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`FILE 'HOME' ENTERED AT 12:19:17 ON 04 JAN 2018
`
`=> b reg
`COST IN U.S. DOLLARS
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`on property searching in REGISTRY, refer to:
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`=>
`
`Uploading C:\Users\alee1\Documents\STN Express 8.6\Queries\14648115v3.
`
`str
`
`

`

`22
`
`NS/
`NPAi
`o+——
`
`LA.)
`
`% ‘18
`
`19
`
`‘14
`
`15
`
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`
`j
`
`(31
`
`chain nodes
`12
`13
`22
`
`ring nodes .
`5
`1
`2
`3
`4
`Chain bonds .
`1-7
`8-12
`9-17
`
`6
`
`7
`
`8
`
`9
`
`10
`
`11
`
`14
`
`15
`
`16
`
`17
`
`18
`
`19
`
`11-13
`
`ring bonds .
`3—4
`1—2
`1—6
`2—3
`18—19
`16—17
`17—18
`exact/norm bonds .
`
`1 2
`1
`6
`1 7
`2 3
`3 4
`4 5
`5
`6
`7 8
`7 11
`8
`9
`8 12
`9 10
`9 17
`14—15
`14—19
`15—16
`16—17
`17—18
`18—19
`
`4—5
`
`5—6
`
`7—8
`
`7—11
`
`8—9
`
`9—10
`
`10—11
`
`14—15
`
`14—19
`
`15—16
`
`10-11
`
`11-13
`
`G1:C,O,N
`
`.
`Match level
`1:CLASS
`2:CLASS
`10:CLASS
`11:CLASS
`18:CLASS
`19:CLASS
`
`8:CLASS
`7:CLASS
`6:CLASS
`5:CLASS
`4:CLASS
`3:CLASS
`12:CLASS
`13:CLASS
`14:CLASS
`15:CLASS
`16:CLASS
`22:CLASS
`23:CLASS
`
`9:CLASS
`17:CLASS
`
`L1
`
`STRUCTURE UPLOADED
`
`

`

`
`:> s 11 sss full
`FULL SEARCH INITIATED 12:20:20 FILE 'REGISTRY'
`FULL SCREEN SEARCH COMPLETED -
`74148 TO ITERATE
`
`100.0% PROCESSED
`SEARCH TIME: 00.00.01
`
`74148 ITERATIONS
`
`L2
`
`3362 SEA SSS FUL L1
`
`3362 ANSWERS
`
`=> b caplus
`COST IN U.S. DOLLARS
`
`FULL ESTIMATED COST
`
`SINCE FILE
`ENTRY
`342.00
`
`TOTAL
`SESSION
`342.34
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`FILE 'CAPLUS' ENTERED AT 12:20:38 ON 04 JAN 2018
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`FILE COVERS 1907 - 4 Jan 2018 VOL 168 ISS 3
`
`3 Jan 2018 (20180103/ED)
`FILE LAST UPDATED:
`REVISED CLASS FIELDS (/NCL) LAST RELOADED: Dec 2015
`USPTO MANUAL OF CLASSIFICATIONS THESAURUS ISSUE DATE:
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`Dec 2015
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`reclassification data for the fourth quarter 0: 2017.
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`
`
`This file contains CAS Registry Numbers for easy and accurate
`
`substance identification.
`
`=> 3 12
`L3
`
`122 L2
`
`=> 3 l3 and "RAD"
`17902 "RAD"
`5635 "RADS"
`23111 "RAD"
`
`L4
`
`("RAD" OR "RADS")
`0 L3 AND "RAD"
`
`
`=> d 13 ibib abs fhitstr tot
`
`

