Scientific Info and Patent Analysis Grp. 4Q2016 Patent Surveillance – Sunvepra

Patent Analysis Report

To: Pamela Mingo, Paul Scola Date: January 16, 2017

ST00001837

Update for 4Q2016

From: Rohit Agarwal

Intellectual property and R&D solutions

Evalueserve, India

+91 124 463 9923

Therapeutic Area / Project:

Virology / Sunvepra (BMS-650032)

Subject:

Q4, 2016 PATENT SURVEILLANCE UPDATE

Specific Structure Searched:

BMS-650032

Type of Search: Patent Surveillance

Object of Search:

To find patents or patent applications that specifically or generically disclose and/or claim the specified compounds. The search results have been analyzed to present relevant hits and remove duplicates.

Sources Searched:

Structure Search:

REGISTRY Chemical structures and Sequences – 1907 to [present]

DERWENT CHEMISTRY RESOURCE (WPIX) Chemical structures - 1999 to [present].

MARPAT Generic chemical structures from patents – 1961 to [present]

CHEMICAL ABSTRACTS Literature and patents – 1907 to [present]

Keyword Search:

HCAPLUS

WPIX

Summary of Search Strategy:

The structure searched for the study is provided below:

The keywords based search strategy for the study is provided below:

ASUNAPREVIR OR ASV OR 630420-16-5 OR BMS-650032 OR SUNVEPRA

Copies of WO, EP, & US granted patents & patent applications can be downloaded immediately to your desktop by clicking (or use Control-click) on the patent number hyperlinks provided in this report. Occasionally, a patent application number will be incorrectly linked and will not lead to a relevant document. Patent application numbers can usually be recognized by their format.

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·  Note: There is a possibility of patent application numbers being hyperlinked within the patent family. These hyperlinks are a result of a “bug” in the software and should be ignored. They will not link to the corresponding application.

If needed, copies of any other patents can usually be obtained from PatBase.

Copies of journal articles may be available by clicking (or use Control-click) on the hyperlinks provided in this report, or from our Electronic Journal collection on Cybrary. They can also be requested using our online photocopy request form

The material in this search report is for in-house use only and is subject to copyright law and policies. In order to comply with copyright law and policies, DO NOT Distribute this report without permission. Contact

Rohit Agarwal if you have any questions.

The BMS Patent Department must be contacted if the patent information provided is to be used for any type of exclusivity or forecast analysis.


Summary of Search Results

A total of five results are identified as interesting for this 4Q2016 update:

·  Three results from HCAPLUS;

·  Two results from WPIX.


Table of Contents

WO2016169573

WO2016164625

Reference 3. JP2016189746A; Primer pair and probe reagents for PCR-based detection of drug-resistant hepatitis C virus for prognosis assessment, Hiroshima University. 8

WO2016141890

US20160303088

Reference 1. WO2016169573A1; Sesquiterpene lactones as potent and broad spectrum antiviral compounds against all genotypes of Hepatitis C virus (HCV).

Full Text

ACCESSION NUMBER: 2016:1734552 HCAPLUS

DOCUMENT NUMBER: 165:553337

TITLE: Sesquiterpene lactones as potent and broad spectrum

antiviral compounds against all genotypes of Hepatitis

C virus (HCV)

INVENTOR(S): Elsebai, Mahmoud Fahmi

PATENT ASSIGNEE(S): Egypt

SOURCE: PCT Int. Appl., 28pp.

CODEN: PIXXD2

LANGUAGE: English

FAMILY ACC. NUM. COUNT: 1

PATENT INFORMATION:

PATENT NO. KIND DATE APPLICATION NO. DATE

------

WO 2016169573 A1 20161027 WO 2016-EG14 20160418

W: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY,

BZ, 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, IR,

IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA,

MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA,

PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK,

SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ,

VC, VN, ZA, ZM, ZW

RW: AL, 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, RS,

SE, SI, SK, SM, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM,

ML, MR, NE, SN, TD, TG, BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW,

SD, SL, ST, SZ, TZ, UG, ZM, ZW, AM, AZ, BY, KG, KZ, RU, TJ, TM

PRIORITY APPLN. INFO.: EG 2015-607 A 20150420

AB The present invention relates to potent HCV entry inhibitors (cynaropicrin

and grosheimol), in addn. to mono-caffoeylquinic acid derivs. which have

also anti-HCV activity but less than cynaropicrin and grosheimol.

