PATENT CLAIM ANALYSIS

Application Number: 16185437
Application Type: Utility
Filing Date: 2018-11
Publication Date: 2019-03
Patent Classification: ["514", "224200"]

Abstract:
The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R 1  is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R 2  is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R 3  is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent, antimicrobial activity against  Clostridium difficile  and is useful for the prevention or treatment of intestinal infection such as  Clostridium difficile -associated diarrhea.

Claim (Index 1):
A compound represented by the formula (I) wherein\n X is or a fluorine atom; \n R is a hydrogen atom; \n R 1  is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; \n R 2  is a hydrogen atom; alkyl optionally substituted by 1 or 2 substituents selected from the group consisting of a halogen atom and hydroxyl; alkoxy; haloalkoxy; a halogen atom; cyano; cyclopropyl; nitro; amino; formyl; alkenyl or alkynyl; \n R 3  is \n (1) a fused heterocyclic group of the formula \n wherein\n  represents a single bond or a double bond, \n X 1  is C (R 5 ) or N, \n R 4  is a hydrogen atom or alkyl, and \n R 5  is (a) a hydrogen atom,\n (b) a halogen atom, \n (c) cyano, \n (d) nitro, \n (e) hydroxy, \n (f) alkyl optionally substituted by 1 to 3 halogen atoms, \n (g) alkenyl or alkynyl, \n (h) aryl, or \n (i) alkoxy optionally substituted by 1 to 3 halogen atoms, \n \n when X 1  is C(R 5 ), R 4  and R 5  are optionally bonded 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 atom, cyano, nitro, hydroxy and alkyl, \n (2) 3-pyridyl optionally substituted by 1 or 2 substituents selected from the group consisting of\n (a) a halogen atom, \n (b) cyano, \n (c) nitro, \n (d) hydroxy, \n (e) amino, \n (f) alkyl optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, alkylamino, dialkylamino and hydroxy, \n (g) alkenyl, alkynyl \n (h) aryl, \n (i) cycloalkyl, \n (j) alkoxy, \n (k) alkylamino, \n (l) dialkylamino, \n (m) phenylamino optionally substituted by 1 to 3 halogen atoms, \n (n) a cyclic amino group optionally substituted by alkoxycarbonyl, \n (o) formyl, \n (p) carbamoyl optionally substituted by alkyl optionally substituted by hydroxy, and \n (q) a 5- to 10-membered aromatic heterocyclic group optionally substituted by alkyl, \n \n (3) 4-pyridyl optionally substituted by a halogen atom, \n (4) a group of the formula \n wherein\n one of Y 1 , Y 2 , Y 3  and Y 4  is N or N + (\u2014O \u2212 ), and the remaining three are each C(R 25 ), C(R 26 ) and C(R 27 ), \n W is O, S, NH or N(R 23 ) \n R 23  is a hydrogen atom or alkyl, and \n R 24 , R 25 , R 26  and R 27  are each independently,\n (a) a hydrogen atom, \n (b) cyano, or \n (c) nitro, \n \n (5) a group of the formula \n wherein\n R 28  is a hydrogen atom or hydroxy, and \n R 29  is a hydrogen atom or alkyl, \n (6) a group of the formula \n wherein R 16  is\n (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) \u2014C(R 17 )\u2550N\u2014OH wherein R 17  is a hydrogen atom, cyano or hydroxy, (h) a 5- to 10-membered aromatic heterocyclic group optionally substituted by alkyl, alkoxycarbonyl, carboxy or phenyl, or (i) cyano, or \n (7) a group of the formula \n wherein\n R 18  is a hydrogen atom or alkyl optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom and phenyl, \n n is 0 or 1, \n R 19 , R 20  and R 33  are each independently,\n (a) a hydrogen atom, \n (b) a halogen atom, \n (c) cyano, \n (d) alkyl optionally substituted by 1 to 3 substituents selected from the group consisting of \n \n (i) a halogen atom \n (ii) cyano, \n (iii) hydroxy, \n (iv) amino, \n (v) alkylamino, \n (vi) dialkylamino, and \n (vii) a cyclic amino group optionally substituted by alkyl,\n (e) alkoxy, \n (f) amino optionally substituted by 1 or 2 substituents selected from the group consisting of \n \n (i) alkylcarbonyl optionally substituted by a cyclic amino group, \n (ii) alkylsulfonyl, \n (iii) carbamoyl, \n (iv) alkyl, cycloalkyl or cycloalkylalkyl, and \n (v) 5- to 10-membered saturated heterocyclic group,\n (g) carboxy, \n (h) alkoxycarbonyl, \n (i) carbamoyl optionally substituted by alkyl optionally substituted by amino, alkylamino, dialkylamino or alkoxycarbonylamino, \n (j) formyl, \n (k) a 5- to 10-membered aromatic heterocyclic group optionally substituted by alkyl, \n (l) \u2014CH\u2550N\u2014OR 21  wherein R 21  is a hydrogen atom or alkyl optionally substituted by alkylamino or dialkylamino, \n (m) nitro, \n (n) a 5- to 10-membered saturated heterocyclic group optionally substituted by amino, \n (o) phenyl, or \n (p) \u2014NHC(SMe)\u2550CHCN.

Metadata:
- Claim Count in Document: 47.0
- Percentile: 98.0
- Lexical Diversity: 2.0
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14193656', '14692200', '15440548', '13262888', '10481367']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8154427501260638
- 35 USC 102 Novelty (BERT): 0.6006500840900129
- Combined Prediction Score: 0.7939634835224587
- Mean Citation Score: 418.661232
- Max Citation Score: 501.5164
- Similarity Product: 490.0023271674156

Labels:
- Claim Label 101: 1
- Claim Label 102: 0
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 0
- Label 101 Adjusted: 1

Dataset: test