`

`bifunctional
`AUTHORcs):
`CORPORATE SOURCE:
`
`ANSWER l 015' l22 CAPLUS
`L3
`FORMAT
`
`(Continued)
`COPYRIGHT 20lB AC5 On STN
`RECORD. ALL CITATIONS AVAILABLE IN THE RE
`
`COPYRIGHT 20lB AC5 On STN
`ANSWER l 015' l22 CAPLUS
`L3
`ACCESSION NUMBER:
`20l7:l734790
`CAPLUS
`DOCUMENT NUMEE
`la? :576607
`
`TITLE:
`Highly enantioselective Michael addition of
`maedisubstituted aldehydes to maleimides
`catalyzed by new primary amineesquaramide
`organocatalysts
`Jun—tao; Liu,
`Ma, zhi—wei; Liu, xiao—feng; Liu,
`zhirjing; Tao. Jingrchao
`Department of Fundamental Courses, No. 2 Yingcai
`Street, Huljl District, Henan University of Animal
`Husbandry and Economy, Henan, 450044, Peop. Rep.
`China
`Tetrahedron Letters (2017), 53(46), 44674490
`SOURCE:
`CODEN: TELEAY;
`ISSN: 00404039
`lO.lDlE/j.tetlet.ZDl7.l0.0ZE
`DIGITAL OBJECT ID:
`ElBEVlEI Ltd.
`PUBLISHER:
`Journal:
`(online computer file)
`DOCUMENT TYPE:
`English
`LANGUAGE :
`CASREACT 167:576607
`OTHER SOURCE(S) :
`AB
`New bifunctional primary amine—squaramides catalyzed asym. Michael
`addition
`reaction of 06,06’dl5ub5tltuted aldehydes to maleimides has been
`developed. This organocatalytic asym. reaction provides easy access to
`functionalized succinimides with a hroad suhstrate scope. Both
`enantiomers of desired succinimide derivs. were ohtained in good to
`excellent yields (up to 93%) with excellent enantioselectiVities (up to
`>99$ee) .
`1352335—27—3P
`RL: SPN (Synthetic preparation),- PREP (preparation)
`(preparation of succinimide derivs. via enantioselective Michael
`addition of
`a,a—disuhstituted aldehydes to maleimides catalyzed by
`primary amineesquaramide bifunctional organooatalysts)
`1352335e27e3
`CAPLUS
`Cyclohexanecarhoxaldehyde,
`lr[(SS)rlr(4rfluorophenyl)r2,5rdioxor3r
`pyrrolidinyl]— (CA INDEX NAME)
`Absolute stereochemistry. Rotation to).
`
`IT
`
`RN
`CN
`
`
`
`REFERENCE COUNT
`THIS
`
`50
`
`THERE ARE 50 CITED REFERENCES AVAILABLE FOR
`
`ANSWER 2 OF 122
`L3
`ACCESSION NUMBER:
`TITLE:
`AUTHORtS):
`CORPORATE SOURCE:
`
`COPYRIGHT 20lB AC5 on STN
`CAPLUS
`2017:1533565
`CAPLUS
`CobaltlIII)-catalyzed l,4—addition of C—H bonds of
`oximes to maleimides
`Chen, xiangxiang; Ren. Jiangtao: xie, Hu; Sun. Wei;
`Sun, Meng; Wu, Biao
`Key Laboratory of Synthetic and Natural Functional
`Molecule Chemistry of Ministry of Education,
`Department of Chemistry
`L Materials Science, Northwest
`University, xi'an, 710127, Peop. Rep. China
`SOURCE:
`Organic Chemistry Frontiers (2017) Ahead of Print
`CODEN: OCE‘RAB;
`ISSN: 2052—4129
`DIGITAL OBJECT ID:
`10.1039/c7qo00637j
`Royal Society of Chemistry
`PUBLISHER:
`Journal
`DOCUMENT TYPE:
`LANGUAGE :
`English
`GI
`
`R1
`
`N/
`
`cue
`
`Me
`
`0
`
`0
`
`N\
`
`Me
`
`1
`
`L3
`
`ANSWER 2 OF 122
`Er
`
`CAPLUS
`
`COPYRIGHT 20lB AC5 on STN
`
`(Continued)
`
`N
`
`n
`
`0
`Meo—N
`H
`Me—C
`
`REFERENCE COUNT:
`THIS
`
`FORMAT
`
`71
`
`THERE ARE 71 CITED REFERENCES AVAILABLE FOR
`
`RECORD. ALL CITATIONS AVAILABLE IN THE RE
`
`IT
`
`AB
`to
`
`Oxime directed cobalt-catalyzed arene sp2 C—H bond conjugation addition
`maleimide was reported,
`the reaction showed great tolerance to different
`functional groups, and various succinimide derivs., e.g., I were
`efficiently produced. This protocol exhihited specific reactivity with
`only producing a monoeCeH bond addition product and no external base was
`needed, which suggested a unique reactivity of this Corbased catalytic
`system.
`2151273—22—2P
`RL: RCT (Reactant); SPN (Synthetic preparation),- PREP (Preparation),- RACT
`(Reactant or reagent)
`(regioseleotive preparation of succinimide derivs. via
`cohaltrcatalyzed
`1,4—addition of C—H honds of oximes to maleimides)
`RN
`2151373e32e2
`CAPLUS
`2. sesyrrolidinedione, Jr (4ehromophenyl) ,3, [2, [la
`CN
`(methoxyimino)ethlephenler
`(CA INDEX NAME)
`
`

