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1. (WO2017093157) PIPERIDINE, PYRROLIDINE AND 2-OXO-1,3-OXAZINANE DERIVATIVES AS INHIBITORS OF BACTERIAL EFFLUX-PUMPS FOR THE TREATMENT OF MICROBIAL INFECTIONS



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INTERNATIONAL SEARCH REPORT (ISR)
Part 1:  1  2  3  4  5  6          Part 2:  A  B  C  D  E 
International application No. Applicant's or agent's file reference
PCT/EP2016/078938 P1106PC00
International filing date (day/month/year) (Earliest) Priority Date (day/month/year)
28 November 2016 30 November 2015
Applicant
BASILEA PHARMACEUTICA AG
FOR FURTHER ACTION: See Form PCT/ISA/220 as well as, where applicable, item 5 below.
This international search report has been prepared by this International Searching Authority and is transmitted to the applicant according to Article 18. A copy is being transmitted to the International Bureau.
It is also accompanied by a copy of each prior art document cited in this report.
1. Basis of the report
a. With regard to the language, the international search was carried out on the basis of:
the international application in the language in which it was filed.
a translation of the international application into                                          which is the language of a translation furnished for the purposes of international search (Rules 12.3(a) and 23.1(b)).
b.
This international search report has been established taking into account the rectification of an obvious mistake authorized by or notified to this Authority under Rule 91 (Rule 43.6bis(a)).
c.
With regard to any nucleotide and/or amino acid sequence disclosed in the international application, the international search was carried out on the basis of a sequence listing:
2. Certain claims were found unsearchable
3. Unity of invention is lacking
4. Title of the invention
The text is approved as submitted by the applicant.
The text has been established by this Authority to read as follows:
PIPERIDINE, PYRROLIDINE AND 2-OXO-1,3-OXAZINANE DERIVATIVES AS INHIBITORS OF BACTERIAL EFFLUX-PUMPS FOR THE TREATMENT OF MICROBIAL INFECTIONS

5. Abstract
The text is approved as submitted by the applicant.
The text has been established, according to Rule 38.2, by this Authority as it appears in Box No. IV. The applicant may, within one month from the date of mailing of this international search report, submit comments to this Authority.

The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof wherein ASC is Ring A represents a 4- to 6-membered saturated ring containing carbon atoms as ring members in addition to the nitrogen atom, wherein a -CH 2 -CH 2 - moiety adjacent to the nitrogen atom is optionally replaced by a -C(=O)-O- moiety to form a carbamate; X represents a bond or -CH 2 -; AR1 and AR2 represent phenyl; R1, R2 and R3 represent independently hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy or C 1 -C 6 haloalkoxy; R4 represents hydrogen, halogen, C 1 -C 6 alkyl optionally substituted by 1 to 5 R10a, C 2 -C 6 alkenyl optionally substituted by 1 to 5 R10a, C 1 -C 6 alkylene-R10b, C 2 -C 6 alkenylene-R10b, C(O)OR11a, CHO, C(O)N(R12)R13 or O-R14; R5, R6 and R7 represent independently hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy or C 1 -C 6 haloalkoxy; R8 represents methyl or is absent, and when R8 is present the respective nitrogen atom carries a positive charge; R9a and R9b represent independently hydrogen or methyl; R10a represents independently at each occurrence halogen, hydroxyl, C 1 -C 6 alkoxy or C 1 -C 6 haloalkoxy; R10b represents C 3 -C 8 cycloalkyl, C(O)OR11a, CHO, C(O)N(R12)R13, N(R12)R13, Cycle-P or Cycle-Q; R11a and R11b represent independently at each occurrence hydrogen or C 1 -C 6 alkyl; R12 and R13 represent independently at each occurrence hydrogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkoxy-C 1 -C 4 alkyl; R14 represents C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 2 -C 6 alkenyl, C 2 -C 6 haloalkenyl, C 1 -C 6 alkylene-Cycle-P, C 1 -C 6 alkylene-Cycle-Q; Cycle-P represents independently at each occurrence a saturated or partially unsaturated C 5 -C 6 carbocyclic ring optionally substituted by 1 to 3 R15 or a saturated or partially unsaturated 5- or 6-membered heterocyclic ring optionally substituted by 1 to 3 R15 containing carbon atoms as ring members and one or two ring members independently selected from N(R11b) and O; Cycle-Q represents independently at each occurrence phenyl optionally substituted by 1 to 3 R16 or a 5- to 6-membered heteroaryl ring containing one to four heteroatoms independently selected from O, S and N, optionally substituted by 1 to 3 R16; R15 and R16 represent independently at each occurrence halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy or C 1 -C 4 haloalkoxy; L1 represents -CH=CH-, -CH 2 -O-, -(CH 2 ) 2 -O-, -0-CH 2 -, -CH 2 -S-, -(CH 2 ) 2 -S-, -S-CH 2 -, -C(CH 3 ) 2 -, -(CH 2 ) 2 -or -CH=CH-CH 2 -; L2 represents C 1 -C 7 alkylene, wherein one or more -CH 2 - moieties in the alkylene moiety are optionally replaced independently by -C(=O)-, wherein within L2 there are no adjacent -C(=O)- moieties and wherein the terminal moiety of L2 is not -C(=O)-; and discloses their use in methods of treating a subject with a microbial infection or susceptible to a microbial infection in combination with an antimicrobial agent.