IT 630420-16-5, Asunaprevir

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL

(Biological study); USES (Uses)

RN 630420-16-5 HCAPLUS

CN Cyclopropanecarboxamide, N-[(1,1-dimethylethoxy)carbonyl]-3-methyl-L-valyl-

(4R)-4-[(7-chloro-4-methoxy-1-isoquinolinyl)oxy]-L-prolyl-1-amino-N-

(cyclopropylsulfonyl)-2-ethenyl-, (1R,2S)- (CA INDEX NAME)

Reference 2. WO2016164625A1; Compositions and methods for the treatment of hepatitis C virus (HCV) infection, Spring Bank Pharmaceuticals.

Full Text

ACCESSION NUMBER: 2016:1650045 HCAPLUS

DOCUMENT NUMBER: 165:497005

TITLE: Compositions and methods for the treatment of

hepatitis C virus (HCV) infection

INVENTOR(S): Iyer, Radhakrishnan P.

PATENT ASSIGNEE(S): Spring Bank Pharmaceuticals, Inc., USA

SOURCE: PCT Int. Appl., 169pp.

CODEN: PIXXD2

LANGUAGE: English

FAMILY ACC. NUM. COUNT: 1

PATENT INFORMATION:

PATENT NO. KIND DATE APPLICATION NO. DATE

------

WO 2016164625 A1 20161013 WO 2016-US26504 20160407

W: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY,

BZ, 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, IR,

IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA,

MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA,

PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK,

SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ,

VC, VN, ZA, ZM, ZW

RW: AL, 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, RS,

SE, SI, SK, SM, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM,

ML, MR, NE, SN, TD, TG, BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW,

SD, SL, ST, SZ, TZ, UG, ZM, ZW, AM, AZ, BY, KG, KZ, RU, TJ, TM

PRIORITY APPLN. INFO.: US 2015-62144299 P 20150407

US 2015-62169931 P 20150602

US 2015-62215543 P 20150908

US 2015-62215618 P 20150908

AB The present invention features a method of treating a subject infected

with the hepatitis C virus (HCV) infection, the method comprises,

administering to the subject a pharmaceutical compd. selected from e.g.

formula: I (RSp, Rp or Sp isomers)or a prodrug or pharmaceutically

acceptable salt thereof to thereby treat the subject. In some

embodiments, the kit further comprises an addnl. agent (e.g. sofosbuvir)

for treatment. In some embodiments, in a method described herein, the

subject has been further diagnosed with an HIV infection.

IT 630420-16-5, Asunaprevir

RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL

(Biological study); USES (Uses)

RN 630420-16-5 HCAPLUS

CN Cyclopropanecarboxamide, N-[(1,1-dimethylethoxy)carbonyl]-3-methyl-L-valyl-

(4R)-4-[(7-chloro-4-methoxy-1-isoquinolinyl)oxy]-L-prolyl-1-amino-N-

(cyclopropylsulfonyl)-2-ethenyl-, (1R,2S)- (CA INDEX NAME)

Reference 3. JP2016189746A; Primer pair and probe reagents for PCR-based detection of drug-resistant hepatitis C virus for prognosis assessment, Hiroshima University.

Full Text

ACCESSION NUMBER: 2016:1818385 HCAPLUS

DOCUMENT NUMBER: 165:553812

TITLE: Primer pair and probe reagents for PCR-based detection

of drug-resistant hepatitis C virus for prognosis

assessment

INVENTOR(S): Chayama, Kazuaki; Ochi, Hidenori

PATENT ASSIGNEE(S): Hiroshima University, Japan

SOURCE: Jpn. Kokai Tokkyo Koho, 20pp.

CODEN: JKXXAF

LANGUAGE: Japanese

FAMILY ACC. NUM. COUNT: 1

PATENT INFORMATION:

PATENT NO. KIND DATE APPLICATION NO. DATE

------

JP 2016189746 A 20161110 JP 2015-72309 20150331

PRIORITY APPLN. INFO.: JP 2015-72309 20150331

AB The primer pair that enable rapid detn. of treatment strategies, probe,

drug-resistant hepatitis C virus detection kit, method for detecting

drug-resistant hepatitis C virus and prognosis method for hepatitis C are

provided. The primer pair, at least 300 consecutive bases contained in

the NS5A region of the genome of hepatitis C virus genotype 1b from the

10th-410th from the 5' end, and it consists of a forward primer and a

reverse primer designed to be contained in the base sequence of the

product of the polymerase chain reaction.