`

`CAP[:05
`COPYRIGHT 2013 AC5 on 5TN
`2017:467676
`CAPLUS
`166:362723
`Novel piperaZine and piperidine derivatives,
`synthesis and use thereof in inhibiting VDAC
`oligomerization, apoptosis and mitochondria
`dysfunction
`Shoshan—Barmatz, Varda,- Lev Gruzman, Arie
`The National Institute for Biotechnology In the Negev
`Ltd., Israel
`PCT Int. Appl.,
`l09pp.
`CODEN: PIXXDZ
`Patent
`English
`
`ANSWER 4 015' 122
`L3
`ACCESSION NUMBER:
`DOCUMENT NUMBE
`
`TITLE:
`
`INVENTDR(S) :
`PATENT ASSIGNEE(S) :
`SOURCE :
`DOCUMENT TYPE:
`LANGUAGE:
`FAMILY ACC. NUM. COUNT:
`PATENT INFORMATION:
`PATENT NO.
`W0 201704 67 94
`w: AE, AG,
`132, CA,
`EG, ES,
`I5,
`JP,
`MA, MD,
`PA, PE,
`SK, SL,
`Uz, VC,
`RW: AL, AT,
`HU,
`IE,
`SE, SI,
`ML, MR,
`SD, SL,
`PRIORITY APPLN.
`INFO
`OTHER SOURCE (5) :
`GI
`
`
`
`COPYRIGHT 2013 ACS on ST"
`CAPLUS
`ANSWER 3 015' 122
`L3
`ACCESSION NUMBER:
`2017:1203974
`CAPLUS
`DOCUMENT NUMBE
`le7:234237
`
`TITLE:
`RutheniumcII3—Catalyzed Hydroarylation of Maleimides
`Using Carboxyllc Acids as a Traceless Directing Group
`ADTHOR(5) :
`Mandal, Anup; 5ahoo, Harekrishna; Dana,
`suman;
`Baidya,
`Mahiuddin
`CORPORATE SOURCE :
`Department of Chemistry, Indian Institute of
`Technology Madras. Tamil Nadu. 600 036,
`India
`SOURCE :
`Organic Letters (2017), 19(15), 413374141
`CODEN: ORLEE7;
`ISSN- 1523-7052
`DIGITAL OBJECT ID:
`l0.lDzl/acs.orglett.1h0l964
`PUBLISHER:
`American Chemical Society
`DOCUMENT TYPE:
`Journal;
`(Onllne computer file)
`LANGUAGE:
`English
`CASREACT 167:234237
`OTHER SOURCE(S) :
`AB
`An efficient RucIIJ—catalyzed hydroarylation of maleimides wlth
`readyestock aryl carboxyll: acids has been developed based on weak
`carhoxylateedirected orthoeCeH alkylation and concomitant decarhoxylation
`processes, fahricating 3—aryl succinimides, a recurrent scaffold in drug
`mols.,
`in high yields (up to 91:.) .
`The protocol features operational
`simplicity, avoids the need for precious metal additives/oxidants. and
`offers broad Substrate scope wlth formal metae and paraeselectivities.
`represents the first Example of Ru(II)-catalyzed direct arylation of
`malelmldaa wlth unblaaad hanzulc aclda.
`3159117217?
`RL: SPN (Synthetic preparation),- PREP (preparation)
`(synthesis of aryl succinimides via Ruthenium(II) catalyzed
`hydroarylation of maleimides with aromatic carhoxylic acids)
`CAPLUS
`3159117217
`l—(4—chlorophenyl)—3—phenyl— (CA INDEX NAME)
`2,5—Pyrrolidinedione,
`
`It.
`
`IT
`
`RN
`CN
`
`E].
`
`
`REFERENCE COUNT:
`THIS
`FORMAT
`
`75
`
`THERE ARE 75 CITED REFERENCES AVAILABLE FOR
`RECORD. ALL CITATIONS AVAILABLE IN THE RE
`
`their
`
`l K
`
`DATE
`APPLICATION NO .
`IND DATE
`
`A1
`20170323
`W0 2016*IL51020
`20160913
`AM, A0, AT, AU, AZ, BA, BB, BG, BH, BN, BR, Bw, BY,
`CL, CN, CO, CR, CU, Cz, DE, DK, DM, DO, Dz, EC, EE,
`GB, GD, GE, GH, GM, GT, HN, HR, HU,
`ID,
`IL,
`IN,
`IR,
`KG, KN, KP, KR, KW, Kz, LA, LC, LK, LR, L5, LU, LY,
`MG, MK, MN, MW, Mx, MY, Mz, NA, NG, NI, NO, NZ, OM,
`PH, PL, PT, OA, RO, RS, RU, RW, SA, SC, SD, SE, SG,
`ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US,
`ZA, ZM,
`ZW
`BG, CH, CY, CZ, DE, DK, EE, E5, PI, FR, GB, GR, HR,
`IT, LT, LU, Lv, MC, MK, MT, NL, NO, PL, PT, RO, RS,
`SM, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GO,
`SW, KM,
`SN, TD, TG, Bw, GH, GM, KE, LR, LS, MW, M2, NA, RW,
`SZ, TZ, UG, ZM, ZW, AM, Az, BY, KG, Kz, RU, TJ,
`TM
`US 2015-62217966
`P
`2.0150914
`CASREACT 166:362723.‘ MARPAT 166:362723
`
`L3
`
`ANSWER 4 015' 122
`
`CAPLU5
`
`COPYRIGHT 20lB AC5 on 5TN
`OCE‘g
`
`NjN
`/u
`
`N
`
`0
`
`11
`
`Cl
`
`(Continued)
`PAGE l—A
`
`(Continued)
`
`L3
`
`ANSWER 4 015' 122
`
`CAP[:05
`
`COPYRIGHT 20lB AC5 on 5TN
`
`Cl
`
`fie
`QNH
`
`AB
`Ph
`
`[wherein A
`provided herein plpEIazlnE and piperidine derivs. of formula I
`is C and N,- R1 is (un)sulostituted aromatic moiety; R2 is (uanuhstituted
`and (un)quostituted naphthyl, R3 is absent, H and heterualkyl; Ll is
`ahsent, NH2. and derivs.,- L2 is a linker, when A is N, L2 is a group
`consisting of 4—lo atoms, optionally forming a closed ring, whereof at
`least one of the atoms is N,
`forming part of an amide group; when A is C,
`[.2 is Cl—4 alkylene;] and enantiomers, diastereomers, mixta. and salts
`thereof,- their preparation and use thereof in inhibiting vnAC
`oligomeriration,
`apoptosis and mitochondria dysfunction.
`Example compound I was prepared
`by
`condensation of l—(4—(trifluoromethoxy)phenyl)piperaZine wlth
`le (4echlorophenyl) elHepyrroleez, sedione.
`The invention compds. were
`evaluated for their VDAC oligomerization inhibitory actiVity (data
`given).
`272923-32-1P
`IT
`RL: PAC (pharmacological activity),- SPN (Synthetic preparation),- THU
`(Therapeutic use): EIOL (Biological study); PREP (Preparation),- U5E5
`(Uses)
`(preparation of plpEIaZlnE and piperidine derivs. for inhihiting VDAC
`oligomerization, apoptosis and mitochondria dysfunction)
`CAP[.05
`B7BQBSS33S1
`2, SIPyrrolldlnelene, 1* (4Ichlorophenyl) ,3, [4*[ [4*
`(CA INDEX NAME)
`(trlfluurumethnxy)phenyl] amino] elepiperidinyl] e
`
`RN
`CN
`
`F3570
`
`PAGE er
`
`