6. Drawings
a.
The figure of the drawings to be published with the abstract is Figure No. ____________
as suggested by the applicant.
as selected by this Authority, because the applicant failed to suggest a figure.
as selected by this Authority, because this figure better characterizes the invention.
b.
none of the figures is to be published with the abstract.

A. CLASSIFICATION OF SUBJECT MATTER

     C07D 405/12 (2006.01)i; A61P 31/04 (2006.01)i; C07D 265/10 (2006.01)i; C07D 207/09 (2006.01)i; C07D 207/14 (2006.01)i; C07D 211/58 (2006.01)i; A61K 31/4468 (2006.01)i; A61K 31/40 (2006.01)i; A61K 31/4025 (2006.01)i; A61K 31/535 (2006.01)i
According to International Patent Classification (IPC) or to both national classification and IPC

B. FIELDS SEARCHED

Minimum documentation searched (classification system followed by classification symbols):
     C07D
Documentation searched other than minimum documentation to the extent that such documents are included in the fields searched:
Electronic data base consulted during the international search (name of data base and, where practicable, search terms used):
EPO-Internal, WPI Data, CHEM ABS Data

C. DOCUMENTS CONSIDERED TO BE RELEVANT

Category* Citation of document, with indication, where appropriate, of the relevant passages Relevant to claim No.
(1)
X
WO 2013124169 A1 (ACRAF [IT]) 29 August 2013 (2013-08-29)
1-19
page 22, line 15, intermediate (xi)
(2)
X
WO 2005047249 A1 (SCHERING AG [DE]) 26 May 2005 (2005-05-26)
1-19
page 75, lines 6, 11; example 9
page 76, line 9 - line 10; example 11
page 77, line 11 - line 12; example 13
page 78, line 32 - line 33; example 14
page 79, line 8 - line 9; example 15
(3)
X
AYESA, SUSANA ET AL, "An expeditious library synthesis of N-monoalkylated aminopiperidines and -pyrrolidines", EUROPEAN JOURNAL OF ORGANIC CHEMISTRY,Vol. 12, December 2004 (2004-12), page 2723-2737,
XP002752935
1-19
page 2730 - page 2732; tables 2-6; compounds 9a, 10a, 11a, 12a, 13a
page 2735; compound 12a
(4)
A
WO 0001714 A1 (MICROCIDE PHARMACEUTICALS INC [US]; DAIICH PHARMACEUTICAL CO LTD [JP]) 13 January 2000 (2000-01-13)
1-26
page 188; compound D329
page 189; compound D331
claims 1,2
*
Special categories of cited documents:
"A"
document defining the general state of the art which is not considered to be of particular relevance
"E"
earlier application or patent but published on or after the international filing date
"L"
document which may throw doubts on priority claim(s) or which is cited to establish the publication date of another citation or other special reason (as specified)
"O"
document referring to an oral disclosure, use, exhibition or other means
"P"
document published prior to the international filing date but later than the priority date claimed
"T"
later document published after the international filing date or priority date and not in conflict with the application but cited to understand the principle or theory underlying the invention
"X"
document of particular relevance; the claimed invention cannot be considered novel or cannot be considered to involve an inventive step when the document is taken alone
"Y"
document of particular relevance; the claimed invention cannot be considered to involve an inventive step when the document is combined with one or more other such documents, such combination being obvious to a person skilled in the art
"&"
document member of the same patent family

D. INFORMATION ON PATENT FAMILY MEMBERS

Patent document cited in search report Publication date
(day/month/year)
Patent family member(s) Publication date
(day/month/year)
WO 2013124169 A1
29 August 2013
AR 090085 A1
AU 2013224313 A1
CA 2860466 A1
CN 104080781 A
DK 2817301 T3
EA 201491448 A1
EP 2817301 A1
ES 2564033 T3
GE P201606552 B
HK 1203931 A1
HR P20160124 T1
JP 2015506995 A
KR 20140122725 A
PT 2817301 E
SG 11201403788V A
SI 2817301 T1
SM T201600054 B
US 2014378455 A1
US 2016045485 A1
WO 2013124169 A1
15 October 2014
17 July 2014
29 August 2013
01 October 2014
14 March 2016
28 November 2014
31 December 2014
17 March 2016
10 October 2016
06 November 2015
11 March 2016
05 March 2015
20 October 2014
14 March 2016
28 August 2014
31 March 2016
29 April 2016
25 December 2014
18 February 2016
29 August 2013
WO 2005047249 A1
26 May 2005
AU 2004289690 A1
BR PI0415874 A
CA 2543913 A1
CN 1902171 A
EP 1687268 A1
JP 2007513082 A
KR 20060123292 A
US 2005101644 A1
WO 2005047249 A1
ZA 200604788 B
26 May 2005
09 January 2007
26 May 2005
24 January 2007
09 August 2006
24 May 2007
01 December 2006
12 May 2005
26 May 2005
27 May 2009
WO 0001714 A1
13 January 2000
AU 5207399 A
US 6399629 B1
WO 0001714 A1
24 January 2000
04 June 2002
13 January 2000
Name and mailing address of the ISA/:
European Patent Office
P.B. 5818, Patentlaan 2, 2280 HV Rijswijk,
Netherlands
Telephone No. (+31-70)340-2040
Facsimile No. (+31-70)340-3016
Date of the actual completion of the international search:
11 January 2017
Date of mailing of the international search report:
20 January 2017
Authorized officer:
Cortés, José
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