IT 630420-16-5, Asunaprevir

RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses)

RN 630420-16-5 HCAPLUS

CN Cyclopropanecarboxamide, N-[(1,1-dimethylethoxy)carbonyl]-3-methyl-L-valyl-

(4R)-4-[(7-chloro-4-methoxy-1-isoquinolinyl)oxy]-L-prolyl-1-amino-N-

(cyclopropylsulfonyl)-2-ethenyl-, (1R,2S)- (CA INDEX NAME)

Reference 4. WO2016141890A1; New fused heterocyclic compounds are hepatitis C virus (HCV) replication inhibitors useful for preventing, managing, treating or lessening the severity of HCV infection or HCV disorder; Sunshine Lake Pharma, Guangdong Dongyangguang Pharm.

Full Text

ACCESSION NUMBER: 2016-57877T [201667] WPIX

TITLE: New fused heterocyclic compounds are hepatitis C virus

(HCV) replication inhibitors useful for preventing,

managing, treating or lessening the severity of HCV

infection or HCV disorder

DERWENT CLASS: A96; B02

INVENTOR: FANG Q; HU B; LIU Z; XIE H; ZHANG J; ZHANG Y

PATENT ASSIGNEE: (SUNS-N) SUNSHINE LAKE PHARMA CO LTD; (GUAN-N) GUANGDONG

DONGYANGGUANG PHARM CO LTD

COUNTRY COUNT: 131

PATENT INFO ABBR.:

PATENT NO KIND DATE WEEK LA PG MAIN IPC

------

WO 2016141890 A1 20160915 (201667)* EN 157[0]

CN 105968101 A 20160928 (201673) ZH

TW 2016032514 A 20160916 (201683) ZH

APPLICATION DETAILS:

PATENT NO KIND APPLICATION DATE

------

WO 2016141890 A1 WO 2016-CN76131 20160311

CN 105968101 A Subst for CN 2015-10108484 20150312

CN 105968101 A Subst for CN 2015-10422786 20150718

CN 105968101 A CN 2016-10141716 20160311

TW 2016032514 A TW 2016-107625 20160311

PRIORITY APPLN. INFO: CN 2015-10422786 20150718

CN 2015-10108484 20150312

CN 2016-10141716 20160311

AN 2016-57877T [201667] WPIX

AB WO 2016141890 A1 UPAB: 20161223

NOVELTY - Fused heterocyclic compounds (I) are new.

DETAILED DESCRIPTION - Fused heterocyclic compounds (I) and their

stereoisomers, geometric isomers, tautomers, enantiomers, N-oxides,

hydrates, solvates, metabolites, salts or prodrugs are new.

A = -(CR7R7a)m-, -CR7=CR7a-, -(CH2)nO-, N=CR7-, -NR7-CR7R7a-,

-CR7R7a-NR7-, -O(CH2)n-, -CR7=N-, -S(CH2)n-, -(CH2)nS- or -NR9a;

X, X1 = N or CR7b;

Y1, Y11 = alkyl, cycloalkyl, heterocyclyl, (hetero)aryl, arylalkyl,

-C(=O)-(CR8R8a)t-N(R9)-R10 or an alpha -amino acid group (all optionally

substituted with 1-4 T1), H or deuterium;

alpha -amino acid group = derived from isoleucine, leucine, lysine,

methionine, phenylalanine, threonine, tryptophane, valine, alanine,

asparagines, aspartic acid, glutamic acid, glutamine, proline, serine,

para-tyrosine, arginine, histidine, cysteine, glycine, sarcosine,

N,N-dimethylglycine, homoserine, norvaline, norleucine, ornithine,

homocysteine, homophenylalanine, phenylglycine, ortho-tyrosine,

meta-tyrosine or hydroxyproline; either

R1-R4 = alkyl, arylalkyl, cycloalkyl, heterocyclyl or (hetero)aryl

(all optionally substituted with 1-4 T1), H or deuterium; or

R1R2+X-CH, R3R4+X1-CH = optionally form 3-8 membered heterocyclyl,

3-8 membered carbocyclyl, fused bicyclyl, fused heterobicyclyl, spiro

bicyclyl or spiroheterobicyclyl (all optionally substituted with 1-4 T1);

R5, R6 = alkyl, haloalkyl, alkenyl, alkynyl, heterocyclyl,

cycloalkyl, (hetero)aryl, arylalkyl, alkoxyalkyl, alkoxy,

(hetero)arylamino, (hetero)arylalkylamino, heteroaryloxy, heteroarylalkyl,

(hetero)arylalkoxy, heterocyclyloxy, heterocyclylalkoxy,

heterocyclylamino, alkylacyl, alkylacyloxy, alkoxyacyl,

heterocyclylalkylamino or aryloxy (all optionally substituted with 1-4

T1), H, deuterium, oxo (=O), OH, amino, halo, CN, mercapto or NO2;