`

`L3
`
`ANSWER 5 OF l22 CAPLUS
`
`COPYRIGHT ZOlB ACS on STN
`
`(Continued)
`
`Cl
`
`N
`
`0
`
`Pb
`REFERENCE COUNT:
`THIS
`FORMAT
`
`49
`
`THERE ARE 49 CITED REFERENCES AVAILABLE FOR
`RECORD. ALL CITATIONS AVAILABLE IN THE RE
`
`L3
`
`ANSWER 6 OF l22 CAPLUS
`0
`H
`0:er1-12
`
`COPYRIGHT ZOlB ACS on STN
`
`(Continued)
`
`Cl
`°
`
`N
`
`
`
`P).
`OS.CITING REF COUNT:
`RECORD
`REFERENCE COUN
`
`THIS
`FORMAT
`
`4
`
`24
`
`THERE ARE 4 CAPLUS RECORDS THAT CITE THIS
`(4 CITINGS)
`THERE ARE 24 CITED REFERENCES AVAILABLE FOR
`RECORD. ALL CITATIONS AVAILABLE IN THE RE
`
`COPYRIGHT ZOlB ACS on STN
`L3
`ANSWER 5 OF l22 CAPLUS
`ACCESSION NUMBER:
`20l7:277652
`CAPLUS
`DOCUMENT NUMBE
`las:3lSBBa
`
`TITLE:
`Evaluation of in silico pharmacokinetic properties
`and
`in vitro cytotoxic activity Of selected newly
`synthesized Nesuccinimide derivatives
`Milosevic, Natasa P.; Kujlc, Vesna; Curcic, Jelena;
`Jaklmuv, Dimitar; Milic, Natasa; Banjac, Nebojsa;
`Uscumlic, Gordana: Kallazan. Roman
`Faculty of Medicine, Department of Pharmacy,
`University of Novi Sad, Novi Sad, 2mm), Serbia
`Journal of Pharmaceutical and Biomedical Analysis
`(2017). 137. 252,257
`CODEN:
`JPBADA;
`ISSN: 0731:7065
`10.1016/j.jpba.2017.01.o42
`DIGITAL OBJECT ID:
`Elsevier B.V.
`PUBLISHER:
`Journal;
`(online computer file)
`DOCUMENT TYPE:
`English
`LANGUAGE:
`AB
`Design of a new drug entity is usually preceded by anal. of guant.
`structure activity (properties) relationships, OSA(P)R. Six newly
`synthesized succinimide derivs. have been determined for
`(i)
`in silico
`physicoechemical descriptors. pharmacokinetic and toxicity predictors.
`in vitIO hiul. activity On four different. carcinoma cell lll’lEa and On
`normal fetal lung cells and (iii) lipophilicity on liquid chromatog. All
`compds. observed were predicted for good permeability and solubility,
`good oral
`absurptiOn rate and moderate vOlume Of distribution as well as fOr mOdeSt
`blood brain permeation,
`followed by acceptable observed toxicity.
`In
`silico
`determined lipophilicity, permeability through jejunum and aqueous
`solubility were
`correlated with exptl. obtained lipophilic consts.
`(by use of high
`pressure liquid chromatog.) and linear correlations were obtained.
`Absorption rate and volume of distribution were predicted by chromatog.
`lipophilicity measurements while permeation through blood bran barrier
`predicted dominantly by mol. size defined with mol. weight Five compds.
`demonstrated antiproliferative activity toward cervix carcinoma HeLa cell
`lines;
`three were cytotoxic against breast carcinoma MCF—7 cells, while
`one inhibited proliferation of colon carcinoma HT—zs cell lines. Only
`compound was cytotoxic toward normal cell lines, while other compds. were
`proven as safe. Antiproliferative potential against HeLa cells was
`described as exponential function of lipophilicity. Based on obtained
`results,
`lead compds. were selected.
`31591I72I7
`RL: ADV (Adverse effect,
`including toxiCity); PAC (Pharmacological
`activity); PRP (Properties); THU (Therapeutic use); BIOL (Biological
`study): USES (Uses)
`(newly synthesized Nesuccinimide derivs. antitumor action and
`pharmacokinetics)
`3l59le72e7
`CAPLUS
`2,5—Pyrrolidinedione,
