http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-087747-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_382ccfc2ebebcaee15aa7cda4cee86bc |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-444 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4709 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-47 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-497 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5383 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-538 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D493-06 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4709 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4738 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-04 |
| filingDate | 2012-08-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e82e03b466fb7ee7e3a497bb7055ec35 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cf9a516862545822e5b5deaf5893016e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2ca9d7f4e6ada36b15687b3a15bacfac http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_553385246b64a4d60b82cbae9922995c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_126203f5aa4bff3e9a158dcb5bab0457 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb07d432b6fe8bc969cda28beec43691 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e3ca23fceab56c07e415cd8924f0a80e |
| publicationDate | 2014-04-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-087747-A1 |
| titleOfInvention | USEFUL QUINOLONA DERIVATIVES AS ANTIBACTERIAL AGENTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
| abstract | The compound herein has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infections such as diarrhea associated with Clostridium difficile. Claim 1: A compound represented by the formula [1] characterized in that X is a hydrogen atom or a fluorine atom; R is a hydrogen or alkyl atom; R¹ is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R² is a hydrogen atom; alkyl optionally substituted by 1 or 2 substituents selected from the group consisting of a halogen and hydroxyl atom; alkoxy; haloalkoxy; a halogen atom; cyano; cyclopropyl; nitro; Not me; formyl; alkenyl or alkynyl; or R¹ and R² are joined to form a 5- or 6-membered ring optionally substituted by alkyl; R³ is (1) a fused heterocyclic group of the formula [2] or [3] where ⁻ ⁻ ⁻ ⁻ ⁻ represents a single bond or a double bond, X¹ is C (R⁵) or N, R⁴ is a hydrogen atom or alkyl, and R⁵ is (a) a hydrogen atom, (b) a halogen atom, (c) cyano, (d) nitro, (e) hydroxy, (f) alkyl optionally substituted by 1 to 3 atoms of halogen, (g) alkenyl or alkynyl, (h) aryl, or (i) alkoxy optionally substituted by 1 to 3 halogen atoms, when X¹ is C (R⁵), R⁴ and R⁵ are optionally joined to form a 5 or 6-membered ring optionally substituted by oxo, said fused heterocyclic group is optionally substituted by 1 or 2 substituents selected from the group consisting of a halogen, cyano, nitro, hydroxy and alkyl atom, (2) a group of the formula [4] where X² is C (R⁸) or N, and R⁶, R⁷ and R⁸ are each independently, (a) a hydrogen atom, (b) a halogen atom, (c) cyano, (d) nitro, (e) amino, (f) alkyl optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, alkoxy and amino, (g) alkenyl, (h ) alkynyl, (i) aryl, (j) formyl or CH = N-OH, (k) carboxy, (l) carbamoyl, (m) a 5- to 10-membered aromatic heterocyclic group optionally substituted by alkyl, or ( n) alkenyloxy, (3) a group of the formula [5] or [6] where X³ and X⁴ are N, or X³ is N and X⁴ is CR, where R is a hydrogen atom, amino, hydroxy, alkyl substituted in optionally by 1 to 3 substituents selected from the group consisting of alkoxy and dimethylamino or mercapto, or X³ is CH and X⁴ is N, R is a hydrogen or alkyl atom optionally substituted by 1 to 3 substituents selected from the group consisting in substituted hydroxyl and amino, and R⁶ is as defined above, (4) a compound selected from the group of formulas [7] where ⁻ ⁻ ⁻ ⁻ ⁻ represents a single bond or a double bond and R⁶ is as defined above, (5) 3-pyridyl optionally substituted by 1 or 2 substituents selected from the group consisting of (a) a halogen atom, (b) cyano, (c) nitro, (d) hydroxy, (e) amino, (f) alkyl optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, alkylamino, dialkylamino and hydroxy, (g) alkenyl, alkynyl (h) aryl, (i) cycloalkyl, (j) alkoxy, (k) alkylamino, (l) dialkylamino, (m) phenylamino optionally substituted by 1 to 3 halogen atoms, (n) an amino group cyclic optionally substituted by alkoxycarbonyl, (o) formyl, (p) carbamoyl optionally substituted by alkyl optionally substituted by hydroxy, and (q) a 5- to 10-membered aromatic heterocyclic group optionally substituted by alkyl, (6) 4-pyridyl optionally substituted by a halogen atom, (7) 5-pyrimidinyl optionally substituted by 1 or 2 substituents selected from the group consisting of amino, alkylamino, dialkylamino and carboxy, (8) 2-indolyl, 3-indolyl, 5-indolyl, 6-indolyl, benzofuranyl, benzothiophenyl, benzoxazolyl or benzothiazolyl, each