R7, R7a, R7b, R8, R8a, R9a = deuterated alkyl, alkyl, haloalkyl,

alkoxy, alkenyl, alkynyl, heterocyclyl, cycloalkyl, (hetero)aryl,

arylalkyl, alkoxyalkyl, heteroarylalkyl, cycloalkylalkyl,

heterocyclylalkyl, (hetero)arylamino, (hetero)arylalkylamino,

heteroaryloxy, arylalkoxy, heteroarylalkoxy, heterocyclyloxy,

heterocyclylalkoxy, heterocyclylamino, alkyl-OC(=O)-, alkyl-C(=O)-,

carbamoyl, alkyl-OS(=O)r-, alkyl-S(=O)rO-, alkyl-OS(=O)rO-, alkyl-S(=O)r-,

heterocyclylalkylamino or aryloxy (all optionally substituted with 1-4

T1), H, deuterium, oxo (=O), OH, amino, halo, CN, mercapto or NO2;

R9, R10 = alkyl, cycloalkyl, heterocyclyl, (hetero)aryl, arylalkyl,

alkyl-OC(=O)-, alkyl-C(=O)-, carbamoyl, alkyl-OS(=O)r-, alkyl-S(O)rO-,

alkyl-S(=O)r- or aminosulfonyl (all optionally substituted with 1-4 T1), H

or deuterium;

m = 1-4;

r = 0-2; and

T1 = OH, deuterium, amino, halo, CN, (hetero)aryl, alkoxy

(optionally substituted), alkylamino, alkylthio, alkyl, haloalkyl,

alkoxyalkyl, haloalkoxyalkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl,

mercapto, NO2, aryloxy, arylamino, heteroaryloxy, heteroarylalkyl, oxo

(=O), carboxy, OH, OH substituted alkyl-C(=O)-, alkyl-C(=O)-,

alkyl-S(=O)-, alkyl-S(=O)2, OH substituted alkyl-S(=O)-, OH substituted

alkyl-S(=O)2 or carboxy substituted alkoxy.

An INDEPENDENT CLAIM is also included for a composition comprising

(I) and a carrier, excipient, diluents, adjuvant and/or vehicle.

ACTIVITY - Antiinflammatory; Hepatotropic; Virucide.

MECHANISM OF ACTION - HCV replication inhibitor; HCV viral protein

function inhibitor. The effect of (I) to inhibit HCV replication was

tested in HCV GT1b L31V resistant strain using biological assays. The

result showed that ((S)-1-((S)-2-(5-(7-(2-((S)-1-((S)-2-

methoxycarbonylamino-3-methyl-butyryl)-pyrrolidin-2-yl)-4,5-dihydro-1H-

naphtho(1,2-d)imidazol-7-yl)-indan-4-yl)-1H-imidazol-2-yl)-pyrrolidine-1-

carbonyl)-2-methyl-propyl)-carbamic acid methyl ester exhibited EC50 value

of 0.002 nM.

USE - (I) are useful for preventing, managing, treating or

lessening the severity of HCV infection or HCV disorder in a subject (all

claimed).

ADVANTAGE - (I): have good inhibitor effect on HCV GT1a, GT1b,

GT2a, GT3a, GT4b, GT5a, GT6a or HCVGT1b L31V, GT1b Y93H resistant strains;

and have anti drug resistance effect and good bioavailability.

AN.S DCR-2088724

CN.P ASUNAPREVIR

CN.S {(S)-1-[(2S,4R)-4-(7-Chloro-4-methoxy-isoquinolin-1-yloxy)-2-((1R,2S)-1-

cyclopropanesulfonylaminocarbonyl-2-vinyl-cyclopropylcarbamoyl)-

pyrrolidine-1-carbonyl]-2,2-dimethyl-propyl}-carbamic acid tert-butyl

ester

SDCN RB3B4M

Reference 5. US20160303088A1; Improving pharmacokinetics of drug used to treat HIV, comprises administering substituted (benzyl-phenyl-(thiazolylmethoxycarbonylamino)-pentyl)- carbamic acid thiazolylmethyl ester; Gilead Sci.

Full Text

ACCESSION NUMBER: 2016-64945N [201676] WPIX

CROSS REFERENCE: 2008-M29459; 2009-L57970; 2011-F02293; 2011-L18966;

2011-P67662; 2012-M13647; 2013-H43011; 2014-B53942;

2014-G76106; 2015-036272; 2015-306730; 2015-464330;

2016-15478R; 2016-15508T

TITLE: Improving pharmacokinetics of drug used to treat HIV,

comprises administering substituted

(benzyl-phenyl-(thiazolylmethoxycarbonylamino)-pentyl)-