`
`AUTHOR(S):
`
`CORPORATE SOURCE:
`SOURCE:
`
`(ll)
`
`was
`have
`
`one
`
`IT
`
`RN
`CN
`
`l—(4—chlorophenyl)—3—phenyl— (CA INDEX NAME)
`
`COPYRIGHT ZOlB AC5 on STN
`ANSWER 6 OF l22 CAPLUS
`L3
`ACCESSION NUMBER:
`20l6:2l667la
`CAPLUS
`TITLE:
`Sigma—2 receptor and progesterone receptor membrane
`component I (PGRMCl) are two different proteins:
`Proofs by fluorescent labeling and binding of sigmaez
`receptor ligands to PGRMCl
`Pati, Maria Laura; Groza, Diana; Riganti, Chiara;
`Kupecka, Joanna; Niso, Mauro; Berardi, Francesco;
`Hager, Sonja; Heffeter, Petra; Hirai, Miwa; Tsugawa,
`
`Hitosh - Kaba. Yaauakl.‘ Suematsu, Makota; Abate.
`Carmen
`Dipartimento di Farmacia—Scienze del Farmaco,
`Universita degli Studi di Bari ALDO MORO, Bari,
`Ie70125. Italy
`Pharmacological Research (201.7), 11.7, 67:24
`SOURCE:
`CODEN: PHMREP;
`ISSN:
`l043e66la
`lo.l0l6/j.phrs.20ls.l2.023
`DIGITAL OBJECT ID:
`Elsevier Ltd.
`PUBLISHER:
`Journal:
`(online computer file)
`DOCUMENT TYPE:
`English
`LANGUAGE:
`AB
`A controversial relationship between sigma—2 and progesterone receptor
`membrane component l (PGRMCl) proteins, both representing promising
`targets for the therapy and diagnosis of tumors. exists since 20ll, when
`the sigman receptor was reported to be identical to PGRMCl. Because a
`misidentification of these proteins will lead to biased future research
`hampering the possible diagnostic and therapeutic exploitation of the two
`targets,
`there is the need to solve the debate on their identity. with
`this aim, we have herein investigated uptake and distribution of
`structurally different fluorescent sigmacz receptor ligands by flow
`cytometry and confocal microscopy in MCF7 cells, where together with
`intrinsic sigma—2 receptors, PGRMCl was constitutively present or
`alternatively silenced or overexpressed. HETllE cells, with constitutive
`or silenced PGRMCl, were also studied.
`These expts. showed that the
`fluorescent sigma—2 ligands bind to their receptor irresp. of PGRMCl
`expression. Furthermore,
`isothermal titration calorimetry was conducted
`examine if DTG and PBZB,
`two structurally distinct nanomolar affinity
`sigma—2 ligands, bind to purified PGRMCl proteins that have recently been
`revealed to form both apoemonomeric and hemeemediated dimeric forms.
`While no binding to apoePGRMCl monomer was detected. a micromolar
`affinityto heme—mediated dimerized PGRMCl was demonstrated in DTG but not in
`PBZB.
`The current data proVide eVidence that sigmae2 receptor and PGRMCl are
`not
`identical, paving the pathway for future unbiased research in which these
`two attractive targets are treated as different proteins while the
`identification of the true sigmae2 protein further needs to be pursued.
`INDExING IN PROGRESS
`33279I49I3, PESBS
`RL: BSU (Biological study, unclassified); BIOL (Biological study)
`(5—2 receptor and progesterone receptor membrane component I
`(PGRMCl) are two different proteins, proofs by fluorescent labeling
`binding of cez receptor ligands to PGRMCl)
`30279—4 9—3
`CAPLUS
`Benzenesulfonamide,
`Sechloroe4e (2, 5edioxoeaephenylelepyrrolidinyl) e
`INDEX NAME)
`
`AUTHOR(S):
`
`CORPORATE SOURCE:
`
`to
`
`IT
`IT
`
`and
`RN
`CN
`
`(CA
`
`

