C07D211/22 , C07D211/46 , C07D211/58 , C07D211/76 , C07D213/81 , C07D213/82 , C07D217/06 , C07D231/12 , C07D231/14 , C07D231/20 , C07D231/56 , C07D235/08 , C07D261/18 , C07D265/30 , C07D265/34 , C07D271/08 , C07D271/10 , C07D277/56 , C07D277/68 , C07D295/185 , C07D295/192 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/04 , C07D451/02 , C07D451/14 , C07D491/08
摘要: A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, —NH2, —C(═O)NH2, and —CH2OH; R4b is either H or Me; R5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.
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公开(公告)号:US20180162829A1
公开(公告)日:2018-06-14
申请号:US15811522
申请日:2017-11-13
申请人: Corsair Pharma Inc.
IPC分类号: C07D321/00 , C07D317/34 , C07C59/72 , C07D317/40 , C07C219/16 , C07D453/02 , C07D257/06 , C07D263/24 , C07D263/26 , C07D265/30 , C07D207/08 , C07D295/088 , C07D211/60 , C07D295/145 , C07C69/74 , C07C69/96 , A61K9/70 , C07C235/20 , A61K31/165 , A61K31/216 , A61K31/365 , C07D307/20 , A61K31/341 , A61K45/06 , A61K9/00 , C07C69/712
CPC分类号: C07D321/00 , A61K9/0014 , A61K9/7023 , A61K31/165 , A61K31/216 , A61K31/341 , A61K31/365 , A61K45/06 , C07C59/72 , C07C69/712 , C07C69/734 , C07C69/74 , C07C69/96 , C07C219/16 , C07C235/20 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07C2603/14 , C07D207/08 , C07D211/60 , C07D257/06 , C07D263/24 , C07D263/26 , C07D265/30 , C07D295/088 , C07D295/145 , C07D307/20 , C07D317/34 , C07D317/40 , C07D453/02
摘要: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
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公开(公告)号:US09980928B2
公开(公告)日:2018-05-29
申请号:US15489186
申请日:2017-04-17
IPC分类号: A61K31/7028 , A61K31/138 , A61K31/192 , A61K31/4015 , A61K31/165 , A61K31/381 , A61K31/5375 , A61K31/7034 , A61K31/451 , A61K31/4045 , A61K31/385
CPC分类号: A61K31/138 , A61K31/165 , A61K31/192 , A61K31/375 , A61K31/381 , A61K31/385 , A61K31/4015 , A61K31/4045 , A61K31/451 , A61K31/5375 , A61K31/7004 , A61K31/7034 , A61K45/06 , C07C59/68 , C07C217/04 , C07C217/48 , C07C217/74 , C07C233/18 , C07C271/16 , C07C2101/08 , C07C2101/14 , C07C2601/08 , C07C2601/14 , C07D207/267 , C07D207/27 , C07D209/08 , C07D211/22 , C07D265/30 , C07D307/62 , C07D333/20 , C07D339/04 , C07H15/18 , C07H15/22
摘要: Hydroxy aliphatic substituted phenyl aminoalkyl ether compounds of formula (I), and compositions thereof, are useful as a medicament in the treatment of nervous system diseases and/or the treatment of developmental, behavioral and/or mental disorders associated with cognitive deficits.
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公开(公告)号:US09969768B1
公开(公告)日:2018-05-15
申请号:US15815587
申请日:2017-11-16
申请人: KING SAUD UNIVERSITY
IPC分类号: C07J63/00 , C07J53/00 , C07D213/36 , A61K31/56 , C07B43/04 , C07B49/00 , C07D265/30
CPC分类号: C07J63/008 , A61K31/56 , C07B43/04 , C07B49/00 , C07D213/36 , C07D265/30 , C07J53/002
摘要: Oleanolic acid methyl ester derivatives demonstrate potent anti-diabetic activities. In in vitro anti-diabetic testing, the derivatives showed more potency regarding dipeptidyl peptidase-4 (DPP-IV) inhibitor activity, peroxisome proliferator-activated receptors (PPARs) agonist activity, and α-Glucosidase inhibitors activity, as compared to reference standards oleanolic acid and acarbose. In in vivo oral hypoglycemic testing, both acute and sub-acute studies demonstrated that the derivatives had high potency and long duration of action compared to the reference standards pioglitazone, acarbose and oleanolic acid.
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公开(公告)号:US20180071304A1
公开(公告)日:2018-03-15
申请号:US15817470
申请日:2017-11-20
申请人: vTv Therapeutics LLC
发明人: Per Sauerberg , Pavel Pihera , Zdenek Polivka , Miroslav Havranek , Ingrid Pettersson , John Patrick Mogensen
IPC分类号: A61K31/5377 , A61K31/495 , A61K31/343 , A61K31/4025 , A61K31/381 , A61K31/445 , A61K31/195 , A61K31/4402 , A61K31/415 , A61K31/5375 , A61K31/192 , A61K31/40
CPC分类号: A61K31/5377 , A61K31/192 , A61K31/195 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4402 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C59/70 , C07C217/48 , C07C323/16 , C07C323/32 , C07C2601/02 , C07D211/46 , C07D213/30 , C07D213/36 , C07D231/12 , C07D265/30 , C07D295/096 , C07D295/112 , C07D307/79 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/54
摘要: Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPARδ and may be useful for treating conditions mediated by the same.
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