optionally substituted by 1 or 2 substituents selected from the group consisting of (a) a halogen atom, (b) cyano, (c) nitro, (d) hydroxy, (e) alkyl optionally substituted by 1 to 3 substituents selected from the group consisting of amino, alkoxycarbonylamino, alkylamino and dialkylamino, (f) alkoxy, (g) formyl, (h) carboxy, and (j) amino optionally substituted by 1 or 2 substituents selected from the group which consists of (i) alkoxycarbonyl, (ii) alkylcarbonyl optionally substituted by a substituent selected from the group consisting of (A) cycloalkyloxy optionally substituted by 1 to 3 alkyl, (B) alkylamino, (C) dialkylamino, (D ) a substituted cyclic amino group e n optionally by alkoxycarbonyl, and (E) a halogen atom, (iii) phenylcarbonyl optionally substituted by 1 to 3 substituents selected from the group consisting of alkyl and alkoxy, (iv) cycloalkylcarbonyl, (v) an aromatic heterocyclylcarbonyl group 5 to 10 members optionally substituted by alkyl optionally substituted by 1 to 3 halogen atoms, (vi) benzylcarbonyl optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom and alkoxy, ( vii) arylsulfonyl optionally substituted by alkoxy, (viii) cycloalkylalkyl sulfonyl optionally substituted by 1 to 3 substituents selected from the group consisting of alkyl and oxo, (ix) a 5- to 10-membered aromatic heterocyclylsulfonyl group optionally substituted by 1 to 3 alkyl, and (x) -C (= N-CN) -SR⁹ where R⁹ is alkyl, (9) a group of the formula [8] or [9] where one of Y¹, Y², Y³ and Y⁴ is N or N⁺ (-O⁻), and what The remaining three are each C (R²⁵), C (R²⁶) and C (R²⁷), W is O, S, NH or N (R²³), R²³ is a hydrogen or alkyl atom, and R²⁴, R²⁵, R²⁶ and R²⁷ are each independently, (a) a hydrogen atom, (b) cyano, or (c) nitro, (10) a group of the formula [10] or [11] where R²⁸ is a hydrogen atom or hydroxy, and R²⁹ is a hydrogen or alkyl atom, (11) a group of the formula [12] where X⁵ is C (R¹¹) or N, X⁶ is CH₂, C (= O), O, S, SO₂ or N (R¹²), X⁷ is CH (R¹³), C (= O) or N (R¹⁴), X⁸ is CH (R¹⁵) or C (= O), R¹⁰, R¹² and R¹⁴ are each independently, (a) a hydrogen atom or (b) alkyl, and R¹¹, R¹³ and R¹⁵ are each independently, (a) a hydrogen atom, (b) a halogen atom, (c) cyano, (d) nitro, ( e) amino, (f) alkylamino, (g) dialkylamino, (h) alkyl optionally substituted by hydroxy, or (i) alkenyl, when X⁵ is C (R¹¹), R¹⁰ and R¹¹ are optionally linked to To form a 5 or 6-membered ring optionally substituted by alkyl or oxo, and when X⁶ is N (R¹²) and X⁷ is CH (R¹³), R¹² and R¹³ are optionally joined to form a 5 or 6 ring members, (12) a group of the formula [13] where R¹⁶ is (a) a hydrogen atom, (b) alkyl optionally substituted by 1 to 3 substituents selected from the group consisting of cyano, alkylamino and dialkylamino, ( c) alkenyl optionally substituted by carboxy, (d) formyl, (e) carboxy, (f) carbamoyl, (g) -C (R¹⁷) = N-OH where R¹⁷ is a hydrogen, cyano or hydroxy atom, ( h) a 5-10 membered aromatic heterocyclic group optionally substituted by alkyl, alkoxycarbonyl, carboxy or phenyl, or (i) cyano, (13) a group of the formula [14] where R¹⁸ is a hydrogen or alkyl atom optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen and phenyl atom, n is 0 or 1, R¹⁹, R²⁰ and R³³ are each independently, (a) a hydrogen atom, (b) a halogen atom, (c) cyano, (d) alkyl optionally substituted by 1 to 3 substituents selected from the group consisting of (i ) a halogen atom, (ii) cyano, (iii) hydroxy, (iv) amino, (v) alkylamino, (vi) dialkylamino, and (vii) a cyclic amino group optionally substituted by alkyl, (e) alkoxy , (f) amino optionally substituted by 1 or 2 substituents selected from the group consisting of (i) alkylcarbonyl optionally substituted by a cyclic amino group, (ii) alkylsulfonyl, (iii) carbamoyl, (iv) alkyl, cycloalkyl or cycloalkylalkyl, and (v) saturated 5-10 membered heterocyclic group, (g) carboxy, (h) alkoxycarbonyl, (i) carbamoyl optionally substituted by alkyl optionally substituted by amino, alkylamino, dialkylamino or alkoxycarbonylamino, ( j) formyl, (k) a 5- to 10-membered aromatic heterocyclic group substituted in fo Optional rma by alkyl, (l) -CH = N-OR²¹ where R²¹ is a hydrogen or alkyl atom optionally substituted by alkylamino or dialkylamino, (m) nitro, (n) a substituted 5-10 membered saturated heterocyclic group optionally by amino, (o) phenyl, or (p) -NHC (SMe) = CHCN, (14) a group of the formula [15] where R³⁰ is (a) a hydrogen atom, (b) an atom halogen, (c) cyano, (d) alkyl optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen and hydroxy atom, (e) alkenyl, (f) alkynyl, (g) alkoxy, ( h) formyl, (i) -CH = N-OH, or (j) carbamoyl, (15) naphthyl or isochromenyl, (16) quinolyl or isoquinolyl, oxides, or their derivatives, (17) a compound of the group of formulas [ 16], (18) a group of the formula [17] where U is O or S, and R³¹ is (a) a hydrogen atom, (b) a halogen atom, (c) alkyl optionally substituted by 1 to 3 halogen atoms, ( |
| priorityDate | 2011-08-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 87.