`

`COPYRIGHT 20lB AC5 on STN
`CAPLUS
`20l6:2l033l2 CAPLUS
`IE7 :4S7l30
`Phthalimide derivative metahotropic glutamate r4
`ligands
`Macaulay,
`John A.
`Merck Sharp C
`U.s. Pat. Appl. Pub1., No pp. given
`CODEN: USXXCO
`Patent
`English
`Z
`
`L3
`
`ANSWER 7 015' l22 CAPLUS
`
`COPYRIGHT 20lB ACS on STN
`
`(Continued)
`
`‘ \N/
`
`
`
`NH
`
`Cl
`
`N
`
`O
`
`Ph
`
`ANSWER 7 015' I22
`L3
`ACCESSION NUMBER:
`DOCUMENT NUMEE
`
`TITLE:
`INVENTOR(5):
`PATENT ASSIGNEE(S) :
`Dohme Corp., USA
`SOURCE:
`DOCUMENT TYPE:
`LANGUAGE :
`FAMILY ACC. NUM. COUNT:
`PATENT INFORMATION:
`DATE
`PATENT NO.
`DATE
`APPLICATION N
`
`20110513
`US 2011-737943
`US 20110310266
`20111229
`
`20090324
`WO 2010033349
`20100325
`W0 2009-0554759
`W: AE, AG,
`AO, AT, Au, AZ, BA, BB, BG, BH, BR, BW, BY, BZ,
`CA, CH,
`Co, CR, CU, Cz, DE, DK, DM, DO, DZ, EC, EE, EG,
`ES, FI,
`GE, GH, GM, GT, HN, HR, HU,
`ID,
`IL,
`IN,
`IS,
`JP,
`KE, KG,
`KP, KR, Kz, LA, LC, LK, LR, LS, LT, LU, LY, MA,
`MD, ME,
`MN, MW, Mx, MY, Mz, NA, NG, NI, NO, Nz, OM, PE,
`PG, PH,
`RO, RS, RU, SC, SD, SE, SE, SK, 5L,
`SM, ST, SV,
`SY, TJ,
`TR, TT, TZ, UA, UG, US, Uz, VC, VN, ZA, ZM,
`ZW
`RW: AT, BE,
`CY, CZ, DE, DK, EE, ES, FI, ER, GB, GR, HR, HU,
`IE,
`IS,
`LU, Lv, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI,
`SK,
`SM,
`BJ, CF, CG, CI, CM, GA, GN, GD, GW, ML, MR, NE,
`SN, TD,
`GH, GM, KE, LS, MW, Mz, NA, SD, SL, SZ, TZ, UG,
`ZM, ZW,
`BY, KG, Kz, MD, RU, TJ,
`TM
`PRIORITY APPLN.
`INFO
`Us 2000—61192139
`P
`20000916
`wo 2009—US54759
`in
`2.0090024
`ASSIGNMENT HISTORY FOR US PATENT AVAILABLE IN LSUS DISPLAY FORMAT
`AD Disclosed are mGluR4 pos. allosteric modulator ligands of general formula
`(I) and radiolaheled derivates,
`their use as therapeutic agents for the
`treatment of central nervous system disorders modulated by mGluR4 and as
`ligands for the labeling and diagnostic imaging of mGluR4 in mammals.
`lZlBPZETéBT'fP
`RL: PAC (Pharmacological activity),- SPN (Synthetic preparation),- THU
`(Therapeutic use); EIDL (Biological study),- PREP (Preparation),- USES
`(Uses)
`(preparation of phthalimidephenylpyridinecarlooxamide derivs. for use
`metahotropic glutamate R4 modulators)
`1210926—40—7
`CAPLUS
`2ePyridinecarhoxamide, Ne[archloroe4e(2,5edioxoe3ephenylele
`pyrrolldlnleFhenle’
`(CA INDEX NAME)
`
`
`
`IT
`
`as
`RN
`CN
`
`ANSWER B 015' I22
`L3
`ACCESSION NUMBER:
`DOCUMENT NUMEE
`
`TITLE:
`
`AUTHORcs):
`
`CORPORATE SOURCE:
`Institute
`
`SOURCE:
`
`DIGITAL OBJECT ID:
`PUBLISHER:
`DOCUMENT TYPE:
`LANGUAGE :
`GI
`
`COPYRIGHT 20lB AC5 on STN
`CAPLUS
`20l6:l94450l
`CAPLUS
`las:32l460
`Novel Compounds Targeting the Mitochondrial Protein
`VDACl Inhibit Apoptosis and Protect against
`Mitochondrial Dysfunction
`DenrHail, Danya; Segaerhvartz, Racheli; Shalev,
`Moran,- Shteinfer—Kuzmine, Anna,- Gruzman, Arie; Reina,
`Simona; De Pinto, Vito,- ShOShan-Barmatz, Varda
`Department Of Life Sciences and the National
`for Biotechnology in the Negev, Ben—Gurion University
`of the Negev, Beer Sheva, B4105, Israel
`Journal of Biological Chemistry (20l6), 29l(43).
`2493925003
`CDDEN:
`J'BCHA3;
`ISSN: 002lr9250
`10.1074/jhc.M116.744234
`American Society for Biochemistry and Molecular
`Blology
`Journal;
`(online computer file)
`English
`
`E3C—o
`
`Cl
`
`NH
`
`
`
`an
`
`AS Apoptosis is thought to play a critical role in several pathol.
`processes,
`such as neurodegenerative diseases (i.e. Parkinson's and Alzheimer's
`diseases) and various cardiovascular diseases. Despite the fact that
`apoptotic mechanisms are well defined.
`there is still no substantial
`therapeutic strategy to stop or even slow this process. Thus,
`there is
`unmet need for therapeutic agents that are able to hlock or 510w
`apoptosis
`in neurodegenerative and cardiovascular diseases.
`The outer
`mitochondrial
`membrane protein voltage—dependent anion channel I
`(VDACl) is a
`convergence point for a variety of cell survival and death signals,
`including apoptosis. Recently,
`the authors demonstrated that VDACl
`oligomerization is involved in mitochondrionrmediated apoptosis.
`Thus,
`VDACl oligomerization represents a prime target for agents designed to
`
`L3
`
`(Continued)
`COPYRIGHT 20lB ACS on STN
`ANSWER B 015' l22 CAPLUS
`modulate apoptosis. Here, highethroughput compd. screening and medicinal
`chem. were employed to develop compds.
`that directly interact with VDACl
`and prevent VDACl oligomerization, concomitant with an inhibition of
`apoptosis as induced by various means and in various cell lines.
`The
`compds. protected against apoptosiseassocd. mitochondrial dysfunction,
`restoring dissipated mitochondrial membrane potential, and thus cell
`energy and metah., decreasing reactive oxidative species prodn., and
`preventing detachment of hexokinase buund to mitochondria and disruption
`of Intracellular Ca2+ levels. Thus.
`thIS Study descrlbes navel drug
`Candldatea wIth a defIned mechanlam Of aCtIun that Involves InthItIOn of
`VDACl oligomerization, apoptosis, and mitochondrial dysfunction.
`The
`compds. I and II offer a therapeutic strategy for treating different
`diseases assocd. with enhanced apoptosis and point to VDACl as a
`promising
`target for therapeutic intervention.
`IT
`279923—32—l
`RL: PAC (Pharmacological activity): THU (Therapeutic use); EIOL
`(Biological study): USES (Uses)
`(novel compds.
`targeting the mitochondrial protein VDACl inhibit
`apoptosis and protect against mitochondrial dysfunction)
`070903—30—1
`CAPLUS
`2.5ePyrrolidinedione,
`lr(4echlorophenyl)r3r[4r[[4e
`(trifluoromethoxy)phenyl]aminoJelepiperidinlee
`(CA INDEX NAME)
`
`RN
`CN
`
`Cl
`
`PAGE 1 —A
`
`“fir0
`QNH
`
`F3C*D
`
`PAGE 2 IA
`
`

`

`COPYRIGHT 201.3 ACS on STN
`(Continued)
`THERE ARE 4 CAPLUS RECORDS THAT CITE THIS
`(4 CITINGS)
`THERE ARE 93 CITED REFERENCES AVAILABLE FOR
`RECORD. ALL CITATIONS AVAILABLE IN
`THERE
`
`COPYRIGHT 20lB ACS on STN
`ANSWER 9 015‘ l22 CAPLUS
`L3
`ACCESSION NUMBER:
`20l6:l932497
`CAPLUS
`DOCUMENT NUMEE
`las:4ao4s4
`
`TITLE:
`Small molecule inhibitors for the treatment or
`prevention of dengue virus infection
`INVENTOR (S) :
`Byrd, Chelsea M.,- Jordan, Robert,- Dai, Dongcheng;
`Hruby, Dennis E.
`PATENT ASSIGNEE (S) :
`Siga Technologies, Inc., USA
`SOURCE :
`U.S., No pp. given
`CODEN: usxxAM
`Patent
`DOCUMENT TYPE:
`English
`LANGUAGE :
`2
`FAMILY ACC. NUM. COUNT:
`PATENT INFORMATION:
`DATE
`
` PATENT NO. DATE APPLICATION N
`
`
`20110313
`US 2011-736965
`US 9029376
`20150512
`
`US 20110153940
`20110630
`20090602
`WO 2009149054
`20091210
`W0 2009*D545921
`13w, BY, BZ,
`w: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR,
`CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, Dz, EC, EE, EG,
`ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU,
`ID,
`IL,
`IN,
`IS,
`JP,
`KE, KG, KM, KN, KP, KR, Kz, LA, LC, LK, LR, LS, LT, LU, LY, MA,
`MD, ME, MG, MK, MN, Mw, Mx, MY, Mz, NA, NG, NI, NO, Nz, OM, PG,
`PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL,
`SM, ST, SV, SY,
`TJ, TM, TN, TR, TT, TZ, UA, UG, US, Uz, VC, VN, ZA, ZM,
`2w
`Rw: AT, BE, BG, CH, CY, Cz, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU,
`IE,
`IS,
`IT, LT, LU, Lv, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI,
`SK, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GO, Gw, ML, MR, NE, SN,
`TD, TG,
`13w, GH, GM, KE, LS, Mw, Mz, NA, SD, SL, SZ, TZ, UG, ZM,
`ZW, AM, AZ, BY, KG, K2, MD, RU, TJ,
`TM
`US 20150202195
`A1
`20150723
`US 2015*14673102
`20150330
`
`PRIORITY APPLN.
`INFO
`US 2003-61053263
`20030603
`P
`W0 2009*“545921
`20090602
`W
`US 2011*736965
`A3 20110313
`ASSIGNMENT HISTORY EOR US PATENT AVAILABLE IN LSUS DISPLAY EORMAT
`AB Methods and pharmaceutical compns. for treating viral infections, by
`administering certain compds.
`in therapeutically effective amts. are
`disclosed. Methods of using the compds. and pharmaceutical compns.
`thereof are also disclosed.
`In particular,
`the treatment and prophylaxis
`of vIral Infectlons Such as caused by flavIvIruS .15 dlsclased.
`:L.e..
`including but not limited to, Dengue virus, West Nile virus, yellow fever
`virus, Japanese encephalitis virus, and tickeborne encephalitis virus.
`522637-31-6
`RL: PAC (Pharmacological activity): THU (Therapeutic use),- EIDL
`(Biological study): USES (Uses)
`(small mol.
`inhibitors for treatment or prevention of dengue virus and
`other viral infection)
`522637—31—6
`CAPLUS
`2. seeyrrolidinedione, 3e [4e (zebenzothiazolyl) elepiperarinyll ele (4e
`fluorophenlee
`(CA INDEX NAME)
`
`RN
`CN
`
`IT
`
`CAPLUS
`
`4 9
`
`3
`
`ANSWER B 015' 1.22
`L3
`OS.CITING REF COUNT:
`RECORD
`REFERENCE COLIN
`THI5
`FORMAT
`
`
`
`L3
`
`ANSWER 9 015' 1.22
`
`CAPLUS
`O
`
`COPYRIGHT 201.3 ACS on STN
`
`(Continued)
`
`
`
`51
`
`THERE ARE 51 CITED REFERENCES AVAILABLE FOR
`RECORD. ALL CITATIONS AVAILABLE IN
`THERE
`
`ANSWER 1.0 OF 1.22
`L3
`ACCESSION NUMBER:
`DOCUMENT NUMEE
`
`TITLE:
`ADTHOR(5) :
`CORPORATE SOURCE :
`
`SOURCE :
`
`DIGITAL OBJECT ID:
`PUBLISHER:
`DOCUMENT TYPE:
`LANGUAGE :
`OTHER SOURCEtS):
`GI
`
`COPYRIGHT 201.3 ACS On STN
`CAPLUS
`2016:1760764
`CAPLUS
`l65:607091
`A chiral analog of the bicyclic guanidine TED:
`synthesis. structure and Hronsted base catalysis
`Goldberg, Mariano,- Sartakov, Denis,- Eats, Jan w.,-
`Bulte, Michael,- Goebel, Michael w.
`Institute for Organic Chemistry and Chemical Biology,
`Goethe University Frankfurt, Frankfurt am Main,
`Dem-133. Germany
`Eeilstein Journal of Organic chemistry (201.6), 12,
`1370-1376
`CODEN: EJOCEH;
`ISSN: 1360-5397
`10.3762/bjoc.12.176
`EeilsteineInstitut zur Foerderung der Chemischen
`WISSenSChaften
`Journal,-
`(online computer file)
`English
`CASREACT 165:607091
`
`
`
`
`A
`
`:11!
`
`AB
`
`Starting from (SJeDephenylalanine, easily accessible by
`lipase—catalyzed kinetic resolution, a chiral triamine was assembled by a
`reductive amination and finally cyclized to form the title compound
`bicyclic
`guanidine e.g., I.
`In the crystals of the guanidinium benzoate salt the
`six membered rings of I adopt conformations close to an envelope with the
`Ph substituents in pseudo—axial positions.
`The unprotonated guanidine I
`catalyzes DielseAlder reactions of anthrones and maleimides (2540A ee) .
`It also promotes as a strong Eronsted base the retroealdol reaction of
`55106 Cycluadducta wah kinetic IeSOlntiOn Of the enantiumera.
`In three
`cases,
`the retroaldol products (43—33% ee) could be recrystd.
`to high
`enantiopurity (295% ee) .
`The absolute configuration of several compds.
`is supported by anomalous xeray diffraction and by chemical correlation.
`2343GE7I29I2E‘
`RL: PRP (Properties),- RCT (Reactant),- SPN (Synthetic preparation),- PREP
`(Preparation),- RACT (Reactant or reagent)
`(crystal and mol. structure,- enantioselective preparation of bicyclic
`guanidine TED and its application as Bronsted base catalyst in
`DielSIAldeI Ieactiuna Of anthrunea wah maleImIdeS)
`2043667-29-2
`CAPLUS
`2,5—Pyrrolidinedione, 1-(4-hrumupheny1)-3-(9,10-dlhydIO-10-OxO-9-
`anthracenyl)’.
`(SRJI
`(CA INDEX NAME)
`Absolute stereochemistry.
`
`IT
`
`RN
`CN
`
`

`

`L3
`
`ANSWER 10 OF 122
`
`CAPLUS
`Br
`
`COPYRIGHT 2013 ACS on STN
`
`(ContInued)
`
`0
`
`R
`
`O
`
`O
`OS.CITING REF COUNT:
`RECORD
`
`1
`
`THERE ARE 1 CAPLUS RECORDS THAT CITE THIS
`(1 CITINGS)
`
`COPYRIGHT 2013 ACS an STN
`CAPLUS
`ANSWER 11 OF 122
`L3
`2016:551469
`CAPLUS
`ACCESSION NUMBER:
`155:227202
`DOCUMENT NUMEE
`
`2, 3, 5, s—Tetrahydro—z, 6-h13(pheny1mathy1)-1H-
`TITLE :
`ImIdazo [1. 2eaJeImIdazo1e
`Tan, ChooneHong; Shen, Juan
`AUTHORcs) :
`CORPORATE SOURCE :
`NatIonal UnIversIty of SIngapore, SIngapore
`SOURCE :
`e—EROS Encyc1opedIa Of Reagents for OrganIc SynthesIs
`(2003),
`1—2.
`Juhn Wr1ey
`E 50115. Ltd.: Chlchaater. UK.
`CODEN: EQKDHI;
`ISBN: 97Beoe47oe34269ea
`URL:
`http:flunllnellbrary.wlley.cum/du1/10.1002/0470B4
`239X.rn00967/pdf
`DOCUMENT TYPE:
`Conference; General ReVIew;
`English
`LANGUAGE :
`OTHER SOURCE(S) :
`CASREACT 156:227202
`AB
`Synthesrs, propertres, app1rcatrons and hand1rng Of
`2. 3. 5. setetrahydroez, 64ers (phenylmethyl) eIHeImIdazo [1. 2eaJeImIdazo1e .‘Ln.
`enantIoseleotIve DIelseAlder reactIon and MIchaeJ. addns. were renewed.
`PiSESE-SE-EP
`RL: SPN (Synthetrc preparatIon); PREP (PreparatIon)
`(synthesIs. propertIes and reactIVIty Of
`2, 3, 5, setetrahydroez, sebIs (phenylmethyl) eIHeImIdazo [1, Zea] eImIdazoIe)
`91595540943
`CAPLUS
`RN
`2,5-PyrIO11d1nEd1unE,
`an
`1— (3, 4—orch1oropheny1J—3—(s, 10-d1hydIO-4 , 5-d1hydIOxy-
`loeoxoeSeanthracenleI,
`(3Rl’
`(CA INDEX NAME)
`Abso1ute StEIEuchEmlatIy. RotatIon (+).
`C1
`
`(onlIne computer fIle)
`
`IT
`
`C1
`
`
`
`5
`
`THERE ARE 5 CITED